Skin treatment using a new retinoid

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Cosmetic – antiperspirant – dentifrice

Reexamination Certificate

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C424S059000, C424S060000, C424S400000, C514S063000, C514S725000

Reexamination Certificate

active

06641824

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to the use of a novel retinoid, particularly a retinol derivative. More particularly, the present invention relates to the use of topical compositions having the retinol derivative, retinoxytrimethylsilane, to treat, including prevent, ameliorate and/or reduce, signs of dermatological aging, especially wrinkles, and/or improve the aesthetic appearance of skin. Still more particularly, the present invention provides the beneficial effects of retinol without causing skin irritation from daily use.
2. Description of the Prior Art
Retinoid or retinoid compounds/derivatives (collectively referred to herein as “retinoid” or “retinoids”) are vitamin A derivatives. They are used in topical compositions to treat a variety of adverse skin conditions. Such skin conditions include acne, actinic damage, dandruff, eczema, fine lines, psoriasis, warts and wrinkles.
Retinoids used in the prior art include, but are not limited to, isotretinoin, retinal, retinol, retinoic acid, retinyl acetate, retinyl palmitate, retinyl propionate, synthetic retinoid mimics, and tretinoin. As is known in the art, the amount of retinoid in a topical composition varies depending on the condition to be treated, as well as on the composition and the retinoids themselves. Representative compositions having a retinoid are discussed, by way of example, in U.S. Pat. Nos. 3,006,939; 3,060,229; 3,932,665; 4,826,828; and 4,934,114.
However, topical compositions having a retinoid have been limited in the amount of retinoid, since retinoid has been found to irritate the skin. Such irritation is acute, especially when the amount of retinoid in the composition is high. However, some consumers with sensitive skin cannot even tolerate a small amount of retinoid.
The irritation can manifest itself in the form of physical discomfort and/or unaesthetic skin appearance. Such an unaesthetic skin appearance can manifest itself by dermatitis or erythema. The irritation may disturb the user to such an extent that the user will discontinue use of the composition having a retinoid. Alternately, the user may reduce the frequency of use, thereby possibly reducing the effectiveness of the composition for its intended purpose.
Heretofore, there has not been an efficacious skin care composition that contains a retinoid, but without the irritation induced by a retinoid. Historically, it has been observed that retinoid-induced skin irritation has a direct correlation to retinoid efficacy. Namely, the greater the concentration of retinol, the more likely that irritation will occur. Thus, simply reducing the retinoid concentration might decrease irritation to the skin, but it would also reduce the desired retinoid efficacy. Consumers require, and would benefit from, a retinol-delivering composition that is both well-tolerated and efficacious. The present composition having the retinoid, retinoxytrimethylsilane, achieves this need.
SUMMARY OF THE INVENTION
It is an object of the present invention to provide a topical composition having retinoxytrimethylsilane to treat, including prevent, ameliorate and/or reduce, signs of dermatological aging, especially wrinkles, and/or improve the aesthetic appearance of skin, and methods of its use.
It is another object to provide such a topical composition that is substantially anhydrous.
It is a further object of the present invention to provide a method for delivering the benefits of retinol without inducing irritation.
These and other objects and advantages of the present invention are achieved by a topical composition that has retinoxytrimethylsilane in an effective amount, preferably about 0.1 weight percent (wt %) to about 50 wt % of the total weight of the composition.
DETAILED DESCRIPTION OF THE INVENTION
The present invention relates to the surprising recognition that retinoxytrimethylsilane, a retinol derivative, delivers retinoid efficacy without skin irritation, dryness or erythema typically caused by the topical use of a retinoid. Further, it has also been discovered in the present invention that moisture-activated, retinol-delivering compositions having retinoxytrimethylsilane will treat, including prevent, ameliorate, and/or reduce, signs of dermatological aging, especially wrinkling and/or improve the aesthetic appearance of the skin upon daily application to skin. The composition is preferably applied topically once or twice daily. The daily application can be for periods up to two weeks, four weeks or more.
The present compositions preferably have an amount of retinoxytrimethylsilane from about 0.1 wt % to about 50 wt %, based on the total weight of the composition. More preferably, the present compositions have retinoxytrimethylsilane in an amount from about 0.5 wt % to about 15 wt %. Most preferably, the present compositions have retinoxytrimethylsilane in an amount from about 0.5 wt % to about 5 wt % of the total composition. To provide guidance to those skilled in the art for practicing the present invention, the efficacy of the retinol-derivative concentration in a topical composition is approximately equivalent to 10
−1
concentration of retinol percent by weight of the composition. For example, to provide the efficacy of about 0.1 wt % (based upon the total weight of the composition) retinol activity, a composition of the present invention preferably includes about 1 wt % of retinoxytrimethylsilane.
In addition to improvements in skin care benefits of the present invention, the retinol-derivative, retinoxytrimethylsilane, results in more stable compositions than those of the prior art. This is evidenced by a lasting white color of the present compositions, without the manifestation of yellowing over time, particularly in a stick product form. The present compositions can also be in other cosmetic product forms, such as, for example, an emulsion, a gel, a lip balm, a lip gloss, a lotion, a mask, an ointment, a patch, a pomade, a solution, a spray, or a towelete.
The present compositions are preferably wax-based, oil-based, or silicone-based compositions, all of which are substantially anhydrous (i.e., contain less than about 1 wt %, more preferably no, water). Alternatively, the compositions may include greater than 1 wt % water as long as contact between the retinoxytrimethylsilane and water is prevented. For example, a two-phase product that is dispensed in a dual-chamber package with each phase in a separate chamber may include an aqueous phase in one chamber and the retinoxytrimethylsilane in substantially anhydrous phase in the other chamber. As the contents from each chamber are dispensed, the phases may combine either via the dispensing mechanism, as is known in the art, or mixed by the user as the user rubs the two phases onto and into the skin.
In a preferred embodiment of the present invention, the retinoxytrimethylsilane used is in soybean oil and is commercially available from Clariant Corp. under the tradename SilCare 1 M 75. The Clariant product is a 12% chemically reactive liquid derivative of retinol, which is readily dispersible in most substantially anhydrous organic cosmetic formulations at room temperature.
The compositions of the present invention yield improvements to the aesthetic appearance of the skin by treating, including preventing, ameliorating and/or reducing at least one of the following: dermatological aging, especially chronological, actinic or hormonal aging, skin fragility, loss of collagen and/or elastin, skin atrophy, skin dryness, skin flakiness, skin discoloration, skin sagging, signs of skin fatigue and/or stress, acne, psoriasis, eczema, and warts. In particular, improvements to the aesthetic appearance of skin include at least one of the following: makes facial lines appear less noticeable, makes facial lines and/or wrinkles feel plumped, improves appearance of suborbital lines and/or periorbital lines, improves appearance of crow's feet, reduces and/or diminishes the appearance of wrinkles, particularly facial wrinkles on the cheeks, forehead and/or

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