Cosmetic compositions containing mulberry extract and retinoids

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Conjugate or complex

Reexamination Certificate

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C424S060000, C424S401000

Reexamination Certificate

active

06261566

ABSTRACT:

FIELD OF THE INVENTION
Cosmetic compositions containing mulberry extract in combination with retinoids and methods of conditioning skin by applying such compositions to the skin.
BACKGROUND OF THE INVENTION
Retinol (vitamin A) is an endogenous compound which occurs naturally in the human body and is essential for normal epithelial cell differentiation. Natural and synthetic vitamin A derivatives have been used extensively in the treatment of a variety of skin disorders and as skin repair and renewal agents. Retinoic acid has been used to treat a variety of skin conditions such as acne, wrinkles, psoriasis, age spots and skin discoloration.
Within the cells, retinol and retinoic acid are bound to specific cellular binding proteins, 2 of the major proteins are CRABP-1 and 2 (Roos et al., Pharmacological reviews: 50, 315-333, 1998). These proteins act in regulating the intracellular concentration of retinoids by acting as both storage or shuttle proteins in retinoid metabolism. The levels of this protein are regulated by the amount of retinoic acid within the cells. Higher cellular levels of retinoids increase the expression of CRABP-2. Therefore, the amount of this protein in the cells, is a measure of the retinoid activity of the cells. Skin cells contain CRABP-2 both in the epidermis and the dermis. CRABP-2 response to retinoid administration in fibroblasts in vitro is used as a reproducible measure of retinoid bioactivity that predict human skin responses (Elder et al., J. Invest. Dermatol., 106: 517-521, 1996). Therefore, CRABP-2 expression of fibroblasts is a measure of retinoid activity leading to various cosmetic skin benefits (antiaging, anti wrinkling, skin conditioning etc.).
Cosmetic compositions containing mulberry and retinoids have been disclosed. See for instance EP 815838 (Shiseido), EP887070 (Kibun Food Chemifa Co.), U.S. Pat. Nos. 5,676,948, 5,676,949, and 5,607,692. U.S. Pat. No. 5,332,575 discloses a method of targeting melanocytes with a compound containing a fucose residue to bind the product to the melanocyte membrane. A cosmetic composition is exemplified containing dry mulberry root bark extract at 0.5% level. In another example, beta carotene or 0.25% vitamin A propionate is employed.
The present invention is based in part on the discovery that mulberry extract in combination with selected retinoids exhibit synergy, when combined within a specific ratio range.
SUMMARY OF THE INVENTION
The present invention includes a cosmetic skin care composition comprising:
(i) a glycolic extract of mulberry root in an amount of from 0.00001 to 10 wt. %,
(ii) a retinoid selected from the group consisting of retinyl acetate, retinyl palmitate and retinyl linoleate, and
(iii) a cosmetically acceptable vehicle,
wherein the weight ratio of retinyl acetate to the mulberry extract is in the range of from 1:80 to 120:1,
the weight ratio of retinyl linoleate to the mulberry extract is in the range of from 1:8 to 120:1, and
the weight ratio of retinyl palmitate to the mulberry extract is in the range of from 1:16 to 6:1.
The present invention also includes a method of improving or preventing the condition of wrinkled, lined, dry, flaky, aged or photodamaged skin and improving skin thickness, elasticity, flexibility, radiance, glow and plumpness, which method includes applying to the skin the inventive composition. Compositions of the invention are intended for topical application to mammalian skin which is already dry, flaky, lined, wrinkled, aged, photodamaged, or the inventive compositions may be applied prophylactically to reduce the deteriorative changes.
DETAILED DESCRIPTION OF THE INVENTION
Except in the examples, or where otherwise explicitly indicated, all numbers in this description indicating amounts of material or conditions of reaction, physical properties of materials and/or use are to be understood as modified by the word “about.” All amounts are by weight of the composition, unless otherwise specified.
The mulberry extract suitable for use in the present invention is a glycolic extract from the root of white mulberry. White mulberry is also known as
Morus alba.
The extract may be obtained from Bioland (South Korea).
In general, the amount of the mulberry extract in the inventive compositions is in the range of from 0.001% to 20% by weight composition. Preferably in order to lower cost and maximize the effect the amount of the mulberry extract is in the range of from 0.01 to 10% and most preferably is in the range of from 0.1% to 5%.
The inventive compositions further comprise a retinoid selected from the group consisting of retinyl acetate, retinyl plamitate and retinyl linoleate. It has been found that these retinoids, act synergistically with the mulberry extract, when the reinoid and the mulberry extract are combined in a specific weight ratio: the weight ratio of retinyl acetate to the mulberry extract is in the range of from 1:80 to 120:1, preferably from 1:8 to 12:1, most preferably from 1:8 to 1.2:1; the weight ratio of retinyl linoleate to the mulberry extract is in the range of from 1:8 to 120:1, preferably from 1:8 to 12:1, most preferably from 1:8 to 1.2:1 of and the weight ratio of retinyl palmitate to the mulberry extract is in the range of from 1:16 to 6:1, preferably from 1:8 to 8:1, most preferably from 1:8to 1.2:1.
The composition according to the invention also comprises a cosmetically acceptable vehicle to act as a diluant, dispersant or carrier for the mulberry extract and the retinoid in the composition, so as to facilitate their distribution when the composition is applied to the skin.
Vehicles other than or in addition to water can include liquid or solid emollients, solvents, humectants, thickeners and powders. An especially preferred nonaqueous carrier is a polydimethyl siloxane and/or a polydimethyl phenyl siloxane. Silicones of this invention may be those with viscosities ranging anywhere from about 10 to 10,000,000 mm
2
/s(centistokes) at 25° C. Especially desirable are mixtures of low and high viscosity silicones. These silicones are available from the General Electric Company under trademarks Vicasil, SE and SF and from the Dow Corning Company under the 200 and 550 Series. Amounts of silicone which can be utilized in the compositions of this invention range anywhere from 5% to 95%, preferably from 25% to 90% by weight of the composition.
The cosmetically acceptable vehicle will usually form from 5% to 99.9%, preferably from 25% to 80% by weight of the composition, and can, in the absence of other cosmetic adjuncts, form the balance of the composition. Preferably, the vehicle is at least 80 wt. % water, by weight of the vehicle. Preferably, water comprises at least 50 wt. % of the inventive composition, most preferably from 60 to 80 wt. %, by weight of the composition.
Optional Skin Benefit Materials and Cosmetic Adjuncts
An oil or oily material may be present, together with an emulsifier to provide either a water-in-oil emulsion or an oil-in-water emulsion, depending largely on the average hydrophilic-lipophilic balance (HLB) of the emulsifier employed.
The inventive compositions preferably include sunscreens. Sunscreens include those materials commonly employed to block ultraviolet light. Illustrative compounds are the derivatives of PABA, cinnamate and salicylate. For example, octyl methoxycinnamate and 2-hydroxy-4-methoxy benzophenone (also known as oxybenzone) can be used. Octyl methoxycinnamate and 2-hydroxy4-methoxy benzophenone are commercially available under the trademarks, Parsol MCX and Benzophenone-3, respectively. The exact amount of sunscreen employed in the emulsions can vary depending upon the degree of protection desired from the sun's UV radiation.
Emollients are often incorporated into cosmetic compositions of the present invention. Levels of such emollients may range from 0.5% to 50%, preferably between 5% and 30% by weight of the total composition. Emollients may be classified under such general chemical categories as esters, fatty acids and alcohols, polyols and hydrocarbons.
Esters may be mono- or di-e

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