U.S. patent application number 11/155359 was filed with the patent office on 2006-01-19 for use of active extracts to improve the appearance of skin, lips, hair and/or nails.
This patent application is currently assigned to AVON PRODUCTS, INC.. Invention is credited to Brian C. Jones, Pornngarm Limtrakul, Harish Mahalingam, Nicole McCain.
Application Number | 20060013782 11/155359 |
Document ID | / |
Family ID | 32507117 |
Filed Date | 2006-01-19 |
United States Patent
Application |
20060013782 |
Kind Code |
A1 |
Mahalingam; Harish ; et
al. |
January 19, 2006 |
Use of active extracts to improve the appearance of skin, lips,
hair and/or nails
Abstract
There is provided a composition having at least one of the
following active extracts Butea frondosa, Naringi crenulata,
Stenoloma chusana, or any combinations thereof. There is also
provided a composition having at least one of the following
additional extracts Azadirachta indica, Glycyrrhiza glabra linn.,
Morinda citrifolia, tomato glycolipid or any combinations thereof
in combination with one or more of the active extracts. The
compositions and methods of the invention are effective to improve
the aesthetic appearance of skin, lips, hair and/or nails,
especially by lightening the skin, lips, hair and/or nails.
Inventors: |
Mahalingam; Harish;
(Ledgewood, NJ) ; Jones; Brian C.; (Flower Mound,
TX) ; McCain; Nicole; (Lexington, VA) ;
Limtrakul; Pornngarm; (Chiang Mai, TH) |
Correspondence
Address: |
CHARLES N.J. RUGGIERO, ESQ.;OHLANDT, GREELEY, RUGGIERO & PERLE, L.L.P.
10th FLOOR
ONE LANDMARK SQUARE
STAMFORD
CT
06901-2682
US
|
Assignee: |
AVON PRODUCTS, INC.
|
Family ID: |
32507117 |
Appl. No.: |
11/155359 |
Filed: |
June 17, 2005 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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PCT/US03/39893 |
Dec 16, 2003 |
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11155359 |
Jun 17, 2005 |
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10321706 |
Dec 17, 2002 |
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PCT/US03/39893 |
Dec 16, 2003 |
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Current U.S.
Class: |
424/61 ; 424/725;
514/18.6; 514/18.8; 514/20.7 |
Current CPC
Class: |
A61K 8/9789 20170801;
A61Q 19/08 20130101; A61K 36/484 20130101; A61Q 19/00 20130101;
A61K 36/11 20130101; A61P 29/00 20180101; A61Q 5/08 20130101; A61K
36/75 20130101; A61P 17/00 20180101; A61K 36/746 20130101; A61K
36/81 20130101; A61Q 19/02 20130101; A61K 36/48 20130101; A61K
36/58 20130101; A61K 8/9741 20170801; A61K 36/11 20130101; A61K
2300/00 20130101; A61K 36/48 20130101; A61K 2300/00 20130101; A61K
36/484 20130101; A61K 2300/00 20130101; A61K 36/58 20130101; A61K
2300/00 20130101; A61K 36/746 20130101; A61K 2300/00 20130101; A61K
36/75 20130101; A61K 2300/00 20130101; A61K 36/81 20130101; A61K
2300/00 20130101 |
Class at
Publication: |
424/061 ;
514/015; 424/725 |
International
Class: |
A61K 38/10 20060101
A61K038/10; A61K 36/58 20060101 A61K036/58 |
Claims
1. A composition for improving the aesthetic appearance of hair,
skin, lips and/or nails, comprising: an effective amount of at
least one active extract selected from the group consisting of
Butea frondosa, Naringi crenulata, Stenoloma chusana, and any
combinations thereof.
2. The composition of claim 1, wherein the at least one active
extract is present in an amount about 0.001 wt % to about 20 wt %
based on the total weight of the composition.
3. The composition of claim 1, wherein the at least one active
extract is present in an amount about 0.05 wt % to about 10 wt %
based on the total weight of the composition.
4. The composition of claim 1, wherein the at least one active
extract is present in an amount about 0.5 wt % to about 5 wt %
based on the total weight of the composition.
5. The composition of claim 1, wherein the at least one active
extract is present in an amount about 1 wt % or less based the
total weight of the composition.
6. The composition of claim 1, wherein the composition is a topical
composition suitable for application to hair, skin, lips, and/or
nails.
7. The composition of claim 6, further comprising a cosmetically
acceptable vehicle.
8. The composition of claim 1, wherein the skin or lips has reduced
irritation and/or irritation is prevented when the composition is
applied to skin or lips.
9. The composition of claim 1, wherein the composition is an oral
composition.
10. The composition of claim 1, further comprising an effective
amount of at least one additional extract selected from the group
consisting of Azadirachta indica, Glycyrrhiza glabra linn., Morinda
citrifolia, tomato glycolipid, and any combinations thereof.
11. The composition of claim 10, wherein the at least one
additional extract is present in an amount about 0.05 wt % to about
10 wt % based on the total weight of the composition.
12. The composition of claim 11, wherein the at least one
additional extract is present in an amount about 0.5 wt % to about
5 wt % based on the total weight of the composition.
13. The composition of claim 10, wherein the at least one active
extract is topically applied to skin or lips to effect a reduction
in or to prevent irritation or inflammation.
14. The composition of claim 1, wherein the at least one active
extract is topically applied to skin or lips to effect a reduction
in or to prevent irritation or inflammation.
15. A method of lightening hair, skin, lips and/or nails,
comprising topically applying to the skin, hair, lips and/or nails
an effective amount of the composition of claim 1.
16. The method of claim 15, wherein the at least one active extract
is present in an amount about 0.001 wt % to about 20 wt % based on
the total weight of the composition.
17. The method of claim 15, wherein the at least one active extract
is present in an amount about 0.05 wt % to about 10 wt % based on
the total weight of the composition.
18. The method of claim 15, wherein the at least one active extract
is present in an amount about 0.5 wt % to about 5 wt % based on the
total weight of the composition.
19. A method of lightening hair, skin, lips and/or nails,
comprising orally ingesting an effective amount of the composition
of claim 1.
20. A method of lightening hair, skin, lips and/or nails,
comprising topically applying to the skin, hair and/or nails an
effective amount of the composition of claim 10.
21. The method of claim 20, wherein the at least one additional
extract is present in an amount about 0.05 wt % to about 10 wt %
based on the total weight of the composition.
22. The method of claim 20, wherein the at least one additional
extract is present in an amount about 0.5 wt % to about 5 wt %
based on the total weight of the composition.
23. A method of lightening hair, skin, lips and/or nails,
comprising orally ingesting an effective amount of the composition
of claim 10.
24. A method for improving the aesthetic appearance of skin, lips,
hair and/or nails comprising: topically applying to the skin, lips,
hair and/or nails an effective amount of at least one active
extract selected from the group consisting of Butea frondosa,
Naringi crenulata, Stenoloma chusana, and any combinations
thereof.
25. The method of claim 24, wherein said effective amount is
effective to provide an anti-aging benefit to the skin, lips, hair
and/or nails.
26. The method of claim 24, wherein the effective amount is from
about 0.001 wt % to about 20 wt % by weight of the composition, and
is effective in the treatment of one or more of the following: a)
decreasing/preventing lines and wrinkles; b) enhancing skin
thickness; and c) reducing skin discoloration.
27. The method of claim 24, wherein the effective amount is from
about 0.001 wt % to about 20 wt % by weight of the composition, and
is effective in the treatment of one or more of the following: a)
reducing or preventing loss of collagen; b) improving skin
firmness/plumpness; c) improving skin texture; d)
decreasing/preventing lines and wrinkles; e) improving skin tone;
f) enhancing skin thickness; g) decreasing pore size; h) reducing
skin discoloration; i) reducing acne; j) reducing psoriasis; k)
reducing skin sensitivity; and l) reducing warts.
Description
RELATED APPLICATIONS
[0001] This is a continuation-in-part application that claims
priority to, and the benefits of, co-pending U.S. patent
application Ser. No. 10/321,706, filed Dec. 17, 2002.
BACKGROUND OF THE INVENTION
[0002] 1. Field of the Invention
[0003] The present invention relates to topical compositions having
an active ingredient naturally or synthetically derived from a
plant or plant material. More particularly, the present invention
relates to topical compositions that improve the appearance of
skin, lips, hair and/or nails, especially by lightening the skin,
lips, hair, and/or nails. Most particularly, the present invention
relates to biologically active extracts for improving the aesthetic
appearance of, especially by lightening, the skin, lips, hair,
and/or nails.
[0004] 2. Description of the Related Art
[0005] Consumers constantly seek to improve the appearance of their
hair, skin, lips and nails. There is a need for products that
effectively lighten and reduce pigmentation in the hair, skin, lips
and nails. Common applications for such products include, for
example, bleaching hyperpigmented hair, skin, lips and/or nails;
reducing age spots; evening or optimizing skin discoloration;
improving the appearance of dark circles under the eyes; treating
melasma, cholasma, freckles, after-burn scars, and post-injury
hyperpigmentation; bleaching hair on the scalp, legs, face, and
other areas where bleaching and color reduction are desired; and
bleaching nail stains.
[0006] Skin, hair, lip and nail pigmentation is determined by the
level of melanin present in the epidermis, hair fiber and nail bed.
Three different types of melanin are present in the epidermis:
DHI-melanin, DHICA-melanin and pheomelanin. The different types of
melanin vary in color or shade. DHI-melanin is the darkest, and is
blackish in color. DHICA-melanin is brownish in color. Pheomelanin
is the lightest, and is reddish in color.
[0007] Melanin is synthesized in specialized organelles called
melanosomes within pigment-producing cells (melanocytes).
Melanocytes respond to stimuli to regulate melanin synthesis.
[0008] Many substances have been applied to the skin to lighten the
skin. Such substances include hydroquinone, kojic acid, licorice
and/or its derivatives, ascorbic acid and/or its derivatives,
arbutin, bearberry, Glycyrrhiza glabra and its derivatives,
Chlorella vulgaris extract, perilla extract, and coconut fruit
extract. Perilla extract is disclosed as a whitening agent in U.S.
Pat. No. 5,980,904 and Japanese Publications Nos. 07025742,
07187989, 10265322, 2001163759, and 2001181173. Coconut fruit
extract is disclosed as a whitening agent in Japanese Patent No.
2896815B2. An extract of the spongy mass of coconut tissue is
employed in a tanning sunscreen composition in U.S. Pat. No.
5,756,099.
[0009] Active ingredients derived from plants and plant seeds have
been employed in topical compositions for a myriad of medicinal,
therapeutic and cosmetic purposes. Such active ingredients can be
obtained from various parts of a plant such as seeds, needles,
leaves, roots, bark, cones, stems, rhizomes, callus cells,
protoplasts, organs and organ systems, and meristems. Such active
ingredients are incorporated in such compositions in a variety of
forms. Such forms include a pure or semi-pure component, a solid or
liquid extract or derivative, or a solid plant matter. Plant matter
may be incorporated in a variety of subforms such as whole, minced,
ground or crushed.
[0010] Extracts of Azadirachta indica, the neem tree, as well as
other plants in the family Meliaceae, are known to have
insecticidal activity. Azadirachtin, a major active ingredient of
many of these extracts, is a liminoid of the tetranortriterpenoid
type useful in commercial insecticides. Tetranortriterpenoids have
been shown to be a potent insect growth regulator and feeding
deterrent. Methods for producing azadirachtin concentrates from
neem seed materials are known in the art. U.S. Pat. No. 5,698,423
to Holowach-Keller et al. is directed to a method for producing
azadiractin by cell culture of Azadiracta indica.
[0011] Extracts of Glycyrrhiza glabra linn. are derived from the
herb, which grows perennially in subtropical and warm temperate
regions. Glycyrrhiza glabra linn., commonly known as licorice, has
been used in food sweetening. The root extract contains
glycyrrhizic acid and glycyrrhetinic acid. The glycyrrhizic acid is
known to have an anti-inflammatory effect. The extract of the
licorice root and glycyrrhetinic acid have been shown to have
desoxycorticosterone and ACTH-like effects. It has been used as a
demulcent and mild expectorant. In vitro studies have shown the
antiviral properties of both glycyrrhetinic acid and glycyrrhizin
(See Badam, "In Vitro Studies on the Effect of Glycyrrhizin from
Glycyrrhiza glabra linn. on Some RNA and DNA Viruses," Ind. J.
Pharma., 26, 194-199 (1994)). The extracts of Glycyrrhiza glabra
linn. can be extracted by a method disclosed in U.S. Pat. No.
6,248,309 to Iyer, et al.
[0012] Extracts of Morinda citrifolia are derived from the Indian
Mulberry plant. Morinda citrifolia has been used in compositions
for reducing oxysterol buildup in the blood and normalizing
cholesterol and blood pressure in mammals as set forth in U.S. Pat.
No. 6,387,370 to Yegorova. A method of extracting and purifying an
essential oil product of Morinda citrifolia is disclosed in U.S.
Pat. No. 6,417,157 to Wadsworth et al.
[0013] Extracts of tomato glycolipid are derived from tomato fruit.
Methods of extracting and synthesizing tomato glycolipids are
disclosed in U.S. Pat. No. 4,745,186 to Mudd et al.
[0014] Extracts of Butea frondosa, also known as Butea monosperma,
are derived from an East Indian deciduous tree. Butea frondosa has
been used as an astringent and in treating diarrhea, dysentery, and
pyrosis. Use of Butea frondosa for its ocular anti-inflammatory
activity has recently been tested (See Mengi, "Evaluation of Ocular
Anti-Inflammatory Activity of Butea frondosa," Ind. J. Pharma. 27,
116-119 (1995)).
[0015] Extracts of Naringi crenulata, also known as Limonia
crenulata, are derived from a small tree indigenous to East
India.
[0016] Stenoloma chusana is a perennial herb found in southeast
Asia. Extracts from this plant are known to have uses in treating
colds, influenza, bronchitis, burns, cuts, and skin sores (See A
Barefoot Doctor's Manual, Running Press, Philadelphia, Pa., p.
638).
[0017] Heretofore, these extracts have not been used as an active
ingredient in a composition for the purpose of lightening skin,
lips, hair or nails.
[0018] It would be desirable to have compositions that employ new
biological extracts that provide an improved aesthetic appearance
to the skin, lips, hair and/or nails, especially that provide
effective levels of lightening, bleaching, hypopigmenting,
whitening and/or depigmenting (hereinafter referred to individually
and collectively as "lightening" or "lighten"). It would further be
desirable to have compositions that are effective in lightening
hair, skin, lips, and/or nails and require minimal concentrations
of the biological material.
SUMMARY OF THE INVENTION
[0019] It is an object of the present invention to provide cosmetic
compositions that improve the aesthetic appearance of skin, lips,
hair and/or nails including remediating the effects of aging.
[0020] It is another object of the present invention to provide
compositions for lightening of hair, skin, lips, and/or nails
having an active plant extract, preferably an active biological
plant extract.
[0021] It is yet another object of the present invention to provide
such compositions for improving the appearance, especially by
lightening, of skin, lips, hair and/or nails in which the
compositions having an effective amount of an active plant
extract.
[0022] It is still another object of the present invention to
provide such compositions for improving the appearance, especially
by lightening, of hair, skin, lips, and/or nails, in which such
compositions are suitable for topical application to the hair,
skin, lips, and/or nails.
[0023] It is still yet another object of the present invention to
provide such compositions for improving the appearance of skin and
lips by ameliorating inflammation of the skin and/or lips,
including inflammation induced by or capable of inducement by
external agents.
[0024] It is a further object of the present invention to provide
compositions for lightening hair, skin, lips, and/or nails that is
suitable for oral ingestion.
[0025] It is a still further object of the present invention to
provide methods of lightening hair, skin, lips, and/or nails that
include topically applying such compositions to hair, skin, lips
and/or nails.
[0026] These and other objects and advantages of the present
invention are provided by compositions for improving the
appearance, especially by lightening, of hair, skin, lips, and/or
nails or by reducing, preventing, or treating inflammation of the
skin or lips, including inflammation occasioned by ailment,
affliction or disease of the skin or lips, or inflammation induced
or inducible by an external agent, in which such compositions have
an effective amount of at least one of the following active
extracts: Butea frondosa, Naringi crenulata, Stenoloma chusana, or
any combinations thereof.
[0027] There is also provided compositions for improving the
appearance, especially by lightening, of skin, lips, hair and/or
nails or by reducing, preventing, or treating inflammation of the
skin or lips, including inflammation occasioned by ailment,
affliction or disease of the skin or lips, or induced or inducible
by an external agent, in which such compositions have an effective
amount of at least one of the active extracts, and an effective
amount of at least one of the following additional extracts:
Azadirachta indica, Glycyrrhiza glabra Linn., Morinda citrifolia,
tomato glycolipid, or any combinations thereof.
[0028] The present invention also provides methods for improving
the appearance, especially by lightening, of hair, skin, lips,
and/or nails or by reducing, preventing, or treating inflammation
of the skin or lips, including inflammation occasioned by ailment,
affliction or disease of the skin or lips, or induced or inducible
by an external agent, comprising topically applying any one of the
compositions of the present invention. The present invention also
provides methods for lightening hair, skin, lips, and/or nails by
orally ingesting any one of the compositions of the present
invention.
DETAILED DESCRIPTION OF THE INVENTION
[0029] The present invention provides compositions for improving
the appearance of hair, skin, lips, and/or nails, especially by
lightening hair, skin, lips, and/or nails. The compositions are
preferably topical compositions for application to the hair, skin,
lips, and/or nails. However, the present compositions can be for
oral ingestion. In all applications, the compositions result in a
lightening of the hair, skin, lips and/or nails. The compositions
of the present invention also provide an anti-inflammatory benefit
when applied to skin or lips, so that the appearance of skin is
improved.
[0030] The compositions have one or more of the following extracts,
as an active biological plant extract or ingredient(s) or in an
active amount: Butea frondosa, Naringi crenulata, Stenoloma
chusana, or any combinations thereof. It has been unexpectedly
found that these active extracts improve the aesthetic appearance
of hair, skin, lips and/or nails and, in particular, reduce
pigmentation and lighten hair, skin, lips, and/or nails. More
particularly, these active extracts have been unexpectedly shown to
decrease melanin production and decrease hypermelanocytic
states.
[0031] It has now been also found that the addition of at least one
of these active extracts, namely Butea frondosa, Naringi crenulata,
Stenoloma chusana, or any combinations thereof, to at least one of
the following other or additional extracts, namely Azadirachta
indica, Glycyrrhiza glabra linn., Morinda citrifolia, tomato
glycolipid, or any combinations thereof, can reduce melanin
pigmentation of hair, skin, lips and/or nails.
[0032] Lightening of hair, skin, lips and/or nails, as used in the
present invention, means one or more of the following benefits is
achieved. These benefits include bleaching hyperpigmented hair,
skin, lips, and/or nails; reducing age spots; evening or optimizing
skin discoloration; improving the appearance of dark circles under
the eyes; treating melasma, cholasma, freckles, after-burn scars,
and post-injury hyperpigmentation; bleaching hair on the scalp,
legs, face, and other areas where bleaching and color reduction are
desired; and bleaching nail stains.
[0033] Most generally, the present invention also provides topical
compositions containing an effective amount of one or more of the
active ingredients of the present invention for application to the
skin to improve the aesthetic appearance of skin. These benefits
are manifest in any of the following: reduction in pore size;
improvement in skin tone, radiance, clarity and/or tautness;
promotion of anti-oxidant activity; improvement in skin firmness,
plumpness, suppleness, and/or softness; improvement in procollagen
and/or collagen production; improvement in skin texture and/or
promotion of retexturization; improvement in skin barrier repair
and/or function; improvement in appearance of skin contours;
restoration of skin luster and/or brightness; replenishment of
essential nutrients and/or constituents in the skin decreased by
aging and/or menopause; improvement in communication among skin
cells; increase in cell proliferation and/or multiplication;
increase in skin cell metabolism decreased by aging and/or
menopause; improvement in skin moisturization; promotion and/or
acceleration of cell turnover; enhancement of skin thickness;
reducing skin sensitivity; increase in skin elasticity and/or
resiliency; and enhancement of exfoliation, with or without the use
of alpha or beta hydroxy acids, keto acids or other exfoliants.
[0034] Collaterally, the present invention also provides for
topical compositions for application to the skin that provide an
anti-aging benefit. The compositions have an effective amount of
one or more active ingredients of the present invention, which,
when applied to human skin, prevent, treat and/or ameliorate the
various signs of aging at the area or portion of skin to which they
are applied. In particular, the present invention provides
compositions and methods for treating skin to prevent, inhibit,
reduce and/or ameliorate the signs of dermatological aging due to,
for example, chronological aging, hormonal aging, and/or
photoaging. Such signs of aging include, but are not limited to
skin fragility; loss of collagen and/or elastin; estrogen imbalance
in skin; skin atrophy; appearance and/or depth of lines and/or
wrinkles, including fine lines; skin discoloration, including dark
eye circles; skin sagging; skin fatigue and/or stress, e.g., skin
breakout due to environmental stress, such as pollution and/or
temperature changes; skin dryness; skin flakiness; cellular aging;
loss of skin tone, elasticity and/or luster; loss of skin firmness;
poor skin texture; loss of skin elasticity and/or resiliency; and
thin skin.
[0035] In its broadest aspects, the present invention is not
limited by any particular characterization of the physiological
and/or chemical effects of the active extract or agents. However,
the active extract used in the present compositions and methods are
believed to reduce melanin in hyperpigmented areas by decreasing
dark pigment formation in melanocytes and shifting the melanin
synthesis path towards light melanin formation by decreasing
melanocyte pH, and/or direct chelation of metals involved in
melanin synthesis or staining, for example, copper.
[0036] In another aspect of the present invention, the topically
applied compositions of the present invention inhibit, mitigate,
ameliorate, and prevent skin and lip irritation or inflammation
occasioned by ailment, illness or disease, or induced by external
factors such as environmental agents, chemical agents, medicinal
agents and cosmetic agents. Skin irritation thus may result from
exposure to wind, heat or cold, air pollutants, and cigarette
smoke. Cosmetic and pharmaceutical products may have ingredients or
combinations of ingredients that produce visible skin irritation as
a side effect. Susceptibility to skin irritation may vary from
individual to individual, and frequently limits the use of certain
products or the use of concentrations of active ingredients that
might produce more advantageous results at higher levels but for
the production of skin irritation as a side-effect. Skin irritation
symptoms or conditions include, but are not limited to, erythema,
psoriasis, edema, hyper-pigmentation, hypo-pigmentation, acne,
warts, wheeling, blotchiness, uneven skin tone, scaling, flaking,
itching or pruritus, tightness, burning, prickling, stinging,
tingling, numbing, wind irritation, temperature irritation, smoke
irritation, chemical irritation, or any combinations thereof.
Accordingly, the method of the present invention provides that an
effective amount from about 0.001 wt % to about 20 wt % by weight
of the composition, is effective in the treatment of one or more of
the following: reducing or preventing loss of collagen; improving
skin firmness/plumpness; improving skin texture;
decreasing/preventing lines and wrinkles; improving skin tone;
enhancing skin thickness; decreasing pore size; reducing skin
discoloration; reducing acne; reducing psoriasis; reducing skin
sensitivity; and reducing warts.
[0037] Cosmetic, dermatological and pharmaceutical products
commonly have an active agent or agents that produce skin
irritation. Examples of active agents having skin irritation as a
side effect include, but are not limited to, hydroxylated acids and
their derivatives, .alpha.-hydroxy acids (i.e., lactic, glycolic,
citric, malic, tartaric, mandelic, gluconic, methyl lactic, phenyl
lactic, atrolactic, glyceric, benzilic, z-hydroxyheptanoic,
z-hydroxyoctanoic and any combinations thereof), .beta.-hydroxy
acids (i.e., salicylic, 5-n-octanoylsalicylic and other derivatives
of salicylic), retinoids (retinoic acid and its derivatives;
retinol and its esters); anthralins (i.e., dioxyanthranol),
anthranoids, peroxides (i.e., benzoyl peroxide), minoxidil, lithium
salts, antimetabolites, vitamin D and its derivatives, hair dyes or
colorants (i.e., para-phenylenediamine and its derivatives;
aminophenols), alcoholic perfuming solutions (i.e., perfumes;
toilet waters; aftershaves; deodorants), antiperspirant agents
(i.e., some aluminum salts), depilatory or hair permanent active
agents (i.e., thiols), depigmentating agents (i.e., hydroquinone),
and some insecticide active agents. If topical products had
anti-irritant protection, it would be possible to increase the
amount of the normal irritant active agent (i.e., AHA or BHA) in
the product without producing unpleasant skin irritation or
irritation side effects. The use of the present compositions makes
it possible to improve the efficacy of cosmetic, dermatological or
pharmaceutical products by increasing the concentration or amount
of cosmetic, dermatological, or pharmaceutical active agent as
compared to the amount or concentration of such agent normally
used.
[0038] In a preferred embodiment of the present invention, the
composition, which improves the appearance of and, in particular,
lightens hair, skin, lips, and/or nails, has an effective amount of
at least one of the following active extracts: Butea frondosa,
Naringi crenulata, Stenoloma chusana, or any combinations thereof.
An effective amount means that the one or more active extracts are
present at about 0.001 percentage by weight (wt %) to about 20 wt %
based on the total weight of the composition. The one or more
active extracts are present preferably at about 0.05 wt % to about
10 wt %, and more preferably at about 0.5 wt % to about 5 wt %,
based on the total weight of the composition. Most preferably, the
one or more active extracts are present in an amount about 1 wt %
or less based on the total weight of the composition.
[0039] As stated above, in another preferred embodiment of the
present invention, the composition for lightening hair, skin, lips,
and/or nails has an effective amount of at least one of the active
extracts, and one or more of the following other or additional
extracts: Azadirachta indica, Glycyrrhiza glabra linn., Morinda
citrifolia, tomato glycolipid, or any combinations thereof, to
synergistically enhance the whitening activity of the
composition.
[0040] The one or more of the additional extracts are present in an
amount about 0.05 wt % to about 10 wt % based on the total weight
of the composition. Preferably, the one or more additional extracts
in an amount about 0.5 wt % to about 5 wt % based on the total
weight of the composition. Most preferably, the one or more
additional extracts are present in an amount equal to or less than
1 wt % based on the total weight of the composition.
[0041] When combined with one or more of the additional extracts,
the active extracts are present in the present compositions in an
amount about 0.001 wt % to about 10 wt %, and the one or more
additional extracts in an amount about 0.05 wt % to about 10 wt %,
based on the total weight of the composition. Preferably, the
active extracts are present in an amount about 0.05 wt % to about
10 wt %, and the one or more additional extracts in an amount about
0.5 wt % to about 5 wt % based on the total weight of the
composition. Most preferably, the one or more active extracts are
present in an amount equal to or less than about 1 wt %, and the
one or more additional extracts are present in an amount equal to
or less than 1 wt %, based on the total weight of the
composition.
[0042] The compositions of the present invention can be used with a
carrier or vehicle. The vehicle can be altered to be appropriate
for the specific use of the composition without altering the
beneficial lightening effects achieved by the use of the one or
more active extracts set forth above. The vehicles that can be used
in compositions of the present invention include, but are not
limited to, water; vegetable oils; esters such as octyl palmitate,
isopropyl myristate and isopropyl palmitate; ethers such as
dicapryl ether and dimethyl isosorbide; alcohols such as ethanol
and isopropanol; fatty alcohols such as cetyl alcohol, stearyl
alcohol and behenyl alcohol; isoparaffins such as isooctane,
isododecane and isohexadecane; silicone oils such as dimethicones
and polysiloxanes; hydrocarbon oils such as mineral oil,
petrolatum, isoeicosane and polyisobutene; polyols such as
propylene glycol, glycerin, butylene glycol, pentylene glycol and
hexylene glycol; or any combinations thereof.
[0043] Preferably, the vehicle is present in an amount about 50 wt
% to about 99.8 wt % based on the total weight of the composition.
More preferably, the vehicle is present in an amount about 80 wt %
to about 99.5 wt % based on the total weight of the
composition.
[0044] The present compositions may also include one or more of the
following ingredients: anesthetic, anti-allergenic, antifungal,
antimicrobial, anti-inflammatory agent, antioxidant, antiseptic,
chelating agent, colorant, depigmenting agent, emollient,
emulsifier, exfollient, film former, fragrance, humectant, insect
repellent, lubricant, moisturizer, pharmaceutical agent,
photostabilizing agent, preservative, skin protectant, skin
penetration enhancer, sunscreen, stabilizer, surfactant, thickener,
viscosity modifier, vitamin, or any combinations thereof.
Preferably, these ingredients are present in an amount about 0.001
wt % to about 10 wt % based on the total weight of the
composition.
[0045] The present compositions may also include skin whiteners.
Some examples of such suitable skin whiteners include, but are not
limited to, one or more of the following: ascorbyl glucoside,
vitamin C, retinol and/or its derivatives, arbutin, bearberry
extract, rumex crispus extract, milk proteins including hydrolyzed
milk proteins, N,N,S-tris(carboxymethyl)cysteamine, oleanolic
acids, perilla oils, placenta extract, saxifragia sarmentosa,
perilla extract, juniperic acid, TDPA, ligusticum chiangxiong
hort., asmunda japonica thunb., stellaria medica (L.) cyr., sedum
sarmentosum bunge, ligusticum lucidum Ait., ilex purpurea hassk,
emblica, apigenin, ascorbyl palmitol, carruba polyphenols,
hesperitin, hydroquinone, inabata polyphenol, isoliquirtigenin,
kaempherol-7-neohesperidose, L-mimosine, luteolin, oil-soluble
licorice extract P-T(40), oxa acid, phenyl isothiocyanate, cococin,
silymarin, T4CA, teterahydro curcumin, unitrienol,
ursolic-oleanolic acid, UVA/URSI, or any combinations thereof.
[0046] The compositions of the present invention can be formulated
in any suitable product form. Such product forms include, but are
not limited to, aerosol spray, cream, dispersion, emulsion, foam,
gel, liquid, lotion, mousse, ointment, patch, pomade, powder, pump
spray, solid, solution, stick, and towelette.
[0047] The present compositions provide for products, especially
cosmetic products that improve lightening of skin, nail, lips,
and/or hair. Also, the present compositions can be formulated to
deliver a consistent level of an active ingredient, or blend of
ingredients, so that a desired cosmetic effect is achieved.
[0048] The following are examples of the present invention.
EXAMPLE 1
[0049] Melanosome Uptake Assay (Stenolama Chusana and Naringi
Crenulata) was done as follows. Confluent cultures of B16
melanocytes produce moderate levels of melanosomes. However, to
induce elevated melanosome production in this cell line,
semi-confluent (60%) cultures of B16 cells were treated for
approximately thirty-six (36) hours with normal growth medium
supplemented with 10 mM ammonium chloride (final conc.). The medium
was then aspirated and the hypermelanotic cells were washed
(2.times.2 ml) with distilled water to provide a hypotonic stress
to the cells. An aliquot (2 ml) of a hypotonic lysis solution
(0.02% NP-40 in water) was added to each plate and the plates were
incubated for approximately five (5) minutes at room temperature.
Following verification of cell lysis using light microscopy, the
cellular material from three (3) culture plates were pooled in a 15
ml conical tube and centrifuged (200.times.g) for 5 minutes to
remove cellular debris. The resulting supernatant containing
melanosomes was transferred to a clean 15 ml conical tube and
centrifuged (850.times.g) for twenty (20) minutes. The resulting
pellet containing the isolated melanosomes were resuspended in 1 ml
of Phosphate Buffered Saline (PBS) and stored at 4.degree. C. until
used.
[0050] The treatment of keratinocytes with melanosomes was measured
as follows. The normal human epidermal keratinocytes (NHEKs)
(available from Clonetics, Inc.) were plated in the wells of
24-well plates at a density of 200,000 cells/well. Approximately
twenty-four (24) hours later, the growth medium was replaced with 1
ml of the appropriate growth medium (i.e., DMEM/KGM-2) containing
the melanosome preparation with or without additional treatment
conditions. The cells were treated with different concentrations of
perilla leaf extract (powder form or aqueous form). The cells were
then returned to the incubator for approximately one and one-half
(1.5) hours. For these studies, each well of keratinocytes was
treated with the amount of melanosomes isolated from a single plate
of B16 cells.
[0051] In some experiments, the 24-well plates of treated
keratinocytes were centrifuged for 15 minutes at 1,000 rpm to
facilitate the deposition of the melanosomes onto the surface
membranes of the keratinocytes. The plates were then returned to
the incubator for 1.25 hours.
[0052] For the analysis of melanosome uptake, the cells in each
well of keratinocytes were rinsed (3.times.1 ml) with PBS, removed
from the plate using trypsin/EDTA, and washed with PBS. To analyze
the uptake of melanosomes by the keratinocytes, the internalized
melanin was extracted from the cells according to a modified method
of Bessou-Touya, S., et al. (Chimeric human epidermal reconstructs
to study the role of melanocytes and keratinocytes in pigmentation
and photoprotection. J. Invest. Dermatol., 111:1103-1108, 1998) and
quantified spectrophoto-metrically by determining the
melanin-specific absorbance at 405 nm.
[0053] The melanocytes synthesize melanin and deposits onto
melanosomes. Visual manifestation of skin color is due to presence
of melanin/melanosomes in keratinocytes. Melanosomes are taken up
by keratinocytes and the rate of uptake, retention and processing
of melanosomes in the keratinocytes is a key determinant of skin
color. The internalized melanin value reflects the amount of
melanin/melanosome uptake and retention by the keratinocytes. Thus,
the lower internalized melanin values, particularly internalized
melanin values that are less than the control with melanin,
indicate that melanin uptake by the keratinocytes has been
inhibited.
[0054] The results are as follows. At 0.5% volume/volume, Stenolama
Chusana showed a 44% decrease in melanosome uptake as compared to
the positive control. At 0.5% volume/volume, Naringi Crenulata
showed a 39% decrease in melanosome uptake as compared to the
positive control.
EXAMPLE 2
[0055] For B16 assay (Naringi Crenulata), the actives were tested
in monolayer cell culture of B16 mouse melanoma cells. These cells
constitutively produce melanin and are a model system for
monitoring the inhibition of melanin synthesis. The cells were
seeded into 96-well plates at 5.times.10.sup.3 cells/well and
culture attached for twenty-four (24) hours. The media were then
replaced with fresh media containing plant extracts. Each active
was applied to six (6) wells of B16 cells on 96-well plates to
allow statistical analysis. The cells were dosed with medium alone
as the negative control, or the test article for seven (7) days.
The plates were read at 540 nM to detect melanin formation. An
increase in absorbance at 540 nM reflects a higher melanin content
in the well.
[0056] At 0.05% weight/volume, Naringi Crenulata showed a 61%
decrease in pigmentation as compared to the positive control
EXAMPLE 3
[0057] For .sup.14C-Dopa incorporation (Butea Frondosa),
melanogenic activity was measured by measuring the radioactive
melanin formed as .sup.14C DOPA is converted to the acid insoluble
melanin biopolymer in B16F10 melanoma cells. Cells were seeded into
24-well plates at a density of 2.times.10.sup.4 cells per well and
cultured attached for forty-eight (48) hours. The media were then
replaced with fresh media containing plant extracts and 0.2 .mu.Ci
of .sup.14C DOPA. The cells were further incubated for 24 hours.
After incubation, media were discarded and the cells were rinsed
with PBS, lysed by adding 0.125 ml of 1N NaOH and incubated at
37.degree. C. for 30 minutes, and then neutralized with 0.025 ml of
5N HCL. The resulting cell lysates were transferred into liquid
scintillation vials and mixed with scintillation cocktail, and the
radioactivity was determined by scintillation counter. A portion of
the cell lysates was kept and the protein content was determined by
Lowry method. The results were normalized to the amount of protein
determined for each assay.
[0058] At 0.005% weight/volume, Butea frondosa showed a 22%
decrease in .sup.14C DOPA conversion as compared to the positive
control.
EXAMPLE 4
[0059] Various natural plant extracts of the present invention were
evaluated for inhibition of the TNF-alpha protein in an in vitro
studies as described below.
TNF-alpha Inhibition Protocol
[0060] To test the efficacy of Stenolama chusana Ching., Naringi
Crenulata, and Butea frondosa Roxb. for the inhibition of TNF-alpha
production, an enzyme linked immunoassay (ELISA) commercially
available from R&D Systems was employed.
[0061] This assay employed the quantitative sandwich enzyme
immunoassay technique in which a monoclonal antibody specific for
TNF-alpha has been pre-coated onto a microtiter plate. Culture
supernatants from cells exposed to active materials were pipetted
into separate wells. TNF-alpha in the supernatant was bound to the
plate via the immobilized antibody. After several washes to remove
unbound antibody, an enzyme-linked polyclonal antibody specific for
TNF-alpha was added to each well. Following a wash to remove
unbound antibody-enzyme reagent, a substrate solution was added to
the wells. Color develops in proportion to the amount of TNF-alpha
bound in the initial step. The results of the tests are provided in
Table I. TABLE-US-00001 TABLE I Results of In Vitro Tests TNF-alpha
Plant Extract Inhibition Stenolama chusana Ching. +++ Naringi
Crenulata + Butea frondosa Roxb. +++ Legend: +, ++, +++, ++++
Significant inhibition (degree of inhibition quantified by number
of plus signs) (0) No change
[0062] These in vitro studies show that the compositions of the
present invention containing an extract of: Stenolama chusana
Ching., Naringi Crenulata, and Butea frondosa Roxb. provide
benefits to the skin by inhibiting TNF-alpha protein production,
whereby the signs of subjective discomfort and/or irritation caused
by cosmetic, pharmaceutical or dermatological products would be
reduced, thus providing an aesthetic improvement in skin
appearance.
EXAMPLE 5
[0063] Stenolama chusana ching. and Butea fondosa were evaluated in
various biopsy studies in which the natural plant extract as set
forth below was incorporated into a cosmetically suitable vehicle
and applied to the volar forearm of a participant in the study, at
a dose of 2 mg/cm.sup.2. The forearm area to which the extract
preparation was applied was then covered with a semi-occlusive
patch. This procedure was repeated for 3 weeks, 5 days per week. At
the end of the treatment the sites were anesthetized with lidocaine
and 2 mm punch biopsies were taken from the treated and one
untreated control site. Biopsies were fixed in formalin, embedded
in paraffin, sectioned, and stained for relevant endpoints.
[0064] For Stenolama chusana ching., 6 of 9 panelists showed
increase in keratinocyte proliferation (visualized by the antibody
to KI67), and 5 of 9 panelists showed increase in viable epidermal
thickness.
[0065] For Butea frondosa provided, 5 of 8 panelists showed
increase in keratinocyte proliferation (visualized by the antibody
to KI67), and 5 of 8 panelists showed increase in viable epidermal
thickness.
[0066] It should be understood that the foregoing description is
only illustrative of the present invention. Various alternatives
and modifications can be devised by those skilled in the art
without departing from the invention. Accordingly, the present
invention is intended to embrace all such alternatives,
modifications and variances which fall within the scope of the
appended claims.
* * * * *