U.S. patent application number 12/141561 was filed with the patent office on 2009-12-24 for compositions for lightening skin color.
This patent application is currently assigned to CONOPCO, INC., D/B/A UNILEVER, CONOPCO, INC., D/B/A UNILEVER. Invention is credited to Stephen Alan Madison.
Application Number | 20090317341 12/141561 |
Document ID | / |
Family ID | 41120037 |
Filed Date | 2009-12-24 |
United States Patent
Application |
20090317341 |
Kind Code |
A1 |
Madison; Stephen Alan |
December 24, 2009 |
Compositions for Lightening Skin Color
Abstract
Skin lightening additives and skin lightening compositions
having at least one of a heterosubstituted, saturated or
unsaturated aliphatic acid are described. The compositions are
suitable for topical application and may comprise 12-hydroxystearic
acid, ricinoleic acid or both.
Inventors: |
Madison; Stephen Alan;
(Newton, CT) |
Correspondence
Address: |
UNILEVER PATENT GROUP
800 SYLVAN AVENUE, AG West S. Wing
ENGLEWOOD CLIFFS
NJ
07632-3100
US
|
Assignee: |
CONOPCO, INC., D/B/A
UNILEVER
Englewood Cliffs
NJ
|
Family ID: |
41120037 |
Appl. No.: |
12/141561 |
Filed: |
June 18, 2008 |
Current U.S.
Class: |
424/59 ; 514/356;
514/557; 514/560; 562/512; 562/577; 562/598 |
Current CPC
Class: |
A61K 8/58 20130101; A61K
8/675 20130101; A61K 8/27 20130101; A61K 8/347 20130101; A61K 8/44
20130101; A61K 8/35 20130101; A61K 8/365 20130101; A61K 8/671
20130101; A61K 8/361 20130101; A61Q 17/04 20130101; A61Q 19/02
20130101; A61K 8/37 20130101; A61K 8/34 20130101 |
Class at
Publication: |
424/59 ; 562/512;
562/577; 562/598; 514/557; 514/560; 514/356 |
International
Class: |
A61K 8/36 20060101
A61K008/36; C07C 53/00 20060101 C07C053/00; C07C 57/03 20060101
C07C057/03; C07C 59/76 20060101 C07C059/76; A61Q 17/04 20060101
A61Q017/04; A61K 31/44 20060101 A61K031/44; A61K 31/201 20060101
A61K031/201; A61K 31/19 20060101 A61K031/19 |
Claims
1. A skin lightening additive comprising a heterosubstituted,
saturated or unsaturated aliphatic acid, or a mixture thereof.
2. The skin lightening additive according to claim 1 wherein
aliphatic acid is ##STR00002## or a mixture thereof wherein each R
is independently hydrogen, hydroxyl, C.sub.1-6 alkoxy, C.sub.1-6
alkyl, arylalkyl or an amine, with the proviso that at least one R
group comprises a heteroatom; each R.sup.1 is independently
hydrogen, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, arylalkyl or an amine;
n is an integer from about 7 to about 19; and s and e are each
independently an integer from about 0 to about 8, where
s+e.gtoreq.6; q is an integer from about 6 to about 11; each r is
independently an integer from 0 to 1, with the proviso that each r
is not 1 when x is 1; x is an integer from 0 to 1 with the proviso
that x is 0 when at least one r is 1; and each t is independently
an integer from 1 to 7.
3. The skin lightening additive according to claim 1 wherein the
heterosubstituted, saturated aliphatic acid is at least one of
aleuritic acid; phloionolic acid,
9,10,13-trihydroxy-11-octadecenoic acid;
9,13-dihydroxy-12-ethoxy-10-octadecenoic acid;
9-hydroxy-10,12-octadecadienoic acid; 4,14-dihydroxy-octadecanoic
acid; 12-hydroxystearic acid or a mixture thereof and the
heterosubstituted, unsaturated aliphatic acid is at least one of
lesquerolic acid; ricinelaidic acid; ambrettolic acid; ricinoleic
acid; beta-dimorphecolic acid; densipolic acid;
8-methoxy-13-hydroxy-9,11-octadecadienoic acid; 7-oxo-octadecanoic
acid; 9-oxo-octadecanoic acid; 12-oxo-octadecanoic acid;
10-oxo-14-methyl-pentadecanoic acid or a mixture thereof.
4. The skin lightening additive according to claim 1 wherein the
skin lightening additive comprises the heterosubstituted, saturated
aliphatic acid and heterosubstituted, unsaturated aliphatic acid at
a weight ratio from about 10:90 to about 90:10.
5. The skin lightening additive according to claim 1 wherein the
skin lightening additive consists essentially of heterosubstituted,
saturated aliphatic acid, heterosubstituted, unsaturated aliphatic
acid, or both.
6. A cosmetic composition comprising a. a skin lightening additive
comprising a heterosubstituted, saturated or unsaturated aliphatic
acid, or a mixture thereof; and b. a cosmetic carrier.
7. The cosmetic composition according to claim 6 wherein aliphatic
acid is represented as formula I, formula II and/or formula III
##STR00003## or a mixture thereof wherein each R is independently
hydrogen, hydroxyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, arylalkyl or
an amine, with the proviso that at least one R group comprises a
heteroatom; each R.sup.1 is independently hydrogen, C.sub.1-6
alkoxy, C.sub.1-6 alkyl, arylalkyl or an amine; n is an integer
from about 7 to about 19; and s and e are each independently an
integer from about 0 to about 8, where s+e.gtoreq.6; q is an
integer from about 6 to about 11; each r is independently an
integer from 0 to 1, with the proviso that each r is not 1 when x
is 1; x is an integer from 0 to 1 with the proviso that x is 0 when
at least one r is 1; and each t is independently an integer from 1
to 7.
8. The cosmetic composition according to claim 7 wherein the
heterosubstituted, saturated aliphatic acid is at least one of
aleuritic acid; phloionolic acid;
9,10,13-trihydroxy-11-octadecenoic acid;
9,13-dihydroxy-12-ethoxy-10-octadecenoic acid;
9-hydroxy-10,12-octadecadienoic acid; 4,14-dihydroxy-octadecanoic
acid; 12-hydroxystearic acid or a mixture thereof and the
heterosubstituted, unsaturated aliphatic acid is at least one of
lesquerolic acid; ricinelaidic acid, ambrettolic acid; ricinoleic
acid; beta-dimorphecolic acid; densipolic acid;
8-methoxy-13-hydroxy-9,11-octadecadienoic acid; 7-oxo-octadecanoic
acid; 9-oxo-octadecanoic acid; 12-oxo-octadecanoic acid;
10-oxo-14-methyl-pentadecanoic acid or a mixture thereof.
9. The cosmetic composition according to claim 6 wherein the skin
lightening additive comprises the heterosubstituted, saturated
aliphatic acid and heterosubstituted, unsaturated aliphatic acid at
a weight ratio from about 90:10 to about 10:90.
10. The cosmetic composition according to claim 6 wherein the skin
lightening additive consists essentially of heterosubstituted,
saturated aliphatic acid, heterosubstituted, unsaturated aliphatic
acid, or a mixture thereof.
11. The cosmetic composition according to claim 6 wherein the
cosmetic composition further comprises an alpha-hydroxy,
beta-hydroxy acid, sunscreen or a mixture thereof.
12. The cosmetic composition according to claim 6 wherein the
cosmetic composition further comprises a vitamin.
13. The cosmetic composition according to claim 12 wherein the
vitamin is niacinamide.
14. The cosmetic composition according to claim 7 wherein the
cosmetic composition further comprises niacinamide.
15. The cosmetic composition according to claim 6 wherein the
composition further comprises conjugated linoleic acid,
petroselinic acid or both.
16. The cosmetic composition according to claim 6 wherein the
composition further comprises antioxidant.
17. The cosmetic composition according to claim 7 whereby a salt or
derivative of the aliphatic acid represented by formula I, II
and/or III is used.
18. A method for lightening skin color comprising the steps of: a.
contacting skin with the composition of claim 6; and b. suppressing
melanin production.
19. The method for lightening skin color according to claim 17
wherein the skin composition further comprise niacinamide,
conjugated linoleic acid, petroselinic acid, sunscreen,
alpha-hydroxy acid, beta-hydroxy acid or a mixture thereof.
Description
FIELD OF THE INVENTION
[0001] The present invention is directed to a skin lightening
additive as well as compositions comprising the same. More
particularly, the present invention is directed to a cosmetic
composition comprising a skin lightening additive whereby the skin
lightening additive comprises a heterosubstituted, saturated or
unsaturated aliphatic acid, or a mixture thereof. The skin
lightening additive, when used, results in a cosmetic composition
that can provide moisturizing benefits. Moreover, it has been
unexpectedly discovered that such aliphatic acids have skin
lightening benefits when topically applied.
BACKGROUND OF THE INVENTION
[0002] Many consumers are concerned with the characteristics of
their skin. For example, consumers are concerned with the degree of
pigmentation of their skin, freckles and/or age spots. Other
consumers wish to reduce skin darkening caused by exposure to
sunlight. To meet the needs of consumers, many attempts have been
made to develop products that improve skin characteristics. The
products developed thus far, however, often tend to have low
efficacy, undesirable side effects or both. Furthermore, such
products can be expensive and are often not an alternative for
lower income consumers.
[0003] There is an increasing interest to develop a cosmetic
composition that comprises new skin lightening additives. This
invention, therefore, is directed to cosmetic compositions that
comprise new skin lightening additives. The cosmetic compositions
of the present invention preferably comprise, as a lightening
additive, compounds like 12-hydroxystearic acid, ricinoleic acid or
both. The cosmetic compositions of this invention result in a
decrease in melanin content which is at least about 8% lower
(preferably, at least about 11% lower) when comparing
MelanoDerm.TM. cultures treated with the same to MelanoDerm
cultures that have not been subjected to a composition with the
newly discovered skin lightening additives of this invention.
ADDITIONAL INFORMATION
[0004] Efforts have been disclosed for making skin care cosmetic
compositions. In U.S. Pat. No. 6,875,425, skin lightening agents
with 4-substituted resorcinol derivative compounds are
described.
[0005] Other efforts have been disclosed for making skin treatment
compositions. In U.S. Pat. Nos. 7,250,158 and 7,247,294, methods
for treating with skin lightening agents are described.
[0006] Still other efforts have been disclosed for treating skin.
In U.S. Pat. No. 5,998,423, compositions with polycyclic nitrogen
heterocycles are described.
[0007] None of the additional information above describes skin
lightening compositions that comprise, as a lightening additive, a
heterosubstituted, saturated or unsaturated aliphatic acid, or
mixture thereof.
SUMMARY OF THE INVENTION
[0008] In a first aspect, the present invention is directed to a
skin lightening additive, the skin lightening additive comprising a
heterosubstituted, saturated or unsaturated aliphatic acid, or
both.
[0009] In a second aspect, the present invention is directed to a
cosmetic composition for skin lightening, the cosmetic composition
comprising a skin lightening agent comprising the skin lightening
additive of the first aspect of this invention.
[0010] In a third aspect, the present invention is directed to a
method for lightening skin with the cosmetic composition of the
second aspect of this invention.
[0011] All other aspects of the present invention will more readily
become apparent upon considering the detailed description and
examples which follow.
[0012] As used herein, a decrease in melanin content means a
melanin content decrease when comparing two (2), three week old
MatTek MelanoDerm cultures that have not been treated with a
composition comprising the skin lightening additive of this
invention to two (2), three week old MatTek MelanoDerm cultures
that have been treated with a composition comprising the skin
lightening additive of this invention wherein treated means: [0013]
(a) placing the MelanoDerm culture within a six (6) well tissue
culture dish and set about 0.3 cm off of the tissue culture dish;
[0014] (b) subjecting the MelanoDerm culture to 0.1 and 5
micromolar compositions having the skin lightening additive of this
invention, the composition being one prepared from a 10 millimolar
solution of skin lightening additive and carrier (e.g., dimethyl
sulfoxide) having been diluted with Dulbecco's Modified Eagle
Media; and [0015] (c) comparing the treated and untreated cultures
by obtaining average melanin content (expressed in micrograms) by
extracting melanin from MelanoDerm and obtaining absorbance
readings at 490 nm (OD490) using a commercially available
spectrophotometer like a Hach Spectrophotometer.
[0016] Cosmetic composition, as used herein, is meant to include a
composition for topical application to skin of mammals, especially
humans. Such a composition may be generally classified as leave-on
or rinse off, and is meant to include conditioners or tonics,
lipsticks, color cosmetics, and general topical compositions that
in some fashion and at the very least, reduce the effect of melanin
on keratinocytes. Lightening and whitening as used herein are meant
to mean the same and they include the lightening of skin directly
as well as the lightening of spots on the skin, like age spots and
freckles. Dulbecco's Modified Eagle Media means the nutrient
solution sold by MatTek Corporation and treated and used according
to instructions supplied with the product commercially identified
as MEL3001OBBLLMM. Skin lightening additive means a component
suitable to result in physical, but especially biological whitening
(i.e., a reduction in melanin production) whereby the skin
lightening additive can comprise, consist essentially of or consist
of the skin lightening additive. MelanoDerm means the product
having normal, human-derived epidermal keratinocytes and
melanocytes which have been cultured to form a multilayered, highly
differentiated model of the human epidermis, all of which is made
commercially available by MatTek Corporation. Unsaturated, as used
herein, means having at least one bond that is not sp.sup.3
hybridized. Comprising, as used herein, is meant to include
consisting essentially of and consisting of.
[0017] The cosmetic composition of the present invention can be in
the form of a liquid, lotion, cream, serum, gel, soap bar or toner,
or applied via a face mask or patch. The composition of this
invention is one that at the very least, lightens skin when skin is
meant to include skin on the face, neck, chest, back, arms, hands,
legs and scalp. All ranges identified herein are meant to
implicitly include all ranges subsumed therein, if, for example,
reference to the same is not explicitly made.
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0018] The only limitation with respect to the skin lightening
additive that may be used in this invention is that the same may be
used in a topical composition suitable for use on humans. The
preferred additive is a heterosubstituted, saturated or unsaturated
aliphatic acid or a mixture thereof.
[0019] In a most preferred embodiment, the skin lightening additive
employed in the present invention comprises a compound having the
formulae:
##STR00001##
or a mixture thereof, wherein each R is independently hydrogen,
hydroxyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl, arylalkyl or an amine,
with the proviso that at least one R group comprises a heteroatom;
each R.sup.1 is independently hydrogen, C.sub.1-6 alkoxy, C.sub.1-6
alkyl, arylalkyl or an amine; n is an integer from about 7 to about
19; and s and e are each independently an integer from about 0 to
about 8, where s+e.gtoreq.6 ; q is an integer from about 6 to about
11; each r is independently an integer from 0 to 1, with the
proviso that each r is not 1 when x is 1; x is an integer from 0 to
1 with the proviso that x is 0 when at least one r is 1; and each t
is independently an integer from 1 to 7.
[0020] The preferred compounds suitable for use in this invention
(either alone or in a mixture) are aleuritic acid; phloionolic
acid; 9,10,13-trihydroxy-11-octadecenoic acid;
9,13-dihydroxy-12-ethoxy-10-octadecenoic acid;
9-hydroxy-10,12-octadecadienoic acid; 4,14-dihydroxy-octadecanoic
acid; 12-hydroxystearic acid(12-hydroxyoctadecanoic acid);
lesquerolic acid; ricinelaidic acid; ambrettolic acid, and
rincinoleic acid (12-hydroxy-9-cis-octadecanoic acid) as
represented by either formula I or II. Other preferred compounds
suitable for use in this invention include beta-dimorphecolic acid;
densipolic acid; 8-methoxy-13-hydroxy-9,11-octadecadienoic acid;
7-oxo-octadecanoic acid; 9-oxo-octadecanoic acid;
12-oxo-octadecanoic acid and 10-oxo-14-methyl-pentadecanoic acid as
represented by formula III. Furthermore it is within the scope of
the present invention to include any derivative (like an ester
derivative) and/or salt of the acid represented by formulae I-III,
and especially, Mg, Na and/or Ca salts thereof. Such compounds are
commercially available from suppliers like Vertellus Specialties,
Inc., Welch, Home & Clark Co., Inc., as well as Croda
Chemicals.
[0021] The cosmetic compositions of the present invention typically
comprise from about 0.001 to about 15% by weight, and preferably,
from about 0.1 to about 12%, and most preferably, from about 1 to
about 10% by weight skin lightening additive, based on total weight
of the cosmetic composition and including all ranges subsumed
therein.
[0022] While it is within the scope of this invention for the skin
lightening additive to consist essentially of and to consist of
heterosubstituted, saturated or unsaturated aliphatic acid or a
mixture thereof, in an often desired embodiment, the skin
lightening additive of this invention comprises from about 0.2 to
about 95%, and preferably, from about 10 to about 85%, and most
preferably, from about 30 to about 65% by weight heterosubstituted
saturated or unsaturated aliphatic acid, or a mixture thereof,
based on total weight of skin lightening additive and including all
ranges subsumed therein.
[0023] In yet another desired embodiment, the cosmetic composition
of this invention comprises from about 2 to about 9%, and
preferably, from about 3 to 8%, and most preferably, from about 3
to about 6% by weight heterosubstituted, saturated or unsaturated
aliphatic acid, or a mixture thereof, based on total weight of the
cosmetic composition and including all ranges subsumed therein.
[0024] When used in combination, the weight ratio of
heterosubstituted, saturated or unsaturated aliphatic acid to
heterosubstituted, saturated aliphatic acid is from about 5:95 to
about 95:5, and preferably, from about 20:80 to about 80:20, and
most preferably, from about 40:60 to about 60:40, including all
ratios subsumed therein.
[0025] It should be known that commercially acceptable and
conventional vehicles may be used, acting as diluents, dispersants
and/or carriers for the skin lightening agents and additives
described herein and for any other optional but often preferred
additives. Therefore, the cosmetically acceptable vehicle suitable
for use in this invention may be aqueous-based, anhydrous or an
emulsion whereby a water-in-oil or oil-in-water emulsion is
generally preferred. If the use of water is desired, water
typically makes up the balance of the cosmetic composition, and
preferably, makes up from about 5 to about 99%, and most
preferably, from about 40 to about 80% by weight of the cosmetic
composition, including all ranges subsumed therein.
[0026] In addition to water, organic solvents may be optionally
included to act as carriers or to assist carriers within the
compositions of the present invention. Illustrative and
non-limiting examples of the types of organic solvents suitable for
use in the present invention include alkanols like ethyl and
isopropyl alcohol, mixtures thereof or the like.
[0027] Other optional additives suitable for use include ester oils
like isopropyl myristate, cetyl myristate, 2-octyldodecyl
myristate, avocado oil, almond oil, olive oil, neopentylglycol
dicaprate, mixtures thereof or the like. Typically, such ester oils
assist in emulsifying the cosmetic composition of this invention,
and an effective amount is often used to yield a stable, and most
preferably, water-in-oil emulsion.
[0028] Emollients may also be used, if desired, as carriers within
the cosmetic composition of the present invention. Alcohols like
1-hexadecanol (i.e., cetyl alcohol) and phenoxyethanol are often
desired as are the emollients generally classified as silicone oils
and synthetic esters. Silicone oils suitable for use include cyclic
or linear polydimethylsiloxanes containing from 3 to 9, preferably
from 4 to 5, silicon atoms. Nonvolatile silicone oils useful as an
emollient material in the inventive cosmetic composition described
herein include polyalkyl siloxanes, polyalkylaryl siloxanes and
polyether siloxane copolymers. The essentially non-volatile
polyalkyl siloxanes useful herein include, for example,
polydimethylsiloxanes.
[0029] The ester emollients that may optionally be used are: [0030]
(1) Alkenyl or alkyl esters of fatty acids having 10 to 20 carbon
atoms.
[0031] Examples thereof include isoarachidyl neopentanoate,
isononyl isonanonoate, oleyl myristate, oleyl stearate, and oleyl
oleate. [0032] (2) Ether-esters such as fatty acid esters of
ethoxylated fatty alcohols. [0033] (3) Polyhydric alcohol esters.
Ethylene glycol mono and di-fatty acid esters, diethylene glycol
mono-and di-fatty acid esters, polyethylene glycol (200-6000) mono-
and di-fatty acid esters, propylene glycol mono- and di-fatty acid
esters, polypropylene glycol 2000 monooleate, polypropylene glycol
2000 monostearate, ethoxylated propylene glycol monostearate,
glyceryl mono- and di-fatty acid esters, polyglycerol poly-fatty
esters, ethoxylated glyceryl mono-stearate, 1,3-butylene glycol
monostearate, 1,3-butylene glycol distearate, polyoxyethylene
polyol fatty acid ester, sorbitan fatty acid esters, and
polyoxyethylene sorbitan fatty acid esters are satisfactory
polyhydric alcohol esters. [0034] (4) Wax esters such as beeswax,
spermaceti, stearyl stearate and arachidyl behenate. [0035] (5)
Sterols esters, of which cholesterol fatty acid esters are
examples.
[0036] Emollients when used, typically make up from about 0.1 to
about 50% by weight of the cosmetic composition, including all
ranges subsumed therein.
[0037] Fatty acids having from 10 to 30 carbon atoms may also be
included as cosmetically acceptable carriers within the composition
of the present invention. Illustrative examples of such fatty acids
include pelargonic, lauric, myristic, palmitic, stearic,
isostearic, oleic, linoleic, arachidic, behenic or erucic acid, and
mixtures thereof. Compounds that are believed to enhance skin
penetration, like dimethyl sulfoxide, may also be used as an
optional carrier.
[0038] Humectants of the polyhydric alcohol type may also be
employed in the cosmetic compositions of this invention. The
humectant often aids in increasing the effectiveness of the
emollient, reduces scaling, stimulates removal of built-up scale
and improves skin feel. Typical polyhydric alcohols include
glycerol, polyalkylene glycols and more preferably alkylene polyols
and their derivatives, including propylene glycol, dipropylene
glycol, polypropylene glycol, polyethylene glycol and derivatives
thereof, sorbitol, hydroxypropyl sorbitol, hexylene glycol,
1,3-butylene glycol, 1,2,6-hexanetriol, ethoxylated glycerol,
propoxylated glycerol and mixtures thereof. For best results the
humectant is preferably propylene glycol or sodium hyaluronate. The
amount of humectant may range anywhere from 0.2 to 25%, and
preferably, from about 0.5 to about 15% by weight of the cosmetic
composition, based on total weight of the cosmetic composition and
including all ranges subsumed therein.
[0039] Thickeners may also be utilized as part of the cosmetically
acceptable carrier in the cosmetic compositions of the present
invention. Typical thickeners include cross-linked acrylates (e.g.
Carbopol 982), hydrophobically-modified acrylates (e.g. Carbopol
1382), cellulosic derivatives and natural gums. Among useful
cellulosic derivatives are sodium carboxymethylcellulose,
hydroxypropyl methylcellulose, hydroxypropyl cellulose,
hydroxyethyl cellulose, ethyl cellulose and hydroxymethyl
cellulose. Natural gums suitable for the present invention include
guar, xanthan, sclerotium, carrageenan, pectin and combinations of
these gums. Amounts of the thickener may range from 0.0 to 5%,
usually from 0.001 to 1%, optimally from 0.01 to 0.5% by
weight.
[0040] Collectively, the water, solvents, silicones, esters, fatty
acids, humectants and/or thickeners will constitute the
cosmetically acceptable carrier in amounts from 1 to 99.9%,
preferably from 80 to 99% by weight.
[0041] Surfactants may also be present in cosmetic compositions of
the present invention. Total concentration of the surfactant will
range from about 0 to about 40%, and preferably, from about 0 to
about 20%, optimally from about 0 to about 5% by weight of the
composition. The surfactant may be selected from the group
consisting of anionic, nonionic, cationic and amphoteric actives.
Particularly preferred nonionic surfactants are those with a
C.sub.10-C.sub.20 fatty alcohol or acid hydrophobe condensed with
from 2 to 100 moles of ethylene oxide or propylene oxide per mole
of hydrophobe; C.sub.2-C.sub.10 alkyl phenols condensed with from 2
to 20 moles of alkylene oxide; mono- and di- fatty acid esters of
ethylene glycol; fatty acid monoglyceride; sorbitan, mono- and di-
C.sub.8-C.sub.20 fatty acids; block copolymers (ethylene
oxide/propylene oxide); and polyoxyethylene sorbitan as well as
combinations thereof. Alkyl polyglycosides and saccharide fatty
amides (e.g. methyl gluconamides) are also suitable nonionic
surfactants.
[0042] Preferred anionic surfactants include soap, alkyl ether
sulfate and sulfonates, alkyl sulfates and sulfonates, alkylbenzene
sulfonates, alkyl and dialkyl sulfosuccinates, C.sub.8-C.sub.20
acyl isothionates, acyl glutamates, C.sub.8-C.sub.20 alkyl ether
phosphates and combinations thereof.
[0043] Perfumes may be used in the cosmetic composition of this
invention. Illustrative non-limiting examples of the types of
perfumes that may be used include those comprising terpenes and
terpene derivatives like those described in Bauer, K., et al.,
Common Fragrance and Flavor Materials, VCH Publishers (1990).
[0044] Illustrative yet non-limiting examples of the types of
fragrances that may be used in this invention include myrcene,
dihydromyrenol, citral, tagetone, cis-geranic acid, citronellic
acid, or cis-geranic acid nitrile, mixtures thereof or the
like.
[0045] Preferably, the amount of fragrance employed in the cosmetic
composition of this invention is in the range from about 0.0% to
about 10%, more preferably, about 0.00001% to about 5 wt %, most
preferably, about 0.0001% to about 2%.
[0046] Various types of optional additional active ingredients may
be used in the cosmetic compositions of the present invention.
Actives are defined as skin benefit agents other than emollients
and other than ingredients that merely improve the physical
characteristics of the composition. Although not limited to this
category, general examples include talcs and silicas, as well as
alpha-hydroxy acids, beta-hydroxy acids, peroxides, zinc salts, and
sunscreens.
[0047] Beta-hydroxy acids include salicylic acid, for example. Zinc
pyrithione is an example of the zinc salts useful in the cosmetic
composition of the present invention.
[0048] Sunscreens include those materials commonly employed to
block ultraviolet light. Illustrative compounds are the derivatives
of PABA, cinnamate and salicylate. For example, avobenzophenone
(Parsol 1789.RTM.) octyl methoxycinnamate and 2-hydroxy-4-methoxyl
benzophenone (also known as oxybenzone) can be used. Octyl
methoxycinnamate and 2-hydroxy-4-methoxy benzophenone are
commercially available under the trademarks, Parsol MCX and
Benzophenone-e, respectively. The exact amount of sunscreen
employed in the compositions can vary depending upon the degree of
protection desired from the sun's UV radiation. Additives that
reflect or scatter the suns rays may also be employed. These
additives include oxides like zinc oxide and titanium dioxide.
[0049] Many cosmetic compositions, especially those containing
water, should be protected against the growth of potentially
harmful microorganisms. Anti-microbial compounds, such as
triclosan, and preservatives are, therefore, typically necessary.
Suitable preservatives include alkyl esters of p-hydroxybenzoic
acid, hydantoin derivatives, propionate salts, and a variety of
quaternary ammonium compounds. Particularly preferred preservatives
of this invention are methyl paraben, propyl paraben,
phenoxyethanol and benzyl alcohol. Preservatives will usually be
employed in amounts ranging from about 0.1% to 2% by weight of the
composition.
[0050] Still other optional ingredients that may be used with the
cosmetic composition of this invention include dioic acids (e.g.,
malonic acid, sebacic acid), antioxidants like vitamin E, vitamins,
like niacinamide and vitamin C and its derivatives, recorcinols and
its derivatives (including those esterified with, for example,
ferulic acid, vanillic acid or the like) and retinoids, including
retinoic acid, retinal, retinol and retinyl esters, conjugated
linoleic acid, petroselinic acid and mixtures thereof, as well as
any other conventional ingredients well known for wrinkle-reducing,
skin whitening, anti-acne effects and reducing the impact of
sebum.
[0051] The cosmetic compositions of the present invention are
intended for use primarily as a product for topical application to
human skin, especially and at least as a product for lightening the
skin. Thus, the inventor has discovered that the described
aliphatic acids have excellent skin lightening capabilities whereby
the same may be employed as skin lightening additives in topical
cosmetic compositions that are applied topically to areas of the
skin where lightening or whitening is desired. Other benefits may
include skin moisturizing, decreasing the effect of sebum on the
skin and skin wrinkle reducing. Often, the cosmetic composition of
the present invention has a melting point from about 30.degree. C.
to about 45.degree. C., including all ranges subsumed therein. In
an especially preferred embodiment, the cosmetic composition of the
present invention has a pH from about 4.5 to about 7.5, including
all ranges subsumed therein.
[0052] When making the cosmetic composition of the present
invention, the desired ingredients are mixed in no particular order
and usually at temperatures from about 70 to about 80.degree. C.
and under atmospheric pressure.
[0053] The packaging for the composition of this invention can be a
patch, bottle, tube, roll-ball applicator, propellant driven
aerosol device, squeeze container or lidded jar.
[0054] The examples which follow are provided to illustrate and
facilitate an understanding of the invention. The examples are not
intended to limit the scope of the claims.
EXAMPLES
[0055] Commercially available human skin equivalents
(MelanoDerm.TM. from MatTek) were obtained for testing the impact
of heterosubstituted, saturated or unsaturated aliphatic acid on
melanogenesis. Solutions having a final concentration of 0.1 to 5
micromolar were prepared from a 10 millimolar dimethyl sulfoxide
stock solution and dosed ten (10) times in a three (3) week period
into the media of the MelanoDerm cultures. The media consisted of
commercially available basal Dulbecco's Modified Eagles media,
prepared and treated in the manner set forth in the manufacturer's
instructions. For long term maintenance of the MelanoDerms, the
basal media was supplemented with bFGF and alpha MSH to stimulate
melanocyte growth and melanogenesis. Each treatment condition was
done in duplicate and three (3) sets were made for each treatment,
as well as for a control (culture not treated with the aliphatic
acid). The cultures were maintained at a temperature of about
37.degree. C. and incubated in a humidified, 5% CO.sub.2 incubator
during the dosing period, but removed while being dosed.
[0056] After a three (3) week period, the MelanoDerm cultures were
removed and solubilized in a centrifuge tube containing 250
microliters of Solvable reagent (GNE9100, Packard) for sixteen (16)
hours (overnight) in a 60.degree. C. oven. Following
solubilization, the centrifuge tube containing the sample was spun
at 12,000 g for five (5) minutes. Two hundred (200) microliters of
supernatant were removed and placed in a ninety-six (96) well
plate. A spectrophotometer was used to measure the absorbance of
the supernatant at 490 nm. A standard curve using synthetic melanin
was set up in parallel to allow quantitation of melanin, in
micrograms, of the samples. The results are provided below:
TABLE-US-00001 TABLES Active Average MC .DELTA.MC MC* Value Range
Control 76.0-78.4 77.2 -- Aliphatic acid.sup.i 67.9-69.2 68.6 8.6
MC Value Range Control 76.0-78.4 77.2 -- Aliphatic acid.sup.ii
69.9-67.6 68.8 8.4 .sup.i= ricinoleic acid (0.1 uM) .sup.ii=
12-hydroxystearic acid (5 uM) *MC = melanin content
[0057] The results, as they relate to MelanoDerm cultures, show
that cosmetic compositions with the aliphatic acids of this
invention unexpectedly result in skin lightening.
* * * * *