Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Silicon containing doai
Patent
1986-12-15
1989-05-02
Schenkman, Leonard
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Silicon containing doai
514725, A61K 3107, A61K 31695
Patent
active
048268283
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
(a) Field of the Invention
This invention relates to stable compositions containing retinol which upon topical application to the skin cause wrinkle effacement and other beneficial effects. It also relates to use of such compositions in combination with or including moisturizers.
(b) State of the Art
Retinol (Vitamin A), though believed to cause beneficial skin effects, has never been successfully formulated in a composition suitable for topical application. It has now been discovered that retinol can be formulated in stable form and can be administered topically in a cosmetic base with minimal irritant side effects. Further, when topically applied as taught by the invention, retinol causes effacement of facial fine lines and wrinkles, increases skin elasticity, reduces pore size and improves skin texture.
SUMMARY OF THE INVENTION
This invention relates to stable cosmetic compositions for reducing facial lines and wrinkles and otherwise enhancing skin quality and to methods of using that composition. The compositions comprise retinol coupled with a volatile silicone carrier by means of a mutual solvent. The preferred composition, which result in optimum stability and efficacy, are those containing volatile silicones, such as cyclomethicone, ethanol as the mutual solvent and retinol. When applied to the skin, the compositions contain 0.005 to 1.0 weight percent retinol. Most preferred compositions for application to the skin contain 0.01 to 0.50 weight percent retinol. The stable compositions of the invention may be formulated with more concentrated levels of retinol and may be diluted to suitable levels of retinol for application to the skin by means of cosmetically acceptable carriers. The compositions may additionally contain or may be applied in conjunction with a moisturizer to enhance the beneficial effects and sensory comfort of the composition.
DETAILED DESCRIPTION OF THE INVENTION
It has been discovered that a cosmetic composition containing retinol in a volatile silicone vehicle is stable, and upon topical application reduces fine lines and wrinkles and otherwise beneficially affects skin quality. More particularly, it has been discovered that a stable retinol composition can be formulated using a volatile silicone carrier and a mutual solvent for the silicone and retinol. Compositions containing 0.005 to 1.0 weight percent retinol can reduce facial fine lines and wrinkles with minimal irritant effects.
The stable retinol compositions of the invention are formulated in a vehicle containing a volatile silicone.
With such a vehicle, retinol levels needed to achieve beneficial effects are minimized and the potential for irritant effects to the skin by retinol are greatly diminished. Moreover, retinol is stable when formulated in the silicone containing compositions of the invention, in contrast to other conventional cosmetic carriers.
The compositions of the invention may be formulated as alcohol lotions containing 0.005 to 1.0 weight percent retinol, in which case they may be applied directly to the skin, or as more concentrated alcohol lotions containing higher levels of retinol, in which case prior to application they are diluted by means of a cosmetically acceptable carrier to a 0.005 to 1.0 weight percent retinol level. In the formulations of the invention, water is optimally minimized or eliminated to maximize the stability of retinol and to minimize the potential for separation of the oil and water. No more than 2 percent water should be present.
When the compositions of the invention are formulated for application as alcohol lotions, a preferred mutual solvent for the volatile silicone and the retinol is ethanol. Preferred silicones are volatile low viscosity polysiloxanes, such as cyclomethicones, including cyclomethicone tetramer and pentamer. In the alcohol lotion formulation, the retinol level is most preferably 0.10 to 0.50 weight percent. The weight ratio of silicone to mutual solvent is optimally about 6:4.5 when cyclomethicone tetramer is the silicon
REFERENCES:
patent: 4224319 (1980-09-01), Marcadet
patent: 4423041 (1983-12-01), Clum et al.
patent: 4425364 (1984-01-01), Vanlerberghe et al.
Kligman et al, J. of Invest. Derm., 73, 354-358, 1979.
Wilmott James M.
Znaiden Alexander P.
Avon Products Inc.
Bender S. Michael
Schenkman Leonard
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