Product for topical application containing a lipase and a...

Drug – bio-affecting and body treating compositions – Enzyme or coenzyme containing – Hydrolases

Reexamination Certificate

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C514S159000, C514S543000, C514S546000, C514S547000

Reexamination Certificate

active

06488928

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention concerns a product for topical application which is capable of releasing a hydroxy acid on the skin, and the use thereof in imparting softness to the skin, including the scalp. The present invention also concerns a process for the cosmetic and/or dermatological treatment of the skin, particularly for the treatment of acne, wrinkles and fine lines, and the use of the present product therein.
2. Discussion of the Background
Hydroxy acids are increasingly used in the cosmetics or dermatological fields for caring for the face and/or the body, and more especially, for giving the face a luminous and radiant complexion, and therefore a healthy, smooth and younger appearance, and for causing the disappearance of blackheads due to acne.
Unfortunately, hydroxy acid compounds are generally provided in compositions having a pH of less than or equal to 4, for the purpose of maintaining the activity of these acids. The application of these compositions to the skin has the major disadvantage of causing stinging, itching and stabbing pains, which can produce great discomfort. The use of these acidic compositions for users with sensitive skin is therefore often out of the question.
There thus remains the need for a cosmetic and/or dermatological product containing hydroxy acid compounds which confers, in particular on the skin, a healthy appearance and rejuvenation, and which is capable of treating acne, wrinkles and fine lines, while minimizing or eliminating the risk of user discomfort.
SUMMARY OF THE INVENTION
Accordingly, one object of the present invention is to provide a novel composition which provides hydroxy acid compounds in an active form, but which reduces or eliminates the risk of discomfort associated with conventional hydroxy acid-containing compositions.
A further object of the present invention is to provide a novel method for administering hydroxy acid compounds to the skin of persons in need thereof, which reduces or eliminates the risk of discomfort which accompanies conventional hydroxy acid-containing compositions.
A further object of the present invention is to provide a novel composition and method for providing hydroxy acid compounds to persons having sensitive skin.
A further object of the present invention is to provide a novel composition and method for treating acne, which reduces or eliminates the risk of discomfort caused by conventional hydroxy acid-containing compositions.
These and other objects of the present invention, which will be readily understood in the context of the following detailed description of the preferred embodiments, have been provided by a composition for topical application, comprising
(a) a lipase, and
(b) an ester of a hydroxy acid compound, in which the ester functional group contains a saturated or unsaturated, linear or branched carbon chain having from 2 to 25 carbon atoms, which may be substituted.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
The present Inventors have unexpectedly found that the use of a specific enzyme, lipase, in combination with esters of hydroxy acids, progressively releases hydroxy acid compounds on the skin, and thus, overcomes the aggressive nature of the hydroxy acids and consequently avoids the disadvantages of conventional hydroxy acid-containing cosmetic and/or dermatological compositions.
Consequently, the present invention concerns a product for topical application, comprising a lipase and an ester having a saturated or unsaturated, linear or branched chain of from 2 to 25 carbon atoms.
In the context of the present application, “product” refers to both cosmetic and dermatological compositions, as well as commercial devices comprising a container in which the enzyme and precursor components are housed in isolation from one another.
The present hydroxy acid ester/lipase combination makes it possible to control the release of the hydroxy acid, and therefore reduce the risk of discomfort. The present composition also makes formulation easy as a result of improved compatibility of the esters with the media commonly used in the cosmetic and dermatological fields. In particular, the present product can be used without disadvantage or discomfort by people having sensitive skin, in particular because the composition may be formulated at a pH in the region of 6 (e.g., the present composition or a component in the present product may be formulated at a pH of from 5 to 8, preferably from 5.5 to 7.5, and more preferably, from 5.7 to 7.0).
Lipase is an enzyme which hydrolyses triglycerides to diglycerides, monoglycerides, glycerol and/or free fatty acids. It is used in particular in detergents (see the article “Lipases as detergent components”, H. Andree et al.,
Journal of Applied Biochemistry,
1980, vol. 2, pages 218 to 229) to remove greasy stains such as those arising from frying fats, oils, sebum or greasy cosmetics such as lipsticks. Due to its ability to hydrolyze triglycerides, it has been used in the cosmetics field in the immobilized form for cleaning the skin (see, for example, U.S. Pat. No. 4,556,554).
The lipase used in the present invention should be sufficiently stable to retain its enzymatic activity. Preferably, the lipase used in the present invention belongs to the group of enzymes of EC 3.1.1.3. classification, which corresponds to a lipase which hydrolyses the ester bonds at the 1- and 3-positions of a triglyceride. It can be chosen, for example, from those sold under the tradenames “LIPASE SP644” and “LIPOLASE 100 L” by the company Novo Nordisk.
The lipase may be included in the present product in an amount of from 0.05% to 30% by weight, preferably from 0.1 to 10% by weight, and more preferably from 0.1 to 5% by weight with respect to the total weight of the composition (e.g., the combination of lipase, ester, cosmetically and/or dermatologically acceptable medium or carrier, additives, adjuvants, etc., not including the weight of any container or packaging in which the composition is contained).
The hydroxy acids to which the present invention applies may be &agr;-hydroxy acids or &bgr;-hydroxy acids; may have a linear, branched or cyclic carbon framework; and may be saturated or unsaturated. Hydrogen atoms in the carbon chain of the hydroxy acid can, in addition, be substituted by halogens or halogenated alkyl, acyl (preferably alkylcarbonyl), acyloxy (preferably alkylcarbonyloxy), alkoxycarbonyl or alkoxy radicals, each of which may have from 2 to 18 carbon atoms. Preferably, the term “acyl” refers to a group of the formula —C(═O)—R, where R is an alkyl group having from 1 to 24 carbon atoms or an alkenyl or alkynyl group having from 2 to 24 carbon atoms which may contain one or more sites of ethylenic unsaturation and which may be substituted.
The hydroxy acids which are the most widely used in cosmetics are, in particular, glycolic, lactic, malic, tartaric, citric, 2-hydroxyalkanoic, mandelic and salicylic acids, and their C
1
- to C
22
-alkylated derivatives, such as 5-(n-octanoyl)salicylic acid, 5-(n-dodecanoyl)salicylic acid or 2-hydroxy-3-methyl-benzoic acid. Alternatively, C
1
- to C
22
-alkoxylated derivatives, such as 2-hydroxy-3-methoxybenzoic acid, may be used. Any of these hydroxy acids or derivatives are suitable in the present invention.
The ester used in the present invention is an ester containing one or more ester functional groups having a saturated or unsaturated, linear or branched chain of from 2 to 25 carbon atoms and optionally containing one or more substituents. The ester functional group is preferably one of the formula —O—C(═O)—R (i.e., an ester of the hydroxyl functional group of a hydroxy acid) or a group of the formula —C(═O)—O—R (i.e., an ester of the carboxyl functional group of a hydroxy acid), in which R is as described above.
The carbon chain of the ester functional group is chosen in particular from acyl (preferably as described above), benzoyl, alkylbenzoyl, acylbenzoyl and 2-hydroxyphenylacetyl radicals, which are optionally substituted. The substituent can be, in p

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