Note: Descriptions are shown in the official language in which they were submitted.
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ADDITIVES FOR BODYWASHES
CROSS-REFERENCE
[0001] This application claims the benefit of U.S. Provisional Application
No. 60/648,961 filed January 31, 2005, and U.S. Patent Application Nos.
11/076,565;
11/076,089; 11/076,517; 11/076,088; and 11/076,507, all filed March 8, 2005,
all of
which are incorporated herein by reference in their entirety.
BACKGROUND OF THE INVENTION
[0002] Exposure to ultraviolet light, primarily through exposure to the sun's
rays,
produces a nuinber of harmful effects including premature skin aging, loss of
elasticity,
wrinkling, drying, and an increased risk of developing skin cancer. Currently
a nuinber of
sunscreen products are marketed to protect against these harmful effects. All
of these
products contain agents known to filter out some of the sun's harmful rays
incorporated
into creams, ointments, lotions, solutions or suspensions. Such products are
applied just
prior to anticipated sun exposure, provide short term protection, and are
removed by
bathing, washing or normal desquamation of skin. Soap in the form of bodywash
has for
years been used to remove oil due to its surfactant composition and associated
charges.
A normal soap contains both charges of a positive and negative nature.
Although
attempts have been made to combine sunscreens with soaps (i.e., surfactant
agents), none
has provided an ideal combination of high sun protection factor (SPF) and long-
lasting
effect in a composition that maintains its integrity. Other additives in
addition to
sunscreen are also potentially useful when applied in conjunction with a
bodywash, but at
present few products utilize this potential. The current invention addresses
these lacks.
SUMMARY OF THE INVENTION
[0003] The invention encompasses bodywashes containing an additive. The
additive
may contain a sunscreen. The invention further encoinpasses methods of making
and
using bodywashes containing an additive, e.g., an additive containing a
sunscreen.
[0004] In one aspect, the invention provides a bodywash containing an additive
that
comprises a sunscreen, wherein after a single application of the bodywash to
skin and
rinsing, the skin is protected from sunlight with an average SPF of at least
about 15. In
some embodiments, the SPF of 15 is maintained for an average of at least about
4 hours
after rinsing. In some embodiments, the sunscreen is encapsulated, e.g., in
sol-gel
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microcapsules. In some embodiments, the sunscreen is an organic sunscreen that
is
aminobenzoic acid, avobenzone, cinoxate, dioxybenzone, homosalate, menthyl
anthranilate, octocrylene, octyl methoxycinnamate, octyl salicylate,
oxybenzone,
padimate 0, phenylbeizzimidazole sulfonic acid, sulisobenzone, or trolamine
salicylate.
In some embodiments, the sunscreen is a cinnamate derivative. In some
embodiments,
the additive contains 3 organic sunscreens. In some embodiments the 3 organic
sunscreens are selected from the group consisting of aminobenzoic acid,
avobenzone,
cinoxate, dioxybenzone, hoinosalate, menthyl anthranilate, octocrylene, octyl
methoxycinnamate, octyl salicylate, oxybenzone, padimate 0,
phenylbenzimidazole
sulfonic acid, sulisobenzone, and trolamine salicylate. Embodiments may
further contain
an inorganic sunscreen. In some embodiments, the inorganic sunscreen is
selected from
the group consisting of zinc oxide and titanium dioxide. In some embodiments,
the
sunscreen is a UVB absorber sunscreen, and the composition also contains a UVA
absorber sunscreen and a physical blocker sunscreen, where the UVB-absorber
sunscreen
is selected from the group consisting of aminobenzoic acid, cinoxate,
dioxybenzone,
homosalate, octocrylene, octyl methoxycinnamate, octyl salicylate, oxybenzone,
padimate 0, phenylbenzimidazole sulfonic acid, sulisobenzone, and trolamine
salicylate;
the UVA-absorber sunscreen is selected from the group consisting of avobenzone
and
menthyl anthranilate; and the physical blocker sunscreen is selected from the
group
consisting of titaniuin dioxide and zinc oxide. Embodiments may further
contain a
cationic polymer. In some embodiments, the catioilic polymer is a
polyquaternium. In
some embodiments, the polyquatemium is polyquatemium-4, -7,-11, -22, -27, -44,
-51, or
-64. In preferred embodiments, the cationic polymer is polyquaternium-4.
Embodiments
may also contain a film former, a preservative, and/or an antioxidant that is
stable upon
exposure to sunlight.
[0005] In another aspect, the invention provides a bodywash containing an
additive that
contains a sunscreen, where, after application of the bodywash to skin and
rinsing, the
sunscreen penetrates an average of no fu.rther than 30 microns into the skin
after
application followed by rinsing. In some embodiments of this aspect, after
application of
the bodywash to skin and rinsing, the skin is protected from sunlight with an
average SPF
of at least about 15.
[0006] In a further aspect, the invention provides a bodywash comprising a UVA-
absorbing sunscreen, a UVB-absorbing sunscreen, a physical blocker sunscreen,
and a
cationic polymer. In some embodiments, the UVB-absorber sunscreen is selected
from
the group consisting of aminobenzoic acid, cinoxate, dioxybenzone, homosalate,
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octocrylene, octyl methoxycinnamate, octyl salicylate, oxybenzone, padimate 0,
phenylbenzimidazole sulfonic acid, sulisobenzone, and trolamine salicylate;
the UVA-
absorber sunscreen is selected from the group consisting of avobenzone and
menthyl
antliranilate; the physical blocker sunscreen is selected from the group
consisting of
titanium dioxide and zinc oxide; and the cationic polymer is a polyquatemium.
Some of
these embodiments contain octyl methoxycinnamate, octocrylene, avobenzone,
titanium
dioxide, and a polyquaternium selected from the group consisting of
polyquatemium-4, -
7,-11, -22, -27, -44, -51, or -64. A preferred polyquaternium is
polyquaterniuin-4. The
octylmethoxy ciniiamate may be encapsulated, e.g., in sol-gel microcapsules.
The octyl
methoxycimlamate can present at about 4.5-9%, the octocrylene can present at
about 0.5-
15%, the avobenzone can present at about 2-4 Jo, and the titanium dioxide can
present at
about 3-9%. Additionally, in embodiments containing polyquatemium-4, the
polyquatemium-4 can be present at about 0.5-3%. In some embodiments, the octyl
methoxycinnamate is present at about 7.6%, the octocrylene is present at about
11.3%,
the avobenzone is present at about 2.8%, and the titanium dioxide is present
at about
6.5%. Additionally, in these embodiments that contain polyquatemium-4, the
polyquatemium-4 can be present at about 2.8%. A film former can also be
present, e.g.,
at about 1.5%. In this aspect, the bodywash of claim can further contain a non-
sunscreen
active. In some embodiments, the non-sunscreen active is selected from the
group
consisting of steroidal anti-inflammatory actives, analgesic actives,
antifungals,
antibacterials, and antiparasitics, anti-allergenics, medicinal actives, skin
rash, skin
disease and dermatitis medications, insect repellant actives, antioxidants,
hair growth
promoter, hair bleaching agents, deodorant compounds, and mixtures and
combinations
thereof. In some embodiments, at least one of the sunscreens is encapsulated,
e.g., in sol-
gel microcapsules. In some embodiments, the cationic polymer is a
polyquatemium. In
some embodiments, the polyquaternium is polyquaternium-4, -7,-11, -22, -27, -
44, -51, or
-64. In preferred embodiments, the cationic polymer is polyquatemium-4.
Embodiments
may also contain a film former, a preservative, and/or an antioxidant that is
stable upon
exposure to sunlight.
INCORPORATION BY REFERENCE
[0007} All publications and patent applications mentioned in this
specification are herein
incorporated by reference to the same extent as if each individual publication
or patent
application was specifically and individually indicated to be incorporated by
reference.
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DETAILED DESCRIPTION OF THE INVENTION
[0008] The present invention encompasses compositions containing one or more
active
ingredients (also referred to herein as "actives") that may be added to a
bodywash
composition to provide an active/bodywash combination. The invention also
encompasses a bodywash containing such an active ingredient. In some
embodiments,
the active ingredient is one or more sunscreens. The invention further
encompasses
methods of use and manufacture of the compositions, and business methods.
[0009] As used herein, "bodywash" encompasses all cleansing vehicles applied
to the
body. Exemplary forms of cleansing vehicles include, but are not limited to,
liquid, bar,
gel, foam, aerosol or pump spray, cream, lotion, stick, powder, or
incorporated into a
patch or a towelette. In addition, soapless cleansers may be used as well. The
bodywash
can be made into any suitable product form. Thus, as used herein, "bodywash"
includes,
but is not limited to, a soap including liquid and bar soap; a shampoo; a hair
conditioner;
a shower gel; including an exfoliating shower gel; a foaming bath product
(e.g. gel, soap
or lotion); a milk bath; a soapless cleanser, including a gel cleanser, a
liquid cleanser and
a cleansing bar; moist towelletes; a body lotion; a body spray, mist or gel;
bath
effervescent tablets (e.g., bubble bath); a hand and nail cream; a bath/shower
gel; a
shower cream; a depilatory cream; a shaving product e.g. a shaving cream, gel,
foam or
soap, an after-shave, after-shave moisturizer; and combinations thereof, and
any other
composition used for cleansing or post-cleansing application to the body,
including the
skin and hair. Especially useful as bodywashes in the invention are soaps,
e.g., liquid
soaps and bar soaps, and shampoos.
1. Compositions
[0010] In one aspect, the invention provides additives containing active
ingredients,
where the additive is designed to be added to a bodywash (e.g., soap or
shampoo). In
some embodiments, the invention provides sunscreen compositions ("sunscreen
additives") that may be added to a bodywash preparation to impart sun
protection. In
some embodiments, the invention provides a combination of a sunscreen additive
and a
bodywash preparation ("sunscreen/bodywash"). Thus, a sunscreen additive of the
invention may be mixed with a conventional bodywasll; alternatively, the
invention
provides pre-mixed sunscreen/bodywash. In either case, the sunscreen/bodywash
composition is generally applied in the same manner as the bodywash alone and,
typically, rinsed, with additive, e.g., sunscreen protection, being left on
the skin after
rinsing. In some cases, e.g., soapless cleansers, the bodywash is applied
without rinsing.
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For suiiscreeri additives as part of a sunscreen/bodywash, the sunscreen
protection after
application and, typically, rinsing is, on average, greater than an SPF of 1,
up to about
SPF 50. As used herein in the context of SPF, "average SPF" is the SPF,
determined as
described herein, for about 5 to about 50 subjects, or about 5 to about 20
subjects, or
about 5 to about 10 subjects, where the subjects preferably have Type II skin.
In some
embodiments, the average SPF provided by the sunscreen/bodywash after rinsing
is about
1 to about 50, or about 2 to about 50, or about 2 to about 40, or about 2 to
about 30, or
about 2 to about 20, or about 2 to about 10, or about 2 to about 5, or about 5
to about 25,
or about 5 to about 20, or about 5 to about 15, or about 5 to about 10. In
some
einbodiments, the average SPF provided by the sunscreen/bodywash, after
rinsing, is
above about 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19,
or 20. In some
preferred einbodiments, the average SPF after rinsing is above about 2. In
some
preferred embodiments, the average SPF after rinsing is above about 5. In some
preferred embodiments, the average SPF after rinsing is above about 10. In
some
preferred embodiments, the average SPF after rinsing is above about 15. In
some
embodiments, the average SPF provided by the sunscreen/bodywash of the
invention
remains above about 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17,
18, 19, or 20,
for an average of at least about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, or more
than about 10
hours after rinsing. In some embodiments the average SPF provided by the
sunscreen/bodywash of the invention increases with each additional washing
after a first
wash, so that after a second, third, _fourth, or fifth wash, the SPF provided
can be above
about 2, 4, 6, 8, 10, 15,, 20, 25, 30, 40, 45, or more than about 45.
[0011] SPF is a commonly used measure of photo protection of a sunscreen
against
erythema. This nu.inber is derived from another parameter, the minimal
erythemal dose
(MED). MED is defined as the "least exposure dose at a specified wavelength
that will
elicit a delayed erythema response." The MED indicates the amount of energy
irradiating
the skin and the responsiveness of the slcin to the radiation. The SPF of a
particular photo
protector is obtained by dividing the MED of protected skin by the MED of
unprotected
skin. The higher the SPF, the more effective the agent in preventing sunburn.
The SPF
value tells how many times longer a person can stay in the sun before the
person will
experience 1 MED. For example, utilizing a sunscreen with an SPF of 6 will
allow an
individual to stay in the sun six times longer before receiving 1 MED. As the
SPF value
of a sunscreen increases, the less chance exists for development of tam-ling
of the skin.
Typically, commercially available sunscreening products have SPF values
ranging from
about 2 to 45.
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[0012] '1Vrethods for measuring SPF are described in, e.g., FDA monograph
C.F.R. 21. A
method for applying the sunscreen prior to measurement is as follows: Wet 50
cm2
square area of testing site with 10 ml of water delivered with a syringe.
Apply test
sample as per FDA monograph to area. Worlc lather on the subject for 3 minutes
to allow
the product to absorb into the skin. Rinse area after 2 additional minutes
with 20m1 of
water. Pat dry and allow 15 minutes before exposure to radiation as per FDA
monograph.
[0013] In some embodiments, after application of the bodywash containing the
additive
(e.g., sunscreen) to the skin followed by rinsing, the additive (e.g.,
sunscreen) penetrates
to an average of at least about 5 microns beneath the skin surface. In some
embodiments,
the additive penetrates to an average of at least about 10, 15, 20, 25, 30,
40, 50, 60, 70,
80, 90, 100,120, or 150 microns beneath the skin surface. In some embodiments,
after
application of the bodywash containing the additive (e.g., sunscreen) to the
skin followed
by rinsing, the additive (e.g., sunscreen) penetrates to an average of no more
than about
30 microns beneath the skin surface. In some embodiments, the additive
penetrates to an
average of no more than about 50, 40, 30, 25, 20, 15, 10, or 5 inicrons
beneath the skin
surface. In some embodiments, after application of the bodywash containing the
additive
(e.g., sunscreen) to the skin followed by rinsing, the additive (e.g.,
sunscreen) penetrates
to an average of about 5 to about 50, or about 5 to about 40, or about 5 to
about 30, or
about 10 to about 40, or about 15 to about 40, or about 20 to about 40, or
about 5, 10, 15,
20, 25, 30, 25, 40, 45, or 50 microns beneath the skin surface. Depth of
penetration may
be tested by tape stripping methods, as are well-known in the art.
[0014] The sunscreen additives and sunscreen/bodywashes of the invention
contain at
least one sunscreen. In some embodiments, the sunscreen additives of the
invention
contain one, two, three, four, or more than four sunscreens. In preferred
embodiments,
the sunscreen additives of the invention include three sunscreens. In other
preferred
embodiments, the sunscreen additives of the invention include four sunscreens.
The
sunscreens may be organic or inorganic. The sunscreens may be a UVA absorber,
a
UVB absorber, a physical blocker, or any combination thereof. In some
embodiments
one or more of the sunscreens is encapsulated. A number of types of
encapsulation may
be employed as described herein.
[0015] Compositions of the invention may include one or more actives that are
not
sunscreens, where the composition is designed to be an additive to a bodywash.
In some
compositions of the invention, the actives are provided in combination with
one or more
sunscreens. In some compositions, the actives are provided without sunscreen.
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[0016] T1ie additives, e.g., sunscreen additives, and additive/bodywashes,
e.g.,
sunscreen/bodywashes, of the invention may further include one or more
components to
provide a positive charge to the system to assist with attaclunent to protein
and other
charged components of skin and/or hair, e.g., cationic polymeric agents. The
cationic
polymer may be, for example, a quaternium, e.g., polyquaternium.
[0017] The additives, e.g., sunscreen additives, and additive/bodywashes,
e.g.,
sunscreen/bodywashes, of the invention may further include a film former.
[0018] Other optional ingredients of the additives, e.g., sunscreen additives,
and
additive/bodywashes, e.g., sunscreen/bodywashes, of the invention include
preservatives,
antioxidants, chelating agents, liquid hydrocarbon (e.g., similar to pentane),
foaming
agents (e.g., a cationic foaming agent), skin nourishing components,
antibacterials,
medicinals, and the like, as described below.
[0019] The additives, e.g., sunscreen additives, of the invention may be
combined with
any conventional bodywash. The bodywash composition with which the additive,
e.g.,
sunscreen additive is coinbined may be any bodywash known in the art or
apparent to one
of skill in the art, as described above. In embodiments where the additive is
a non-
sunscreen active, the additive may be combined with any composition intended
for
topical application. In these embodiments, the additive is often encapsulated,
e.g., in sol-
gel microcapsules.
[0020] In some embodiments the invention provides an additive, e.g., sunscreen
additive,
in combination with a bodywash composition to provide an additive/bodywash,
e.g.
sunscreen/bodywash, composition. In these embodiments, the additive, e.g.,
sunscreen
additives, of the invention are provided in combination with one or more
surfactants.
The surfactant(s) may be cationic, anionic, nonionic, zwitterionic,
amphoteric, or any
combination thereof. In preferred embodiments, the sunscreen/bodywash
compositions
of the invention include at least one cationic surfactant.
A. Sunscreens
[0021] The sunscreen additives and sunscreen/bodywashes of the invention
contain at
least one sunscreen. The sunscreen may be organic or inorganic, or a
combination of
both may be used. Sunscreens of use in the invention include UV absorbers or
blockers
(e.g., many inorganic sunscreens are UV blockers). UV absorbers may be a UVB
or
UVA absorber (e.g., UVA I or UVA II absorber). In some embodiments, the
sunscreen
additives or sunscreen/bodywashes of the invention include an organic and an
inorganic
sunscreen. In some embodiments, the sunscreen additives or
sunscreen/bodywashes of
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the invention include more tnan one organic sunscreen (e.g., at least one LIVB
absorber
and at least one UVA absorber) and at least one inorganic sunscreen. In some
embodiments, the sunscreen additives of the invention include only a physical
blocker
sunscreen, e.g., titanium dioxide. These embodiments may further contain a
cationic
polymer and/or a film former, as well as any other components described herein
for
sunscreen additives.
[0022] Additional ingredients may include film formers, cationic polymers,
antioxidants,
preservatives, and the lilce, as described herein. In some embodiments, the
sunscreen
additives or sunscreen/bodywashes of the invention include an organic and an
inorganic
sunscreen. In some enibodiments, the sunscreen additives or
sunscreen/bodywashes of
the invention include more than one organic sunscreen (e.g., at least one UVB
absorber
and at least one UVA absorber) and at least one inorganic sunscreen.
[0023] In preferred embodiments, one or more of the sunscreens used in the
invention are
encapsulated.
[0024] Any sunscreen known in the art or apparent to the skilled artisan inay
be used in
the invention. The term "sunscreen" or "sunscreen agent" as used herein
defines
ultraviolet ray-blocking compounds exhibiting absorption or blockage within
the
wavelength region between about 290 and 420 nin. Sunscreens may be classified
into
five groups based upon their chemical structure: para-amino benzoates;
salicylates;
cinnamates; benzophenones; and miscellaneous chemicals including menthyl
anthralinate
and digalloyl trioleate. Inorganic sunscreens may also be used including
titanium
dioxide, zinc oxide, iron oxide and polymer particles such as those of
polyethylene and
polyamides.
[0025] Specific suitable sunscreens iuiclude, for example: p-aminobenzoic
acid, its salts
and its derivatives (ethyl, isobutyl, glyceryl esters; p-dimethylaminobenzoic
acid);
Anthranilates (i.e., o-aminobenzoates; methyl, menthyl, phenyl, benzyl,
phenylethyl,
linalyl, terpinyl, and cyclohexenyl esters); Salicylates (amyl, phenyl,
benzyl, menthyl,
glyceryl, and dipropylene glycol esters); Cinnamic acid derivatives (methyl
and benzyl
esters, alpha-phenyl cinnamonitrile; butyl cinnamoyl pyruvate);
Dihydroxycinnamic acid
derivatives (umbelliferone, methylumbelliferone, methylaceto-umbelliferone);
Trihydroxycinnamic acid derivatives (esculetin, methylesculetin, daphnetin,
and the
glucosides, esculin and daphnin); Hydrocarbons (diphenylbutadiene, stilbene);
Dibenzalacetone and benzalacetophenone; Naphtholsulfonates (sodium salts of 2-
naphthol-3,3-disulfonic and of 2-naphthol-6,8-disulfonic acids);
Dihydroxynaphthoic
acid and its salts; o- and p-Hydroxybiphenyidisulfonates; Cou.marin
derivatives (7-
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hydroxy, 7-methyl, 3-phenlyll); Diazoles (2-acetyl-3-bromoindazole, phenyl
benzoxazole, methyl naphthoxalole, various aryl benzothiazoles); Quinine salts
(bisulfate, sulfate, chloride, oleate, and tannate); quinoline derivatives (8-
hydroxyquinoline salts, 2-phenylquinoline); Hydroxy-or methoxy substituted
benzophenones; Uric and vilouric acids; Tannnic acid and its derivatives
(e.g.,
hexaethylether); (Butyl carbityl) (6-propyl piperonyl) ether; Hydroquinone;
Benzophenones (Oxybenzene, Sulisobenzone, Dioxybenzone, Benzoresorcinol,
2,2',4,4'-
Tetrahydroxybenzophenone, 2,2'-Dihydroxy4,4'-dimethoxybenzophenone,
Octabenzone;
4-Isopropyhldibenzoylmethane; Butylmethoxydibenzoylmethane; Etocrylene; and 4-
isopropyl-di-benzoylmethane; titanium dioxide, iron oxide, zinc oxide, and
mixtures
thereof. Other cosmetically-acceptable sunscreens and concentrations (percent
by
weight of the total cosmetic sunscreen composition) include diethanolamine
methoxycinnamate (10% or less), ethyl-[bis(hydroxypropyl)]aminobenzoate (5% or
less),
glyceryl aminobenzoate (3% or less), 4-isopropyl dibenzoylmethane (5% or
less), 4-
methylbenzylidene camphor (6% or less), terephthalylidene dicamphor sulfonic
acid
(10% or less), and sulisobenzone (also called benzophenone-4, 10% or less).
[0026] In preferred embodiments, sunscreens are FDA-approved or approved for
use in
the European Union. For example, FDA-approved sunscreens may be used, singly
or,
preferably, in combination. See, e.g., U.S. Patent Nos. 5,169,624; 5, 543,136;
5,849,273;
5,904,917; 6,224,852; 6,217,852; and Segarin et al., chapter Vil, pages 189 of
Cosmetics
Science and Technology, and Final Over-the-Counter Drug Products Monograph on
Sunscreens (Federal Register, 1999:64:27666-27963), all of which are
incorporated
herein by reference.
[0027] For example, for a product marketed in the United States, preferred
cosmetically-
acceptable sunscreens and concentrations (reported as a percentage by weight
of the total
cosmetic sunscreen composition, and referring to the final percentage of the
sunscreen
after addition to the bodywasli) include: aminobenzoic acid (also called para-
aminobenzoic acid and PABA; 15% or less; a UVB absorbing organic sunscreen),
avobenzone (also called butyl methoxy dibenzoylmethane; 3% or less, a UVA I
absorbing organic sunscreen), cinoxate (also called 2-ethoxyethyl p-
methoxycinnamate;
3% or less, a UVB absorbing organic sunscreen), dioxybenzone (also called
benzophenone-8; 3% or less, a UVB and UVA II absorbing organic sunscreen),
homosalate (15% or less, a UVB absorbing organic sunscreen), menthyl
anthranilate
(also called menthyl 2-aminobenzoate; 5% or less, a UVA II absorbing organic
sunscreen), octocrylene (also called 2-ethylhexyl-2-cyano-3,3
diphenylacrylate; 10% or
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less, a UVB absorbing organic sunscreen), octyl methoxycinnamate (7.5% or
less, a UVB
absorbing organic sunscreen), octyl salicylate (also called 2-ethylhexyl
salicylate; 5% or
less, a UVB absorbing organic sunscreen), oxybenzone (also called benzophenone-
3; 6%
or less, a UVB and UVA II absorbing organic sunscreen), padimate O(also called
octyl
dimethyl PABA; 8% or less, a WB absorbing organic sunscreen),
phenylbenzimidazole
sulfonic acid (water soluble; 4% or less, a UVB absorbing organic sunscreen),
sulisobenzone (also called benzophenone-4; 10% or less, a UVB and UVA II
absorbing
organic sunscreen), titanium dioxide (25% or less, an inorganic physical
blocker of UVA
and UVB), trolamine salicylate (also called triethanolamine salicylate; 12% or
less, a
UVB absorbing organic sunscreen), and zinc oxide (25% or less, an inorganic
physical
blocker of UVA and UVB).
[0028] For a product marketed in the European Union, prefeffed cosmetically-
acceptable
photoactive compounds and concentrations (reported as a percentage by weight
of the
total cosmetic sunscreen composition, and referring to the final percentage of
the
sunscreen after addition to the bodywash) include: PABA (5% or less), campllor
benzalkonium methosulfate (6% or less), homosalate (10% or less), benzophenone-
3
(10% or less), phenylbenzimidazole sulfonic acid (8% or less, expressed as
acid),
terephthalidene dicamphor sulfonic acid (10% or less, expressed as acid),
butyl
methoxydibenzoylmethane (5% or less), benzylidene camphor sulfonic acid (6% or
less,
expressed as acid), octocrylene (10% or less, expressed as acid),
polyacrylamidomethyl
benzylidene camphor (6% or less), octyl methoxycinnamate (10% or less), PEG-25
PABA (10% or less), isoamyl p-methoxycinnamate (10% or less), ethylhexyl
triazone
(5% or less), drometrizole trielloxane (15% or less), diethylhexyl butamido
triazone (10%
or less), 4-inethylbenzylidene camphor (4% or less), 3-benzylidene camphor (2%
or less),
ethylhexyl salicylate (5% or less), ethylhexyl dimethyl PABA (8% or less),
benzophenone-4 (5%, expressed as acid), methylene bis-benztriazolyl
tetramethylbutylphenol (10% or less), disodium phenyl dibenzimidazole
tetrasulfonate
(10% or less, expressed as acid), bis-ethylhexyloxyphenol methoxyphenol
triazine (10%
or less), methylene bisbenzotriazolyl tetramethylbutylphenol (10% or less,
also called
TINOSORB M), and bisethylhexyloxyphenol methoxyphenyl triazine.(10% or less,
also
called TINOSORB S).
[0029] In some embodiments, the sunscreen additives or sunscreen/bodywashes of
the
invention include a silicone long-chain molecule with chromophores, e.g.,
PARASOL
SLX (DSM Nutritional Products), which contains benzyl malonate chromophores
attached to specific points on a polysiloxane chain. Thus, in some
einbodiments, the
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invention provides a sunscreen additive or sunscreen/bodywash composition that
contains
sunscreen that comprises a silicone long-chain molecule with chromophores. For
example, compositions of the invention include a composition containing octyl
methoxycinnamate, octocrylene, avobenzone, titanium dioxide, and a silicone
long-chain
molecule with chromophores. The silicon long-chain molecule may be used in
sunscreen
additives at about 0.5 to about 5%, or in sunscreen/bodywashes at about 0.2 to
about 2%.
[0030] Inorganic physical blockers of UVA and UVB useful in the invention
further
include iron oxide and polymer particles such as those of polyethylene and
polyamides.
[0031] In some embodiments, the sunscreen additives and sunscreen/bodywashes
contain
at least one sunscreen active that is cinnamate (e.g., Octylmethoxycinnamate
(ethyl hexyl
methoxycimiamate), (available under the tradename PARSOL MCX), oxybenzone
(e.g.,
benzophenone-3 (2-Hydroxy4-Methoxybenzophenone), avobenzone (4-tert-Butyl-4'-
methoxydibenzoylmethane or PARSOL 1789), octyl salicylate (2-Ethylhexyl
Salicylate),
octocrylene (2-Ethylhexyl2-Cyano-3,3-Diphenylacrylate), methyl anthranilate,
and/or
titanium dioxide, or combinations thereof.
[0032] Sunscreen additives and sunscreen/bodywashes of the invention may, in
some
embodiinents, contain as a sunscreen component only titanium dioxide. When
titanium
dioxide is used in compositions of the invention, either alone or in
combination with
other sunscreens, the titanium dioxide can have an anatase, rutile, or
amorphous
structure. The titaniuin dioxide particles can be uncoated or can be coated
with a variety
of materials including, but not limited to, aluminum compounds such as
aluminum oxide,
aluininuin stearate, aluminum laurate and the like; phospholipids such as
lecithin;
silicone compounds; and mixtures thereof. Various grades and forms of titanium
dioxide
are described in CTFA Cosmetic Ingredient Dictionary, Third Edition (1982),
pp. 318-
319; U.S. Pat. No. 4,820,508 to Wortzinan, issued Apr.11, 1989; and World
Patent No.
WO 90/11067 to Elsom et al, published Oct. 4, 1990; these three references are
incorporated by reference herein in their entirety. Suitable grades of
titanium dioxide for
use in the compositions of the present invention are available conunercially
such as the
MT micronized series from Tri-K Industries (Emerson, NJ). These micronized
titanium
dioxides generally have a mean primary particle size ranging from about 10 nm
to about
50 nm. For example, titaniuin dioxide having a mean primary particle size of
about 15
nm is available under the trade designations MT-150W (uncoated) and MT-100T
(coated
witli stearic acid and aluminum compounds). Uncoated titanium dioxides having
mean
primary particle sizes of around 35 nm and around 50 nm are available under
the trade
designations MT-500B and MT-600B, respectively. Other coated titanium dioxides
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having a mean primary particle size around 15 nm include MT-IOOF (modified
with
stearic acid and iron hydroxide) and MT-100S (treated with lauric acid and
aluminum
hydroxide). Mixtures of two or more types and particle size variations of
titanium dioxide
can be used in the present invention.
[0033] A particularly preferred form of titanium dioxide is silica-coated
Ti02. Such a
silica-coated Ti02 is available under the tradename T-AVO (Eusolex).
[0034] If a zinc compound is chosen as the inorganic sunscreen, some zinc-
based
compositions (e.g., Z-CoteTM HP1 [registered trademark, SkinCeuticals])
provide
micro-fine zinc oxide coated with a form of dimethicone. As expressed by the
manufacturer, the dimethicone coating transfonns the frequently granular and
pasty
particles of zinc oxide to a smooth formulation which is transparent. The
micronizing of
these particles achieves the important advantage of providing effective
sunscreening
without giving the appearance of skin coated with white paint. '
[0035] Also to be noted in relation to inorganic blockers are Tioveil and
Spectraveil
(both of the Tioxide Group). Tioveil include products which are 40%
dispersions of
surface-treated titanium dioxide in a range of cosmetic vehicles. Spectraveil
include
products which are 60% dispersions of zinc oxide in a range of cosmetic
vehicles. In
certain variations, these products may be film-formers and may have
advantageous uses
here.
[0036] In sunscreen additives, the total sunscreens comprise about 0.1-50%, or
about 1-
30%, or about 1-25%, or about 3-25%, or about 5-25%, or about 10-25% or about
15-
25%, or about 5, 10, 15, 20, 25, 30, 35, 40, 45, or 50% of the composition
(all
percentages herein are weight percent unless otherwise specified). In
sunscreen/bodywash compositions, the total sunscreens can comprise 0.05-30%,
or about
0.5-15%, or about 0.5-12%, or about 1.5-12%, or about 2.5-12%, or about 5-12%
or
about 7-12%, or about 2.5, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 33, 35, 40, 45,
50, or more
than 50% of the composition.
[0037] In some embodiments, a sunscreen additive of the invention includes
octyl
methoxycinnamate at about 4.5-9%, Octocrylene at about 0.5-15%, Avobenzone
(e.g.,
PARSOL 1789) at about 2-4%, and titanium dioxide at about 3-9%. In some
embodiments, the octyl methoxy cimZamate is encapsulated, e.g., in amorphous
silica.
Such encapsulated octyl methoxy cinnamate is commercially available under the
trade
name UV PEARLS; about 20-40% UV PEARLS supplies about 4.5-9% octyl methoxy
cinnamate. In some embodiments, a sunscreen additive of the invention includes
octyl
methoxycinnamate at about 7.6% (in some embodiments, encapsulated as
described, e.g.,
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in W PEARL~ wherein the UV PEARLS are provided at about 33.3%), Octocrylene at
about 11.3 %, Avobenzone (PARSOL 1789) at about 2.8%, and titanium dioxide at
about 6.4%. The sunscreen additives may further include a polyquatemium, e.g.,
polyquaternium-4. In some embodiments, the polyquaternium-4 is present at
about 0.5%
to about 5%, in some embodiments, the polyquaternium-4 is present at about
2.8%. The
sunscreen additives may further include a film-former, which may comprise
dimethicone
and/or petrolatum, and/or a preservative, such as BHT. This sunscreen additive
may be
added to a conventional bodywash formulation (e.g., SUAVE Bodywash) in a ratio
of
about one part sunscreen additive to two parts bodywash (w/w). Other ratios
are
encompassed by the invention, e.g., about one part sunscreen additive to about
0.2, 0.5,
0.7 1.0, 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, 1.7, 1.8, 1.9, 2.0, 2.1, 2.2, 2.3, 2.4,
2.5, 2.6, 2.7, 2.8,
2.9, 3.0, 3.2, 3.5, 3.7, 4.0, 4.2, 4.5, 4.7, 5.0, 6.0, 7.0, 8.0, 9.0, 10, 12,
15, or 20 parts
bodywash (w/w).
[0038] It will be appreciated by those of skill in the art that the various
ingredients of the
sunscreen additive may be added to the bodywash all at once, or in groups, or
separately.
In some embodiments, the sunscreen additive comprises at least two components.
For
example, the first component may comprise all the ingredients except an
inorganic or
physical blocker sunscreen, and the second component may comprise the
inorganic or
physical blocker sunscreen. The first component is added to the bodywash with
thorough
mixing, then the second component is added. For example, in some embodiments,
all
ingredients except the titanium dioxide are mixed, then added to the bodywash,
and then
the titanium dioxide is added (see Examples).
[0039] In some embodiments, the sunscreen additives of the invention include
about 0.1
to 7.5 weight percent of octylmethoxy cinnamate, about 0.1 to 6 parts weight
percent of
octyl salicylate, about 0.1 to 5 parts weight percent of oxybenzone, about 1
to 10 weight
percent of cationic surfactant, and about 0.01 to 1 weight percent of a
quaternized
compound. These composition may further include a film former. These
compositions
may further include 0.01 to 1 weight percent of a preservative.
[0040] Encapsulation Sunscreens and other actives used in the invention may be
encapsulated. One or more of the sunscreens used in a composition may be
encapsulated;
preferably, all sunscreens used are encapsulated. Sunscreen actives may be
encapsulated
together, or may be encapsulated separately, in any combination, in the same
or in
different types of encapsulations. Generally, encapsulation involves trapping
the
sunscreen in, e.g., a vesicle. Depending on the vesicle of choice, the vesicle
may break
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open when apphect. without being limited by theory, it is thought that the
vesicle breaks
open in various types of encapsulation due to friction, temperature, or pH
from the skin
or hair, or some coinbination of these. By choosing the appropriate capsule
and additives
for the system, the stability, durability, and/or SPF provided by the
sunscreen additives
and sunscreen/bodywashes of the invention can be increased.
[0041] Any means of encapsulation known in the art, including but not limited
to
liposoines, maltodextrin capsules, silica gels, siloxanes, and the like, may
be used in the
compositions of the invention. A cationic or catanionic in dry powder form may
also be
used to encapsulate sunscreen. Commercial embodiments of encapsulated
sunscreens or
vehicles suitable for encapsulating sunscreens include CATEZOMES (Engelhard
Corp.),
EUSOLEX UV PEARLS (EMD Biosciences), and others known in the art. Methods of
encapsulation suitable for delivering benefit agents that are mixed with a
bodywash
composition are well-known in the art. See, e.g., U.S. Patent Nos. 6,825,161;
6,436,375;
6,238,650; 6,468,509, 6,362,146; 6,074,630; 5,455,048; 5,770,556; 5,955,409;
5,876,755;
4,803,195; 5,508,259; 4,749,501 ; 6,248,703 ; 5,476,660; and 4,904,524 and EP
Pat. Nos.
0,254,447; 0,025,379; and 0,399,911.
[0042] A particularly preferred method of encapsulation is sol-gel
encapsulation. This
technique is described in, e.g., U.S. Patent Nos. 6,238,650; 6,436,375,
6,303,149; and
6,468,509. Any or all of the sunscreens and/or other active ingredients of the
compositions of the invention may be encapsulated by such sol-gel
encapsulation. The
sol-gel capsules may be prepared so as to have a surface charge, e.g., a
cationic charge.
This is advantageous in that otherwise water-insoluble components may be
encapsulated
within the microcapsules, which are then freely miscible in water, e.g.,
without the need
for an emulsifying agent. For example, in some embodiments, a UVA absorber, a
UVB
absorber (e.g., octyl methoxycinnamate) and/or a physical blocker, e.g.,
titanium dioxide,
is provided as a silica sol-gel encapsulate, optionally with fixrther
ingredients including
PVP, Chlorphenesin, and an antioxidant such as BHT. A commercial embodiment of
such an encapsulation containing octyl methoxycinnamate, PVP, chlorphenesin,
and
BHT, is available under the trade name EUSOLEX UV PEARLS (EMD Biosciences).
Such a silica sol-gel encapsulated UVB absorber, e.g., octyl methoxycinnamate,
may be
used in a sunscreen additive at a concentration that results in a final
concentration of the
UVB absorber of about 1% to about 40%, or about 2% to about 20%, or about 2%
to
about 10%, or about 5% to about 10%, or about 6%, 7%, 7.4%, 7.5%, 7.6%, 8%, or
9%.
The preferred final concentration is about 7.6%. In other embodiments, more
than one
sunscreen is encapsulated as silica sol-gel encapsulate. In these embodiments,
the final
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concentration of each of the sunscreens, independently, in the final sunscreen
additive, is
about 1% to about 40%, or about 2% to about 20%, or about 2% to about 10%, or
about
1 10, 2%, 3 10, 4%, 5 10, 6 10, 7%, 7.5%, 8%, 9%, or 10%. The sunscreens maybe
encapsulated together or separately, or any combination thereof. In some
embodiments,
the invention provides an additive for addition to a bodywash that includes a
sunscreen
encapsulated in a sol-gel microcapsule and a cationic polymer (described
below). Further
ingredients in these embodiments may include a film former, antioxidant,
preservative,
chelating agent, thickener, emollient, and/or other active and inactive
ingredients as
described herein.
[0043] In some embodiments wherein encapsulation, e.g., sol-gel
microencapsulation, is
utilized, the composition of the microcapsule, e.g., sol-gel microcapsule, may
be varied
so as to allow for varying amounts of the active, e.g., sunscreen, within the
microcapsule
to be released. The microcapsules, e.g., sol-gel microcapsules, can be
prepared so as to
experience no or minimal breakage when applied to the skin and when left on
the skin.
Alternatively, the microcapsules, e.g., sol-gel microcapsules, can be prepared
so as to
experience various degrees of breakage, on average, when applied to the skin
and when
left on the skin. Thus, the microcapsules, e.g., sol-gel microcapsules, may be
prepared so
as to experience about 0% breakage, or breakage in a range from about 0.1,
0.5, 1, 2, 5,
10, 20, 30, 40, 50, 60, 70, 80, or 90% to about 0.5, 1, 2, 5, 10, 20, 30, 40,
50, 60, 70, 80,
or 90%, after application (or application and rinsing in the case of a or
bodywash
containing the microcapsules). Furthermore, the microcapsules may be
formulated so as
to break open in response to conditions that occur on the skin, so that after
application the
microcapsules act to release their contents in a time-release or controlled
manner. Non-
limiting exemplary skin or hair conditions that can vary with the user's
environment, the
variation of which can trigger breakage of microcapsules, include pH,
temperature,
friction, exposure to light or air, pressure, and the like.
[0044] Other forms of inunobilization or entrapnzent of sunscreen and other
active
components are also useful. For example, as a further variant of the use of
chemical
sunscreen agents, compositions of the invention may employ an organic
sunscreen such
as octyl methoxycinnamate trapped within a matrix. A commercial example of
such a
composition is 'found in SunCapsTM) (trademark, SkinCeuticals) in which the
organic
sunscreen molecules are evenly distributed throughout the particle.
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B. Non-sunscreen actives
[0045] In one aspect, the invention provides additives containing non-
sunscreen active
ingredients, where the additive is designed to be added to a composition for
topical
application, e.g., a bodywash. These actives may be used in combination with
the
sunscreens described above in a sunscreen additive or sunscreen/bodywash, or
may be
used in separate, non-sunscreen compositions. In some embodiments, at least
one of the
actives is encapsulated. In another aspect, the invention provides a
composition for
topical application, e.g., a bodywash, containing one or more such actives.
These actives
may be used in combination with the sunscreens described above in a sunscreen
additive
or sunscreenlbodywash, or may be used in separate, non-sunscreen compositions.
[0046] Non-limiting examples of non-sunscreen actives useful in compositions
of the
invention include sunless tanning actives, skin lightening actives, anti-acne
actives, anti-
skin wrinkling and anti-skin aging actives, vitamins, anti-inflainmatory
actives,
anesthetic actives, analgesic actives, anti-pruritic actives, anti-microbial
actives (e.g.
antifungals, antibacterials, and antiparasitics), anti-virals, anti-
allergenics, medicinal
actives (e.g., skin rash, skin disease and dermatitis medications), anti-
cellulite additives,
insect repellant actives, antioxidants, hair growth promoters, hair growth
inhibitors, hair
bleaching agents, deodorant compounds, and mixtures and combinations thereof.
[0047] Sunless tanning actives include dihydroxyacetone (DHA); glyceryl
aldehyde;
tyrosine and tyrosine derivatives such as malyltyrosine, tyrosine glucosinate,
and ethyl
tyrosine; phospho-DOPA, indoles and derivatives; and mixtures thereof
[0048] Non-limiting examples of skin lightening actives include EMBLICA (also
an
antioxidant), monobenzone (a depigmenting agent), kojic acid, arbutin,
ascorbic acid and
derivatives thereof (e.g., magnesium ascorbyl phosphate or sodium ascorbyl
phosphate),
and extracts (e.g., mulberry extract, placental extract). Non-limiting
examples of skin
lightening agents suitable for use herein also include those described in WO
95/34280,
WO 95/07432, and WO 95/23780.
[0049] Vitamins may be included in the coinpositions of the present invention.
Examples
include Vitamin A and derivatives thereof (including, for example, retinol,
see anti-
wrinkling actives), ascorbic acid (Vitamin C and derivatives), Vitamin B
(e.g., riboflavin,
vitainin B2), biotin, Vitamin D(a1l forms), Vitamin E and derivatives thereof
such as
tocopheryl acetate, beta-carotene, panthothenic acid and mixtures thereof.
[0050] Anti-acne actives include benzoyl peroxide, erythromycin, clindamycin
phosphate, 5,7-dichloro-8-hydroxyquinoline, resorcinol, resorcinol acetate,
salicylic acid,
azaleic acid, long chain dicarboxylic acids, sulfur, zinc, various natural
agents such as
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tnose ctenvect trom green tree, and mixtures thereof. Other non-limiting
examples of
suitable anti-acne actives for use herein are described in U.S. Pat. No.
5,607,980, which
description is incorporated herein by reference.
[0051] Anti-skin wrinlcling actives include a variety of agents, often in
combination, that
prevent or treat wrinkling through a variety of actions. Many approaches are
taken to
reduce the appearance of facial wrinkles based on the understanding of the
molecular
basis of wrinkle formation. Such treatments include cosmetic products, drug
therapy and
surgical procedures. For example, many cosmetic products contain hydroxy
acids, which
may stimulate collagen synthesis. Another conunon treatment utilizes retinol,
retinoic,
retinol palmitate, a derivative of vitamin A, (or its stronger, prescribed
version Retin-A
and Renova) which helps collagen production. Bicyclic aromatic compounds with
retinoid-type activity, which are useful in particular in preventing or
treating various
keratinization disorders, are described in EP 679 630. These compounds are
particularly
active for repairing or coinbating chronological or actinic ageing of the
skin, for example
such as in anti-wrinkle products. Antioxidants such as vitamin C and E and
coenzyme Q-
10 are believed to counteract free radicals, which damage cells and cause
aging and have
been used in treatments of wrinkles. Recently, the FDA approved cosmetic use
of Botox
(an extremely diluted form of botulinum toxin) to treat glabella frown lines.
Thus non-
sunscreen actives of the invention that are anti-skin aging or anti-wrinkling
actives may
contain, alone or in combination, the bicyclic aromatic compounds defined
above, other
compounds which have retinoid-type activity, free-radical scavengers, hydroxy
or keto
acids or derivatives thereof. The term "free-radical scavenger" refers to, for
example, cx
tocopherol, superoxide dismutase, ubiquinol or certain metal-chelating agents.
Hydroxy
acids include, e.g., alpha-llydroxy acids such as lactic acid and glycolic
acid or beta-
hydroxy acids such as salicylic acid and salicylic acid derivatives such as
the octanoyl
derivative; other hydroxy acids and keto acids include malic, citric,
mandelic, tartaric or
glyceric acids or the salts, amides or esters thereof.
[0052] Other anti-wrinkling agents and anti-skin aging agents useful in the
invention
include sulfur-containing D and L amino acids and their derivatives and salts,
particularly
the N-acetyl derivatives, a preferred example of which is N-acetyl-L-cysteine;
thiols, e.g.
ethane thiol; fat-soluble vitamins, ascorbyl palmitate, ceramides,
pseudoceramides (e.g.,
pseudoceramides described in U.S. Pat. Nos. 5,198,210; 4,778,823; 4,985,547;
5,175,321, all of which are incorporated by reference herein), phospholipids
(e.g.,
distearoyl lecithin phospholipid), fatty acids, fatty alcohols, cholesterol,
plant sterols,
phytic acid, lipoic acid; lysophosphatidic acid, and skin peel agents (e.g.,
phenol and the
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like), and mixtures thereot: Preferred fatty acids or alcohols are those that
have straight
or branched alkyl chains containing 12-20 carbon atoms. A particularly
preferred fatty
acid is linoleic acid since linoleic acid assists in the absorption of
ultraviolet light and
furthermore is a vital component of the natural skin lipids. Other non-
limiting examples
of suitable anti-wrinlcle actives for use herein are described in U.S. Pat.
No. 6,217,888,
which description is incorporated herein by reference.
[0053] Anti-inflammatory actives include steroidal, non-steroidal, and other
compounds.
[0054] Non-limiting examples of steroidal anti-inflammatory agents suitable
for use
herein include corticosteroids such as hydrocortisone, hydroxyltriamcinolone,
alpha-
methyl dexamethasone, dexamethasone-phosphate, beclomethasoia.e dipropionates,
clobetasol valerate, desonide, desoxymethasone, desoxycorticosterone acetate,
dexamethasone, dichlorisone, diflorasone diacetate, diflucortolone valerate,
fluadrenolone, fluclorolone acetonide, fludrocortisone, flumethasone pivalate,
fluosinolone acetonide, fluocinonide, flucortine butylesters, fluocortolone,
fluprednidene
(fluprednylidene) acetate, flurandrenolone, halcinonide, hydrocortisone
acetate,
hydrocortisone butyrate, methylprednisolone, triamcinolone acetonide,
cortisone,
cortodoxone, flucetonide, fludrocortisone, difluorosone diacetate,
fluradrenolone,
fludrocortisone, diflurosone diacetate, fluradrenolone acetonide, medrysone,
amcinafel,
amcinafide, betamethasone and the balance of its esters, chloroprednisone,
chlorprednisone acetate, clocortelone, clescinolone, dichlorisone,
diflurprednate,
flucloronide, flunisolide, fluoromethalone, fluperolone, fluprednisolone,
hydrocortisone
valerate, hydrocortisone cyclopentylpropionate, hydrocortamate, meprednisone,
paramethasone, prednisolone, prednisone, beclomethasone dipropionate,
triamcinolone,
and mixtures thereof may be used. The preferred steroidal anti-inflammatory
for use is
hydrocortisone.
[0055] Nonsteroidal anti-inflammatory agents are also suitable for use herein
as skin
active agents in the compositions of the invention. Non-limiting examples of
non-
steroidal anti-inflammatory agents suitable for use herein include oxicams
(e.g.,
piroxicam, isoxicam, tenoxicam, sudoxicam, CP-14,304); salicylates (e.g.,
aspirin,
disalcid, benorylate, trilisate, safapryn, solprin, diflunisal, fendosal);
acetic acid
derivatives (e.g., diclofenac, fenclofenac, indomethacin, sulindac, tolmetin,
isoxepac,
furofenac, tiopinac, zidometacin, acematacin, fentiazac, zomepirac, clindanac,
oxepinac,
felbinac, ketorolac); fenamates (e.g., mefenamic, meclofenamic, flufenamic,
niflumic,
tolfenamic acids); propionic acid derivatives (e,g., ibuprofen, naproxen,
benoxaprofen,
flurbiprofen, ketoprofen, fenoprofen, fenbufen, indopropfen, pirprofen,
carprofen,
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oxaprozin, pranoprofen, miroprofen, tioxaprofen, suprofen, alminoprofen,
tiaprofenic);
pyrazoles (e.g., phenylbutazone, oxyphenbutazone, feprazone, azapropazone,
trimethazone); and combinations thereof as well as any dermatologically
acceptable salts
or esters of thereof. COX-2 inhibitors are also suitable for use herein, and
include, but
are not limited to, AZD 3582 (ASTRAZENECA and NicOx), Celecoxib (PHARMACIA
Corp.) (4-[5-(4-inethylphenyl)-3-(trifluoromethyl)-1H-pyrazol-l-yl]
benzenesulfonamide), Meloxicam (BOEHRINGER INGELHEIM Pharmaceuticals) (4-
hydroxy-2-inethyl-N-(5-methyl-2-thiazolyl)-2H-1,2GW-4063 81
(GLAXOSMITHKLINE), Etoricoxib (MERCK & Co.), Rofecoxib (MERCK & Co.) (4-
[4-(methylsulfonyl) phenyl]-3-phenyl-2(5H)-furanone), Lumiracoxib (NOVARTIS
Pharma AG), Valdecoxib (PHARMACIA Corp.) (4-(5-methyl-3-phenyl-4-isox-azolyl)
benzenesulfonamide), and Etodolac (WYETH Ayerst Laboratories) ((±) 1,8-
diethyl-
1,3,4,9-tetrahydropyrano-[3,4-b] acid).
[0056] Other non-limiting examples of suitable anti-inflammatory or similar
other skin
active agents include candelilla wax, bisabolol (e.g., alpha bisabolol), aloe
vera, plant
sterols (e.g., phytosterol), Manjistha (extracted from plants in the genus
Rubia,
particularly Rubia Cordifolia), and Guggal (extracted from plants in the genus
Commiphora, particularly Commiphora Mukul), kola extract, cllamomile, red
clover
extract, sea whip extract, anise oil, garlic oil, ginger extract,
vasoconstrictors such as
phenylepluine hydrochloride, and combinations thereof.
[0057] Further non-limiting examples of suitable anti-inflammatory or similar
other skin
active agents include compounds of the Licorice (the plant genus/species
Glycyrrhiza
glabra) family, including glycyrrhetic acid, glycyrrhizic acid, and
derivatives thereof
(e.g., salts and esters). Suitable salts of the foregoing compounds include
metal and
ammonium salts. Suitable esters include C2-C24 saturated or unsaturated esters
of the
acids, preferably Clo-CZ4, more preferably C16-C24. Specific non-limiting
examples of the
foregoing include oil soluble licorice extract, the glycyrrhizic and
glycyrrhetic acids
themselves, monoammonium glycyrrhizinate, monopotassium glycyrrhizinate,
dipotassium glycyrrhizinate, 1-beta-glycyrrhetic acid, stearyl
glycyrrhetinate, and 3-
stearyloxy-glycyrrhetinic acid, disodium 3-succinyloxy-beta-glycyrrhetinate,
and
combinations thereof.
[0058] Anesthetic actives include butamben picrate, lidocaine, xylocaine,
benzocaine,
bupivacaine, chlorprocaine, dibucaine, etidocaine, mepivacaine, tetracaine,
dyclonine,
hexylcaine, procaine, cocaine, ketamine, pramoxine, phenol, and
pharmaceutically
acceptable salts thereof.
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[0059] Analgesic actives include dyclonine hydrochloride, aloe vera, fentanyl,
capsaicin,
and the like.
[0060] Anti-pruritic actives include alclometasone dipropionate, betamethasone
valerate,
and isopropyl myristate MSD.
[0061] Anti-microbial actives include antifungal, antibacterial, and
antiseptic
compounds. Antifungal compounds include, but are not limited to, compounds
such as
iinidazole antifungals. Specific antifungals include butocouazole nitrate,
miconazole,
econazole, ketoconazole, oxiconizole, haloprogin, clotrimazole, and butenafine
HCI,
naftifine, terbinafine, ciclopirox, and tolnaftate. Antibacterial and
antiseptic compounds
include phenol-TEA complex, mupirocin, triclosan, chlorocresol, chlorbutol,
iodine,
clindamycin, CAE (Anjinomoto Co., Inc., containing DL-pyrrolidone Carboxylic
acid
salt of L-Cocoyl Arginine Ethyl Ester), povidone-iodine, polymyxin b sulfate-
bacitracin,
zinc-neoinycin sulfate-hydrocortisone, chloramphenicol, methylbenzethonium
chloride,
and erythromycin and antiseptics (e.g., benzalkonium chloride, benzethonium
chloride,
chlorllexidine gluconate, mafenide acetate, nitrofurazone, nitromersol and the
like may be
included in compositions of the invention. Many deodorant compounds are also
antimicrobial (see below). Antiparasitics, such as lindane may also be
included.
[0062] Further examples of antimicrobial and antifungal actives useful in the
compositions of the present invention include, but are not limited to, 0-
lactam drugs,
quinolone drugs, ciprofloxacin, norfloxacin, tetracycline, amikacin, 2,4,4'-
trichloro-2'-
hydroxy diphenyl ether, 3,4,4'-trichlorocarbanilide, phenoxyethanol, phenoxy
propanol,
phenoxyisopropanol, doxycycline, capreomycin, chlorhexidine,
chlortetracycline,
oxytetracycline, ethambutol, hexamidine isethionate, metronidazole,
pentamidine,
gentamicin, kanamycin, lineomycin, methacycline, methenamine, minocycline,
neomycin, netilmicin, paromomycin, streptomycin, tobramycin, miconazole,
tetracycline
hydrochloride, erythromycin, zinc erythromycin, erythromycin estolate,
erythromycin
stearate, amikacin sulfate, doxycycline hydrochloride, capreomycin sulfate,
chlorhexidine
gluconate, chlorhexidine hydrochloride, chlortetracycline hydrochloride,
oxytetracycline
hydrochloride, clindamycin hydrochloride, ethambutol hydrochloride,
metronidazole
hydrochloride, pentamidine hydrochloride, gentamicin sulfate, kanamycin
sulfate,
lineoinycin hydrochloride, methacycline hydrochloride, methenamine hippurate,
methenamine mandelate, minocycline hydrochloride, neomycin sulfate, netilmicin
sulfate, paromomycin sulfate, streptomycin sulfate, tobramycin sulfate,
miconazole
hydrochloride, amanfadine hydrochloride, amanfadine sulfate, octopirox,
parachlorometa
xylenol, nystatin, tolnaftate, zinc pyrithione and clotrimazole
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[0063] Compositions of the invention may include antiviral agents. Suitable
anti-viral
agents include, but are not limited to, metal salts (e.g., silver nitrate,
copper sulfate, iron
chloride, etc.) and organic acids (e.g., malic acid, salicylic acid, succinic
acid, benzoic
acid, etc.). In particular compositions which contain additional suitable anti-
viral agents
include those described in copending U.S. patent applications Ser. Nos.
09/421,084
(Beerse et al.); 09/421,131 (Biedermaim et al.); 09/420,646 (Morgan et al.);
and
09/421,179 (Page et al.), which were each filed on Oct. 19, 1999
[0064] Anti-allergenics include antihistamines. Antihistamines can be of Hl or
H2
antagonists or otller types of histamine release inhibitors. The Hl
antagonists can be
sedating or non-sedating. Examples ofHl -sedating antihistamines include
diphenhydramine (Benadryl), chlorpheniramine, tripelennamine, promethazine,
clemastine, doxylamine, benadryl etc. Examples of Hl -non-sedating
antihistainines
include astemizole, terfenadine, loratadine etc. Examples of H2 antagonists
include
cimetadine, famotidine, nizatidine, and ranitidine. Examples of histamine-
release-
inhibitors include cromolyn.
[0065] A further active useful in the invention may be a medicinal for
treatinent of
dermatological conditions such as psoriasis, acne, eczema, and other skin
conditions due
to disease, pathology, accident, and the like. Medicinals include burn relief
ointments,
such as o-amino-p-toluenesulfonamide monoacetate; dermatitis relief agents,
such as the
active steroid amcinonide, diflorasone diacetate, and hydrocortisone; diaper
rash relief
agents, such as methylbenzethonium chloride and the like; herpes treatment
drugs, such
as O-[(2-hydroxyethoxy)methyl]guanine; psoriasis, seborrhea and scabicide
agents, such
as shale oil and derivatives thereof, elubiol, ketoconazole, coal tar and
petroleum
distillates, salicylic acid, zinc pyrithione, selenium sulfide,
hydrocortisone, sulfur,
menthol, psoralen, pramoxine hydrochloride anthralin, and methoxsalen;
steroids, such as
2-(acetyloxy)-9-fluoro-1',2',3',4'-tetrahydro-11-hydroxypregna-1,4-dieno[ 1
6,17-
b]napllthalene-3,20-dione and 21-chloro-9-fluoro-1',2',3',4'-tetrahydro-11b-
hydroxypregna-1,4-dieno[16z, 17-b]naphthalene-3,20-dione, and others including
those
that are antiinflammatories. Other medicinals include those useful in the
treatment of
exposure to poison oak, poison ivy, poison sumac, and the like. These include
camphor,
menthol, benzocaine, butamben picrate, dibucaine, dibucaine hydrochloride,
dimethisoquin hydrochloride, dyclonine hydrochloride, lidocaine, metacresol,
lidocaine
hydrochloride, pramoxine hydrochloride, tetracaine, tetracaine hydrochloride,
benzyl
alcohol, camphorated metacresol, juniper tar, phenol, phenolate sodium,
resorcinol,
diphenhydramine hydrochloride, tripelennamine hydrochloride, hydrocortisone, a
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corticosteroid, and nyarocorEisone acetate. Any other medication capable of
topical
adniiilistration also can be incorporated in a composition of the present
invention in an
amount sufficient to perform its intended function.
[0066] Anticellulite actives include isobutylmethylxaiithine, caffeine,
theophylline,
theobromine, aminophylline,yollimbine, and mixtures thereof.
[0067] Examples of actives suitable for treating hair loss include, but are
not limited to
potassium channel openers or peripheral vasodilators such as minoxidil,
diazoxide, and
compounds such as N*-cyano-N-(tert-pentyl)-N-3-pyridinyl-guanidine ("P-1075")
as
disclosed in U.S. Pat. No.: 5,244,664, which is incorporated herein by
reference;
vitamins, such as vitamin E and vitamin C, and derivatives thereof such as
vitamin E
acetate and vitamin C palmitate; honnones, such as erythropoietin,
prostaglandins, such
as prostaglandin El and prostaglandin F2-alpha; fatty acids, such as oleic
acid; diruretics
such as spironolactone; heat shock proteins ("HSP"), such as HSP 27 and HSP
72;
calcium channel blockers, such as verapamil HCL, nifedipine, and
diltiazemamiloride;
immunosuppressant drugs, such as cyclosporin and Fk-506; 5 alpha-reductase
inhibitors
such as finasteride; growth factors such as, EGF, IGF and FGF; transforming
growth
factor beta; tumor necrosis factor; non-steroidal anti-inflammatory agents
such as
benoxaprofen; retinoids such as tretinoin; cytokines, sucll as IL-6, IL-1
alpha, and IL-1
beta; cell adhesion molecules such as ICAM; glucorcorticoids such as
betametasone;
botanical extracts such as aloe, clove, ginseng, rehmannia, swertia, sweet
orange,
zanthoxylum, Serenoa repens (saw palmetto), Hypoxis rooperi, stinging nettle,
pumpkin
seeds, and rye pollen; other botanical extracts including sandlewood, red beet
root,
chrysantheinum, rosemary, burdock root and other hair growth promoter
activators which
are disclosed in DE 4330597 which is incorporated by reference in its entirety
herein;
homeopathic agents such as Kalium Phosphoricum D2, Azadirachta indica D2, and
Joborandi DI; genes for cytokines, growth factors, and male-pattered baldness;
antifungals such as ketoconazole and elubiol; antibiotics such as
streptomycin; proteins
inhibitors such as cycloheximide; acetazolainide; benoxaprofen; cortisone;
diltiazem;
hexachlorobenzene; hydantoin; nifedipine; penicillamine; phenothaiazines;
pinacidil;
psoralens, verapamil; zidovudine; alpha-glucosylated rutin having at least one
of the
following rutins: quercetin, isoquercitrin, hespeddin, naringin, and
methyihesperidin, and
flavonoids and transglycosidated derivatives thereof which are all disclosed
in JP
7002677, which is incorporated by reference in its entirety herein; and
mixtures thereof.
Preferred hair loss treatment agents include minoxidil, 6-(I-piperdinyl)-2,4-
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pyrimidinediamine-3-oxide, N'-cyano-N-(tert-pentyl)-N'-3-pyridinyl-guanidine,
finasteride, retinoids and derivatives thereof, ketoconazole, elubiol or
mixtures thereof.
[0068] Examples of actives suitable for use in inhibiting hair growth include:
serine
proteases such as trypsin; vitamins such as alpha-tocophenol (vitamin E) and
derivatives
thereof such as tocophenol acetate and tocophenol palmitate; antineoplastic
agents, such
as doxorubicin, cyclophosphamide, chlor.methine, methotrexate, fluorouracil,
vincristine,
daunorubicin, bleomycin and hydroxycarbamide; anticoagulants, such as heparin,
heparinoids, coumaerins, detran and indandiones; antithyroid drugs, such as
iodine,
thiouracils and carbimazole; lithium and lithium carbonate; interferons, such
as interferon
alpha, interferon alpha-2a and interferon alpha-2b; retinoids, such as retinol
(vitamin A),
isotretinoin: glucocorticoids such as betainethasone, and dexamethosone;
antihyperlipidaemic drugs, such as triparanol and clofibrate; thallium;
mercury;
albendazole; allopurinol; amiodarone; amphetamines; androgens; broinocriptine;
butyrophenones; carbamazepine; cholestyramine; cimetidine; clofibrate;
danazol;
desipramine; dixyrazine; ethambutol; etionamide; fluoxetine; gentamicin, gold
salts;
hydantoins; ibuprofen; impramine; immunoglobulins; indandiones; indomethacin;
intraconazole; levadopa; maprotiline; methysergide; metoprolol; metyrapone;
nadolol;
nicotinic acid; potassium thiocyanate; propranolol; pyridostimine;
salicylates;
sulfasalazine; terfenadine; thiamphenicol; thiouracils; trimethadione;
troparanol; valproic
acid; and mixtures thereof. Preferred hair growth inhibitory agents include
serine
proteases, retinol, isotretinoin, betamethoisone, alpha-tocophenol and
derivatives thereof,
or mixtures thereof.
[0069] Examples of hair bleaching agents include perborate or persulfate
salts.
[0070] Deodorant compounds include astringent salts and bioactive compounds.
The
astringent salts include organic and inorganic salts of aluminum, zirconium,
zinc, and
mixtures thereof. The anion of the astringent salt can be, for example,
sulfate, chloride,
chlorohydroxide, alum, formate, lactate, benzyl sulfonate or phenyl sulfonate.
Exemplary
classes of antiperspirant astringent salts include aluminum halides, aluminum
hydroxyhalides, zirconyl oxyhalides, zirconyl hydroxyhalides, and mixtures
thereof.
Exemplary aluminum salts include aluminum chloride and the aluminum
hydroxyhalides
having the general formula Ala (OH) XQyXH2O, wherein Q is chlorine, bromine or
iodine;
x is about 2 to about 5; x+y is about 6, wherein x and y are not necessarily
integers; and
X is about 1 to about 6. Exemplary zirconium compounds include zirconium oxy
salts
and zirconium hydroxy salts, also referred to as zirconyl salts and zirconyl
hydroxy salts,
and represented by the general empirical formula ZrO(OH)2-nz LZ, wherein z
varies from
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about 0.9 to about z anct is not necessarily an integer; n is the valence of
L; 2-nz is greater
than or equal to 0; and L is selected from the group consisting of halides,
nitrate,
sulfamate, sulfate, and mixtures thereof.
[0071] Exemplary deodorant compounds therefore include, but are not limited
to,
aluminum bromohydrate, potassium alum, sodium aluminum chlorohydroxy lactate,
aluminuni sulfate, aluminum chlorohydrate, aluminum-zirconium
tetrachlorohydrate, an
aluminum-zirconium polychloroliydrate complexed with glycine, aluminum-
zirconium
trichlorohydrate, aluminum-zirconium octachlorohydrate, aluininum
sesquichlorohydrate,
aluminum sesquichlorohydrex PG, aluminum chlorohydrex PEG, aluminum zirconium
octachlorohydrex glycine complex, aluminum zirconium pentachlorohydrex glycine
complex, aluminuni zirconium tetrachlorohydrex glycine complex, aluminum
zirconiuin
trichlorohydrex glycine complex, aluminum chlorohydrex PG, zirconium
chlorohydrate,
aluminum dichlorohydrate, aluminum dichlorohydrex PEG, aluminum dichlorohydrex
PG, aluminum sesquichlorohydrex PG, aluminum chloride, aluminum zirconium
pentachlorohydrate, numerous other useful antiperspirant compounds listed in
the CTFA
Handbook at p. 56, incorporated herein by reference, and mixtures thereof.
[0072] In addition to the astringent salts, the deodorant compound can be a
bacteriostatic
quaternary ammonium compound, such as, for example, cetyl trimethyl ammonium
bromide, cetyl pyridinium chloride, benzethonium chloride,
diisobutylbenzoxyethoxyethyldimethylbenzyl ammonium chloride, sodium N-lauryl
sarcosine, sodium N-polymethyl sarcosine, lauroyl sarcosine, N-myristolyl
glycine,
potassium N-lauroyl sarcosine, and stearyl trimethyl ammonium chloride; or a
bioactive
compound; or a carbonate or bicarbonate salt, such as, for example, the alkali
metal
carbonates and bicarbonates, and the ammonium and tetralkylammonium carbonates
and
bicarbonates. Other useful deodorant compounds include chlorophyllin copper
complex,
aluminum chloride, aluminum chloride hexahydrate, and methylbenzethonium
chloride.
[0073] Antioxidants are also useful in formulations of the invention. Typical
suitable
antioxidants include propyl, octyl and dodecyl esters of gallic acid,
butylated
hydroxyanisole (BHA, usually purchased as a mixture of ortho and meta
isomers),
butylated hydroxytoluene (BHT), nordihydroguaiaretic acid, Vitamin A, ascorbic
acid
and its salts, ascorbyl esters of fatty acids, ascorbic acid derivatives
(e.g., magnesium
ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl sorbate), tocopherol,
tocopherol acetate, other esters of tocopherol, tocotrienols and their esters,
and 6-
hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (commercially available
under
the tradename TROLOX). Other suitable antioxidants include uric acid and its
salts and
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allcyl esters, sorbic acid and its salts, lipoic acid, amines (e.g., N,N-
diethylhydroxylamine,
amino-guanidine), sulth.ydryl compounds (e.g., glutathione, N-acetyl
cysteine),
dihydroxy fumaric acid and its salts, lycine pidolate, arginine pilolate,
nordihydroguaiaretic acid, bioflavonoids, curcumin, lysine, metllionine,
proline,
superoxide dismutase, silymarin, tea extracts, grape skin/seed extracts,
melanin, and
rosemary extracts may be used.
[0074] Preferred antioxidants are photostable antioxidants. An exemplary
photostable
antioxidant is marketed under the tradename EMBLICA by EMD Chemicals. See,
e.g.,
U.S. Patent No. 6,831,191. Antioxidants, preferably photostable antioxidants
(e.g.,
EMBLICA), maybe included in sunscreen additives at about 0.05 to about 5%, or
about
0.05 to about 2%, or about 0.1%, 0.2%, 0.3%, or 0.4%, or in
sunscreen/bodywashes at
about 0.02 to about 2%, or about 0.02 to about 1%, or about 0.04%, 0.06%,
0.08%, 0.1%,
0.2%, or 0.3%.
[0075] Insect repellants include the most widely used active agent for
personal care
products, N,N-Diethyl-m-toluamide, frequently called "DEET" and available in
the form
of a concentrate containing at least about 95 percent DEET. Other synthetic
chemical
repellents include dimethyl phthalate, ethyl hexanediol, indalone, di-n-
propylisocinchoronat- e, bicycloheptene, dicarboximide and
tetrahydrofuraldehyde.
Certain plant-derived materials also have insect repellent activity, including
citronella oil
and other sources of citronella (including lemon grass oil), limonene,
rosemary oil and
eucalyptus oil. Choice of an insect repellent for incorporation into
compositions of the
invention will frequently be influenced by the odor of the repellent. The
amount of
repellent agent used will depend upon the choice of agent; DEET is useful at
high
concentrations, such as up to about 15 percent or more, while some of the
plant-derived
substances are typically used in much lower amounts, such as 0.1 percent or
less
[0076] The compositions of the present invention may contain a wide range of
additional
active coinponents. The CTFA Cosmetic Ingredient Handbook, Seventh Edition,
1997
and the Eighth Edition, 2000, which are incorporated by reference herein in
its entirety,
describes a wide variety of active ingredients commonly used in skin care
compositions,
which are suitable for use in the compositions of the present invention. Other
topically-
active compounds are listed in Remington's Pharmaceutical Sciences, 20th Ed.,
Lippincott Williams & Witkins, Baltimore, MD (2000) (hereinafter Remington's),
U.S.
Pharmacopeia and National Formulary, The United States Pharmacopeial
Convention,
Inc., Rockville, Md. and Physician's Desk Reference, Medical Economics Co.,
Inc.,
Oradell, N.J.incorporated herein by reference.
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[00771 The non-sunscreen active may be provided as is or in encapsulated form.
Encapsulation is described for sunscreen additives, above. Besides the
encapsulated
active, in some embodiments an additive or composition for topical application
containing the active furtlier includes a cationic polymer, as described
herein, as well as,
optionally, a film former, a preservative, and/or an antioxidant that is
stable upon
exposure to sunlight. Other components may be as described herein. In some
embodiments the additive or composition for topical application may comprise
two,
tluee, four, five, six, seven, eight, nine, ten, or more than ten actives,
each of which may
be encapsulated or non-encapsulated, in any combination.
[0078] In preferred embodiments, the active is encapsulated sol-gel
microcapsules, such
as silica sol-gel microcapsules. Such microcapsules are described in U.S.
Patent Nos.
6,238,650; 6,436,375, 6,303,149; and 6,468,509. Thus, in some embodiments the
invention provides an additive for addition to a coinposition for topical
application,
wlzere the additive comprises an encapsulated non-sunscreen active, and
optionally
further comprises a cationic polymer. In other embodiments the invention
provides a
composition for topical application that contains an additive, where the
additive
comprises an encapsulated non-sunscreen active, and optionally further
comprises a
cationic polymer. Further ingredients include film fonners, antioxidants,
preservatives,
and other ingredients as listed herein. The composition for topical
application may be,
e.g., a bodywash.
[0079] In some embodiments the invention provides microcapsules, e.g., sol-gel
microcapsules (e.g., as described in U.S. Patents No. 6,238,650; 6,436,375,
6,303,149;
and 6,468,509) that act as a protective barrier on the skin when used either
alone, or as an
additive in a bodywash. In these embodiments, the sol-gel microcapsules may be
used
without any additional active ingredients (i.e., empty) , providing a physical
barrier, or
they may be used with additional encapsulated active ingredients that enhance
their
barrier function. For example, the microcapsules may contain substances that
act to
screen toxic agents (e.g., biological or chemical warfare agents) or radiation
(e.g., alpha,
beta, or gamma radiation) partially or completely from penetrating the user's
skin. In
some embodiments, the microcapsules may contain one or more agents that absorb
radiation, such as graphite, lead, tungsten, and others known in the art, or
agents that
reflect radiation such as ceramic beads. As the microcapsules may be designed
so as to
experience minimal or no breakage when applied to the skin, as well as to
experience
minimal penetration of the skin, it is possible to use even toxic substances
(e.g., lead) that
provide a screening effect, since these substances will not be released or
will be released
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in only minimal amounts. 'l ne microcapsules are eventually removed from the
skin
through repeated washing and/or normal sloughing of the external skin cell
layers.
Especially for agents used for one-time or very few exposures, such as can
occur for
personnel engaged in combating or containing terrorist attacks or in warfare,
the
invention provides a means to deliver a last line of defense on the skin of
personnel
where the active used in the microcapsules may be one that is not appropriate
for long-
term use, but that is appropriate for a limited number of applications in
order to protect
the wearer from a greater rislc (e.g., microcapsules encapsulating lead to
protect against a
radiation attack).
[0080] The microcapsules, e.g., sol-gel microcapsules, can be prepared so as
to
experience no or minimal breakage when applied to the skin, either as is or in
the form of
a bodywash. Alternatively, the microcapsules, e.g., sol-gel microcapsules, can
be
prepared so as to experience various degrees of breakage, on average, when
applied as is
or in a bodywash. Thus, the microcapsules, e.g., sol-gel microcapsules, may be
prepared
so as to experience about 0% breakage, or breakage in a range from about 0.1,
0.5, 1, 2,
5, 10, 20, 30, 40, 50, 60, 70, 80, or 90% to about 0.5, 1, 2, 5, 10, 20, 30,
40, 50, 60, 70,
80, or 90%, after application (or application and rinsing in the case of a
bodywash
containing the microcapsules). Furthermore, the microcapsules may be
formulated so as
to break open in response to conditions that occur on the skin, so that after
application the
microcapsules act to release their contents in a time-release or controlled
manner. Non-
limiting exemplary skin or hair conditions that can vary with the user's
environment, the
variation of which can trigger breakage of microcapsules, include pH,
temperature,
friction, exposure to light or air, pressure, and the like.
C. Cationic component
[0081] In some embodiments the additives, e.g., sunscreen additives and
sunscreen/bodywashes of the invention further include a cationic component.
Without
being bound by theory, it is thought that this component serves as a protein
binder, to
provide a positive charge to promote attachment of the composition to proteins
of the
skin and hair, thus increasing retention of the components, e.g., sunscreen,
after rinse and
during normal activities. This positive charge creates a strong affinity for
the protein in
the hair or skin. Any means of iinparting a positive charge may be used.
[0082] Preferred means are by including one or more cationic polymers in the
composition. Various cationic polymers may be used. Examples of cationic
polymers
are described in U.S. Pat. Nos. 6,224,852; 3,816,616; 4,272,515; 4,298,494;
4,080,310;
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4,049;301; 4,00'9,256; and 3,186,911. Cationic polymers are available
commercially,
e.g., from Union Carbide Corp. under the trademark POLYMER JR., from Celanese-
Stein Hall under the trademark JAGUAR, from GAF Corporation under the
tradename
Gafquatm and from Merck & Co., Inc under the trademark MERQUAT by.
Representative one are Merquat 100, a highly charged cationic
dimethyldiallylammonium chloride homopolymer, and MerquatTM 550, a highly
charged
cationic copolymer prepared with dimethyidiallylammonium chloride and
acrylamide.
These materials are designated in the CTFA dictionary as Quaternium40 and
Quaternium-41, respectively.
[0083] Especially preferred are polyquaterniums. Quaternized material in
powder form,
not limited to the polyquaterniums, may also be used. Exemplary
polyquaterniums of use
in the invention include polyquatemium-4, -7, -11, -22, -37, -44, -51, and -
64.
Polyquatemium compounds are available coinmercially, e.g., CELQUAT L-200 for
polyquaternium-4. Further exemplary polyquatemiums can be quaternized
copolynZers
of vinylpyrrolidone, methacrylamide, vinylimidiazole, and quaternized
vinylimidiazole
and or with vinyl caprolactum. They all range with different charge densities.
We are
mainly concerned with those of gretaer cationic charges. Some of the new
polyquaterniums we havent listed are the 68, 46,16Without being limited by
theory, it is
thought that with the trapping of the encapsulate (e.g., sunscreen active
inside the
capsule) by this cationic component. rinse off is difficult and renders the
active
substantive to the protein in the skin and hair.
[0084] Useful in some embodiments of the invention is a dry cationic
component, such
as sold under the tradename CAE (Anjinomoto Co., Inc.), containing DL-
pyrrolidone
Carboxylic acid salt of L-Cocoyl Arginine Ethyl Ester, whicli is a cationic
agent useful
for binding to proteins and providing an antimicrobial effect.
[0085] In some embodiments of additives, e.g., sunscreen additives, the
cationic
component (e.g., cationic polymer) comprises about 0.1 to about 20%, or about
0.1 to
about 10%, or about 0.5 to about 10%, or about 1 to about 10%, or about 0.5 to
about 5%,
or about 0.5 to about 3%or about 1 to about 5%, or about 1 to about 3%, or
about 1% of
the total composition. In some embodiments, the cationic component is
polyquaternium-
4; in some embodiments the polyquaternium-4 is present at about 1%.
[0086] In some embodiments of active/bodywashes, e.g., sunscreen/bodywashes,
the
cationic component (e.g., cationic polymer) comprises about 0.03 to about 7%,
or about
0.03 to about 4%, or about 0.2 to about 4%, or about 0.3 to about 4%, or about
0.2 to
about 2%, or about 0.3 to about 4%, or about 0.3 to about 1%,, or about 0.3 or
0.4% of
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the total composition. in some embodiments, the cationic component is
polyquatemium-
4; in some embodiments the polyquaternium-4 is present at about 0.33%.
D. Film formers
[0087] In some embodiments, compositions of the invention further include a
component
that provide a film barrier system, typically a hydrophobic layer that serves
to maintain
the residual sunscreen after rinse. Film barrier systems are well-known in the
art and
include, without limitation, petrolatum, silicon derivatives, and combinations
thereof.
Also useful are polymers with carboxylic ends which render themselves
insoluble until
neutralized. After being neutralized they can act as film formers. Film
formers also
include emollient esters, lanolin derivatives (e.g., acetylated lanolins), and
superfatted
oils. Fihn formers are available commercially, e.g., a preferred film former
is
MOISTUREGUARDTM, which contains petrolatum, dimethicone, stearamidopropyl
dimethylamine stearate, and tocopheryl acetate, available from Engelhard.
[0088] It may also be desirable to add acrylic co-polymers to the formulations
of the
invention as film formers. An exemplary liquid acrylic copolymer fonnulation
is
DERMACRYL, marketed by National Starch and Chemical. Acrylic co-polymers may
be included in sunscreen additives at about 0.1 to about 5%, or about 0.2 to
about 3%, or
about 0.2%, 0.3%, 0.4%, or 0.5%, or in sunscreen/bodywashes at about 0.05 to
about 2%,
or about 0.1 to about 1%, or about 0.05%, 0.1%, 0.2%, 0.3 Jo, 0.4%, or 0.5%.
[0089] A secondary film former may also beused, e.g., keratin or other protein
derivative
in an amino acid complex such as cysteine.
[0090] The film former may be present in the sunscreen additive in the range
of about
0.1 to about 25%, or about 1 to about 10%; or about 2 to about 6%; or about 3,
4, or 5%.
In some embodiments, the film former MoistureGuard is used at a concentration
of about
4.2%. Equivalent film formers, at equivalent concentrations, may also be used.
[0091] As noted, some preparations may perform more than one function, for
example,
inorganic blockers such as Tioveil and Spectraveil (both of the Tioxide
Group), in certain
variations, may be film-formers and may have advantageous uses here.
[0092] In addition, many emollients may also perform a film former function in
that they
provide a barrier on the skin. Thus, compositions of the invention may include
water-
insoluble emollients that include fatty acids such as oleic and stearic; fatty
alcohols such
as cetyl, and hexadecyl (ENJAY); esters such as diisopropyl adipate, benzoic
acid esters
of C9 -C15 alcohols, and isononyl iso-nonanoate; alkanes such as mineral oil;
silicones;
such as dimethyl polysiloxane and ethers such as polyoxypropylene butyl ethers
and
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polyoxypropylene cetyl ethers. If a water-insoluble emollient is used it may
be in an
amount from about 2% to about 15% by weight, and most preferably from about 4%
to
about 10%.
[0093] Other useful film formers include polythylenes, such as those available
from New
Phase Technologies as PERFORMALENE 400, a polyethylene having a molecular
weight of 400. Another suitable water-proofing agent is polyethylene 2000
(molecular
weight of 2000), which is available from New Phase Technologies as
PERFORMALENE
2000.
[0094] Yet another suitable film former/waterproofing agent is synthetic wax,
also
available from New Phase Tecluiologies as PERFORMA V-825. Still yet another
suitable film former/waterproofing agent is octadecene/MA copolymer
[0095] Additional film fom-iers which also may be used within the framework of
the
invention include any film former chemistry known in the art. Thus, suitable
additional
film formers include acacia gum, cellulose derivatives, guar derivatives and
all those set
forth on pages 68-69 of the C.T.F.A. Cosmetic Ingredient Handbook, First
Edition, 1988,
which is hereby incorporated by reference. Such film formers include
acrylamides
copolymer, acrylamide/sodiuin aciylate copolymer, acrylate/acrylamide
copolymer,
acrylate/ammonium methacrylate copolymer, acrylates copolymer,
acrylates/diacetoneacrylamide copolymer, acrylic/acrylate copolyiner, adipic
acid/dimethylaminohydroxypropyl diethlenetnamine copolymer, adipic
acid/epoxypropyl/diethlenetriamine copolymer, albuinen, allyl stearate/VA
copolymer,
aminoethylacrylate phosphate/acrylate copolymer, ammonium acrylates copolymer,
ammonium alginate, ammoniuin vinyl acetate/acrylates copolymer, AMP
acrylates/diacetoneacrylamide copolymer, balsam canada, balsam oregon, balsam
peru,
balsam tolu, benzoi acid/pllthalic anhydride/pentaerythritol/neopentyl
glycol/palmitic
acid copolymer, benzoin extract, butadiene/acrylonitrile copolymer, butylated
urea-
formaldehyde resin, butyl benzoic acid/phthalic anhydride trimethylolethane
copolymer,
butyl ester of ethylene maleic anhydride copolymer, butyl ester of PVM/MA
copolymer,
calcium carrageenean, calcium/sodium PVM/MA copolymer, carboxymethyl
hydroxyethyl cellulose, cellulose gum, collodion, copal, corn
starch/aciylainide/sodium
acrylate copolymer, damar, diethylene glycolamine/epichiorohydrin/piperazine
copolymer, DMJ-IF, dodecanedoic acid/cetearyl alcoholglycol copolymer,
ethylcellulose,
ethylene/acrylate copolymer, ethylene/maleic anhydride copolymer,
ethylene/vinyl
acetate copolymer, ethyl ester of PVM/fvlA. copolymer, flexible collodian, gum
benzoin,
gutta percha, hydroxybutyl methylceflulose, hydroxyethylcellulose,
hydroxyethyl ethyl
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cellulose, hydroxypropylceilulose, hydroxypropyl guar, hydroxypropyl
methylcellulose,
isopropyl ester of PVM/MA copolymer, maltodextrin, melamine/formaldehyde
resin,
methacryloyl ethyl betainelmethacrylates copolyrner, nitrocellulose,
octylacrylamide/acrylateslbutylaminoethylmethaciylate copolymer,
octylacrylamide/acrylates copolymer, phthalic anhydride/glycerin/gycidyl
decanoate
copolymer, phthalic/trimellitic/glycols copolymer, polyacrylamide,
polyaciylarnidomethylpropane sulfone acid, polyacrylic acid, polybutylene
terephthalate,
polychlorotrifluoroethylene, polyethylacrylate, polyethylene, polyethylene
terephthalate,
polyisobutene, Polyquaternium-1, Polyquaternium-2, Polyquaternium-4,
Polyquaternium-5, Polyquatemium-6, Polyquaternium-7, Polyquaternium-8,
Polyquaternium-9, Polyquaternium-10, Polyquaternium-11, Polyquaternium-12,
Polyquaternium-13, Polyquaternium-14, Polyquaternium-15, polystyrene,
polyvinyl
acetate, polyvinyl alcohol, polyvinyl butyral, polyvinyl imidazolinium
acetate, polyvinyl
laurate, polyvinyl methyl ether, potassium carrageenan, PVM/MA copolymer, PVP,
PVP/dimethylaminoethymethacrylate copolymer, PVP/eicosene copolymer, PVP/ethyl
methacrylatehnethacrylic acid copolyerm, PVP/hexadecene copolymer, PVP/VA
copolymer, PVP/vinyl acetate/itaconic acid copolyrner, rosin, serum albumin,
shellac,
sodiunl acrylate/vinyl alcohol, copolymer, sodium carrageen, sodium
polymethacrylate,
sodium polystyrene sulfonate, starch/acrylates/acrylamide copolymer, starch
diethylaminoethyl ether, steaxyvinyl ether/maleic anhydride copolymer,
styrene/acrylate/acrylonitrile copolymer, styrene/acrylate/ammonium
metllacrylate
copolymer, styrene/maleic anhydride copolymer, styrene/PVP copolymer, sucrose
benzoate/sucrose acetate isobutyrate/butyl benzyl phthalate copolymer, sucrose
benzoate/sucrose acetate isobutyrate/butyl benzyl phthalate/methyl
methaciylate
copolymer, sucrose benzoate/sucrose acetate isobutyrate copolymer,
toluenesulfonamide/formaldehyde resin, tragacath gum, vinyl acetate/crotonates
copolymer, vinyl acetate/crotonic acid copolymer, vinyl acetate/crotonic
acid/methacryloxybenzophenon-1 copolymer, vinyl acetate/crotonic aid/vinyl
neodecanoate copolymer, and zein
[0096] Additional film formers include those set forth in U.S. Pat. Nos.
6,838,419;
6,838,088; 6,780,422,; 6,531,118; and 5,916,541, all of which are incorporated
herein by
reference
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E. Other components
[0097] A wide variety of additional components may be added to the
compositions of the
present invention, as long as the components are selected so as to avoid any
undesirable
reaction with the primary components (e.g., one or more of the sunscreen
agents) of the
composition. The CTFA Cosmetic Ingredient Handbook, Seventh Edition, 1997 and
the
Eighth Edition, 2000 (incorporated by reference herein), provide a broad
source of
possible cosmetic and pharmaceutical ingredients typically used in skin care
compositions. Examples of such additional components include one or more of
the
following: Absorbents, abrasives, anticaking agents, antifoaming agents,
binders,
biological additives, buffering agents, bulking agents, chelating
agents/sequestrants (e.g.,
disodium EDTA), chemical additives, colorants, cosmetic astringents, cosmetic
biocides,
denaturants, drug astringents, emollients (including glycerin alovera, and
Vitainins A, C,
and D [hydrating agents and skin protectants]), foam boosters, fragrance
components,
gums, humectants/moisturizers (including urea, guanidine, glycolic acid,
polyhydroxy
alcohols such as sorbitol, glycerin, hexanetriol, propylene glycol, hexylene
glycol and the
like, polyethylene glycol, sugars and starches, sugar and starch derivatives,
D-pantllenol,
hyaluronic acid, lactamide monoethanolamine, acetamide monoethanolamine, and
mixtures tliereof), hydrotropes, neutralizing agents, opacifying agents and
pigments, pH
adjusters, plasticizers, preservatives, propellants, reducing agents, skin
bleaching agents,
skin protectants, solubilizing agents, and suspending agents (e.g., Carbomer
1382).
[0098] In some embodiments, the additives and bodywashes of the invention,
e.g.,
sunscreen additives or sunscreen/bodywashes include a preservative. Exemplary
preservatives useful in the invention include citric acid, tartaric acid,
phosphoric acid,
iminodiacetic acid, nitrilotriacetic acid, hydroxyethyleneaminodiacetic acid
and
ethylenediaminetetraacetic acid and salts thereof; para-hydroxybenzoates such
as butyl
paraben, methyl paraben and propyl paraben; imidazolines (e.g.,
imidiazolinylurea),
triclosan, hydantoins (e.g., dimethyloldimethylhydantoin), isothiazolidinone
compounds
and mixtures thereof. Commercially available preservatives include KATHON CG
and
KATHON CGII, which contain methylchloroisothiazolinone and
methylisothiazolinone
(Rohin and Haas). When present, the quantity of preservative is in the range
from 0.001
to 2%, preferably from 0.01 to 0.2%.
[0099] In certain embodiments the compositions of the invention include a
chelating
agent. Chelating agents are substances used to chelate or bind metallic ions,
such as with
a heterocyclic ring structure so that the ion is held by chemical bonds from
each of the
participating rings. Suitable chelating agents include ethylene
diaminetetraacetic acid
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WO 2006/083843 PCT/US2006/003365
(EDTA), EDTA disodium, calcium disodium edetate, EDTA trisodium, EDTA
tetrasodium and EDTA dipotassiuin. One or more chelating agents can optionally
be
included in the additives or additive/bodywashes in amounts ranging from about
0.001 to
about 0.2 weight percent, or about 0.01% weight percent.
[00100] Thickening agents or gellants may be added as desired to adjust the
texture and
viscosity of the composition. Exemplary agents or gellants may be selected
from
CarbopolTM resins [e.g., 934, 971, 974, 980, 981] and PemulenTM [TR-1 and TR-
2] [both
Carbopol TMand PemulenTM are registered trademarks of BF Goodrich], Noveon AA-
1,
ETD resins, and UltrezTM resins [registered trademarlc, BF Goodrich]. In
addition,
carbomers might be useful for this purpose.
[00101] It may be desired to include a non-polar wax. Examples of such useful
waxes
include ester waxes, diester waxes, hydrocarbon waxes, silicone waxes and
triglyceride
waxes and mixtures thereof.
[00102] Other components may include a liquid hydrocarbon (similar to
pentane), and/or a
cationic foaming agent derived from arginine and or cysteine.
[00103] Further optional ingredients which can be present in the composition
include
fragrance, dyes, antimicrobial materials such as triclocarban, triclosan,
iodophors, iodine
formulations, phenolic compounds, e.g. hexachlorophene, and bisbiguanides,
e.g.
chlorhexidene gluconate, and the like. See, e.g., U.S. Patent Nos. 6,827,795;
6,517,854;
6,010,817; 5,173,216; 5,719,113; 5,259,984; 5,562,912; 5,629,006; 5,728,662;
5,767,163;
5,750,579; 5,591,442; 5,650,143; 5,772,640; and 4,478,821.
[00104] The components of the composition are generally mixed in water.
F. Surfactants and bodywashes
[00105] Compositions of the invention may be formulated as products for
washing the
skin, for example, bath or shower gels, hand washing compositions or facial
washing
liquids; pre- and post-shaving products; rinse-off, wipe-off and leave-on skin
care
products; products for washing the hair and for dental use. Shower gels are
particularly
preferred product forms.
[00106] If it is desired to prepare a sunscreen/bodywash coniposition, the
sunscreen
additives of the invention may be combined with other ingredients to produce a
bodywash (e.g., a liquid or solid formulation). The sunscreen/bodywash may
include one
or more surfactants. The use of surfactants in bodywashes is well-known in the
art. Any
surfactant known in the art and appropriate for a bodywash composition may be
used.
See, McCutcheon's Detergefzts & Eynulsifiers, M.C. Publishing Co. (North
American
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WO 2006/083843 PCT/US2006/003365
edition 1999); Schwartz, et al., Suiface Active Agents, Tlaeif= Chefnistry and
Technology,
New York, Interscience Publishers, 1949, and U.S. Patent Nos. 6,096,697;
4,741,855;
4,788,066; 5,104,646; 5,106,609; 2,658,072; 2,438,091; 2,528,378; 2,486,921;
2,486,922; 2,396,278; 2,979,465; 3,179,599; 5,322,643; 5,084,212; 3,332,880;
4,122,029;
4,265,878; 4,421,769; 3,929,678; 3,959,461; 4,387,090; 4,303,543; and
6,224,852; and
in British Patent Nos. 848,224 and 791,415. Also see CTFA Cosmetic Ingredient
Dictionary, 4th Edition 1991, pages 509-514 for various long chain alkyl
cationic
surfactants; and Richmond, James M., Cationic Surfactants, Marcel Dekker,
Inc., New
York and Basel, 1990.
[00107] The surfactant(s) may be cationic, anionic, nonionic, zwitterionic,
amphoteric, or
any combination thereof.
[00108] Specific examples of anionic surfactants include those selected from
the group
consisting of alkyl and allcyl ether sulfates, sulfated monoglycerides,
sulfonated olefins,
alkyl aryl sulfonates, primary or secondary alkane sulfonates, alkyl
sulfosuccinates, acyl
taurates, acyl isethionates, alkyl glycerylether sulfonate, sulfonated methyl
esters,
sulfonated fatty acids, alkyl phosphates, ethoxylated alkyl phosphates, acyl
glutamates,
acyl sarcosinates, alkyl sulfoacetates, acylated peptides, alkyl ether
carboxylates, acyl
lactylates, anionic fluorosurfactants, and combinations thereof. Combinations
of anionic
surfactants can be used effectively in the present invention. Specific
examples of alkyl
sulfates that may be used are sodium, ammonium, potassium, magnesium, or TEA
salts
of lauryl or myristyl sulfate. Examples of alkyl ether sulfates that may be
used include
ammonium, sodium, magnesium, or TEA laureth-3 sulfate.
[00109] Another suitable class of anionic surfactants are the sulfated
monoglycerides of
the form R1CO--O--CHa-C(OH)H--CHZ-O-SO3M, wherein Rl is a saturated or
unsaturated, branched or unbranched alkyl group from about 8 to about 24
carbon atoms,
and M is a water-soluble cation such as ammoniuin, sodium, potassium,
magnesium,
triethanolamine, diethanolamine and monoethanolamine. An example of a sulfated
monoglyceride is sodium cocomonoglyceride sulfate.
[00110] Other suitable anionic surfactants include olefin sulfonates of the
form R1S03M,
wherein Rl is a mono-olefin having from about 12 to about 24 carbon atoms, and
M is a
water-soluble cation such as ammonium, sodium, potassium, magnesium,
trietlianolamine, diethanolamine and monoethanolamine. An example of a
sulfonated
olefin is sodiuin C 14/C 16 alpha olefin sulfonate.
[00111] Other suitable anionic surfactants are the linear allcylbenzene
sulfonates of the
fonn Rl-C6H4-S03M, wherein R1 is a saturated or unsaturated, branched or
unbranched
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alkyl group from about 8 to about 24 carbon atoms, and M is a water-soluble
cation such
as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and
monoethanolamine. An example of this anionic surfactant is sodium
dodecylbenzene
sulfonate.
[00112] Still other anionic surfactants suitable for the compositions of the
present
invention include the primary or secondary alkane sulfonates of the form Rl
SO3M,
wherein Rl is a saturated or unsaturated, branched or unbranched alkyl chain
from about
8 to about 24 carbon atoms, and M is a water-soluble cation such as ammonium,
sodium,
potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine. An
example of an alkane sulfonate useful herein is alkali metal or ammonium C13-
C17
paraffin sulfonates.
[00113] Still other suitable anionic surfactants are the alkyl
sulfosuccinates, which
include disodium N-octadecylsulfosuccinamate; dianunonium lauryl
sulfosuccinate;
tetrasodium N-(1,2-dicarboxyethyl)-N-octadecylsulfosuccinate; diamyl ester of
sodium
sulfosuccinic acid; dihexyl ester of sodium sulfosuccinic acid; and dioctyl
esters of
sodium sulfosuccinic acid.
[00114] Also useful are taurates that are based on taurine. Exainples of
taurates include
N-alkyltaurines such as the one prepared by reacting dodecylamine with sodium
isethionate as detailed in U.S. Pat. No. 2,658,072.
[00115] Another class of suitable anionic surfactants is the acyl
isethionates. Nonlimiting
examples of these acyl isethionates include ammonium cocoyl isethionate,
sodium cocoyl
isethionate, sodium lauroyl isethionate, and mixtures thereof.
[00116] Still other suitable anionic surfactants are the alkylglyceryl ether
sulfonates of the
form Rl-OCH2-C(OH)H--CH2-SO3M, wherein Rl is a saturated or unsaturated,
branched
or unbranched alkyl group from about 8 to about 24 carbon atoms, and M is a
water-
soluble cation such as ammonium, sodium, potassium, magnesium,
triethanolamine,
diethanolamine and monoethanolamine. One example is sodiunl cocoglyceryl ether
sulfonate.
[00117] Other suitable anionic surfactants include: Sulfonated fatty acids of
the form Rl-
CH(S04)-COOH and sulfonated methyl esters of the from Rl-CH(SO4)-CO--O-CH3,
where Rl is a saturated or unsaturated, branched or unbranched alkyl group
from about 8
to about 24 carbon atoms (e.g., alpha sulphonated coconut fatty acid and
lauryl methyl
ester); phosphates such as monoalkyl, dialkyl, and trialkylphosphate salts
formed by the
reaction of phosphorous pentoxide with monohydric branched or unbranched
alcohols
having from about 8 to about 24 carbon atoms (e.g., sodimn mono or
dilaurylphosphate,
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ethoxylated monoalkyl phosphates, etc.); acyl glutamates corresponding to the
formula
Rl CO--N(COOH)--CH2CH2-C02M wherein Rl is a saturated or unsaturated, branched
or unbranched alkyl or alkenyl group of about 8 to about 24 carbon atoms, and
M is a
water-soluble cation (e.g., sodium lauroyl glutamate and sodium cocoyl
glutamate);
alkanoyl sarcosinates corresponding to the formula R1 CON(CH3)-CH2CH2-CO2M
wherein R1 is a saturated or unsaturated, branched or unbranched alkyl or
alkenyl group
of about 10 to about 20 carbon atoms, and M is a water-soluble cation (e.g.,
sodium
lauroyl sarcosinate, sodium cocoyl sarcosinate, and ammonium lauroyl
sarcosinate); allcyl
ether carboxylates corresponding to the formula R1-(OCH2CH2)x-OCHz-CO2M
wherein
R1 is a saturated or unsaturated, branched or unbranched alkyl or alkenyl
group of about
8 to about 24 carbon atoms, x is 1 to 10, and M is a water-soluble cation
(e.g., sodium
laureth carboxylate); acyl lactylates corresponding to the formula R1CO-[O--
CH(CH3)-
CO]x-CO2M wlierein Rl is a saturated or unsaturated, branched or unbranched
alkyl or
alkenyl group of about 8 to about 24 carbon atoms, x is 3, and M is a water-
soluble cation
(e.g., sodium cocoyl lactylate); carboxylates, nonlimiting examples of which
include
sodium lauroyl carboxylate, sodium cocoyl carboxylate, and ammonium lauroyl
carboxylate; anionic flourosurfactants; and natural soaps derived from the
saponification
of vegetable and/or animal fats & oils examples of which include sodium
laurate, sodium
inyristate, palmitate, stearate, tallowate, cocoate.
[00118] Any counter cation, M, can be used on the anionic surfactant.
Preferably, the
counter cation is selected from the group consisting of sodium, potassium,
ammonium,
monoethanolamine, diethanolamine, and triethanolamine.
[00119] Nonlimiting examples of nonionic surfactants that may be included in
the
compositions of the present invention include those selected from the group
consisting of
alkyl glucosides, alkyl polyglucosides, polyhydroxy fatty acid amides,
alkoxylated fatty
acid esters, sucrose esters, amine oxides, and mixtures thereof.
[00120] Alkyl glucosides and alkyl polyglucosides are useful herein, and can
be broadly
defined as condensation products of long chain alcohols, e.g., C8-30 alcohols,
with
sugars or starches or sugar or starch polymers, i.e., glycosides or
polyglycosides. These
compounds can be represented by the formula (S)õ --O--R wherein S is a sugar
moiety
such as glucose, fructose, mannose, and galactose; n is an integer of from
about 1 to
about 1000, and R is a C8-30 alkyl group. Exainples of long chain alcohols
from which
the alkyl group can be derived include decyl alcohol, cetyl alcohol, stearyl
alcohol, lauryl
alcohol, myristyl alcohol, oleyl alcohol, and the like. Preferred examples of
these
surfactants include those wherein S is a glucose moiety, R is a C8-20 alkyl
group, and n
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WO 2006/083843 PCT/US2006/003365
is an integer ot trom about 1 to about 9. Commercially available examples of
these
surfactants include decyl polyglucoside (available as APG 325 CS from Henkel)
and
lauryl polyglucoside (available as APG 600CS and 625 CS from Henkel). Also
useful are
sucrose ester surfactants such as sucrose cocoate and sucrose laurate.
[00121] Other usef-ul nonionic surfactants include polyhydroxy fatty acid
amide
surfactants, more specific examples of which include glucosamides Processes
for
making compositions containing polyhydroxy fatty acid amides are disclosed,
for
example, in G.B. Pat. Specification 809,060, published Feb. 18, 1959, by
Thomas Hedley
& Co., Ltd.; U.S. Pat. No. 2,965,576, to E. R. Wilson, issued Dec. 20, 1960;
U.S. Pat.
No. 2,703,798, to A. M. Schwartz, issued Mar. 8, 1955; and U.S. Pat. No.
1,985,424, to
Piggott, issued Dec.25, 1934.
[00122] Other examples of nonionic surfactants include amine oxides. Amine
oxides
correspond to the general formula Ri R2 R3 N- 0, wherein Rl contains an alkyl,
alkenyl
or monohydroxy alkyl radical of from about 8 to about 18 carbon atoms, from 0
to about
10 ethylene oxide moieties, and from 0 to about 1 glyceryl moiety, and R2 and
R3 contain
from about 1 to about 3 carbon atoms and from 0 to about 1 hydroxy group,
e.g., methyl,
ethyl, propyl, hydroxyethyl, or hydroxypropyl radicals. The arrow in the
formula is a
conventional representation of a semipolar bond. Examples of amine oxides
suitable for
use in this invention include dimethyl-dodecylamine oxide, oleyldi(2-
hydroxyethyl)
amine oxide, dimethyloctylamine oxide, dimethyl-decylamine oxide, dimethyl-
tetradecylamine oxide, 3,6,9-trioxaheptadecyldiethylamine oxide, di(2-
hydroxyethyl)-
tetradecylamine oxide, 2-dodecoxyethyldimethylamine oxide, 3-dodecoxy-2-
hydroxypropyldi(3-hydroxypropyl)amine oxide, dimethylhexadecylamine oxide.
[00123] The term "amphoteric surfactant," as used herein, is also intended to
encompass
zwitterionic surfactants, which are well known to formulators skilled in the
art as a subset
of amphoteric surfactants.
[00124] A wide variety of amphoteric lathering surfactants can be used in the
compositions of the present invention. Particularly useful are those which are
broadly
described as derivatives of aliphatic secondary and tertiary amines,
preferably wherein
the nitrogen is in a cationic state, in which the aliphatic radicals can be
straight or
branched chain and wherein one of the radicals contains an ionizable water
solubilizing
group, e.g., carboxy, sulfonate, sulfate, phosphate, or phosphonate.
[00125] Nonlimiting examples of amphoteric or zwitterionic surfactants are
those selected
from the group consisting of betaines, sultaines, hydroxysultaines,
alkyliminoacetates,
iminodialkanoates, aminoalkanoates, and mixtures thereof.
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[00126] Examples of betaines include the higher alkyl betaines, such as coco
dimethyl
carboxymethyl betaine, lauryl dimethyl carboxymethyl betaine, lauryl dimethyl
alphacarboxyethyl betaine, cetyl dimethyl carboxymethyl betaine, cetyl
dimethyl betaine
(available as Lonzaine 16SP from Lonza Corp.), lauryl bis-(2-hydroxyethyl)
carboxymethyl betaine, oleyl dimethyl gamma-carboxypropyl betaine, lauryl bis-
(2-
hydroxypropyl)alpha-carboxyethyl betaine, coco dimethyl sulfopropyl betaine,
lauryl
dimethyl sulfoethyl betaine, lauryl bis-(2-hydroxyethyl) sulfopropyl betaine,
amidobetaines and amidosulfobetaines (wherein the RCONH(CH<sub>2</sub>)<sub>3</sub>
radical is
attached to the nitrogen atom of the betaine), oleyl betaine (available as
ainphoteric
Velvetex OLB-50 from Henkel), and cocamidopropyl betaine (available as
Velvetex BK-
35 and BA-35 from Henkel).
[00127] Examples of sultaines and hydroxysultaines include materials such as
cocamidopropyl hydroxysultaine (available as Mirataine CBS from Rhone-
Poulenc).
[00128] Examples of amphoteric surfactants of the present invention include
the
following compounds: Cetyl dimethyl betaine (this material also has the CTFA
designation cetyl betaine); Cocamidopropylbetaine; Cocamidopropyl hydroxy
sultaine.
Examples of other useful amphoteric surfactants are alkyliminoacetates, and
iminodialkanoates and aminoalkanoates of the formulas RN[(CH2) CO2 M] 2 and
RNH(CH2).,,, CO2 M wherein m is from 1 to 4, R is a C8 -C22 alkyl or alkenyl,
and M is
H, alkali metal, alkaline earth metal ammonium, or alkanolammonium. Also
included are
imidazolinium and ammonium derivatives. Specific examples of suitable
amphoteric
surfactants include sodium 3-dodecyl-aminopropionate, sodium 3-
dodecylaminopropane
sulfonate, N-higher alkyl aspartic acids such as those produced according to
the teaching
of U.S. Pat. 2,438,091; and the products sold under the trade name "Miranol"
and
described in U.S. Pat. 2,528,378. Other examples of useful amphoterics include
amphoteric phosphates, such as coamidopropyl. PG-dimonium chloride phosphate
(commercially available as Monaquat PTC, from Mona Corp.). Also useful are
amphoacetates such as disodium lauroamphodiacetate, sodium lauroamphoacetate,
and
mixtures thereof.
[00129] In preferred embodiments, the sunscreen/bodywashes of the invention
include at
least one cationic surfactant. Many cationic surfactants are known to the art.
Suitable
cationic surfactants include, but are not limited to, fatty amines, di-fatty
quatenlary
amines, tri-fatty quaternary amines, imidazolinium quatenlary amines, and
combinations
thereof. Suitable fatty amines include monalkyl quaternary amines such as
cetyltrimethylammonium bromide. A suitable quaternary ainine is
dialklamidoethyl
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hydroxyethylmonium methosulfate. By way of example, the following may be
mentioned: stearyldimenthylbenzyl ammonium chloride; dodecyltriinethylammonium
chloride; nonylbenzylethyldimethyl ammonium nitrate; tetradecylpyridinium
bromide;
laurylpyridinium chloride; cetylpyridinium chloride; laurylpyridinium
chloride;
laurylisoquinolium bromide; ditallow(Hydrogenated)dimethyl ammonium chloride;
dilauryldimethyl ammonium chloride; and stearalkonium chloride.
Additional cationic surfactants are disclosed in U.S. Pat. No. 4,303,543 see
column 4,
lines 58 and column 5, lines 1-42, incorporated herein by references. Also see
CTFA
Cosmetic Ingredient Dictionary, 4th Edition 1991, pages 509-514 for various
long chain
alkyl cationic surfactants; incorporated herein by reference.
[00130] The total surfactants, e.g., cationic surfactant, may be present in
the
sunscreen/bodywash at about 0.1 to about 20%, or about 0.1 to about 10%, or
about 0.1
to about 5%, or about 0.5 to about 5%, or about 1 to about 10%, or about 1 to
about 5%,
or about 0.1 to about 2%, or about 1 to about 2%. In some embodiments, a
sunscreen/bodywash composition of the invention contains a surfactant, e.g., a
cationic
surfactant, at about 1%.
[00131] In addition to surfactants, other ingredients, as described above for
additives, may
be included in the additive/bodywash. Any component known in the art or useful
in
bodywashes may be used.
[00132] hi some embodiments, soapless cleansers maybe used in addition to, or
instead
of, soaps/surfactants. For example, OilatumTM AD (registered trademark,
Stiefel
Laboratories), AquanilTM (registered trademark, Person & Covey, Inc.),
CetaphilTm
(trademark, Galderma Laboratories, Inc.) or SpectroDermTM (registered
trademark,
Draxis Pharmaceutical Inc.), or their equivalents, may be utilized as a
soapless
component in the present invention.
[00133] As noted above, the sunscreen additives of the invention may also be
combined
with conventional bodywash compositions, as well as with shampoos for hair,
and post-
wash skincare compositions. Proportions for addition and mixing are given
above as
well as in more detail hereafter. An exemplary bodywash that may be used with
additives of the invention is exemplified by SUAVE Body Wash. Ingredients of a
typical
SUAVE bodywash include: Water, Aminonium Lauryl Sulfate, Ammonium Laureth
Sulfate, Cocamidopropyl Betaine, Fragrance, Glycerin, Hydrolyzed Milk Protein
&
Honey Extract, PEG- 10 Sunflower Glycerides, Cocamide MEA, Guar
Hydroxypropylrimonium Chloride, Acrylates Copolymer, PEG-5 Cocamide,
Helianthus
Annuus (Sunflower) Seed Oil or Glycine Soja (Soybean) Oil, Tetrasoidum EDTA,
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Propylene Glycol, Ammonium Chloride, Sodium Hydroxide,
MethylchloroisotlZiazolinone, Methylisothiazolinone, Titanium Dioxide (CI
77891)
II. Methods
A. Preparation
[00134] The compositions of the invention may be prepared by any suitable
method. In
one preferred method, a"Phase I," which is a "water phase," is prepared by
mixing the
more water-soluble components of the composition. For example, Polyquaternium-
4, a
film former (e.g., in MOISTUREGUARD), and encapsulated sunscreen (e.g., in UV
PEARLS), may be mixed until uniform. A "Phase II," which is an "oil phase," is
prepared by mixing the more hydrophobic components of the composition. For
example,
Avobenzone (e.g., PARSOL 1789) may be mixed with Octocrylene, with heating,
until
dissolved. Then Phase I and Phase II are combined with gentle agitation, until
a unifonn
composition is obtained (Phase III). Phase III may be further combined with a
bodywash
composition (e.g., SUAVE bodywash) and mixed until unifonn. A further
sunscreen,
such as titanium dioxide, may be added to the Phase IIUbodywash composition
and
mixed until uniform. Alternatively, the sunscreen may be added before addition
to the
bodywash or soap to provide an additive ready for formulation with a bodywash
or soap.
B. Use
[00135] Additives, e.g., sunscreen additives of the invention are generally
designed to be
used in combination with a bodywash. Thus, the compositions of the invention
are
typically designed to be applied while washing. This characteristic
facilitates ease of use
and may have the added benefit of being cumulative. Compositions of the
present
invention are readily applied during washing in a suitable or effective amount
and may be
generally applied all over the body. Shampoos may be applied specifically to
the hair. A
selected amount of a composition may be applied directly to the skin or may be
used
through inteilnediate application to a washcloth, pad, sponge, or other
applicator. After
lathering, dirt and sloughed-off skin may be washed away by rinsing with water
leaving
behind one or more of the additives, e.g., sunscreen components. Additives of
the
invention, e.g., sunscreen additives of the invention are also useful in hair
shampoos and
conditioners, and in after-wash lotions.
[00136] Thus, methods of the invention include methods for protection of skin
from
sunlight, comprising applying a bodywash comprising a sunscreen to the skin,
wherein
after application of the bodywash to skin and rinsing, the skin is protected
from sunlight
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with an average SPF of at least about 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13,
14, 15, 16, 17,
18, 19, 20, or more than 20. In some preferred embodiments, the skin is
protected from
sunlight with an average SPF of at least about 2. In some preferred
embodiments, the
skin is protected from sunlight with an average SPF of at least about 5. In
some preferred
embodiments, the skin is protected from sunlight with an average SPF of at
least about
10. In some preferred embodiments, the slcin is protected from sunlight wit11
an average
SPF of at least about 15. In some embodiments, the bodywash is applied more
than once;
in these cases, the SPF may be cumulative and can increase with the second
wash to, e.g.,
an average of more than 2, 5, 6, 7, 8, 9, 10, 11, 12, 13, 15, 15, 16, 17, 18,
19, 20, 21, 22,
23, 24, 25, 30, 35, 40, 45, or more than about 45. In some einbodiments the
bodywash is
applied once per day. In some embodiments, the bodywash is applied more than
once per
day, for example, 2, 3, 4, or more than 4 times per day. In some embodiments,
the
bodywash is applied about every other day. In some embodiments, the body wash
is
applied about 10, 8, 7, 6, 5, 4, 3, 2 or 1 time per week.
[00137] In these methods, the active additive, e.g., sunscreen, often does not
penetrate
beyond a certain level in the skin, typically due to encapsulation. Thus, in
some
embodiments of the methods of the invention, the active additive, e.g.,
sunscreen, does
not penetrate more than about 10, 20, 25, 30, 35, 40, 45, or 50 microns into
the skin with
one washing with a bodywash containing the additive. In some embodiments, the
active
additive, e.g., sunscreen, does not penetrate more than about 10, 20, 25, 30,
35, 40, 45,
50, 60, 70, 80, 90, 100, 120, or 150 microns into the skin, even with repeated
washings.
[00138] In other embodiments the sunscreen or other additive is designed to
penetrate into
the skin, thus, in these embodiments, the active additive, e.g., sunscreen,
penetrates to at
least about 10, 20, 25, 30, 35, 40, 45, or 50 microns into the skin with one
washing with a
bodywash containing the additive. In some embodiments, the active additive,
e.g.,
sunscreen, penetrates more than about 10, 20, 25, 30, 35, 40, 45, 50, 60, 70,
80, 90, 100,
120, or 150 microns into the skin. In some embodiments this penetration occurs
with a
single washing and rinsing. In some embodiments this penetration occurs with
repeated
washings and rinsings.
[00139] Any additive described herein, e.g., sunscreen additives, generally as
a component
of a bodywash, may be used in the methods of the invention. In some
embodiments, the
additive is a non-sunscreen additive and is encapsulated, e.g., in the form of
sol-gel
microcapsules. In these embodiments, the additive may be used in combination
with a
non- bodywash vehicle, such as a skin lotion, gel, cream, and the like, as are
well-known
in the art.
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[00140] While it is ordinarily preferred to use the compositions of the
present invention in
a manner similar to ordinary soap (i.e., wetting, application of composition,
rinsing), it is
also anticipated that the composition may be used by application without
wetting
followed by removal through, for example, wiping. This is the case for
soapless
cleansers.
C. Business Methods
[00141] The invention also encompasses methods of doing business in the field
of topical
delivery of cosmeceuticals and the transdermal delivery of pharmaceuticals
using
lathering products, including everyday soap and shampoo, as the delivery
agents.
[00142] Consumers spend more than $30 billion annually on products that talce
advantage
of topical and transdermal delivery methods. Despite enormous growth in this
area, there
have been few major innovations. Most delivery methods still rely on lotions,
creams or
patches. By combining a cosmetic or even pharmaceutical regimen with an
activity as
routine as washing up or showering, the business methods of the invention
capture a
significant share of the topical and transdermal delivery market. Products
enable
personal care product makers to secure a piece of the growing market for
cosmeceuticals,
like sunscreen, by enhancing existing product lines. They will also enable
drug makers
to offer consumers more appealing ways to administer prescription and over-the-
counter
pharmaceuticals
[00143] Business methods of the invention encompass a method of doing business
comprising marketing an additive for use with an existing bodywash, wherein
the
additive, when combined with the bodywash, causes an additional effect to the
normal
effect of the soap or the bodywash. The business methods include methods
involving any
of the additives described herein, including sunscreens, insect repellants,
anti-acne
medications, anti-wrinkling agents, deodorants, and all others described
herein In some
embodiments, the methods include marketing a sunscreen benefit agent
(additive) for use
with a bodywash, e.g., bar and liquid soaps, and shampoos, to add the benefit
of a
sunscreen. The sunscreen may be any one of the sunscreen additives described
herein.
This embodiment is designed to appeal to soap manufacturers looking to broaden
the
market for their products among the growing population of consumers concenled
about
skin cancer and wrinkles. Generally, the benefit agent is marketed as a brand-
neutral
additive for use with existing brands. In some cases, a stand-alone brand may
be created.
[00144] The sunscreen or other benefit agent may be licensed as an additive,
in both
liquid and bar soap forms, to personal care product makers of all sizes, to
enhance and
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differentiate their brand.ea product offerings. The license may be exclusive
or,
preferably, non-exclusive. If exclusive, it may be exclusive in a defined
geographical
territory, for a defined time period (often with an option to renew or right
of first refusal
at the expiration of the time period), for a defined type of skin care
product, or any
combination of these. The methods also include supplying one or more customers
with
an option to license or buy the additive, generally for a defined period of
time. As with
licenses, such an option may be exclusive or non-exclusive. Alteznatively, the
sunscreen
or otller benefit agent may be manufactured and supplied to personal care
product
makers. A further alternative is to manufacture a stand-alone brand of
soap/bodywash
that includes the additive.
[00145] A further component of the business methods of the invention typically
includes
receiving payment for supplying the additive, license, or the like, to the
customer. It will
be appreciated that "payment" may be any form of consideration, included
monetary
consideration. Typically, license payments take the form of an up-front
payment,
royalties, license maintenance fees or some combination thereof. Also included
in
payment options are equity in the company receiving the additive or the
license to the
additive. It will be appreciated that any other form of consideration may also
constitute
payment in the business methods of the invention
[00146] The business methods of the invention may further include
manufacturing the
additive and/or the additive/bodywash. In some embodiments, different entities
perform
different aspects; for example, a first entity may manufacture the additive
and a second
entity may market and/or distribute it. In some embodiments, a single entity
performs
both manufacturing and marketing.
(001471 Business methods of the invention further include a method including
the steps
of: a) designing an additive for use in a personal care product; b) testing
the additive for
safety and effectiveness in huinans; c) arranging for distribution and
marketing of the
additive. In some embodiments, steps a) and c) are perfonned by a first
entity, typically a
business entity, and step b) is performed by a second entity, such as a
business entity or
an academic entity. In some or these embodiments, step b) is performed as a
joint
venture between the two entities.
[00148] All publications and patent applications mentioned in this
specification are herein
incorporated by reference to the same extent as if each individual publication
or patent
application was specifically and individually indicated to be incorporated by
reference.
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[00149] It will be apparent to one of ordinary skill in the art that many
changes and
modification can be made to the disclosures presented herein without departing
from the
spirit or scope of the appended claims.
EXAMPLES
EXAMPLE 1
[00150] A sunscreen additive for addition to a bodywash was prepared as
follows: To
13.7 g water was added 1 g of polyquaternium-4 (CELQUAT-200), 1.5 gm of
MOISTUREGUARD, and 12 g of UV PEARLS. The mixture was stirred until uniform,
to produce Phase I. Separately, 1 g of PARSOL 1789 was added to 4 g of
Octocrylene
witlZ heating, and stirred until uniform, to produce Phase II. Phase I and
Phase II were
combined with gentle agitation until uniform to produce Phase III, a sunscreen
additive.
[00151] The sunscreen additive of Phase III was added to 64.5 g of SUAVE
Bodywash
and stirred until uniform. Finally, 2.3 g of titanium dioxide were added with
stirring.
The final composition was a sunscreen/bodywash.
EXAMPLE 2
[00152] The sunscreen/bodywash of Example 1 was tested for SPF capability as
follows:
50 cm2 of testing site was wetted with 10m1 of water delivered with a syringe.
The test
sample was applied as per FDA monograph C.F.R. 21 to the area. Lather was
worked
into the subject for 3 minutes to allow the product to absorb into the skin.
The area was
rinsed after 2 additional minutes with 20m1 of water, then the area was patted
dry and
allowed 15 minutes before exposure to radiation as per FDA monograph. The skin
was
exposed to UV radiation and the MED was noted and compared to the MED for skin
without treatment. Results are shown in the Table below.
Table
(Lather Method*)
Subject Sex MED/ I Skin MED I MED II STD SPF
ID # Hr (Amps) Type J/M2 J/M2 (8% HMS) Value
46 8676 F 127.8 7.0 II 46.20 46.20 4.40 15.00
50 3379 F 126.4 7.0 II 46.20 46.20 4.00 18.00
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36 0202 F 125.8 7.0 11 46.20 46.20 4.40 21.60
56 2392 F 125.8 7.0 II 46.20 46.20 4.00 18.00
501415 F 125.8 7.0 11 46.20 46.20 4.40 21.60
MEAN (x) 4.24 18.84
STANDARD DEV (s) 0.22 2.80
STD. ERROR 0.10 1.25
S.E. % OF MEAN 2.36 6.63
N 5 5
MED: Minimal Erythemal Dose
I: Intensity of light source
[00153] This Example demonstrates that the sunscreen/bodywash enhanced the sun
protection as measured by this protocol, as coinpared to untreated skin, by an
average
SPF of over 18.
EXAMPLE 3
[00154] A sunscreen/bodywash is prepared by mixing the following ingredients:
0.1 to 7.5
parts by weight of octylmethoxy cinnamate, 0.1 to 6 parts by weight of octyl
salicylate,
0.1 to 5 parts by weight of oxybenzone, I to 10 parts by weight of cationic
surfactant,
0.01 to 1 part by weight of a quatemized compound and 0.01 to 1 part by weight
of a
preservative.
EXAMPLE 4
[00155] A sunscreen/bodywash is prepared by mixing the following ingredients:
Water 20-65%
Polyquat 4 .01-3.75%
Dimethicone.01-7%
Octylmethoxycinnamate in amorphous silica
Petrolatum .01-10%
Titanium Dioxide.01-20%
Octocrylene .01-10%
Parso11789(Avobenzone) .01-3%
Kathon .01-2%
Bodywash generic 5-99%
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EXAMPLE 5
[00156] Generic type soap bases for shampoos, body washes, facial cleansers or
specialty
washes can consist of base such as;
Water 45
Dermacryl AQF 4.7
Polyquat 4 3.8
Cocamido propyl betaine Unibetain BA-35 6
Aminonium Lauryl Sulfate Unipol A 24
Ammonium Laureth Sulfate Unipol EA-2 6
Dimethicone Moistureguard 10
preseivative 0.5
100
[00157] This base shows an example of adding a polyquat to enhance the
benefits of SPF
added at the mixtures mentioned in the art. Ranges of polyquats in the base
can vary
from .001 %- 10% to the base to enhance the system. The addition of additional
film
formers can also enhance the additive, an example being the Acrylate
Copolymer,
Dermacryl AQFtin . Acrylates especially carboxylated added at a.001 l0- 20%
level,
being hydrophobic offer substantial water resistance allowing the final
product to be
water resistant to a greater degree. These components can all be added in the
soap base
formulation to create a synergistic effect with the additive.
EXAMPLE 6
[00158] 50 subjects were tested with the sunscreen/bodywash of Example 1 of
the
invention for skin irritation. Subjects bathed or washed as usual, then 0.2m1
or 0.2g of
test material was dispensed on a designated area of the subject's back and
allowed to air
dry. The procedure was completed nine consecutive times (Monday, Wednesday,
and
Friday for three consecutive weeks). Areas of application were monitored for
erythema
and edema. Subjects were then given a 10-14 day rest followed by reapplication
at
another test site, equivalent to any one of the original nine exposures.
[00159] No adverse reactions of any kind were noted during the course of this
study.
EXAMPLE 7
[00160] A water resistance test was performed using the sunscreen/bodywash of
Example
1. Per the FDA Monograph for Water Resistant and Very Water Resistant claims,
the
product sample was applied to dry skin of subjects, then submersed in a
whirlpool bath
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tor 40 or 80 minutes prior to measurement. The average SPF after the 40 minute
immersion was 12.45 and after the 80 minute immersion was 10.35.
[00161] While preferred embodiments of the present invention have been shown
and
described herein, it will be obvious to those skilled in the art that such
embodiments are
provided by way of example only. Numerous variations, changes, and
substitutions will
now occur to those skilled in the art without departing from the invention. It
should be
understood that various alternatives to the embodiments of the invention
described herein
may be employed in practicing the invention. It is intended that the following
claims
define the scope of the invention and that methods and structures within the
scope of
these claims and their equivalents be covered thereby.
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