Note: Descriptions are shown in the official language in which they were submitted.
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SHEET-LIKE DEVICES
Technical Field
The present invention relates to novel pre-formed, unilamellar sheet-like
devices. In
particular it relates to pre-formed, unilamellar sheet-like devices which are
patches or
masks, comprising at least one polymeric gel forming agent for delivering
benefit agents
to the skin, hair or nails. Said devices are suitable for topical delivery of
at least one
benefit agent and display improved mechanical properties such as strength and
flexibility.
Further, the devices of the present invention are unobtrusive and conform to
the contours
of a target surface when applied.
Back~,round of the Invention
The benefits of using a patch or mask device comprising a polymeric gel
forming agent
instead of creams and lotions and the like, to cosmetically treat the skin,
hair or nails, or
to promote the healing of burns or wounds has been recognised in the art. A
variety of
cosmetic patches or devices are commercially marketed or described as being
useful for
the delivery of skin care actives such as vitamins, anti-acne actives,
moisturisers and the
like. Patches and devices have also been described in the literature and
marketed in the
medical field as a useful means for the transdermal administration of drugs.
However,
many of these patches or devices suffer drawbacks in their physical product
forms
resulting in undesirable in-use characteristics as perceived by the consumer
or wearer.
For example, some patches or devices may be too wet or sticky, as the gel
forming agents
comprising the patch or device do not form a solid gel structure and as a
result, the
patches or devices are difficult to handle and apply to the skin. Others are
strongly
adhesive, tight and uncomfortable to wear and remove, and many patches do not
provide
an effective release and penetration of benefit agents.
Some patches or devices require formation in situ on the skin and are
therefore messy to
apply. For example, US-A-4,291,025 relates to a thermally reversible agar gel
topical
dressing comprising 5 to 12% agar, 20 to 75% diethylene glycol and water to
100%; and
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methods for preparing said dressing. The compositions may additionally
comprise gel
strengthening agents and special purpose ingredients (e.g. vitamins,
antibiotics).
According to one aspect of the invention of US-A-4,291,025, solid, high
strength,
yieldable agar gels are prepared and then subdivided into smaller pellets or
pieces.
According to another aspect, the agar gel is then converted into a sol upon
heating, the sol
is applied to the target skin and cooled in situ to form a removable gel form.
Further, some patches or devices are too dry or inflexible and therefore do
not conform
well to the contours of the surface to which they are applied. For example, EP-
A-161 681
discloses gel plates comprising a polysaccharide and an aqueous solution of a
polyhydric
alcohol. Preferred polysaccharides for the gel plates are a blend of
carrageenan and a
galactomannan, or carrageenan alone. The compositions optionally comprise
medical
components such as skin stimulants, antiphlogistics, analgesics and
antibiotics. The gel
plates are disclosed as being transparent or inconspicuous, having a
refreshing feeling and
good adhesion, as well as being sufficiently elastic, stretchable and strong.
Flexibility and strength are further important features of a gelled device.
W097/17944
discloses cosmetic formulations made up of a gel material consisting of a
balanced
mixture of polysaccharides containing a soluble alginate (0.1-5%), agar (0.01-
0.5%),
pectin (0.01-0.5%), xanthan gum (0.05-1 %) with the balance consisting of
water. The gel
material is optionally enriched with water-soluble or water-dispersible active
ingredients.
The gel material may be processed to form a structured gel which is disclosed
as being
easy to handle and well adapted to the skin surface.
W090/14110 discloses pharmaceutical preparations which may take the form of a
self
supporting slab, pad or wafer of a desired size, shape and thickness
comprising a water
insoluble alginate and suspending agents such as xanthan gum alone, or xanthan
gum in
combination with locust bean gum. Gellan gum is also disclosed as a further
useful
suspending agent. The suspending agents in the preparations may also act as
gel forming
agents. The preparations optionally comprise anti-inflammatory agents, or the
antiseptic
agent, iodine. The slab or wafer forms of a preparation may be flexible and
applied onto a
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plastic backing to form an integral surgical dressing, with the gel either
exposed or
covered with a gauze.
US-A-4,318,746 relates to a gel comprising at least 0.5% of a first polymer
that disperses,
dissolves or hydrates in hot water and that forms, or can be made to form, a
rigid gel on
cooling, at least 2% of a second polymer that is insoluble in hot water and
that dissolves
or hydrates on cooling and is compatible with the first polymer, and water.
The document
describes the gel as being firm, cohesive and adhesive and useful for example,
as an
electrode or for the topical administration of drugs. The document outlines
that one of the
advantages of the gel is that it is relatively rigid and adhesive at
temperatures below 60-
65°C.
JP-A-63-200760 discloses a bi-layered patch comprising a gelled matrix and a
support
sheet (or backing). The description teaches that the skin-engaging surface of
the gelled
matrix is preferably flat. Alternatively, the skin-engaging surface may
include a mesh-
like array of channels (Figure 3), an imprint of a logo or the like (Figure
2), a substantially
parallel arrangement of channels (Figure 5) or an array of projections (Figure
7). The
gelled matrix comprises a protein (gelatin, casein, albumen or serecin) or a
water-soluble
polymer, to which an inorganic filler, a humectant, possibly a binder and/or a
cross-
linking agent is added. The bi-layered patch is made by casting into a mould
of the
desired shape.
W098/17287 concerns a hollow flexible silicone cushion for treating keloid and
hypertrophic scars, by developing a negative electric charge near the scar.
The cushions
may be made from textured silicone sheeting, the term "textured" being defined
as an
irregular surface containing, for example, corners, indentations or related
textural features
which may be regular or irregular in shape and appearance. It is taught that
texturing
results in a non-uniform distribution of charge. No method for texturing
silicone sheeting
is disclosed.
US-A-4,289,125 discloses polymeric sheets for use as burn dressings whose skin-
facing
surface, at least, is textured. It is taught that this is advisable to provide
a reservoir for
wound debris and for adherence to the wound area. Burn dressings with a
textured
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surface on one surface or on both surfaces are disclosed. Fig. 1D discloses a
unilamellar
device, in which both surfaces are textured. The fabric textured sheet acts as
a skeleton,
to carry polymer, which is then cured. Thereafter, the skeleton fabric sheet
is removed by
solvent leaching, leaving an integral unilamellar self supporting polymeric
sheet. Figures
SF-SI disclose a laminated device having one "textured" surface. This
comprises a
smooth surfaced polymeric membrane in which is partially embedded a material
which
will impart a fabric texture to its surface. The material to be embedded can
be uncoated
or coated gauze or mesh or the above-mentioned fabric sheets (with or without
leaching
of the skeleton sheet). Fig. 6D illustrates a non-laminated embodiment having
one
"textured" surface. The fabric material is stretched over an appropriate
surface, to act as a
skeleton to carry a membrane layer of polymer which forms a continuous phase
with the
polymer coating in the fabric material (see Fig. 6C). The fabric material may,
thereafter,
be leached.
W094/02674 concerns a dual textured treatment pad comprising a paper layer
laminated
to a synthetic fiber, non-woven layer having a repeating pattern comprising at
least two
adjacent delineated regions simultaneously not having the same thickness or
having
regularly or irregularly spaced apertures. Dual texturing permits both gentle
and vigorous
cleansing from the same pad.
W098/50085 concerns an article being, for example, a wound dressing or a
target strip
for a disposable diaper. The article comprises a substrate and a textured,
matte-finish,
low adhesion backsize coating. The document teaches that the matte-finish
surface on a
wound dressing is achievable by "mechanical action" and makes the dressing
less visible
when applied to the skin.
US-A-5,026,446 concerns a physically abraded target strip for disposable
diapers. The
physical abrasion is to improve adhesion of adhesive closure tabs to the
target strip.
While the above-mentioned patches or sheets from the cosmetic and medical
field provide
advances in attaining desirable physical and in-use characteristics, the
documents do not
describe self supporting, pre-formed sheet-like devices which are unilamellar,
wherein the
devices have desirable mechanical properties of strength, robustness and
flexibility, as
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well as desirable in-use properties of ease of handling, unobtrusiveness and
conformability to the contours of a target surface when applied.
It has now been surprisingly found that a pre-formed, unilamellar sheet-like
device may
be formulated as a self supporting, high strength structure which is
sufficiently flexible to
conform to the contours of a target surface when applied. The devices
according to a first
aspect herein have a non-planar topography, the topography of which is
selected
according to the target surface of application, making them easy to handle and
apply. For
example, thicker ridges around the perimeter of the device facilitate ease of
handling and
robustness, whereas thinner regions fit better to target surfaces in areas of
increased
curvature. Additionally or alternatively, a textured surface on the surface of
the device
either distal, in use, the skin, hair or nails of a user makes the device less
obtrusive. The
desirable physical properties are achieved by selecting the chemical
composition and
rheological characteristics of the gelled devices with reference to the
relationship between
strength and flexibility and the desirable in-use characteristics are achieved
by selecting a
suitable non-planar topography being at least two adjacent delineated regions
simultaneously not having the same mean thickness and/or a suitable textured
surface or
surfaces.
The preferred pre-formed, unilamellar sheet-like devices of the present
invention display a
low level of syneresis, which makes the devices moist to the touch and helps
provide a
cooling sensation. The surface liquid can facilitate adhesion of the devices
to a target
surface, thus obviating the need for either an additional adhesive overlying
the gelled
form or an adhesive coated substrate.
The present unilamellar sheet-like devices do not require supporting or
strengthening by
an occlusive or non-occlusive backing material often referred to as a
substrate. However,
a substrate, if present, may be combined with a unilamellar sheet-like device
and would
confer further support or strengthening. In addition, substrates may also be
employed to
prevent evaporation of active ingredients, or act as a means for adhering a
device to the
skin when an adhesive is coated around its periphery. A substrate may be
impregnated
with, adhered, or laminated to one surface of the device.
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EP-B-507,160 relates to an external preparation for application to the skin
comprising a
drug retaining layer placed on a support wherein the drug retaining layer
comprises
lidocaine, and an adhesive gel base comprising 0.5% to 50% of a water soluble,
high
molecular weight substance, 20 to 70% ,water and 1 to 70 % of a water
retaining agent.
Suitable supports are described as flexible materials such as non-woven
fabrics.
The substrate, if present to confer further support or strengthening, must be
compatible
with the gel. A substrate is not compatible with the gel if the gel
delaminates from the
substrate. Even when a gel composition is found having desirable flexibility
and strength,
difficulties may still be incurred in matching such a gel with a substrate
which is
compatible with these gel properties. Combining a flexible substrate with a
flexible gel
does not necessarily produce a flexible patch or mask device. Aside from the
problem of
delamination, many flexible substrates often display a degree of porosity such
that the wet
gel infiltrates the substrate and forms strong gel networks within its fibers.
Such
networks are thought to reduce the flexibility of the resultant device.
Further, the
substrate may not provide a patch or mask device with an unobtrusive
appearance on the
skin, hair, or nails. This will often depend on the choice of substrate and
its
characteristics.
The sheet-like devices herein are preferably patches or masks for cosmetic or
therapeutic
application.
Summar~of the Invention
The present invention relates, in a first aspect, to a pre-formed, unilamellar
sheet-like
device for delivering benefit agents to the skin, hair or nails, the device
having a perimeter
defining first and second spaced-apart surfaces; the device comprising at
least one benefit
agent and at least one polymeric gel forming agent; and the device having a
non-planar
topography on at least one of the first and second surfaces.
According to a second aspect of the present invention there is provided a pre-
formed,
unilamellar sheet-like device for delivering benefit agents to the skin, hair
or nails, the
device having a perimeter defining first and second spaced-apart surfaces; the
device
comprising at least one benefit agent and at least one polymeric gel forming
agent; and the
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device having a non-planar topography on at least one of the first and second
surfaces, the
non-planar topography comprising at least two adjacent delineated regions
simultaneously
not having the same mean thickness.
According to a third aspect of the present invention there is provided a pre-
formed,
unilamellar sheet-like device for delivering benefit agents to the skin, hair
or nails, the
device comprising at least one benefit agent and at least one polymeric gel
forming agent;
and the device having a perimeter defining first and second spaced-apart
surfaces, the first
surface being adjacent, in use, the skin, hair or nails, and the second
surface having a non-
planar topography, the non-planar topography comprising a textured surface
that is the
negative image of a texturing surface, the negative image of the texturing
surface having a
texture defined by Ra of greater than 10~m.
Devices of the invention having textured surfaces are preferably not just
visibly textured
but also textured to the touch.
The devices of the invention are suitable for topical application to the skin,
hair or nails.
They provide excellent in-use characteristics such as unobtrusiveness,
comfort, fit,
flexibility, visual appearance, strength, ease of handling and conformability
upon topical
application. Further, the devices described herein have excellent mechanical
properties
and form a high strength structure which is flexible and has a degree of
elasticity. The
preferred devices of the present invention show a low level of syneresis
providing further
in-use characteristics of hydration and moisturisation benefits upon topical
application.
According to a fourth aspect of the invention there is provided a method of
producing a
pre-formed, unilamellar sheet-like device according to the first or second
aspects of the
invention, the method comprising the steps of providing a gel-forming mixture
comprising at least one benefit agent and at least one gellable polymeric gel
forming agent
in a mould having at least one surface that is the negative image of the, or
each, non-
planar topography, the non-planar topography comprising at least two
delineated regions
simultaneously not having the same mean thickness or a textured surface that
is the
negative image of a texturing surface, the texturing surface having a texture
defined by Ra
of greater than 10~m or both; and thereafter gelling the gel-forming mixture.
In a
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preferred embodiment, the mould has opposed texturing surfaces having a
texture defined
by Ra of greater than 10~m, in order to imprint textured surfaces on opposed
first and
second surfaces of the device. More preferably, the mould is configured
additionally to
provide a non-planar topography comprising at least two delineated regions
simultaneously not having the same mean thickness on at least one surface of
the device,
preferably the second surface which is that distal the skin, hair or nails
when the device is
in use.
In a fifth aspect, the present invention provides a method of producing a pre-
formed,
unilamellar sheet-like device according to the first or third aspect of the
invention, the
method comprising the steps of providing a gel-forming mixture comprising at
least one
benefit agent and at least one gellable polymeric gel forming agent in a
mould, with a first
mould surface which has a topography which is the negative image of the first
device
surface; bringing a second texturing surface into contact with the second
device surface of
the gel-forming mixture; gelling the gel-forming mixture; and removing the
texturing
surface from the device.
In a sixth aspect, the present invention provides a method of delivering at
least one benefit
agent to the skin, hair or nails, the method comprising contacting the skin,
hair or nails
with a device according to a first, second or third aspect of the invention,
the device
comprising at least one cosmetic benefit agent and at least one polymeric gel
forming
agent.
Brief Description of the Drawings
Figs. la, 1b and lc are plan, sectional perspective and perspective views of a
first
embodiment of a device according to a first or second aspect of the invention.
Figs. 2 and 3 are sectional views of second and third embodiments of a device
according
to the first or second aspect of the invention.
Fig. 4 is a sectional perspective, partial view of a fourth embodiment of a
device
according to the first, second or third aspect of the invention.
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Fig. S is a sectional perspective, partial view of a second embodiment of a
device
according to the first or third aspect of the invention.
Fig. 6 is a schematic view of a fifth embodiment of a pre-formed, unilamellar
sheet-like
device according to a first or second aspect of the invention, in situ on a
user's face.
Figs. 7a and 7b are plan and sectional views of the device of Figure 6.
Fig. 8 is a schematic view of a sixth embodiment of a device according to the
first or
second aspect of the invention, in situ on a user's face.
Fig. 9 is a plan view of the pre-formed, unilamellar sheet-like device of
Figure 8.
Fig. 10 is a schematic view of a seventh embodiment of a device according to
the first or
second aspect of the invention, in situ on a user's face.
Fig. 11 is a plan view of the pre-formed, unilamellar sheet-like device of
Figure 10.
Fig. 12 is a sectional view of an eighth embodiment of a device according to
the
invention, in its third aspect, wherein the device is textured on first and
second surfaces.
Detailed Description of the Invention
The pre-formed, unilamellar sheet-like devices of the present invention
comprise at least
one benefit agent and at least one polymeric gel forming agent, as well as
various optional
ingredients as indicated below. All levels and ratios are by weight of total
composition of
the device, unless otherwise indicated. When a substrate is used as an adjunct
to the
device, the total weight of the composition of the device is calculated
without including
the weight of the substrate.
The term "pre-formed" as used herein, means that the device so described is
manufactured
into a product form having a predetermined thickness, shape and size, wherein
the device
may be removed from any associated packaging and placed or draped onto the
target
surface by the fingers without the need to spread, rub or coat the target area
with the
product form. Devices herein are preferably packaged in a sealed, protective
wrapper.
The term "sheet-like device", as used herein, means that the device described
is a patch or
mask for cosmetic or medical application wherein the patch is a continuous
sheet, the
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shape of which is pre-determined according to the specific area of skin, hair
or nails to be
treated and wherein the mask is a non-continuous sheet covering the facial
area with
apertures for the eyes, nose or mouth.
The term "unilamellar" as used herein, means that the device so described is a
single layer
which is self supporting.
The term "non-planar topography" as used herein, means at least two adjacent
delineated
regions simultaneously not having the same mean thickness. Alternatively or
additionally, the term "non-planar topography" means a textured surface that
is the
negative image of a texturing surface, the negative image of the texturing
surface having a
texture defined by Ra of greater than 10~m. The term "Ra" as used herein means
the
surface-based average deviation from a best fit plane, described in detail
below in the
section headed "Methods of Evaluation".
The phrase "adj acent delineated regions simultaneously not having the same
mean
thickness" refers to adjacent regions of a device which are visually distinct
and, when
small scale thickness variations at particular points, such as that provided
by the texturing
described herein, are averaged out, their mean thicknesses are different.
The term "water-soluble" as used herein, means the ability of a gellable
polymeric gel
forming agent to dissolve in an aqueous solution either at room temperature or
upon
heating thereby forming a continuous phase.
The term "syneresis" as used herein, means the process whereby a gel contracts
on
standing with the exudation of liquid. Without being limited by theory, it is
believed that
gel compositions form 3-dimensional matrices which bind or encapsulate other
ingredients of the composition. Syneresis is believed to involve a spontaneous
separation
of an initial homogeneous system into a coherent gel phase and a liquid. The
exuded
liquid is a solution whose composition depends upon that of the original gel.
When a
preferred device of the present invention is applied to a target area, the
device loses some
of its volume such that ingredients bound within the gel matrices such as
water or benefit
agents, are released towards, and penetrate the target area.
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The term "polysaccharide" as used herein, means a naturally occurnng or
synthetically
produced, linear, branched or cross-linked polymer of monosaccharide units,
which swells
when dispersed in water at low dry concentrations and gels the aqueous phase.
The term "percentage compression at rupture" as used herein, is a measure of
the
flexibility of a gel. Said method is described in detail below in the section
headed
"Methods of Evaluation".
The term "force to rupture" as used herein, is a measure of gel strength. Said
method is
described in detail below in the section headed "Methods of Evaluation".
The term "periodicity" as used herein, means a pattern of repeating units and
is a measure
of the distance between the start point and end point of a repeat unit of
pattern.
The non-planar topography of devices of the present invention may have
periodicity or no
periodicity. Preferred periodic patterns are sinusoidal, saw tooth or conical.
The
preferred periodicity is from about O.lmm to about lOmm, preferably from about
O.Smm
to about Smm. When the devices comprise textured first and second surfaces,
the pattern
on each surface can be the same or different and each pattern may have
periodicity or no
periodicity. If the patterns are both periodic the periodicity can be the same
or different.
In embodiments where the periodicity is the same, the pattern created by the
periodicity
on both surfaces may be aligned, so that peaks on one surface are directly
opposed to
peaks or troughs on the other, or staggered. Preferably, the pattern is
staggered as it has
been found that the devices are less visually obtrusive with staggered
patterns.
In the drawings, similar numerals have been given to like parts.
Figs. 1 a, 1 b and 1 c illustrate a first embodiment of a pre-formed,
unilamellar sheet-like
device according to the present invention, generally indicated as 10. The
sectional
perspective view of Fig. 1b is taken along line lb-lb of Fig. la. The device
10 has a peri-
meter 12 defining first and second spaced-apart surfaces 14, 16. The device 10
has a non-
planar topography on the second surface 16. The non-planar topography includes
a
delineated thickened region in the form of a rim 18 adjacent the perimeter 12
and a
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delineated thickened region in the form of a ridge 20 intermediate the
perimeter 12, as
well as a delineated thinner region 22.
In use, it is intended that the substantially planar first surface 14 would be
adjacent the
skin, hair or nails of a user. It will, of course, be appreciated that both of
the first and
second surfaces 14, 16 might be provided with a non-planar topography (not
shown).
Equally, the non-planar topography might only be provided on the first surface
14 (not
shown). The device 10 is suitable, for example, for delivering a benefit agent
to the area
of the skin under the eyes or around the mouth of a user.
The device 10 of Figs. 1 a, 1b and 1 c may have any suitable size, dependent
on its
intended use and product characteristics. The device is broadly crescent-
shaped with
overall dimensions, as defined by a notional rectangle bounding the shape, of
about 60mm
by about 27mm. The substantially crescent-shape has curved first and second
apices
proximal a first longitudinal side of the notional rectangle (not shown). The
device 10 has
dimensions of l3mm, l7mm, 20mm, 23mm and 2lmm, respectively, at angles of
22.5°,
45°, 90°, 135° and 157.5° from the junction of the
transverse mid-line of the notional
rectangle with the first longitudinal side of the notional rectangle.
Fig. 2 illustrates a second embodiment of a pre-formed, unilamellar sheet-like
device
according to the first or second aspect of the invention, generally indicated
as 110. The
device 110 has a perimeter 112 defining first and second spaced-apart surfaces
114, 116,
the device 110 having a non-planar topography comprising a delineated
thickened region
in the form of a rim 118 adjacent the perimeter 112 on the second surface 116,
and a
delineated thinner region 122, the delineated thickened and thinner regions
118, 122
simultaneously not having the same mean thickness. Rim 118 helps prevent
tearing of the
device 110 during handling and the thinner region 122 fits better, in use, to
the skin of the
user, in areas of greater curvature. Preferably, at least the thinner region
122 has, in
addition, a non-planar topography on the second surface 116 comprising a
textured
surface that is the negative image of a texturing surface, the negative image
of the
texturing surface having a texture defined by Ra of greater than 10~m (not
shown).
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Fig. 3 illustrates a third embodiment of a device according to the first or
second aspect of
the invention, generally indicated as 210. The device 210 has a perimeter 212
defining
first and second spaced-apart surfaces 214, 216, the device 210 having a non-
planar
topography comprising a delineated thickened region in the form of a ridge 220
intermediate the perimeter 212, and a delineated thinner region 222 adjacent
the perimeter
212. Ridge 220 confers greater strength and resilience to handling and the
thinner region
222 fits better, in use, to a target surface of greater curvature.
Fig. 4 illustrates, in a sectional perspective, partial view, a fourth
embodiment of a pre-
formed, unilamellar sheet-like device according to the first or second or a
third aspect of
the invention, generally indicated as 310. The device 310 has first and second
spaced-
apart surfaces 314, 316, the device 310 having a non-planar topography
comprising a
plurality of delineated thickened regions in the form of spaced-apart ridges
320
intermediate the perimeter (not shown), and a plurality of delineated thinner
regions 322.
As shown, although the device could alternatively be considered as being
textured
transverse to the ridges, there is no texturing along the length of the
ridges. However, the
illustrated non-planar topography may further comprise a textured surface,
that is the
negative image of a texturing surface, with texture defined by Ra of greater
than 10~m.
Fig. 5 shows, in a sectional perspective, partial view, a second embodiment of
a pre-
formed, unilamellar sheet-like device according to the first or third aspect
of the
invention, generally indicated as 410. The device 410 has first and second
spaced-apart
surfaces 414, 416, the first surface 414 being adjacent, in use, the skin,
hair or nails and
the second surface 416 having a non-planar topography comprising a textured
surface that
is the negative image of a texturing surface, with a texture defined by Ra of
greater than
10~m. It will be appreciated that the first and/or second surfaces 414, 416
may, in
addition, have a non-planar topography comprising at least two delineated
regions
simultaneously not having the same mean thickness (not shown). It will also be
appreciated that the first surface 414 may, optionally, have a non-planar
topography
comprising a textured surface that is the negative image of a texturing
surface, with a
texture defined by Ra of greater than 10~m (not shown).
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Figs. 6, 7a and 7b show a fifth embodiment of a pre-formed, unilamellar sheet-
like device
according to the first or second aspect of the invention, generally indicated
as 510. The
sectional view of Fig. 7b is taken along line 7b-7b of Fig. 7a. The device 510
has an
irregular perimeter S 12 defining first and second spaced-apart surfaces 514,
516. The
device 510 has a non-planar topography comprising two adjacent delineated
thinner and
thickened regions 522, 524, respectively, simultaneously not having the same
mean
thickness. In the present embodiment, the non-planar topography is on the
second surface
516. The thinner region 522 fits better in use, to the nasal area - an area of
greater
curvature.
Figs. 8 and 9 show a sixth embodiment of a pre-formed, unilamellar sheet-like
device
according to the first or second aspect of the invention, generally indicated
as 610. The
device 610 is a mask, shaped and dimensioned to substantially cover a user's
face and has
first and second spaced-apart surfaces 614, 616, the device 610 having a non-
planar
topography on the second surface 616 comprising at least two adjacent
delineated thinner
and thickened regions 622, 624, respectively, simultaneously not having the
same mean
thickness. The device 610 also comprises apertures 626 shaped and dimensioned
to
accommodate the eyes, nose and mouth of a user. The thinner regions 622 are
spaced-
apart about the perimeter 612 adjacent cut-away areas 628. In use, as
illustrated in Fig. 8,
the adj acent thinner regions 622 are contacted, so that the pre-formed,
unilamellar sheet-
like device 610 in the form of a mask substantially covers the face of a user,
to deliver at
least one benefit agent to the facial skin.
Figs. 10 and 11 show a seventh embodiment of a pre-formed, unilamellar sheet-
like
device according to the first or second aspect of the invention, generally
indicated as 710.
Device 710 is a mask, shaped and dimensioned to substantially cover the face
of a user.
Peripheral slits 730 are provided adjacent a perimeter 712. The device has a
non-planar
topography on a second surface 716, the non-planar topography comprising at
least two
adjacent delineated thinner and thickened regions 722, 724, respectively,
simultaneously
not having the same mean thickness. The thinner regions 722 are adjacent, in
use, the
eyes and nose/mouth region of a user, for the comfort of a user. Device 710
also includes
14
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
slits 732 and apertures 726, each shaped and dimensioned to accommodate the
nose and
mouth and eyes, respectively, of a user. In use, facing surfaces of peripheral
slits 730 may
be placed over each other, so that the pre-formed, unilamellar sheet-like
device 710 in the
form of a mask substantially covers the face of a user.
Fig. 12 illustrates an eighth embodiment, a device according to first, second
and third
aspects of the invention, generally indicated as 810. Device 810 has a
perimeter 812
defining first and second spaced apart surfaces 814, 816, the device 810
having a non-
planar topography comprising a delineated thickened region in the form of a
rim 818
adjacent perimeter 812 on second surface 816, and a delineated thinner region
822, the
delineated thickened and thinner regions 818, 822 simultaneously not having
the same
mean thickness. Additionally, the device has on both first and second surfaces
814, 816 a
textured surface that is the negative image of a texturing surface, with a
texture defined by
Ra of greater than 10~m.
Alternatively or additionally, the non-planar topography of the patch or mask
device 10,
110, 210, 310, 410, 510, 610, 710, 810 may comprise a symbol (not shown). The
symbol
could take the form of, for example, a trade mark, being a logo device and/or
a series of
alphanumeric characters.
Preferably, the non-planar topography, being either a textured surface or at
least two
delineated regions simultaneously not having the same mean thickness or both,
is
provided on the second surface (distal, in use, the skin, hair or nails of a
user) of the
device. More preferably, non-planar topography, being a textured surface and
at least two
delineated regions simultaneously not having the same mean thickness, is
provided on the
second surface (distal, in use, the skin, hair or nails of a user) wherein
additionally, non-
planar topography, being a textured surface, is provided on the first surface
of the device.
Polymeric Gel Forming Agents
As an essential component of the pre-formed, unilamellar sheet-like devices
described
herein, the devices comprise at least one polymeric gel forming agent. In
general, the pre-
formed, sheet-like devices of the present invention comprise less than 70%,
preferably
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
less than 50%, more preferably less than 30% and especially less than 10% by
total weight
of a polymeric gel forming agent.
The at least one polymeric gel forming agent may be naturally or synthetically
derived.
The at least one polymeric gel forming agent can be self gelling or may only
form gels in
combination with other substances. Alternatively, the at least one polymeric
gel forming
agent may be physically or chemically cross linked.
Polymeric gel forming agents may either be self gelling or may only form gels
in
combination with other substances such as sugar, alcohol, or mono- or mufti-
valent salts.
Mono- or mufti- valent salts may additionally act as gel strengthening agents
imparting
added strength to the pre-formed, unilamellar sheet-like devices herein.
Suitable canons
may be selected from the mono- or mufti- valent canons such as, for example,
potassium,
sodium, ammonium, zinc, aluminium, calcium and magnesium ions, or mixtures
thereof.
Suitable anions associated with the aforementioned canons may be selected from
chloride, citrates, sulfate, carbonate, borate and phosphate anions, or
mixtures thereof.
Physical cross linking refers to polymers having cross links which are not
chemical
covalent bonds but are of a physical nature such that there are areas in the
device having
high crystallinity or areas having a high glass transition temperature.
Chemical cross
linking refers to polymers which are linked by chemical bonds. Preferably, the
polymer is
chemically cross linked by radiation techniques such as thermal-, E beam-, UV-
, gamma
or micro-wave radiation. In addition when chemical crosslinks are formed in
the system,
a polyfunctional crosslinker and/or a free radical initiator may be present in
the premix to
initiate the crosslinking upon irradiation. Such components can be present
preferably in
quantities of up to 5% by weight.
The polymeric gel forming agents are water soluble or non-water soluble.
Preferably, the
at least one polymeric gel forming agent is a water soluble gel forming agent.
The
polymeric gel forming agents may, alternatively, comprise non-water soluble
polymeric
gel forming agents, comprising silicone polymeric gel forming agents/silicones
(organopolysiloxane resins) or block co-polymer thermoplastic elastomers.
16
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
Non-Water Soluble Polymeric Gel Forming Agents
Silicones may be described as soluble, hydroxyl-functional organopolysiloxane
resins
comprising R3Si0~z siloxane units and Si04/2 wherein R is a monovalent radical
selected from hydrocarbon and halogenated hydrocarbon radicals having 1 to 20
carbon
atoms. In the R3Si0~z and Si04/2 nomenclature, the 1/2 and 4/2 represent the
number of
half bonds on the molecule shown. For example in R3Si0/Z there is one 1/2 bond
which
is on the oxygen, the other half of that bond being bonded to some other atom.
This
group may also be described as
R
I
R- Si-O
R
Similarly, Si04/2 has four 1/2 bonds in the molecule shown, the other half of
each bond
being bonded to some other molecule. This group may also be described as
- Si-O
The term "soluble resin" as used herein, means that the gellable
organopolysiloxane can
be dissolved substantially completely, in either a hydrocarbon liquid such as
benzene,
toluene, xylene, heptane and the like or in a silicone liquid such as cyclic
or linear poly-
diorganosiloxanes. Preferably the resin is soluble in the silicone fluid.
In the formula for the silicone resin, R denotes a monovalent radical selected
from
hydrocarbon and halogenated hydrocarbon radicals, preferably having less than
20 carbon
atoms, and most preferably having from 1 to 10 carbon atoms. Examples of
suitable R
radicals include alkyl radicals, such as methyl, ethyl, propyl, pentyl, octyl,
undecyl,
octadecyl and others; cycloaliphatic radicals, such as cyclohexyl; aryl
radicals such as
phenyl, tolyl, xylyl, benzyl, alpha-methyl styryl, 2-phenylethyl and others;
alkenyl radicals
such as vinyl; and chlorinated hydrocarbon radicals such as 3-chloropropyl,
dichlorophenyl and others.
17
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
To enhance the solubility of the silicone resin in the silicone fluid, it is
desirable to select
the predominant organic radicals of the silicone resin to match the
predominant organic
radicals of the silicone fluid. Preferably, at least one-third, and more
preferably
substantially all, R radicals in the formula for the silicone resin are methyl
radicals.
Examples of preferred R3Si0~/2 siloxane units include Me3Si0~2 and PhMe2Si0/2
and
Ph2MeSi0~2 where Me denotes methyl and Ph denotes phenyl.
It is preferred that the ratio of R3Si0/Z siloxane units to Si04~2 units has a
molar ratio of
0.5 to 1.2, respectively. It is further preferred that the mole ratio of the
total R3Si0/2
siloxane units to Si04/2 units be between 0.6 and 0.8.
The silicone resin can be prepared by well known methods. It is preferably
prepared by
the silica hydrosol capping process of US-A-2,676,182 (Daudt et al.) as
modified by US-
A-3,627,851 (Brady) and US-A-3,772,247 (Flannigan); each patent being
incorporated
herein by reference to teach how to prepare soluble organopolysiloxanes which
are useful
in pre-formed, unilamellar sheet-like devices of the invention. The resulting
resin can be
used without further modification or it can be capped with trialkylsilyl
groups to reduce
the silanol content. This can be accomplished by well known methods, such as
reacting
the resin with a compound such as trimethylchlorosilane or
hexamethyldisilazane.
The silicone fluid is preferably a hydroxyl-terminated diorganopolysiloxane
polymer. The
repeat units of the silicone fluid are R2Si02/2 siloxy units wherein R is
independently
selected from the same hydrocarbon and halogenated radicals as defined above
for the
silicone resin. In general, the silicone fluid can be comprised of a single
polymer or
copolymer or it can be a mixture of two or more such polymers. The silicone
fluid can be
a liquid or gum at 25°C. It is preferred that at least 50%, and
preferably at least 85%, of
the organic radicals along the chain of the silicone fluid are methyl
radicals, which can be
distributed in any manner in the silicone fluid. Further, the silicone fluid
can comprise up
to about 10 mole percent of siloxane branching sites.
The silicone resin is preferably employed in amount of from about 40 to 70
parts by
weight in the pre-formed, unilamellar sheet-like device, and the silicone
fluid is employed
18
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
from about 30 to about 60 parts by weight, wherein the total parts of the
silicone resin and
the fluid are 100 parts. It is usually preferred that the silicone resin be
employed from
about 50 to 60 parts by weight, and correspondingly, the silicone fluid be
employed from
about 40 to 50 parts by weight, wherein the total parts by weight equals 100.
The silicone
resin and silicone fluid may be blended or condensed together to produce the
pre-formed,
unilamellar sheet-like device. Methods of condensing together the silicone
resin and
silicone fluid are well known in the art.
One preferred class of silicone resins consists of a mixture of a
trimethylsilyl-endblocked
polysilicate resin such as a silicone resin consisting of a benzene-soluble
resinous
copolymer containing silicon-bonded hydroxyl radicals and consisting
essentially of
triorganosiloxy units of the formula R13Si0/z and tetrafunctional siloxy units
of the
formula Si04/2 in a ratio of about 0.6 to 0.9 triorganosiloxy units for each
tetrafunctional
siloxy unit present in the copolymer, wherein Rl is a monovalent organic
radical
independently selected from hydrocarbon radicals of from 1 to 6 carbon atoms;
and a
silanol-endcapped polydiorganosiloxane fluid such as a polydimethylsiloxane
fluid. US-
A-2,736,721 to Dexter et al. and US-A-2,814,601 to Currie et al. are hereby
incorporated
by reference to teach of such or similar resins.
Another suitable class are those in US-A-2,857,356 (Goodwin, Jr.), which is
hereby
incorporated by reference, or resins similar to those in Goodwin. US-A-
2,857,356
discloses a silicone which consists of a mixture of ingredients comprising (i)
a co-
hydrolysis product of a trialkyl hydrolyzable silane and alkyl silicate,
wherein the co-
hydrolysis product contains a plurality of silicon-bonded hydroxy groups; and
(ii) linear,
high viscosity organopolysiloxane fluid containing silicon-bonded hydroxy
groups.
The silicone resin (i) and the silicone fluid (ii) may optionally be condensed
together
according to a procedure such as described in CA-A-711,756 to Pail, which
patent is
hereby incorporated by reference. In such a condensation reaction, the
silicone resin (i)
and silicone fluid (ii) are mixed together in the presence of a catalytic
amount of a silanol
condensation catalyst, and then the silicone resin (i) and the silicone fluid
(ii) are
condensed, for example, by heating under reflux conditions for 1 to 20 hours.
Examples
19
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
of silanol condensation catalysts are primary, secondary and tertiary amines,
carboxylic
acids of these amines and quaternary ammonium salts.
Another class are those compositions described in US-A-4,591,622 and 4,584,355
to
Blizzard et al., US-A-4,585,836 (Roman et al.), and US-A-4,655,767 (Woodard et
al.),
hereby incorporated by reference. Generally, these consist of a blend of (i) a
silicone resin
and (ii) a silicone fluid, which are chemically treated to reduce the silicone-
bonded
hydroxyl content of the blend. These may optionally be condensed, as described
previously, prior to the chemical treatment.
Silicone polymeric gel forming agents should not be confused with silicone
rubbers,
which are not useful in these applications. Silicone polymeric gel forming
agents are
usually fillerless or contain low amounts (less than 5%) of fillers. By
contrast, silicone
rubbers typically contain about 15 to 35% filler. Fillers are generally not
required in high
quantities in silicone polymeric gel forming agents, because high quantities
often cause
the silicone polymeric gel forming agents to lose tack and adhesiveness and to
increase in
dynamic viscosity, making it more difficult to apply a coating of the silicone
polymeric
gel forming agent.
Other classes of suitable silicone polymeric gel forming agents are those
described in FR-
A-2 735 024 and EP-A-0 764 441, each hereby incorporated by reference.
As another alternative, the non-water soluble polymeric gel forming agents may
be block
copolymer thermoplastic elastomers such as ABA block copolymers such as
styrene-
olefin-styrene block copolymers or ethylene-propylene block copolymers. More
preferably such polymers include hydrogenated grade Styrol/Ethylene-
Butylene/Styrol
(SEBS), Styrene/Isoprene/Styrene (SIS), and Styrol/Ethylene-Propylene/Styrol
(SEPS).
Water-soluble polymeric gel forming agents
The water-soluble polymeric gel forming agents for use in the present
invention are
selected from synthetic or natural polymers, and mixtures thereof. In general,
the pre-
formed, sheet-like devices of the present invention comprise less than 50%,
more
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
preferably less than 30% and especially less than 20% by total weight of a
water-soluble
polymeric gel forming agent.
Synthetic Polymers: Suitable synthetic polymers for use herein include non-
ionic water-
soluble polymers; acrylic acid based polymers or derivatives thereof; or
cellulose
derivatives; and mixtures thereof. The synthetic polymers useful herein can be
categorised by their charge or constituent monomers. However, it is to be
understood that
the classifications herein are made for the sake of convenience and there may
be overlap
between the categories.
Non-Ionic Water-Soluble Polymers: Suitable non-ionic water-soluble polymers
for use
herein include polydimethyl acrylamide, polyvinyl pyrrolidones, polyethylene
glycol
monomethacrylate, poly-2-ethyl-2-oxazoline, polyvinyl alcohol, polyethylene
oxide, poly-
vinyl ethers, copolymers of polyvinylethers and polyvinylpyrrolidone and
derivatives
thereof, methyl vinyl ether and malefic anhydride, copolymers of ethylene and
malefic
anhydride, and mixtures thereof. The uncrosslinked polymer includes repeating
units
derived from vinyl alcohols, vinyl ethers and their copolymers, carboxy vinyl
monomer,
vinyl ester monomers, esters of carboxy vinyl monomers, vinyl amide monomers,
hydroxy vinyl monomers, cationic vinyl monomers containing amines or
quaternary
groups, N-vinyl lactam monomer and sulphonated polymers such as acrylamide
sulphonated polymers and mixtures thereof. Alternatively, the uncrosslinked
polymer
may be a homopolymer or copolymer of a polyvinyl ether, or a copolymer derived
from
half ester of malefic ester. Similarly any other compatible polymer monomer
units may be
used as copolymers such as, for example, polyvinyl alcohol and polyacrylic
acid or
ethylene and vinyl acetate.
Acrylic Acid Based Polymers or Derivatives thereof: Suitable acrylic acid
based polymers
or derivatives thereof include polymers of acrylic acid,
hydroxyethylmethacrylate,
methoxydiethoxyethyl methacrylate, and hydroxydiethoxyethyl methacrylate;
salts of
polyacrylic acids such as ammonium polyacrylate and sodium polyacrylate;
polymers of
2-acrylamido-2-methylpropanesulphonic acid or its salts (AMPS); copolymers of
acrylamide and N,N'-methylene bisacrylamide; and polyacrylamide, or mixtures
thereof.
21
W~ ~l/01951 CA 02373980 2002-O1-07 pCT~JS00/18108
Further suitable polymers for use herein include copolymers based on 2-
hydroxyethylmethacrylate ("HEMA") which include the copolymer of "HEMA" and
one
or more co-monomers as described in US-A-5,804,107 at column 14, lines 36-67
and
column 1 S, lines 1-34; incorporated herein by reference.
Cellulose Derivatives: Examples of cellulose derivatives suitable for use
herein include
carboxymethyl hydroxyethylcellulose, carboxymethyl cellulose,
carboxymethylcellulose
sodium, cellulose acetate propionate carboxylate, hydroxyethylcellulose,
hydroxyethyl
ethylcellulose, hydroxypropylcellulose, methyl cellulose, methylcellulose
sodium,
hydroxypropyl methylcellulose, methyl hydroxyethylcellulose, microcrystalline
cellulose,
sodium cellulose sulfate, and mixtures thereof. Also useful herein are the
alkyl
substituted celluloses. In these polymers, the hydroxy groups of the cellulose
polymer is
hydroyxalkylated (preferably hydroxyethylated or hydroxypropylated) to form a
hydroxyalkylated cellulose which is then further modified with a Cl0-C30
straight chain
or branched chain alkyl group through an ether linkage. Typically these
polymers are
ethers of Cl0-C30 straight or branched chain alcohols with
hydroxyalkylcelluloses.
Examples of alkyl groups useful herein include those selected from the group
consisting
of stearyl, isostearyl, lauryl, myristyl, cetyl, isocetyl, cocoyl (i.e. alkyl
groups derived from
the alcohols of coconut oil), palmityl, oleyl, linoleyl, linolenyl,
ricinoleyl, behenyl; and
mixtures thereof. Preferred among the alkyl hydroxyalkyl cellulose ethers is
the material
given the CTFA designation cetyl hydroxyethylcellulose, which is the ether of
cetyl
alcohol and hydroxyethylcellulose. This material is sold under the tradename
Natrosol~
CS Plus from Aqualon Corporation.
Natural Polymers: Suitable natural polymers for use herein include gelatin,
poly-
saccharides, and mixtures thereof. Polysaccharides for use herein are
preferably selected
from red seaweed polysaccharides; glucomannans; galactomannans; fermentation
polysaccharides, or derivatives thereof; brown seaweed polysaccharides;
extracts of
marine invertebrates; starch, or derivatives thereof; natural fruit extracts;
plant fiber
derivatives; kelp; natural plant exudates; resinous gums; and mixtures
thereof. When the
devices herein contain one or more polysaccharides as the water-soluble
polymeric gel
22
CA 02373980 2002-O1-07
WO 01/01951 PCT/LTS00/18108
forming agent(s), the devices comprise less than 10%, preferably less than 5%
and more
preferably less than 3% by total dry weight of a polysaccharide or mixtures
thereof.
Gelatin: When gelatin is used in the devices herein, a high-molecular weight
gelatin is
combined with a low-molecular weight one to control the solubility. A gelatin
having a
low molecular weight of 20,000 or less is poor in gelling ability.
Brown Seaweed Polysaccharides: Polysaccharides which are classified as brown
seaweed
polysaccharides are isolated by extraction from various species of
Phaebophyceae.
Suitable brown seaweed polysaccharides for use herein include algin, alginic
acid,
ammonium alginate, calcium alginate, potassium alginate, sodium alginate,
propylene
glycol alginate, and mixtures thereof.
Red Seaweed Polysaccharides: Polysaccharides which are classified as red
seaweed
polysaccharides are isolated from marine plant species belonging to the class
of
Rhodophyceae. Red seaweed polysaccharides provide mechanical strength to an
aqueous
gel. Suitable red seaweed polysaccharides for use in the present invention
include agar
known in the industry under the (CTFA) trade designation as agar agar flake
derived from
various Gelidium plant species or closely related red algae commercially
available as
"Agar Agar 100" or "Agar Agar 150" from TIC Gums (Belcamp, MD, USA) or "Agar
Agar K-100" from Gumix International Inc. (Fort Lee, NJ, USA); agarose
commercially
available as "Sea Plaque~" from FMC (Philadelphia, PA, USA) and "Agarose Type
1-b"
from Sigma - Aldrich Co. Ltd. (Poole, UK); carrageenan, comprising the
fractions
lambda-, iota- and kappa- which are the water extracts obtained from various
members of
the Gigartinaceae or Solieriaceae families, known in the industry under the
(CTFA) trade
designation as chondrus, commercially available as "Gelcarin~ LA", "Seakem~
3/LCM",
or "Viscarin~ XLV", all from FMC (Philadelphia, PA, USA); and furcellaran
available
from Gum Technology Corporation (Tucson, Arizona, USA) and Continental
Colloids
Inc. (Chicago, IL, USA), or mixtures thereof. Preferably, the red seaweed
polysaccharide
for use herein is selected from agar, agarose, kappa-carrageenan and
furcellaran, or
mixtures thereof.
23
WO ~l/01951 CA 02373980 2002-O1-07 pCT~JS00/18108
Glucomannan: Glucomannans are polysaccharides which comprise an essentially
linear
backbone of glucose and mannose residues. Glucomannans have short side
branches
attached to the linear backbone and acetyl groups are randomly present at the
C-6 position
of a sugar unit. The acetyl groups are generally found on one per six sugar
units to one
per twenty sugar units. Suitable glucomannans or derivatives thereof for use
herein have
a ratio of mannose to glucose of from about 0.2 to about 3. Preferred
glucomannans for
use herein include konjac mannan, which is the generic name for the flour
formed from
grinding the tuber root of the Amorphophallus konjac plant (elephant yam),
commercially
available under the trade name "Nutricol~ konjac flour" from FMC
(Philadelphia, PA,
USA); and deacetylated konjac mannan; or mixtures thereof.
Galactomannan: Galactomannans are vegetable reserve polysaccharides which
occur in
the endosperm cells of numerous seeds of Leguminosae. The collective term
"galacto-
mannan" comprises all polysaccharides which are built up of galactose and
mannose
residues. Galactomannans comprise a linear backbone of (1,4)-linked 13-D-manno-
pyranosyl units. To these rings are attached as branches, isolated
galactopyranose
residues by a-(1,6)-glucoside bonds. Galactomannans may in addition also
contain minor
amounts of other sugar residues. Suitable galactomannans for use herein are
fenugreek
gum; lucern; clover; locust bean gum known for example in the industry under
the
(CTFA) trade designation as carob bean gum, available as "Seagul L" from FMC
(Philadelphia, PA, USA); tara gum available from Starlight Products (Rouen,
France) or
Bunge Foods (Atlanta, GA, USA); guar gum derived from the ground endosperms of
Cyamopsis tetragonolobus, available as "Burtonite V7E" from TIC Gums (Belcamp,
MD,
USA), "Jaguar C" from Rhone-Poulenc (Marietta, GA, USA), or "Supercol" from
Aqualon (Wilmington, DE, USA); and cassia gum available from Starlight
Products
(Rouen, France), or mixtures thereof. Preferably, the galactomannans for use
herein have
an average one of every 1 to about 5 mannosyl units substituted with a (1,6)-
linked-a-D-
galactopyranosyl unit and are selected from guar gum, locust bean gum and
cassia gum, or
mixtures thereof.
24
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
Fermentation Polysaccharides or derivatives thereof: Fermentation
polysaccharides are
polysaccharides which are commercially produced by the fermentation of micro-
organisms in a medium containing a carbon and nitrogen source, buffering
agent, and
trace elements. Suitable fermentation polysaccharides or derivatives thereof,
for use in
the present invention include gellan gum known in the industry under the
(CTFA) trade
designation as gum gellan, a high molecular weight hetero polysaccharide gum
produced
by a pure-culture fermentation of a carbohydrate with Pseudomonas elodea,
commercially
available as "Kelcogel" from Kelco (San Diego, CA, USA); xanthan gum which is
a high
molecular weight hetero polysaccharide gum produced by a pure-culture
fermentation of a
carbohydrate with Xanthomonas campestris, known in the industry under the
(CTFA)
trade designation as xanthan, commercially available for example as "Keltrol
CG
1000/BT/F/GM/RD/SF/T/TF", from Calgon (Pittsburgh, PA, USA), or "Kelzan" from
Kelco (San Diego, CA, USA); natto gum; pullulan; rhamsan gum; curdlan;
succinoglycan; welan gum; dextran, commercially available as "Sephadex G-25"
from
Pharmacia Fine Chemicals (Piscataway, NJ, USA) and derivatives thereof; and
sclerotium
gum, commercially available as "Amigel" from Alban Muller International
(Montreil,
France), or mixtures thereof. Preferred fermentation polysaccharides or
derivatives
thereof are selected from gellan gum and xanthan gum, or mixtures thereof.
More
preferably the fermentation polysaccharide or derivative thereof is xanthan
gum.
Extracts of Marine Invertebrates: Polysaccharides derived from marine
invertebrates,
specifically the exoskeleton of such invertebrates, consist chiefly of N-
acetyl-D-
glucosamine residues. Examples of such polysaccharides suitable for use herein
include
chitosan, available e.g. as "Marine Dew" from Ajinomoto (Teakneck, NJ, USA);
and
hydroxypropyl chitosan available e.g. as "HPCH Liquid" from Ichimaru Pharcos
(Yamagata Gun Gifu-Pref, Japan) and derivatives; or mixtures thereof.
Starch or Derivatives thereof: Starches are polysaccharides which consist of
various
proportions of two glucose polymers, amylose and amylopectin. Suitable
materials for
use herein include starch; amylopectin; and dextrin commercially available as
"Nadex
360" from National Starch (Bridgewater, NJ, USA) and derivatives; or mixtures
thereof.
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
Natural Fruit Extracts: Examples of natural fruit extracts suitable for use
herein include
pectin; and arabian; or mixtures thereof.
Plant Fiber Derivatives: A suitable example of a plant fiber derivative for
use herein is
cellulose.
Natural Plant Exudates: Suitable polysaccharides obtained from natural plant
exudates for
use herein include karaya gum, tragacanth gum, arabic gum, tamarind gum, and
ghatty
gum, or mixtures thereof.
Resinous Gums: Examples of resinous gums suitable for use herein include
shellac gum
which is obtained from the resinous secretion of the insect Laccifer
(Tachardia) lacca;
damar gum; copal gum and rosin gum; or mixtures thereof.
Preferably, the pre-formed, unilamellar sheet-like devices herein comprise a
mixture of
water-soluble polymeric gel forming agents. The mixture is selected from one
or more
non-ionic water-soluble polymers; one or more acrylic acid based polymers or
derivatives
thereof; one or more polysaccharides; and mixtures thereof. For example, a
preferred
water-soluble polymeric gel forming agent mixture herein may comprise a
polysaccharide
and a non-ionic water-soluble polymer or, alternatively, it may comprise two
polysaccharides. More preferably, the water-soluble polymeric gel forming
agent is a
polysaccharide mixture, wherein the polysaccharide mixture comprises (1) at
least one red
seaweed polysaccharide; brown seaweed polysaccharide; or mixtures thereof; and
(2) at
least one fermentation polysaccharide; galactomannan; glucomannan; natural
plant
exudate; or natural fruit extract; and derivatives or mixtures thereof. Even
more
preferably, the water-soluble polymeric gel forming agent of the devices of
the present
invention is a polysaccharide mixture comprising (1) at least one red seaweed
polysaccharide; and (2) at least one fermentation polysaccharide; glucomannan;
or
galactomannan; and derivatives or mixtures thereof. ,
In a preferred embodiment, the water-soluble polymeric gel forming agent of
the present
invention is a polysaccharide mixture, comprising a red seaweed polysaccharide
and a
glucomannan or a galactomannan. Without being limited by theory, it is
believed that in
such a polysaccharide mixture, the incorporation of a glucomannan or
galactomannan
26
WO 01/01951 CA 02373980 2002-O1-07 pCT~S00/18108
may complement the red seaweed polysaccharide, and contribute to the
mechanical
strength of the pre-formed, unilamellar sheet-like devices of the present
invention.
Further, from the viewpoint of providing improved mechanical properties and
preferably,
a low level of syneresis from a pre-formed, unilamellar sheet-like device,
preferably, the
ratio of red seaweed polysaccharide to glucomannan or galactomannan in the
polysaccharide mixture is from about 20:1 to about 1:5 and more preferably
from about
5:1 to about 1:2.
When the polymeric gel forming agents are natural in origin, all such gels
undergo
syneresis, as herein before defined, to some degree. Syneresis provides one
mechanism
for the delivery of a benefit agent to a target area. The liquid layer exuded
onto the
surface of the coherent gel phase is readily available for diffusion,
facilitating a short wear
time of the device. The pre-formed, unilamellar sheet-like devices of the
present
invention desirably display a low level of syneresis and preferably, the
devices herein are
moist to the touch. An excessive amount of syneresis results in an ineffective
and
unattractive product.
The present inventors have also found that, in order to attain a
polysaccharide gel with
desirable mechanical properties of strength and flexibility when
polysaccharide polymeric
gel forming agents selected for their strength are combined with agents
imparting a
plasticising effect, the total level of polysaccharide polymeric gel forming
agents should
be kept as low as possible without compromising on mechanical strength and
flexibility.
It is believed that low total polysaccharide levels impart an open gel
structure such that
the other components of the original gel are not as tightly bound within the
gel network
and are freely available for diffusion.
The pre-formed, unilamellar sheet-like devices of the present invention
preferably display
a low level of syneresis and are moist to the touch. As aforementioned, while
a device
comprising a gel will always undergo some syneresis, an excessive amount of
syneresis
results in an ineffective and unattractive product.
27
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WO 01/01951 PCT/US00/18108
Water
In a preferred embodiment of the present invention in which the at least one
polymeric gel
forming agent is water-soluble, the pre-formed, unilamellar sheet-like devices
of the
present invention include water. The total water content, if present, of a pre-
formed,
unilamellar sheet-like device of the present invention is from about 20% to
about 99.5%,
preferably from about 30% to about 95%, more preferably from about 40% to
about 85%
by weight of the device.
Substrate
The pre-formed, unilamellar sheet-like devices of the present invention are
self
supporting and do not require supporting or strengthening by an occlusive or
non-
occlusive backing material often referred to as a substrate. However, a
substrate, if
present, may be combined with a unilamellar sheet-like device and would confer
further
support or strengthening. Preferably the substrate is non-occlusive. In
addition, a
substrate is particularly useful when the device according to the present
invention has a
large surface area. If the substrate is to be used to confer fiu-ther support
or strengthening,
the substrate will be sufficiently compatible with the device of the present
invention, so as
not to delaminate therefrom.
A wide variety of materials can be used as the substrate. The following
characteristics are
desirable: (i) sufficient wet strength for use, (ii) sufficient flexibility,
(iii) sufficient loft
and porosity, (iv) sufficient hydrophilicity such that the gel mixture may
diffuse and
infiltrate into the substrate, (v) sufficient compatibility with the mixture
to prevent de-
lamination, (vi) sufficient transparency or translucency, and (vii)
appropriate size.
Alternatively, the substrate may be used as a texturing surface. If the
substrate is to be
used as a texturing surface, the substrate will, preferably, delaminate easily
from the
device.
Examples of suitable substrates meeting one or more of the above criteria and
useful
herein include woven and nonwoven materials; polymeric sheet materials such as
formed
films; and paper substrates.
28
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
Benefit Agents
As an essential component of the present invention, the pre-formed,
unilamellar sheet-like
devices herein comprise a safe and effective amount of at least one benefit
agent. The
term "benefit agent" as used herein, means an active ingredient which provides
a cosmetic
and/or therapeutic effect to the area of application. Included in this
definition of benefit
agents are the categories listed below as well as, for example, vitamins, and
humectants.
The term "safe and effective amount" as used herein, means an amount of a
benefit agent
high enough to modify the condition to be treated or to deliver the desired
skin, hair or
nail benefit, but low enough to avoid serious side effects, at a reasonable
benefit to risk
ratio within the scope of sound medical judgement. What is a safe and
effective amount
of the benefit agent will vary with the specific agent, the ability of the
agent to penetrate
through the skin or into, or onto the hair and/or nails; the user's age, the
user's health
condition, the condition of the skin, hair or nails of the user, and other
like factors.
The benefit agents include their pharmaceutically-acceptable salts and by
"pharmaceutically-acceptable salts" are meant any of the commonly-used salts
that are
suitable for use in contact with the tissues of humans without undue toxicity,
irntation,
incompatibility, instability, irritation, allergic response, and the like.
In general, the pre-formed, unilamellar sheet-like devices of the present
invention
comprise from about 0.01% to about 60%, preferably from about 0.05% to about
30% and
most preferably from about 0.1% to about 20% by weight of the device of at
least one
benefit agent, or mixtures thereof.
The benefit agents useful herein can be categorised by their cosmetic or
therapeutic
benefit or their postulated mode of action. However, it is to be understood
that the benefit
agents useful herein can in some instances provide more than one cosmetic or
therapeutic
benefit or operate via more than one mode of action. Therefore,
classifications herein are
made for the sake of convenience and are not intended to limit the benefit
agent to that
particular application or applications listed. The following benefit agents
are useful in the
pre-formed, unilamellar sheet-like devices of the present invention.
29
VVO 01/019$1 CA 02373980 2002-O1-07 pCT~S00/18108
Anti-Acne Actives: Anti-acne actives can be effective in treating and
preventing acne
vulgaris, a chronic disorder of the pilosebaceous follicles. The condition
involves
inflammation of the pilosebaceous apparatus thereby resulting in lesions,
which may
include papules, pustules, cysts, comedones, and severe scarring. The bacteria
Corynebacterium aches and Staphylococcus epidermis are usually present in the
pustular
contents. Examples of useful anti-acne actives include the keratolytics
described in
W098/18444 incorporated herein by reference. Further useful actives include
retinoids
such as retinoic acid (e.g., cis and/or trans) and its derivatives (e.g.,
esters); retinol and its
esters (e.g., retinyl propionate, retinyl acetate); abietic acid, adapalene,
tazarotene,
allantoin, aloe extracts, arbietic acid and its salts, ASEBIOL (from
Laboratories
Serobiologiques, Somerville, NJ), azaleic acid, barberry extracts, bearberry
extracts,
belamcanda chinensis, benzoquinolinones, benzoyl peroxide, berberine,
BIODERMINE
(from Sederma, Brooklyn, NY), bioflavonoids as a class, bisabolol, s-
carboxymethyl
cysteine, carrot extracts, cassin oil, clove extracts, citral, citronellal,
climazole,
COMPLETECH MBAC-OS (from Lipo, Paterson, NJ), CREMOGEN M82 (from
Dragoco, Totowa, NJ), cucumber extracts, dehydroacetic acid and its salts,
dehydroepi-
androsterone and its sulfate derivative, dichlorophenyl imidazoldioxolan, d,l-
valine and
its esters, DMDM hydantoin, erythromycin, escinol, ethyl hexyl monoglyceryl
ether, ethyl
2-hydroxy undecanoate, farnesol, farnesyl acetate, geraniol, geranyl geraniol,
glabridin,
gluconic acid, gluconolactone, glyceryl monocaprate, glycolic acid, grapefruit
seed
extract, gugu lipid, HEDERAGENIN (from Maruzen, Morristown, NJ), hesperitin,
hinokitol, hops extract, hydrogenated rosin, 10 hydroxy decanoic acid,
ichthyol,
interleukin 1 alpha antagonists, KAPILARINE (from Greentech, Saint Beauzire,
France),
ketoconazole, lactic acid, lemon grass oil, LOCHOCHALCONE LR15 (from Maruzen,
Mornstown, NJ), linoleic acid, LIPACIDE C8C0 (from Seppic, Paris, France),
lovastatin,
4 methoxysalicylic acid, metronidazole, minocycline, mukurossi, neem seed oil,
niacinamide, nicotinic acid and its esters, nisin, panthenol, 1-pentadecanol,
peonia extract,
peppermint extract, phelladendron extract, 2-phenyl-benzothiophene
derivatives,
phloretin, PHLOROGINE (from Secma, Pontrieux, France), phosphatidyl choline,
proteolytic enzymes, quercetin, red sandalwood extract, rosemary extract,
rutin, sage
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
extract, salicin, salicylic acid, serine, skull cap extract, siber hegner
extract, Siberian
saxifrage extract, silicol, sodium lauryl sulfate, sodium sulfoacetamide,
SOPHORA
EXTRACT (from Maruzen, Morristown, NJ), sorbic acid, sulfur, sunder vati
extract, tea
tree oil, tetra hydroabietic acid, threonine, thyme extract, tioxolone,
tocopherol and its
esters, trehalose 6-undecylenoate, 3 tridecene-2-ol, triclosan, tropolone,
UNITRIENOL
T27 (from Unichem, Chicago, IL), vitamin D3 and its analogs, white thyme oil,
willow
bark extract, wogonin, ylang ylang, zinc glycerolate, zinc linoleate, zinc
oxide, zinc
pyrithione, zinc sulfate, zwitterionic surfactants (e.g. cetyl dimethyl
betaine) and mixtures
thereof.
Emollients: Examples of emollients useful herein include mineral oil,
petrolatum, C7-
C40 branched chain hydrocarbons, C1-C30 alcohol esters of C1-C30 carboxylic
acids,
C1-C30 alcohol esters of C2-C30 dicarboxylic acids, monoglycerides of Cl-C30
carboxylic acids, diglycerides of Cl-C30 carboxylic acids, triglycerides of C1-
C30
carboxylic acids, ethylene glycol monoesters of C1-C30 carboxylic acids,
ethylene glycol
diesters of Cl-C30 carboxylic acids, propylene glycol monoesters of C1-C30
carboxylic
acids, propylene glycol diesters of C1-C30 carboxylic acids, C1-C30 carboxylic
acid
monoesters and polyesters of sugars, for example, sefa cottonate (sucrose
polycottonseedate), polydialkylsiloxanes, polydiarylsiloxanes,
polyalkarylsiloxanes,
cyclomethicones having 3 to 9 silicon atoms, vegetable oils, hydrogenated
vegetable oils,
polypropylene glycol C4-C2p alkyl ethers, di Cg-C30 alkyl ethers, and mixtures
thereof.
These agents are described in more detail in W098/18444, which is incorporated
herein
by reference.
Non-Steroidal Anti-Inflammatory Actives (NSAIDS): Examples of suitable NSA>DS
and
their esters for use herein are described in W098/18444, incorporated herein
by reference.
Further non-limiting examples of non-steroidal anti-inflammatory drugs
(NSA>DS)
include flufenamic acid; panthenol and ether and ester derivatives thereof
e.g. panthenol
ethyl ether, panthenyl triacetate; pantothenic acid and salt and ester
derivatives thereof,
especially calcium pantothenate; aloe vera, bisabolol, allantoin and compounds
of the
liquorice (the plant genus/species Glycyrrhiza glabra) family, including
glycyrrhetic acid,
31
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
glycyrrhizic acid, and derivatives thereof e.g. salts such as ammonium
glycyrrhizinate
and esters such as stearyl glycyrrhetinate.
Topical Anaesthetics: Examples of suitable topical anaesthetic drugs for use
herein are
benzocaine and bupivacaine. Further suitable examples are described in
W098/18444,
incorporated herein by reference.
Artificial Tanning A gents and Accelerators: Artificial tanning agents can
help in
simulating a natural suntan by increasing melanin in the skin or by producing
the
appearance of increased melanin in the skin. Non-limiting examples of
artificial tanning
agents and accelerators include glucose tyrosinate and acetyl tyrosine,
brazilin, caffeine,
coffee extracts, DNA fragments, isobutyl methyl xanthine, methyl xanthine,
PHOTOTAN
(from Laboratoires Serobiologiques, Somerville, NJ), prostaglandins, tea
extracts,
theophylline, UNIPERTAN P2002 and UNIPERTAN P27 (from Unichem, Chicago, IL);
and mixtures thereof. Further useful artificial tanning agents herein are
described in
W098/18444 incorporated herein by reference.
Antiseptics: Examples of suitable antiseptics for use herein include alcohols,
benzoate,
sorbic acid, and mixtures thereof.
Anti-microbial and Anti-fungal Actives: Anti-microbial and anti-fungal actives
can be
effective to prevent the proliferation and growth of bacteria and fungi. Non-
limiting
examples of antimicrobial and antifungal actives include ketoconazole,
ciclopirox,
benzoyl peroxide, tetracycline, azelaic acid and its derivatives, ethyl
acetate,
alantolactone, isoalantolactone, alkanet extract (alaninin), anise, arnica
extract (helenalin
acetate and 11, 13 dihydrohelenalin), aspidium extract (phloro, lucinol
containing
extract), bayberry extract (berberine chloride), bay sweet extract, bayberry
bark extract
(myricitrin), benzalkonium chloride, benzethonium chloride, benzoic acid and
its salts,
benzoin, benzyl alcohol, blessed thistle, bletilla tuber, bloodroot, bois de
rose oil,
burdock, butyl paraben, cade oil, CAE (from Ajinomoto, Teaneck, NJ), cajeput
oil,
cangzhu, caraway oil, cascarilla bark (sold under the trade name ESSENTIAL
OIL),
cedarleaf oil, chamomille, chaparral, chlorophenesin, chlorxylenol, cinnamon
oil,
citronella oil, clove oil, dehydroacetic acid and its salts, dill seed oil,
DOWICIL 200
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WO 01/01951 CA 02373980 2002-O1-o7 pCT/LJS00/18108
(from Dow Chemical, Midland, MI), echinacea, elenolic acid, epimedium, ethyl
paraben,
FO-TI, galbanum, garden burnet, GERMALL 115 and GERMALL II (from ISP-Sutton
Labs, Wayne, NJ), german chamomile oil, giant knotweed, GLYDANT and GLYDANT
PLUS (from Lonza, Fairlawn, NJ), grapefruit seed oil, hexamidine
diisethionate,
hinokitiol, honey, honeysuckle flower, hops, immortelle, iodopropynl butyl
carbamide
(available from Lonza, Fairlawn, NJ), isobutyl paraben, isopropyl paraben, JM
ACTICARE (from Microbial Systems International, Nottingham, UK), juniper
berries,
KATHON CG (from Rohm and Haas, Philadelphia, PA, USA), labdanum, lavender,
lemon balm oil, lemon grass, methyl paraben, mint, mume, mustard, myrrh, neem
seed
oil, ortho phenyl phenol, OLIVE LEAF EXTRACT (from Bio Botanica, Hauppauge,
NY), parsley, patchouli oil, peony root, PHENONIP (from Nipa Labs, Wilmington,
DE),
phytosphingosine, pine needle oil, PLANSERVATIVE (from Campo Research, Raffles
Quay, Singapore), propyl paraben, purslane, quillaira, rhubarb, rose geranium
oil,
rosemary, sage, salicylic acid, sassafras, savory, Sichuan lovage, sodium meta
bisulfate,
sodium sulfite, SOPHOLIANCE (from Soliance, Compiegne, France), sorbic acid
and its
salts, sphingosine, stevia, storax, tannic acid, tea, tea tree oil (cajeput
oil), thyme,
triclosan, triclocarban, tropolone, turpentine, umbelliferone (antifungal),
and yucca, or
mixtures thereof. Further examples of anti-microbial and antifungal actives
useful herein
are described in W098/18444 incorporated herein by reference.
Skin Soothin~ents: Skin soothing agents can be effective in preventing or
treating
inflammation of the skin. The soothing agent enhances the skin appearance
benefits of
the present invention, e.g., such agents contribute to a more uniform and
acceptable skin
tone or colour. Non-limiting examples of skin soothing agents include
absinthium,
acacia, aescin, alder buckthorn extract, allantoin, aloe, APT (from
Centerchem, Stamford,
CT), arnica, astragalus, astragalus root extract, azulene, BAICALIN SR 15
(from Barnet
Products Dist., Englewood, NJ), baikal skullcap, baizhu, balsam Canada, bee
pollen,
BIOPHYTEX (from Laboratories Serobiologiques, Somerville, NJ), bisabolol,
black
cohosh, black cohosh extract, blue cohosh, blue cohosh extract, boneset,
borage, borage
oil, borage seed oil, bromelain, calendula, calendula extract, CANADIAN
WILLOWBARK EXTRACT (from Fytokem), candelilla wax, cangzhu, canola
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WO 01/01951 PCT/US00/18108
phytosterols, capsicum, carboxypeptidase, celery seed, celery stem extract,
CENTAURILTM (from Sederma, Brooklyn, NY), centaury extract, chamazulene,
chamomile, chamomile extract, chaparral, chaste tree, chaste tree extract,
chickweed,
chicory root, chicory root extract, chirata, chishao, collodial oatmeal,
comfrey, comfrey
extract, CROMIST CM GLUCAN (from Croda, Parsippany, NJ), darutoside, dehurian
angelica, DEVIL'S CLAW (from MMP Plainfield, NJ), divalent metals (such as
magnesium, strontium, manganese), doggrass, dogwood, EASHAVE (from Pentapharm,
Basel, Switzerland), eleuthero, ELHIBIN (from Pentapharm, Basel, Switzerland),
ENTELINE 2 (from Secma, Pontrieux, France), ephedra, epimedium, esculoside,
evening
primrose, eyebright, EXTRACT LE-100 (from Sino Lion, World Trade Centre, NY),
fangfeng, feverfew, ficin, forsythia fruit, ganoderma, gaoben, GATULINE A
(from
Gattefosse, Saint Priest, France), gentian, germanium extract, gingko bilboa,
ginkgo,
ginseng extract, goldenseal, gorgonian extract, gotu kola, grape fruit
extract, guaiac wood
oil, guggal extract, helenalin esters, henna, honeysuckle flower, horehound
extract,
horsechestnut, horsetail, huzhang, hypericum, ichthyol, immortelle, ipecac,
job's tears,
jujube, kola extract, LANACHRYS 28 (from Lana Tech, Paris, France), lemon oil,
lianqiao, licorice root, ligusticum, ligustrum, lovage root, luffa, mace,
magnolia flower,
manjistha extract, margaspidin, margaspidin, matricin, MICROAT IRC (from
Nurture,
Missoula, MT) mints, mistletoe, MODULENE (from Seporga, Sophia Antipolis,
France),
mung bean extract, musk, oat extract, orange, panthenol, papain, peony bark,
peony root,
PHYTOPLENOLIN (from Bio Botanica, Hauppauge, NY), PREREGEN (from
Pentapharm, Basel, Switzerland), purslane, QUENCH T (from Centerchem,
Stamford,
CT), quillaia, red sage, rehmannia, rhubarb, rosemary, rosmarinic acid, royal
jelly, rue,
rutin, sandalwood, sanqi, sarsaparilla, saw palmetto, SENSILINE (from Silab,
Brive,
France), SIEGESBECKIA (from Sederma, Brooklyn, NY), stearyl glycyrrhetinate,
STIMLJTEX (from Pentapharm, Basel, Switzerland), storax, sweet birch oil,
sweet
woodruff, tagetes, tea extract, thyme extract, tienchi ginseng, tocopherol,
tocopheryl
acetate, triclosan, turmeric, urimei, ursolic acid, white pine bark, witch
hazel, xinyi,
yarrow, yeast extract, yucca, and mixtures thereof.
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Sunscreenin~ A, eiritS: Examples of suitable sunscreening agents useful herein
are
described in W098/18444, incorporated herein by reference. Further examples of
sunscreens which are useful herein include diethanolamine p-methoxycinnamate,
dioxybenzone, ethyl dihydroxypropyl PABA, glyceryl aminobenzoate, lawsome and
dihydroxyacetone, menthyl anthranilate, methyl anthranilate, octyl dimethyl
PABA, red
petroleum, sulisobenzone, triethanolamine salicylate, and mixtures thereof.
Skin Barrier Repair Aids: Skin barrier repair actives are those skin care
actives which can
help repair and replenish the natural moisture barrier function of the
epidermis. Non-
limiting examples of skin barner repair aids include brassicasterol, caffeine,
campesterol,
canola derived sterols, CERAMAX (from Quest, Ashford, England), CERAMIDE
H03TM (from Sederma, Brooklyn, NY), CERAMIDE II and CERAMIDE III (from
Quest, Ashford, England), CERAMIDE IIIB (available from Cosmoferm, Delft,
Netherlands), CERAM>DE IS 3773 (from Laboratories Serobiologiques, Somerville,
NJ),
CERAMINOL (from Inocosm, Chatenay Malabry, France), CERASOL and CEPHALIP
(from Pentapharm, Basel, Switzerland), cholesterol, cholesterol
hydroxystearate,
cholesterol isostearate, 7-dehydrocholesterol, DERMATEIN BRC and DERMATEIN
GSL (from Hormel, Austin, MN), ELDEW CL 301 (from Ajinomoto, Teaneck, NJ),
ELDEW PS 203 (from Ajinomoto, Teaneck, NJ), FITROBROSIDE (from Pentapharm,
Basel, Switzerland), GENEROL 122 (from Henkel, Hoboken, NJ), glyceryl serine
amide,
lactic acid, LACTOMIDE (from Pentapharm, Basel, Switzerland), lanolin, lanolin
alcohols, lanosterol, lauric acid n laurylglucamide, lipoic acid, n-acetyl
cysteine, serine, n-
acetyl-L-serine, n-methyl-L-serine, NET STEROL-ISO (from Barnet Products,
Englewood, NJ), niacinamide, nicotinic acid and its esters, nicotinyl alcohol,
palmitic
acid, panthenol, panthetine, phosphodiesterase inhibitors, PHYTO/CER (from
Intergen,
Purchaser, NY), PHYTOGLYCOLIPID MILLET EXTRACT (from Barnet Products
Distributor, Englewood, NJ), PHYTOSPHINGOSINE (from Gist Brocades, King of
Prussia, PA), PSENDOFILAGGRIN (from Brooks Industries, South Plainfield, NJ),
QUESTAMIDE H (from Quest, Ashford, England), serine, stigmasterol, sitosterol,
stigmastanol, soybean derived sterols, sphingosine, s-lactoyl glutathione,
stearic acid,
SUPER STEROL ESTERS (from Croda, Parsippany, NJ), thioctic acid, THSC
CA 02373980 2002-O1-07
WO 01/01951 PCT/LTS00/18108
CERAMIDE OIL (from Campo Research, Raffles Quay, Singapore), trimethyl
glycine,
tocopheryl nicotinate, vitamin D3 and analogs or derivatives thereof, and Y2
(from Ocean
Pharmaceutical), or mixtures thereof.
Anti-Wrinkle and Anti-Skin Atroph~Actives: Anti-wrinkle and anti-skin atrophy
actives
can be effective in replenishing or rejuvenating the epidermal and/or dermal
layer. These
actives generally provide these desirable skin care benefits by promoting or
maintaining
the natural process of desquamation and/or building skin matrix components
(e.g.,
collagen and glycosaminoglycans). Non-limiting examples of antiwrinkle and
anti-skin
atrophy actives include nicotinic acid and its esters, nicotinyl alcohol,
estrogens and
estrogenic compounds, or mixtures thereof. Further suitable antiwrinkle and
anti-skin
atrophy actives useful herein are described in W098/18444 incorporated herein
by
reference.
Skin Repair Actives: Skin repair actives can be effective in repairing the
epidermal and/or
dermal layer. Non-limiting examples of skin repair actives include actein 27 -
deoxyactein cimicifugoside (cimigoside), adapalene, tazarotene, ademethionine,
adenosine, aletris extract, aloe derived lectins, 3-aminopropyl dihydrogen
phosphate,
AMADORINE (from Barnet Products, Englewood, NJ), anise extracts, AOSINE (from
Secma, Pontrieux, France), arginine amino benzoate, ASC III (from E. Merck,
Darmstadt,
Germany), ascorbic acid and derivatives thereof, ascorbyl palmitate, asiatic
acid,
asiaticosides, ARLAMOL GEO (from ICI, Wilmington, DE), azaleic acid, benzoic
acid
derivatives, bertholletia extracts, betulinic acid, BIOCHANIN A, BIOPEPTIDE CL
and
BIOPEPTIDE EL (from Sederma, Brooklyn, NY), biotin, blackberry bark extract,
blackberry lily extracts, black cohosh extract, blue cohosh extract, butanoyl
betulinic acid,
catecholamines, chalcones, chaste tree extract, cis retinoic acid, citric acid
esters, clover
extracts, coenzyme Q10 (ubiquinone), coumestrol, CPC PEPTIDE (Barnet Products,
located in Englewood, NJ), daidzein, dang gui extract, darutoside, debromo
laurinterol, 1-
decanoyl-glycero-phosphonic acid, dehydrocholesterol, dehydrodicreosol,
dehydrodieugenol, dehydroepiandrosterone, DERMOLECTINE (from Sederma,
Brooklyn, NY), dehydroascorbic acid and derivatives thereof,
dehydroepiandrosterone
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CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
sulfate, dianethole, 2,4-dihydroxybenzoic acid, diosgenin, disodium ascorbyl
phosphate,
dodecanedioic acid, EDERLINE (from Seporga, Sophia Antipolis, France),
ELESERYL
SH (from Laboratories Serobiologiques, Somerville, NJ), ENDONUCLEINE (from
Laboratories Serobiologiques, Somerville, NJ), equol, ergosterol, eriodictyol,
estrogen
and its derivatives, ethocyn, eythrobic acid, farnesol, farnesyl acetate,
fennel extract,
FIBRASTIL (from Sederma, Brooklyn, NY), FIBROSTIMULINES S AND P (from
Sederma, Brooklyn, NY), FIRMOGEN IS 8445 (from Laboratories Serobiologiques,
Somerville, NJ), flavonoids (especially flavanones such as unsubstituted
flavanone and
chalcones such as unsubstituted chalcone and monohydroxy and dihydroxy
chalcones),
formononetin, forsythia fruit extract, gallic acid esters, gamma amino butyric
acid,
GATULINE RC (from Gattlefosse, Saint Priest, France), genistein, genisteine,
genistic
acid, gentisyl alcohol, gingko bilboa extracts, ginseng extracts, ginsenoside,
RO, R6-1,
R6-2~ R6-3~ RC~ RD~ RE~ RF~ RF-2~ RG-1~ RG-2~ gluco pyranosyl-1-ascorbate,
glutathione and its esters, glycitein, eptyloxy 4 salicylic acid, hesperitin,
hexahydro
curcumin, hmg-coenzyme A reductase inhibitors, hops extracts, 11 hydroxy
undecanoic
acid, 10 hydroxy decanoic acid, 25-hydroxycholesterol, ISOFAVONE SG 10 (from
Barnet Products, Englewood, NJ), kinetin, 1-2-oxo-thiazolidine-4-carboxylic
acid esters,
lactate dehydrogenase inhibitors, 1-lauryl,-lyso-phosphatidyl choline,
lectins,
LICHOCHALCONE LR15 (from Maruzen, Mornstown, NJ), licorice extracts, lipoic
acid, lumisterol, luteolin, magnesium ascorbyl phosphate, melatonin,
melibiose,
metalloproteinase inhibitors, methoprene, methoprenic acid, 4-methoxy
salicylic acid,
mevalonic acid, MPC COMPLEX (from CLR, Berlin, Germany), N-acetyl cysteine, N-
methyl serine, N-methyl taurine, N,N'-bis (lactyl) cysteamine, naringenin,
neotigogenin,
5-octanoyl salicylic acid, O- desmethylangoiensin, oleanolic acid, pantethine,
phenylalanine, photoanethone, phytic acid and its salts, piperidine, placental
extracts,
pratensein, pregnenolone, pregnenolone acetate, pregnenolone succinate,
premarin,
quillaic acid, raloxifene, REPAIR FACTOR 1 (from Sederma, Brooklyn, NY),
REPAIR
FACTOR SPC (from Sederma, Brooklyn, NY), retinal, retinoates (esters of C2-C20
alcohols), retinol, retinyl acetate, retinyl glucuronate, retinyl linoleate,
retinyl palmitate,
retinyl propionate, REVITALIN BT (from Pentapharm, Basel, Switzerland), s-
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carboxymethyl cysteine, salicylic acid, SEANAMINE FP (from Laboratories
Serobiologiques, Somerville, NJ), sodium ascorbyl phosphate, soya extracts,
spleen
extracts, tachysterol, taurine, tazarotene, thymulen, thymus extracts, thyroid
hormones,
tigogenin, tocopheryl retinoate, toxifolin, trans retinoic acid, traumatic
acid, tricholine
citrate, trifoside, uracil derivatives, ursolic acid, vitamin D3 and its
analogs, vitamin K,
vitex extract, yam extract, yamogenin, and zeatin, or mixtures thereof.
Lipids: Examples of suitable lipids include cetyl ricinoleate, cholesterol
hydroxystearate,
cholesterol isostearate, CREMEROL (from Amerchol, Edison, NJ), ELDEW C1301
(from Ajinomoto, Teaneck, NJ), lanolin, MODULAN (from Amerchol, Edison, NJ),
OHLAN (from Amerchol, Edison, NJ), petrolatum, phytantriol, and SUPER STEROL
ESTERS (from Croda, Parsippany, NJ), or mixtures thereof.
Skin Li h_g tenin~ Agents: Skin lightening agents can actually decrease the
amount of
melanin in the skin or provide such an effect by other mechanisms. Skin
lightening
agents suitable for use herein are described in EP-A-758,882 and EP-A-748,307,
both of
which are incorporated herein by reference. Further examples of skin
lightening agents
include adapalene, aloe extract, aminotyrosine, ammonium lactate, anethole
derivatives,
apple extract, arbutin, ascorbic acid and derivatives thereof, ascorbyl
palmitate, azelaic
acid, bamboo extract, bearberry extract, bletilla tuber, bupleurum falcatum
extract, burnet
extract, BURNET POWDER (from Barnet Products, Englewood, NJ), butyl hydroxy
anisole, butyl hydroxy toluene, chuanxiong, dang-gui, deoxyarbutin, 1,3-
diphenyl propane
derivatives, 2, 5 dihydroxybenzoic acid and its derivatives, 2-(4-
acetoxyphenyl)-1,3
dithane, 2-(4-hydroxyphenyl)-1,3 dithane, ellagic acid, escinol, estragole
derivatives,
esculoside, esculetin, FADEOUT (from Pentapharm, Basel, Switzerland),
fangfeng,
fennel extract, gallic acid and its derivatives, ganoderma extract, gaoben,
GATULINE
WHITENING (from Gattefosse, Saint Priest, France), genistic acid and its
derivatives,
gentisyl alcohol, glabridin and its derivatives, gluco pyranosyl-1-ascorbate,
gluconic acid,
glucosamine, glycolic acid, glycyrrhizinic acid, green tea extract, 4-hydroxy-
5-methyl-
3[2h]-furanone, hydroquinine, 4-hydroxyanisole and its derivatives, 4-hydroxy
benzoic
acid derivatives, hydroxycaprylic acid, inositol ascorbate, kojic acid, lactic
acid, lemon
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WO 01/01951 CA 02373980 2002-O1-07 pCT/US00/18108
extract, licorice extract, LICORICE P-TH (from Barnet Products, Englewood,
NJ),
linoleic acid, magnesium ascorbyl phosphate, MELFADE (from Pentapharm, Basel,
Switzerland), MELAWHITE (from Pentapharm, Basel, Switzerland), morus alba
extract,
mulberry root extract, niacinamide, nicotinic acid and its esters, nicotinyl
alcohol, 5-
octanoyl salicylic acid, parsley extract, phellinus linteus extract, placenta
extract,
pyrogallol derivatives, retinoic acid, retinol, retinyl esters (acetate,
propionate, palmitate,
linoleate), 2,4 resorcinol derivatives, 3,5 resorcinol derivatives, rose fruit
extract, rucinol,
salicylic acid, song-yi extract, SOPHORA POWDER (from Barnet Products,
Englewood,
NJ), 4-thioresorein, 3,4,5 trihydroxybenzyl derivatives, tranexamic acid,
TYROSLAT
10,11 (from Fytokem), vitamin D3 and its analogs, yeast extract, or mixtures
thereof.
Sebum Inhibitors: Sebum inhibitors can decrease the production of sebum in the
sebaceous glands. Examples of suitable sebum inhibitors include aluminium
hydroxy
chloride, ASEBIOL (from Laboratories Serobiologiques, Somerville, NJ),
BIODERMINE
(from Sedertna, Brooklyn, NY), climbazole, COMPLETECH MBAC-OS (from Lipo,
Peterson, NJ), corticosteroids, cucumber extracts, dehydroacetic acid and its
salts,
dichlorophenyl imidazoldioxolan, ketoconazole, LICHOCHALCONE LR 15 (available
from Maruzen), niacinamide, nicotinic acid and its esters, nicotinyl alcohol,
phloretin,
PHLOROG1NE (from Secma, Pontrieux, France), pyridoxine and derivatives
thereof, s-
carboxylmethyl cysteine, SEPICONTROL AS, spironolactone, tioxolone,
tocopherol,
UNITRIENOL T27 (from Unichem, Chicago IL), and ZINCIDONE (from UCIB, Clifton,
NJ), or mixtures thereof.
Sebum Stimulators: Sebum stimulators can increase the production of sebum by
the
sebaceous glands. Non-limiting examples of sebum stimulators include bryonolic
acid,
COMPLETECH MBAC-DS (from Lipo, Paterson, NJ), dehydroepiandrosterone (also
known as DHEA), orizanol, and mixtures thereof.
Skin Sensates: Non-limiting examples of suitable skin sensates for use herein
include
agents which impart a cool feel such as camphor, thymol, 1-menthol and
derivatives
thereof, eucalyptus, carboxamides; menthane ethers and menthane esters; and
agents
imparting a warm feel such as cayenne tincture, cayenne extract, cayenne
powder,
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vanillylamide nonanoate, nicotinic acid derivatives (benzyl nicotinate, methyl
nicotinate,
phenyl nicotinate, etc.), capsaicin, nasturtium officinale extract,
Zanthoxylum piperitum
extract and ginger extract, or mixtures thereof.
Protease Inhibitors: Protease inhibitors are compounds which inhibit the
process of
proteolysis, that is, the splitting of proteins into smaller peptide fractions
and amino acids.
Examples of suitable protease inhibitors include A E COMPLEX (from Barnet
Products,
Englewood, NJ), ALE (from Laboratoires Seporgia, Sophia Antipolis, France),
allicin,
AOSAINE (from Secma Biotechnologies Marine, Pontrieux, France), APROTININ
(from
Pentapharm AG, Basel, Switzerland), areca catechu extracts, BLUE ALGAE EXTRACT
(from Collaborative Labs Inc., East Setauket, NY), CENTAURILTM (from Sederma,
Brooklyn, NY), CMST (from Bioetica Inc., Portland, ME), DERMOPROTECTINE (from
Sederma, Brooklyn, NY), DISACOSIDE HF 60 (from Barnet Products, Englewood,
NJ),
ELHIBIN (from Pentapharm AG, Basel, Switzerland), FLUID OUT COLLOID (from
Vegetech, Glendale, CA), HYPOTAURINE (from Sogo Pharmaceutical Co. Ltd.,
Chiroda-ku Tokyo), IN CYTE HEATHER (from Collaborative Labs Inc., East
Setauket,
NY), MICROMEROL (from Collaborative Labs Inc, East Setauket, NY), PEFABLOC SP
(from Pentapharm AG, Basel, Switzerland), SEPICONTROL AS (from Seppic, Paris,
France), SIEGESBECKIA (from Sederma located in Brooklyn, NY), SOPHORINE and
THIOTAINE (from Barnet Products, Englewood, NJ), and mixtures thereof.
Skin Ti htgh enin~ Agents: Examples of skin tightening agents include BIOCARE
SA
(from Amerchol, Edison, NJ), egg albumen, FLEXAN 130 (from National Starch,
Bridgewater, NJ), GATULINE LIFTING (from Gattefosse, Saint Priest, France),
PENTACARE HP (from Pentapharm AG, Basel, Switzerland), VEGESERYL (from
Laboratories Serobioloques, Somerville, NJ), and mixtures thereof.
Anti-Itch Ingredients: Examples of anti-itch ingredients include STIMU-TEX
(from
Pentapharm AG, Basel, Switzerland), TAKANAL (from Ikeda-Distributor, Tokyo,
Japan), ICHTHYOL (from International Sourcing-Distributor, Upper Saddle River,
NJ),
OXYGENATED GLYCERYL TRIESTERS (from Laboratoires Seporgia, Sophia
Antipolis, France ), and mixtures thereof.
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Agents for Inhibiting Hair Growth: Examples of suitable agents for inhibiting
hair growth
include 17 beta estradiol, adamantyguanidines, adamantylamidines,
adenylosuccinate
synthase inhibitors, anti angiogenic steroids, aspartate transcarbamylase
inhibitors,
betamethasone valerate, bisabolol, copper ions, curcuma extract, cycloxygenase
inhibitors, cysterne pathway inhibitors, dehydroacetic acid,
dehydroepiandrosterone,
diopyros leak extract, epidermal growth factor, epigallocatechin, essential
fatty acids,
evening primrose oil, gamma glutamyl transpeptidase inhibitors, ginger oil,
glucose
metabolism inhibitors, glutamine metabolism inhibitors, glutathione, green tea
extracts,
heparin, KAPILANNE (from International Sourcing Distributor, Upper Saddle
River,
NJ), L-5-diaminopentanoic acid, L-aspargine synthase inhibitors, linoleic
acid,
lipoxygenase inhibitors, Tonga extract, mimosinamine dihydrochloride,
mimosine, nitric
oxide synthase inhibitors, non-steroidal anti-inflamatories, ornithine
decarboxylase
inhibitors, ornithine aminotransferase inhibitors, panthenol, phorhetur,
phosphodiesterase
inhibitors, pleione extract, protein kinase C inhibitors, 5-alpha reductase
inhibitors,
sulfhydral reactive compounds, tioxolone, transforming growth factor beta 1,
urea, zinc
ions, and mixtures thereof.
5-Alpha Reductase Inhibitors: Examples of 5-alpha reductase inhibitors include
CLOVE
55 (from Barnet Products Distributor, Englewood, NJ), ethynylestradiol,
genisteine,
genistine, Licochalcone LR-15, saw palmetto extracts, SOPHORA EXTRACT (from
Maruzen, Mornstown, NJ), ZINCIDONE (from UCIB, Clifton, NJ), and mixtures
thereof.
Desquamation Enzyme Enhancers: These agents enhance the activity of endogenous
desquamating enzymes. Non-limiting examples of desquamation enzyme enhancers
include N-methyl serine, serine, trimethyl glycine, and mixtures thereof.
Anti-Glycation Agents: Anti-glycation agents prevent the sugar induced
crosslinking of
collagen. A suitable example of an anti-glycation agent includes AMADORINE
(from
Barnet Products Distributor, Englewood, NJ).
Preferred examples of benefit agents useful herein include those selected from
the group
consisting of ascorbic acid and derivatives thereof, salicylic acid,
niacinamide, tocopheryl
nicotinate, benzoyl peroxide, 3-hydroxy benzoic acid, flavonoids (e.g.,
flavanone,
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chalcone), farnesol, phytantriol, glycolic acid, lactic acid, 4-hydroxy
benzoic acid, acetyl
salicylic acid, 2-hydroxybutanoic acid, 2-hydroxypentanoic acid, 2-
hydroxyhexanoic acid,
cis-retinoic acid, trans-retinoic acid, retinol, retinyl esters (e.g., retinyl
propionate), phytic
acid, N-acetyl-L-cysteine, lipoic acid, tocopherol and its esters (e.g.,
tocopheryl acetate),
azelaic acid, arachidonic acid, tetracycline, ibuprofen, naproxen, ketoprofen,
hydrocortisone, acetominophen, resorcinol, phenoxyethanol, phenoxypropanol,
phenoxyisopropanol, 2,4,4'-trichloro-2'-hydroxy diphenyl ether, 3,4,4'-
trichloro-
carbanilide, octopirox, lidocaine hydrochloride, clotrimazole, miconazole,
ketoconazole,
neomycin sulfate, theophylline, and mixtures thereof.
For cosmetic methods of treatment of the skin, hair or nails, the cosmetic
benefit agent is
preferably selected from anti-wrinkle and anti-skin atrophy actives, anti-acne
actives,
artificial tanning agents and accelerators, emollients, humectants, skin
repair actives, skin
barner repair aids, skin lightening agents, skin sensates, skin soothing
agents, lipids,
sebum inhibitors, sebum stimulators, sunscreening agents, protease inhibitors,
skin
tightening agents, anti-itch ingredients, and desquamation enzyme enhancers,
or mixtures
thereof.
Humectants
Preferred pre-formed, unilamellar sheet-like devices comprise at least one
humectant.
Humectants can be added to achieve a plasticising effect and to increase the
moisturising
characteristics of the pre-formed unilamellar sheet-like device when applied
to the target
surface. Certain humectants such as hexylene glycol may also contribute to the
antibacterial properties and characteristics of a pre-formed, unilamellar
sheet-like device
of the present invention. Further, without wishing to be limited by theory, it
is thought
that incorporating humectants into the pre-formed, sheet-like unilamellar
devices of the
present invention, increases the stability of the devices such that they are
less likely to
undergo decomposition under extreme temperature conditions. In general, the
pre-
formed, unilamellar sheet-like devices of the present invention comprise from
about 1.0%
to about 45%, preferably from about 5% to about 40%, more preferably from
about 10%
to about 30% by weight of a humectant.
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WO 01/01951 CA 02373980 2002-O1-07 pCT~S00/18108
Suitable humectants for use in the present invention are described in
W098/22085,
W098/18444 and W097/01326, all incorporated herein by reference. Further
suitable
humectants include amino acids and derivatives thereof such as proline and
arginine
aspartate, 1,3-butylene glycol, propylene glycol and water and codium
tomentosum
extract, collagen amino acids or peptides, creatinine, diglycerol,
biosaccharide gum-1,
glucamine salts, glucuronic acid salts, glutamic acid salts, polyethylene
glycol ethers of
glycerin (e.g. glycereth 20), glycerin, glycerol monopropoxylate, glycogen,
hexylene
glycol, honey and extracts or derivatives thereof, hydrogenated starch
hydrolysates,
hydrolyzed mucopolysaccharides, inositol, keratin amino acids, LAREX A-200
(available
from Larex), glycosaminoglycans, methoxy PEG 10, methyl gluceth-10 and 20
(both
commercially available from Amerchol, Edison, NJ), methyl glucose, 3-methyl-
1,3-
butandiol, N-acetyl glucosamine salts, panthenol, polyethylene glycol and
derivatives
thereof (such as PEG 15 butanediol, PEG 4, PEG 5 pentaerythritol, PEG 6, PEG
8, PEG
9), pentaerythritol, 1,2 pentanediol, PPG-1 glyceryl ether, PPG-9, 2-
pyrrolidone-5-
carboxylic acid and its salts such as glyceryl PCA, saccharide isomerate,
SEACARE
(available from Secma), sericin, silk amino acids, sodium acetylhyaluronate,
sodium
hyaluronate, sodium poly-aspartate, sodium polyglutamate, sorbeth 20, sorbeth
6, sugar
and sugar alcohols and derivatives thereof such as glucose, mannose and
polyglycerol
sorbitol, trehalose, triglycerol, trimethyolpropane, tris (hydroxymethyl)
amino methane
salts, and yeast extract, or mixtures thereof.
Preferably, the humectants for use herein are selected from glycerine,
butylene glycol,
hexylene glycol, panthenol and polyethylene glycol and derivatives thereof, or
mixtures
thereof.
Emulsifiers/Surfactants
The pre-formed, unilamellar sheet-like devices of the present invention can
also
optionally comprise one or more surfactants and/or emulsifiers. Emulsifiers
and/or
surfactants, generally help to disperse and suspend the discontinuous phase
within the
continuous phase. A surfactant may also be useful if the product is intended
for skin, hair
or nail cleansing. For convenience hereinafter emulsifiers will be referred to
under the
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WO 01/01951 PCT/tTS00/18108
term 'surfactants', thus 'surfactant(s)' will be used to refer to surface
active agents whether
used as emulsifiers or for other surfactant purposes such as skin, hair or
nail cleansing.
Known or conventional surfactants can be used in the composition, provided
that the
selected agent is chemically and physically compatible with essential
components of the
composition, and provides the desired characteristics. Suitable surfactants
include
silicone materials, non-silicone materials, and mixtures thereof.
The compositions of the present invention preferably comprise from about 0.01
% to about
15% of a surfactant or mixture of surfactants. The exact surfactant or
surfactant mixture
chosen will depend upon the pH of the composition and the other components
present.
Preferred surfactants are nonionic.
Among the nonionic surfactants that are useful herein are the condensation
products of
alkylene oxides with fatty acids (i.e. alkylene oxide esters of fatty acids).
These materials
have the general formula RCO(X)nOH wherein R is a C10-30 alkyl group, X is -
OCH2CH2- (i.e. derived from ethylene glycol or oxide) or -OCH2CHCH3- (i.e.
derived
from propylene glycol or oxide), and n is an integer from about 6 to about
200. Other
nonionic surfactants are the condensation products of alkylene oxides with 2
moles of
fatty acids (i.e. alkylene oxide diesters of fatty acids). These materials
have the general
formula RCO(X)nOOCR wherein R is a C10-30 alkyl group, X is -OCH2CH2- or -
OCH2CHCH3-, and n is an integer from about 6 to about 100. Other nonionic
surfactants
are the condensation products of alkylene oxides with fatty alcohols (i.e.
alkylene oxide
ethers of fatty alcohols). These materials have the general formula R(X)nOR'
wherein R
is a C10-30 aliphatic group, X is -OCH2CH2- or -OCH2CHCH3-, n is an integer
from
about 6 to about 100 and R' is H or a C10-30 aliphatic group, examples of
which include
PEG 40 hydrogenated castor oil and PEG 60 hydrogenated castor oil,
respectively
available under the trade names "Cremophor RH 40" and "Cremophor RH 60" from
BASF (Parsippany, NJ, USA); isoceteth-20, available under the trade name
"Arlasolve
200" from ICI (Wilmington, MA, USA); and oleth-20, available under the trade
name
"Volpo N20" from Croda Chemicals Ltd. (Goole, North Humberside, England).
Still
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WO 01/01951 PCT/LTS00/18108
other nonionic surfactants are the condensation products of alkylene oxides
with both
fatty acids and fatty alcohols [i.e. wherein the polyalkylene oxide portion is
esterified on
one end with a fatty acid and etherified (i.e. connected via an ether linkage)
on the other
end with a fatty alcohol]. These materials have the general formula RCO(X)nOR'
wherein R and R' are C 10-30 alkyl groups, X is -OCH2CH2- or -OCH2CHCH3- , and
n is
an integer from about 6 to about 100, examples of which include ceteth-6,
ceteth-10,
ceteth-12, ceteareth-6, ceteareth-10, ceteareth-12, steareth-6, steareth-10,
steareth-12,
PEG-6 stearate, PEG-10 stearate, PEG-100 stearate, PEG-12 stearate, PEG-20
glyceryl
stearate, PEG-80 glyceryl tallowate, PEG-10 glyceryl stearate, PEG-30 glyceryl
cocoate,
PEG-80 glyceryl cocoate, PEG-200 glyceryl tallowate, PEG-8 dilaurate, PEG-10
distearate, and mixtures thereof.
Other nonionic surfactants that are useful herein are alkyl glucosides and
alkyl
polyglucosides which are described in more detail in W098/18444, incorporated
herein
by reference. Still other useful nonionic surfactants include polyhydroxy
fatty acid amide
surfactants, which are described in more detail in W098/04241.
Other nonionic surfactants suitable for use herein include sugar esters and
polyesters,
alkoxylated sugar esters and polyesters, C1-C30 fatty acid esters of C1-C3p
fatty alcohols,
alkoxylated derivatives of C1-C30 fatty acid esters of C1-C30 fatty alcohols,
alkoxylated
ethers of C1-C30 fatty alcohols, polyglyceryl esters of C1-C30 fatty acids, C1-
C30 esters
of polyols, C1-C30 ethers of polyols, alkyl phosphates, polyoxyalkylene fatty
ether
phosphates, fatty acid amides, acyl lactylates, and mixtures thereof. Examples
of these
non-silicon-containing surfactants include: polysorbate 20, polyethylene
glycol 5 Soya
sterol, steareth-20, ceteareth-20, PPG-2 methyl glucose ether distearate,
polysorbate 80;
polysorbate 60, available under the trade name "Tween 60" from ICI
(Wilmington, MA,
USA); glyceryl stearate, sorbitan monolaurate, polyoxyethylene 4 lauryl ether
sodium
stearate, polyglyceryl-4 isostearate, hexyl laurate, PPG-2 methyl glucose
ether distearate,
and mixtures thereof.
CA 02373980 2002-O1-07
WO 01/01951 PCT/US00/18108
Preferred among the nonionic surfactants are those selected from the group
consisting of
ceteareth-12, sucrose cocoate, steareth-100, polysorbate 60, PEG-60
Hydrogenated Castor
Oil, isoceteth-20, oleth-20, PEG-100 stearate, and mixtures thereof.
Other suitable emulsifiers for use herein are polyoxypropylene,
polyoxyethylene ethers of
fatty alcohols. These materials have the general formula R(CH2CHCH30)x-
(CH2CH20)~H, wherein R is an OC10-C30 alkyl group or C10-C30 alkyl group, x
has
an average value from 1 to 20 and y has an average value from 1 to 30,
examples of which
include PPG-6-decyltetradeceth-30, available under the trade name "Pen 4630"
from
Nikko Chemicals Co. Ltd. (Tokyo, Japan); PPG-6-Decyltetradeceth-20, available
under
the trade name "Pen 4620" from Nikko Chemicals Co. Ltd. (Tokyo, Japan); and
PPG-5-
Ceteth-20, available under the trade name "Procetyl AWS" from Croda Chemicals
Ltd.
(Goole, North Humberside, England).
Another emulsifier useful herein is a fatty acid ester blend based on a
mixture of sorbitan
or sorbitol fatty acid ester and sucrose fatty acid ester, as described in
more detail in
W098/22085, incorporated by reference herein.
The hydrophilic surfactants useful herein can alternatively or additionally
include any of a
wide variety of cationic, anionic, zwitterionic, and amphoteric surfactants
such as are
known in the art. See, e.g., McCutcheon's, Detergents and Emulsifiers, North
American
Edition (1986), published by Allured Publishing Corporation; US-A-5,011,681 to
Ciotti
et al., issued April 30, 1991; US-A-4,421,769 to Dixon et al., issued December
20, 1983;
and US-A-3,755,560 to Dickert et al., issued August 28, 1973; these four
references are
incorporated herein by reference in their entirety.
A wide variety of cationic surfactants are useful herein. Suitable cationic
surfactants for
use herein are disclosed in W098/18444, incorporated herein by reference.
A wide variety of anionic surfactants are also useful herein. See, e.g., US-A-
3,929,678,
to Laughlin et al., issued December 30, 1975, which is incorporated herein by
reference in
its entirety. Exemplary anionic surfactants include the alkoyl isethionates
(e.g., C12 '
C3p), alkyl and alkyl ether sulfates and salts thereof, alkyl and alkyl ether
phosphates and
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WO 01/01951 PCT/US00/18108
salts thereof, alkyl methyl taurates (e.g., C12 - C30), and soaps (e.g.,
alkali metal salts,
e.g., sodium or potassium salts) of fatty acids.
Amphoteric and zwitterionic surfactants are also useful herein. Examples of
amphoteric
and zwitterionic surfactants which can be used in the compositions of the
present
invention are those which are broadly described as derivatives of aliphatic
secondary and
tertiary amines in which the aliphatic radical can be straight or branched
chain and
wherein one of the aliphatic substituents contains from about 8 to about 22
carbon atoms
(preferably Cg - Clg) and one contains an anionic water solubilising group,
e.g., carboxy,
sulfonate, sulfate, phosphate, or phosphonate. Examples are alkyl imino
acetates, and
iminodialkanoates and aminoalkanoates, imidazolinium and ammonium derivatives.
Other suitable amphoteric and zwitterionic surfactants are those selected from
the group
consisting of betaines, sultaines, hydroxysultaines, alkyl sarcosinates (e.g.,
CI2 - C30)
and alkanoyl sarcosinates.
The pre-formed, unilamellar sheet-like devices of the present invention may
optionally
contain a silicone containing emulsifier or surfactant. A wide variety of
silicone
emulsifiers are useful herein. These silicone emulsifiers are typically
organically
modified organopolysiloxanes, also known to those skilled in the art as
silicone
surfactants. Useful silicone emulsifiers include dimethicone copolyols. These
materials
are polydimethyl siloxanes which have been modified to include polyether side
chains
such as polyethylene oxide chains, polypropylene oxide chains, mixtures of
these chains,
and polyether chains containing moieties derived from both ethylene oxide and
propylene
oxide. Other examples include alkyl-modified dimethicone copolyols, i.e.,
compounds
which contain C2-C3p pendant side chains. Still other useful dimethicone
copolyols
include materials having various cationic, anionic, amphoteric, and
zwitterionic pendant
moieties.
Other Optional Ingredients
The devices of the present invention can comprise a wide range of other
optional
components. These additional components should be pharmaceutically acceptable.
The
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CTFA Cosmetic Ingredient Handbook: Second Edition, 1992, incorporated by
reference
herein in its entirety, describes a wide variety of cosmetic and
pharmaceutical ingredients
commonly used in the cosmetic industry, which are suitable for use in the
compositions of
the present invention. Non-limiting examples of functional classes of
ingredients are
described at page 537 of this reference. Examples of these and other
functional classes
include: abrasives, absorbents, antibiotics, anticaking agents, anti-dandruff
agents, anti-
perspirant agents, antioxidants, biological additives, bleach activators,
brighteners,
builders, buffering agents, chelating agents, chemical additives, colorants,
cosmetics,
cleansers, denaturants, dental treatments, deodorants, desquamation actives,
depilatories,
drug astringents, dyes, dye transfer agents, enzymes, external analgesics,
flavors, film
formers, fragrance components, insect repellants, mildewcides, opacifying
agents,
oxidative dyes, oxidising agents, pest control ingredients, pH adjusters, pH
buffers,
pharmaceutical actives, plasticizers, preservatives, radical scavengers, skin,
hair or nail
bleaching agents, skin, hair or nail conditioners, skin, hair or nail
penetration enhancers,
stabilisers, surface conditioners, reducing agents, temperature depressors,
and warmth
generators.
Also useful herein are aesthetic components such as colorings, essential oils,
and skin,
hair or nail healing agents. Other optional materials herein include pigments.
Pigments
suitable for use in the compositions of the present invention can be organic
and/or
inorganic. Also included within the term pigment are materials having a low
colour or
lustre such as matte finishing agents, and also light scattering agents.
Examples of
suitable pigments are iron oxides, acyglutamate iron oxides, titanium dioxide,
ultramarine
blue, D&C dyes, carmine, and mixtures thereof. Depending upon the type of
composition, a mixture of pigments will normally be used.
The pH of the pre-formed, unilamellar sheet-like devices herein is preferably
from about 3
to about 9, more preferably from about 4 to about 8.
The pre-formed, unilamellar sheet-like devices of the present invention are
patches or
masks having a size and shape adapted to conform to a desired target area.
Thus, devices
according to the present invention may have sizes ranging from a surface area
of about
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0.25cm2 to about 1,OOOcm2. Preferably, at least one surface dimension of the
device,
preferably two surface dimensions of the device, is/are greater than the depth
of the
device, with preferred ratios of surface dimensions) to depth of the device of
about 2:1 to
about 100:1, more preferably about 5:1 to about 50:1.
The term "surface dimension" as used herein, means a dimension in the x- or y-
axes,
depth being measured along the z-axis. The exact size and shape will depend
upon the
intended use and product characteristics. The pre-formed sheet-like devices
herein are
suitable for topical application to the nails or cuticles, the hair or scalp,
a human face or
part thereof, legs, hands, arms, feet, or human torso. The devices herein may
be, for
example, square, circular, rectangular, oval, or other shapes which are
composites of
these, such as shapes that could be described as "semi-circle", "donut", or
others. Devices
shaped to fit the face have a surface area ranging from about 0.25 cm2 to
about 500 cm2,
preferably from about 1 cm2 to about 400 cm2. The patch or mask devices
according to a
third aspect of the invention have a thickness of from about 0.5mm to about
20mm,
preferably from about lmm to about 5mm. The patch or mask devices according to
a
second aspect of the invention have a thickness of from about 0.5mm to about
20mm,
preferably from about 0.5mm to about 3mm in their delineated thickened
regions) and
have a thickness of from about 0.5mm to about 17.5mm, preferably from about
0.5mm to
about 2.5mm in their delineated thinner region(s).
The pre-formed, sheet devices of the present invention may also be made and
used in the
form of handwear, footwear, or a body wrap. Typically, the handwear will
comprise a
glove for the hand or any portion thereof, and the footwear will comprise a
sock for the
foot or any portion thereof. As used herein, the term "glove" is meant to be
inclusive of
"mitten." Preferably, the handwear comprises a glove body comprising a middle
section,
from one to four finger receptacles connected with the middle section, a thumb
receptacle
connected with the middle section, a palm side and an opposite back side.
Preferably, the
footwear comprises a sock body forming a tubular foot portion having a closed
end and an
open end. The inventive devices may also be made or used in the form of a body
wrap.
The body wrap is wrapped radially around any body part having a longitudinal
axis. Its
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ends may communicate with each other, or its length may be shortened so as to
only wrap
partially around. In either case, the wraps should exhibit excellent
conformity to the
shape of the body part. Typically, such body parts will include the user's
back, upper arm,
lower arm, upper leg, lower leg, neck, and torso.
Following application of the device, it may be left on the target area for
about 3 hours,
preferably about 1 hour, more preferably less than 15 minutes. The pre-formed,
unilamellar sheet-like device can then be removed all in one piece.
Depending on the benefit agent (or benefit agents) contained therein, the
devices of the
present invention may have at least one of the following uses; hydrating the
skin, hair or
nails, smoothing fine lines and wrinkles; cosmetically treating acne; firming
the skin,
strengthening; softening; exfoliating; improving and/or evening skin tone
and/or texture;
skin, hair or nail lightening; tanning; reducing the appearance of pores;
absorbing or
controlling secretions; protecting and/or soothing the skin, hair or nails,
muscles, aches or
pains; reducing puffiness, and/or dark circles; stimulating wound healing;
warming,
refreshing or cooling the skin, hair or nails; relieving inflammation;
brightening the
complexion; decongesting; reducing swelling; treating dermatological
conditions;
cushioning; purifying; fragrancing; reducing bacterial or micro-organism
growth; healing;
repelling insects; removing unwanted hair, dirt, or make-up; and colouring or
bleaching
the target area to which the device is applied. Preferably, the pre-formed
unilamellar
sheet-like devices herein are cosmetically used for hydrating the skin, hair
or nails;
smoothing fine lines and wrinkles; and improving and/or evening the skin tone
and/or
texture.
Methods of Production
By subjecting the at least one benefit agent and the at least one gellable
polymeric gel
forming agent to a gelling step, a pre-formed, unilamellar sheet-like device
which is self
supporting, is formed. The nature of the gelling step is dependent on the
nature of the
polymeric gel forming agent used. For example, the gelling step may involve
the addition
of metal ions to cross-link a polymer solution or it may involve irradiation
with ultraviolet
rays to produce a self supporting gel.
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In many cases, the gelling step is achieved via cooling. This involves heating
a liquid, the
at least one benefit agent and the at least one gellable polymeric gel forming
agent,
together with any other optional ingredients present (or gel-forming mixture),
to a first
temperature above the gel point of the gel-forming mixture, to solubilize the
gel-forming
mixture; placing the gel-forming mixture in a suitably shaped mould; and
gelling the gel-
forming mixture at a second temperature, which is cooler than the first
temperature at or
below the gel point of the gel-forming mixture to produce a unilamellar self
supporting
device. In an alternative embodiment, the at least one benefit agent and the
at least one
gellable polymeric gel forming agent and any optional components present are
heated,
once placed in the suitably shaped mould.
In forming the self supporting device, the components may be added together or
sequentially in any order. The order of adding the components may depend on
the
properties and characteristics thereof. Preferably, the at least one benefit
agent and the at
least gellable polymeric gel forming agent are sufficiently dissolved in the
liquid before
any other components are added. By the term "sufficiently dissolved" is meant
that the
gel-forming mixture appears substantially or completely transparent. The
temperature of
the gel-forming mixture is maintained above the gel point until all of the
components are
added. In alternative embodiments, it may be beneficial to begin to lower the
temperature
of the gel-forming mixture prior to adding the final components.
The at least one benefit agent and the at least one gellable polymeric gel
forming agent are
maintained at an elevated temperature for an effective length of time. An
"effective"
length of time is sufficient to allow the at least one gellable polymeric gel
forming agent
sufficient time to dissolve completely (or substantially) in the liquid.
In a preferred embodiment, the self supporting device may be produced through
injection
moulding. It is believed that the device so produced is stronger due to the
smoother finish
of the surface, which provides a greater resistance to tearing. An injection
moulding
process for producing a self supporting device comprises the steps of
injecting the gel-
forming mixture into a suitably shaped mould, the mixture being maintained
prior to the
injection step at a first temperature above the gel point of the gel-forming
mixture; and
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cooling the gel-forming mixture in the suitably shaped mould to a second
temperature
below the gel point of the gel-forming mixture, to form a unilamellar self
supporting
device.
In an alternative injection moulding process, the at least one benefit agent
and the at least
one gellable polymeric gel forming agent and any other optional components, if
present,
are added sequentially in any order or all at once. For injection moulding,
the at least one
benefit agent and the at least one gellable polymeric gel forming agent is
adapted to be
fluid enough to enable it to be readily supplied to a die by any conventional
means, in
addition to injection moulding processes. Lubricants may be added to assist in
feeding
the gel-forming mixture along the bore of an extruding barrel.
The gel-forming mixtures may be supplied to the suitably shaped mould by any
other
variety of well known technique including gravity feed systems and pneumatic
or
mechanical injection systems. Injection moulding is the most preferred
technique because
of the fluidity and low processing temperatures of the mixtures. A very wide
range of
moulding pressures may be employed. Generally, the moulding pressure is
between about
105 Pa (1 atmosphere) and about Sx106 Pa (50 atmospheres), although higher or
lower
pressures may be employed depending on the moulding technique used. An
advantage of
the present invention is the ability to mould the devices of the present
invention using low
pressures.
When gelling is achieved via cooling, the moulding temperature must, of
course, be at or
below the gel point of the gel-forming mixture in order to produce a self
supporting
device. The appropriate mould temperature can be achieved before, during, or
after the
mixture is supplied to the mould. After the device is moulded and cooled to a
temperature below the gel point, the device is removed from the mould. The
device,
being self supporting, requires no special handling during removal from the
mould.
In a device according to a first or second or fourth aspect of the invention
wherein the
device has a non-planar topography on at least one of the first and second
surfaces,
preferably the second surface, of the device, the non-planar topography
comprising at
least two delineated regions not simultaneously having the same mean
thickness, the
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mould has at least one of first and second mould surfaces, the at least one of
first and
second mould surfaces being the negative image of the at least one of first
and second
surfaces of the device itself and the at least one of the first and second
mould surfaces
being a negative image of the non-planar topography. The non-planar topography
is of a
freely selectable shape including, but not limited to those illustrated in
Figures 1-4, 6-7, 8-
9 and 10-12 of the accompanying drawings. If the non-planar topography has
periodicity,
the at least one of the first and second mould surfaces has periodicity, which
confers a
negative image of the periodicity to the at least one of first and second
surfaces of the
device itself.
According to a first and third aspect of the present invention, the device has
at least one of
the first and second surfaces, preferably the second surface, having a non-
planar
topography comprising a textured surface that is the negative image of a
texturing surface,
the negative image of the texturing surface having a texture defined by Ra of
greater than
10~m. If the non-planar topography has periodicity, the texturing surface has
periodicity,
which confers a negative image of the periodicity to the at least one of first
and second
surfaces of the device itself. The method for its production involves
preparing a gel-
forming mixture comprising at least one benefit agent and at least one
polymeric gel
forming agent and the optional components, if present, and heating said
mixture to a first
temperature above the gel point of the mixture, to solubilise the gel-forming
mixture;
placing the mixture in a suitably shaped mould having at least one of first
and second
mould surfaces being the negative image of at least one of the first and
second surfaces of
the device itself; on at least one of which first and second mould surfaces is
pre-
positioned a texturing surface whose negative image has a texture defined by
Ra of
greater than 10~m; gelling the mixture at a second temperature cooler than the
first
temperature at or below the gel point of the gel-forming mixture; and removing
the, or
each, texturing surface from the device. The removing step may take place
during or after
the gelling step. The texturing surface is selected from the substrates
described
hereinabove, provided that the negative image of an outer surface of the
substrate has Ra
of greater than 10~m. Formed films are the preferred texturing surfaces.
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In an alternative embodiment, the mixture is heated once placed in the mould.
In a further
alternative embodiment, the at least one of the first and second mould
surfaces is textured
to form the texturing surface by an etching process or any other process known
in the art.
When the non-planar topography has periodicity on both the first and second
surfaces of a
device, either as a result of the mould surface or the texturing surface
having periodicity,
the pattern produced by the periodicity on both surfaces may be aligned or
staggered.
Preferably, the pattern is staggered.
The present method also includes a method of producing a pre-formed,
unilamellar sheet-
like device according to the first, second and third or fourth aspects of the
invention, the
method comprising preparing a gel-forming mixture comprising at least one
benefit agent
and at least one polymeric gel forming agent and the optional components, if
present;
heating the mixture to a first temperature above the gel point of the mixture,
to solubilize
the gel-forming mixture; placing the mixture in a suitably shaped mould having
at least
one of first and second mould surfaces being the negative image of at least
one of the first
and second surfaces of the device itself, the topography of the at least one
of the first and
second device surfaces defining at least two delineated regions simultaneously
not having
the same mean thickness; on at least one of which first and second mould
surfaces is pre-
positioned a texturing surface whose negative image has a texture defined by
Ra of
greater than lOqm; gelling the mixture at a second temperature cooler than the
first
temperature at or below the gel point of the gel-forming mixture; and removing
the, or
each, texturing surface from the device.
In an alternative embodiment, the mixture is heated once placed in the mould.
In a further
alternative embodiment, the at least one of the first and second mould
surfaces is textured
to form the texturing surface by an etching process or any other process known
in the art.
Methods Of Evaluation
Gel Compressive Rupture Test
The mechanical properties of the pre-formed unilamellar sheet-like devices of
the present
invention are measured via compressive failure testing of the gel. Parameters
of interest
are the gel strength (measured via the compressive force required to rupture a
moulded gel
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cylinder) and the gel flexibility (measured as the extent of gel compression
at the point of
rupture). A more detailed description of the test method follows.
Compressive failure testing is performed using a Stable Micro Systems (SMS)
Texture
Analyser (TA), model TA-XT2i available from Stable Micro Systems Ltd
(Godalming,
Surrey, UK). The system is controlled through SMS's Texture Expert Exceed
software
(version 2.03) running within Windows-98. A 100 mm diameter aluminum
compression
plate (P-100 probe) is attached to a 50 Kg load cell. This is mounted within
the TA Probe
Carrier, the extended arm whose vertical travel is under computer control.
To create test samples, a gel formulation of interest is prepared as described
below. Gel
discs of a precise cylindrical-solid shape (26 mm diameter by 12 mm depth) are
formed in
correspondingly shaped moulds. The moulds with sample are hermetically sealed
against
evaporation during storage. These gel discs are stored at ambient temperature
overnight.
Each gel disc is removed from its mould just prior to testing and visually
inspected for
defects. Any gel discs with defects (e.g. trapped air bubbles) are discarded
as these
defects may impact the measured mechanical properties. The non-defective gel
disc is
then centered under the P-100 compression plate.
The Texture Expert Exceed software is set-up in Force / Compressive mode. The
compression plate is pre-set to a starting height of 12.0 mm. Its rate of
descent is set to
0.8 mm/second and total travel distance set to 10.8 mm (i.e. measurement stops
when the
gel disc is compressed by 90% of its original height). Data is automatically
collected on
force and position of the compression plate at the rate of 200 pps (points per
second). The
software is pre-set to mark compression plate position at the maximum force
achieved.
This maximum force is the rupture strength, that is, the force required to
rupture the gel
disc. The distance travelled by the plate from its original starting height to
the point of gel
rupture represents the extent of deformation of the gel. The maximum force at
the point
of rupture is averaged across samples (typically 5 replicates) and reported in
Newtons.
The uni-axial deformation (compression) at the gel's point of rupture is
expressed as a
percent of its original moulded height, i.e.
Compression = distance travelled ~ plate (in mm) at maximum force X 100
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12 (original sample height in mm)
If gel rupture has not occurred by the end of the 10.8 mm stroke, (i.e. 90%
compression),
the gel is classified as 'non-rupturing' under these test conditions.
Surface Roughness
Surface topography was measured using a CADEYES Surface Analysis System
(Medar,
USA), a moue interferometry technique, configured with a 30.7 ~m x-axis
resolution,
35.8 ~m y-axis resolution, and 1.6 ~.m z-axis resolution. Textured surfaces
representative
of devices of the first or third aspects of the invention were prepared by
making negative
silicone casts (Silflo Silicone Impression Material; Flexico Developments,UK)
of
texturing surfaces useful in the production of pre-formed, unilamellar sheet-
like devices
according to a first or third aspect of the present invention. Silicone casts
were used
instead of actual pre-formed, unilamellar sheet-like devices because the
optical properties
of the silicone casting material are more suitable for optical surface
analysis.
Silicone casts were prepared as follows:
1. A 2.54 cm (1 inch) diameter circle of silicone paste was mixed thoroughly
with 1 drop
of catalyst for approximately 1 minute.
2. Using a spatula, the silicone mixture was applied to the texturing surface
and allowed
to cure at room/ambient temperature for approximately 7 minutes.
3. After curing, the silicone cast was removed from the texturing surface and
analysed.
The data reported for describing the surface roughness of the silicone cast
representative
of the textured surface of devices of a first or third aspect of the invention
include Ra,
n
surface-based average deviation from a best fit plane, wherein Ra = 1/n ~ z;
where z,
a=
at a point, is the absolute value of the calculated best fit elevation at a
point minus the
measured elevation at that point; the calculated best fit elevation at the
point is the
elevation of the best fit plane to the measured surface at that point. The
data reported for
describing the surface roughness also include Rq, surface-based root mean
square
deviation from a best fit plane and Rz, 10-point roughness.
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n
Rq is surface-based root mean square deviation from a best fit plane Rq = 1 /
n~ z;2
m
Rz is ten-point roughness averaged over all scan lines in the x-direction,
Rz = ((S1 + S3 + SS + S7 + S9) - (S2 + S4 + S6 + Sg + S10)) / 5
where S 1 ~, S3, S5, S7, S9 are the 5 highest peaks from the best fit plane
along the scan
line and S2, S4, S6, Sg, S10 are the 5 lowest valleys from the best fit plane
along the scan
line. The best fit plane as described herein is automatically calculated by
the CADEYES
Surface Analysis System, i is an index referring to a particular point
analysed and n is the
total number of points analysed, e.g., for a lcm2 area, n is 90,987.
Although the surface topographies of these samples were acquired using a moue
interferometry technique, any appropriately configured (x and y axis
resolution less than
40 Vim; z axis resolution less than 2 Vim), surface profiling technique (e.g.,
stylus
profilometry, laser profilometry, or fringe projection) could be used to
acquire the surface
topographies to produce these data. An alternative method of measuring Ra and
Rq is via
the line based method described in IS04287 (1997) where Ra is defined as the
arithmetical mean deviation of the assessed profile and Rq is defined as the
root mean-
square deviation of the assessed profile.
Surface Glossiness
A texturing surface was placed on a gel-forming mixture comprising 0.83%
agarose, 0.3%
Kelgum~ (1:l mixture of xanthan gum and locust bean gum supplied by Kelco, San
Diego, CA, USA), 20% glycerin, 10% niacinamide, 1% panthenol, 5% butylene
glycol,
0.15% Nipagin A (ethyl paraben, supplied by Nipa Laboratories, Inc.,
Wilmington, DE,
USA), 0.1 % Hampene Na2 (disodium EDTA, supplied by Hampshire Chemical,
Lexington, MA, USA), 62.62% deionized water. The texturing surface was removed
once the gel structure has set. Gloss measurements (i.e. surface reflectance)
were then
measured on the textured surface of such a pre-formed, unilamellar sheet-like
device
according to the first or third aspect of the invention, on the opaque (black)
section of a
Leneta Card, available from The Leneta Company. Measurements of % surface
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reflectance were taken using a BYK-Gardner Micro Tri-Gloss meter (BYK Gardner,
Sliver Spring, MD) set to read at 20 degrees (20°), 60 degrees
(60°) and 85 degrees (85°).
Gel Transparency
Gel transparency was measured by assessing the visibility of printed text
through a device
according to the present invention. The printed text was prepared by printing
the English
alphabet (capital letters) onto transparency film (Universal Office Supplies)
using
Microsoft Word Arial font and a LaserJet 4 Plus printer (Hewlett Packard)
fitted with a
black ink cartridge. Printed transparency films were prepared in font sizes
ranging from 4
points to 28 points. The printed transparency films were then laid over white
paper sheets
to ensure a uniform background and all samples were assessed under normal
indoor
lighting conditions.
A sample of the gel of interest was moulded to produce a gel disc with a
thickness (depth)
of 7 mm. This gel disc was placed onto the transparency film printed with 4
font size and
the visibility of the printed alphabet was assessed through the disc of gel.
If the text was
not legible through the gel disc, the disc was transferred to the next largest
font sizeand
the assessment repeated. This process was repeated until a font size was
reached that was
legible through the gel. The smallest font size legible through the gel sample
was then
assigned the "transparency threshold" for that gel. The preferred
"transparency threshold"
for the gels used to make the devices of the present invention is 10 font
size, more
preferred is 7 font size and especially preferred is 4 font size.
Examples
The invention is illustrated by the following examples.
Examples 1 - 3
1 2 3
Ingredient % w/w % w/w % w/w
Agarose - 0.4 0.8
Locust Bean Gum - 0.27 -
Konj ac Mannan 0.3 - -
Xanthan Gum 0.1 0.13 -
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KelgumTM 1 - - 0.3
Gellan Gum 1.0 0.4 -
Glycerin 20.0 20.0 15.0
Butylene Glycol 5.0 - 8.0
Panthenol 1.0 2.0 2.0
Niacinamide . - S.0 -
Sucrose Polycottonseedate- - 0.5
Polysorbate 60 - - 0.2
Dimethicone Copolyol0.02 0.02 -
Benzyl Alcohol - 0.3 0.2
Ethyl Paraben 0.2 0.1 -
Propyl Paraben - 0.05 -
Disodium EDTA - 0.1 -
Calcium Chloride 0.1 0.08
Water to 100 to to
100 100
Force To Rupture/N 82 73 102
Compression 26 44 58
Substrate Paper2 '
lKelgumTM is a 1:1 mixture of xanthan gum and locust bean gum supplied by
Kelco, San
Diego, CA, USA.
2Paper is "Kimwipes EX-L" from Kimberley-Clark Corp., Roswell, GA, USA.
The polysaccharide gums are mixed with water to form a uniformly dispersed
mixture
(this can be facilitated by pre-dispersing the polysaccharides in a non-
solvent e.g.
polyhydric alcohol) and any additional components are added. The mixture is
heated with
stirnng to a first temperature above the gel point of the mixture (ca.
90°C) to fully hydrate
the polysaccharide gums. The liquid gel is then dispensed into a suitably
shaped mould
(Example 3). The devices of Examples 1 and 2 are injection moulded into a
suitably
shaped mould. Injection moulding is preferred. This eliminates any defects
which may
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be introduced by cutting the gel and so improves the robustness of the device.
Injection
moulding also allows the device to be readily formed into a three-dimensional
structure.
The liquid gel is then cooled to a second temperature cooler than the first
temperature at
or below the gel point of the mixture (ambient temperature) to set up the gel
structure.
The device may then be removed from the mould. The devices of Examples 1-3 are
illustrated in, respectively, Figures 1-3 of the accompanying drawings. The
devices
herein are then packaged into materials which have low water vapour
permeability to
minimise drying out of the device during storage. Suitable packaging for
devices herein
include sachets or sealed trays. If the device is packaged in a sachet, it is
preferably
protected prior to use. This protection can be provided by a substrate or by a
release liner
such as a plastic film, which provides easy release for the device.
If a substrate is to be used (Example 1), this may be placed in the suitably
shaped mould
prior to dispensing the gel or it may be placed on the surface of the liquid
gel during the
cooling stage.
In some compositions, metal ions (e.g. Ca2+, K+) may be included in the
formulation to
increase the gel strength of the device (Examples l and 2). In this case, the
metal ions are
added in the form of an aqueous solution and are stirred into the liquid gel
immediately
before the dispensing step.
The above method may be modified as necessary depending on the nature of any
additional components. For example, if non-aqueous components are present, the
liquid
gel may be homogenised immediately prior to moulding or casting to ensure
dispersion of
the non-aqueous components. Similarly, if heat sensitive ingredients are
incorporated, the
formulation should be cooled to an appropriate temperature (dependent on the
ingredient)
after the gum hydration step and the heat sensitive ingredient added at this
stage.
The liquid gel may be de-gassed, e.g. by vacuum, to remove air bubbles
dispersed within
the liquid. This de-gassing step, if followed, would be the final step
immediately prior to
dispensing the liquid gel.
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As shown above, the pre-formed, sheet-like devices herein have excellent
strength and
flexibility.
Example 4
A formulation of a pre-formed, sheet-like device has been prepared containing
50/50
(weight/weight) silicone gel forming agent and ascorbic acid and derivatives
thereof as a
benefit agent. The formulation is prepared by condensing at 115 to
120°C, in the presence
of 0.025 parts anhydrous ammonia, 67 parts of a 70wt% xylene solution of a
siloxane
resin copolymer consisting essentially of (CH3)3Si01/2 units and Si04/2 units
in a molar
ratio of approximately 0.75:1 and containing approximately 2.7 weight percent
hydroxyl
based on solids as determined by FTIR (ASTM E-168), 31 parts of a hydroxyl
terminated
polydimethylsiloxane having a viscosity of about 13,500 cP (mP.s) at
25°C and 2 parts of
xylene. Following the condensation reaction, the mixture was heated to
140°C for 1 hour
to remove any excess ammonia.
The silicone mass was then mixed with an equal weight of ascorbic acid and
derivatives
thereof (ultrafine powder, Hoffinan-LaRoche) for 17 minutes using a Lee
stainless steel
tilt kettle with a built-in Eppinbach high shear mixer.
The silicone solution is transferred to a suitably shaped mould and allowed to
air dry
overnight to allow evaporation of the solvents. The resulting device is
removed from the
mould and packaged. This silicone-containing pre-formed, sheet-like device was
found to
be suitable for delivering ascorbic acid and derivatives thereof as a benefit
agent to the
skin, hair or nails.
Example 5
50 parts (dry weight) of medical grade acrylic pressure sensitive adhesive
(Draize scale
score 0-1), dissolved in ethyl acetate and toluene, is mixed with 50 parts
(ascorbic acid
and derivatives thereof and sodium ascorbate, both as dry powders, in a 1:22
(wt/wt)
ratio) to form the cosmetically effective adhesive matrix. It is transferred
to a suitably
shaped mould and then cured at 121.2°C. This pre-formed, sheet-like
device was found to
be suitable for delivering at least one benefit agent to the skin, hair or
nails.
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Example 6
Ingredient % w/w
Agar 0.6
Agarose 0.3
Locust Bean Gum 0.1
Konjac Mannan 0.2
Xanthan Gum 0.1
Glycerin 15.0
Panthenol 3.0
Polysorbate 60 0.08
Benzyl Alcohol 0.3
Ethyl Paraben 0.1
Propyl Paraben 0.05
Water to 100
Force To Rupture/N 78
Compression 58
The polysaccharide gums are mixed with water to form a uniform dispersion and
any
additional components are added. Formation of a uniform dispersion can be
facilitated by
pre-dispersing the polysaccharides in a non-solvent, for example, polyhydric
alcohol. The
mixture is heated with stirnng to about 90°C to fully hydrate the
polysaccharide gums.
The liquid gel may be de-gassed, for example, by vacuum, to remove air bubbles
dispersed within the liquid. The liquid gel is then dispensed into a suitably
shaped mould
and is then cooled to ambient temperature to set up the gel structure. The
device may then
be removed from the mould. Alternatively, the liquid gel may be cast into a
sheet and an
appropriately shaped device may be cut from the gel sheet. The device of
Example 6 is
illustrated in Figure 4 of the accompanying drawings. The device is then
packaged into
materials which have a low water vapour permeability to minimise drying out of
the
device during storage.
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Replicates of the device were then assessed for surface roughness (Table 1)
and surface
reflectance (Table 2) using a variety of texturing surfaces. The texturing
surface may be
brought into contact with the device, either before or during gelling of the
liquid gel.
Table 1 - Surface Roughness of Silicone Casts
Texturing Surface
Ra ~q Rz
None 4.85 6.32 14.13
60 mesh, X-71892 21.10 34.37 93.93
40 hex, X-251372 92.27 133.51 353.78
VFE, 3.4mi1, X-159282 160.22 189.26 441.45
DRI-WEAVE, pattern #35/7 171.18 206.07 527.44
Hydroformed filml 315.26 360.85 786.01
1 A hydroformed film having both micro and macro apertures as described in US-
A-
4,609,518 to Curro et al, issued September 2, 1986. Preferably, the macro
apertures have
a teardrop pattern with 12% open area disposed in a pattern having 24 macro
apertures/cm2 wherein the base of each macro aperture is 1.54mm2, the tip is
0.3mm2 in
diameter and the micro apertures are formed on a screen having a 100 mesh
pattern.
2 from Tredegar Film Products, 1100 Boulders Parkway, Richmond, VA, USA 23225.
All of the texturing surfaces are, as is preferred, formed films, described
above in
connection with substrates.
The negative image of all suitable texturing surfaces as defined here will
have Ra of
greater than lOgm, preferably greater than 20~m, when measured as described
above.
The preferred range for a negative image of a texturing surface for the
devices of the
present invention is Ra greater than 10~m and less than 316gm when measured as
described above. The negative image of a suitable texturing surface as defined
here will
have Rq of greater than 7~m, preferably greater than 30pm and/or most
preferably less
than 375~m. The negative image of a suitable texturing surface will have RZ of
greater
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WO 01/01951 PCT/US00/18108
than 15~m, preferably greater than 75pm, more preferably greater than 90~m
and/or most
preferably less than 800~.m.
Table 2 - % Surface Reflectance of Textured Surface
Texturing Surface 20 60 85
None 48 64.8 72.8
60 mesh, X-71892 0.9 4.0 4.3
40 hex, X-2S 1372 1.8 7.2 4.3
DRI-WEAVE, pattern # 2.5 14.3 17.2
35/7
l 0.3 0.8 0.35
Hyrdroformed film
VFE, 3.4mi1, X-159282 2.7 23.6 19.2
1 A hydroformed film having both micro and macro apertures as described in US-
A-
4,609,518 to Curro et al, issued September 2, 1986. Preferably, the macro
apertures have
a teardrop pattern with 12% open area disposed in a pattern having 24 macro
apertures/cm2 wherein the base of each macro aperture is 1.54mm2, the tip is
0.3mm2 in
diameter and the micro apertures are formed on a screen having a 100 mesh
pattern.
2 from Tredegar Film Products, 1100 Boulders Parkway, Richmond, VA, USA 23225.
All textured surfaces as defined herein will have preferred levels of gloss in
the range of <
40, < 58, and < 65 for the 20°, 60° and 85° geometries,
respectively. The preferred ranges
of gloss for devices of the present invention are 0-10, 0-30 and 0-25 for the
20°, 60° and
85° geometries, respectively. The most preferred gloss ranges are 0-5,
0-25 and 0-20 for
the 20°, 60° and 85° geometries, respectively.
Example 7
w/w)
Agarose 0.9
Glycerine 20.0
Butylene Glycol 5.0
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Ethyl Paraben 0.15
Disodium EDTA 0.1
Water to 100
The polysaccharide gums are mixed with water to form a uniform dispersion and
any
additional components are added. The formation of a uniform dispersion can be
facilitated by pre-dispersing the polysaccharides in a non-solvent, for
example, polyhydric
alcohol. The gel-forming mixture is heated with stirring to about 90°C
to fully hydrate the
polysaccharide gums. Following de-gassing (by vacuum for example), the liquid
gel-
forming mixture is transferred to a suitably shaped mould (for example, a
mould shaped
to produce the patch device illustrated in Figures 6 and 7 of the accompanying
drawings).
The gel transparency of the present device was assessed as described above -
its
transparency threshold is 4 font size.
