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United States Patent (19) 11 Patent Number: 5,855,897 Pelle (45) Date of Patent: Jan

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United States Patent (19) 11 Patent Number: 5,855,897 Pelle (45) Date of Patent: Jan USOO5855897A United States Patent (19) 11 Patent Number: 5,855,897 Pelle (45) Date of Patent: Jan. 5, 1999 54 TOPICAL COMPOSITION AND METHOD OTHER PUBLICATIONS FOR ENHANCING LIPID BARRIER SYNTHESIS Miller et al., Kahweol and Cafestol: Inhibitors of Hamster Buccal Pouch Carcinogenesis, Nutrition and Cancer 15: 75 Inventor: Edward Pelle, Valley Stream, N.Y. 41–46, 1991. Hugget et al., Chemoprotective Effects of Coffee and its 73 Assignee: E-L Management Corp., New York, Components Cafestol and Kahweol: Effects Xenobiotic N.Y. Metabolizing Enzymes, Colloq. Sci. Int. Cafe (C.R.) 16(1): 65–72, 1995. 21 Appl. No.:712,988 Urgert et al., Effects of Cafestol and Kahweol from Coffee Grounds on Serum Lipids and Serum Liver Enzymes in 22 Filed: Sep. 13, 1996 Humans, Am. J. Clin. Nutr. 61: 149-154, 1995. (51) Int. Cl. ................................................. A61K 9/08 Melnick et al., J. Invest. Dermoatol 92:231–234, 1989. 52 U.S. Cl. .............................. 424/401; 424/59; 424/63; 424/400; 514/174; 514/461 Primary Examiner Neil S. Levy 58 Field of Search ..................................... 424/400, 401, Attorney, Agent, Or Firm-Karen A. Lowney, Esq. 424/59, 63; 514/169-171, 172, 174, 182, 57 ABSTRACT 469, 461 The present invention relates to topical compositions useful 56) References Cited in enhancing lipid synthesis in Skin comprising an effective amount of cafestol, in combination with a pharmaceutically U.S. PATENT DOCUMENTS or cosmetically acceptable carrier. Such compositions are 4,793,990 12/1988 Grollier et al. ........................... 424/59 useful in treatment or prevention of dry skin and conditions in which the skin's lipid barrier is defective or damaged. FOREIGN PATENT DOCUMENTS 1770352 10/1992 Russian Federation. 14 Claims, 6 Drawing Sheets 90 8O 70 60 > 50 cd s is 40 as s 30 2O 10 O CONTROL - O TME (DAYS) U.S. Patent Jan. 5, 1999 Sheet 1 of 6 5,855,897 U.S. Patent 5,855,897 U.S. Patent Jan. 5, 1999 Sheet 3 of 6 5,855,897 a 22 2 Z2 TI 2 2 2 3 i O O O U.S. Patent Jan. 5, 1999 Sheet 4 of 6 5,855,897 O Lid O LC) Co Lad O Ad O H9NGS W9 NSW30N U.S. Patent 5,855,897 1.I.T.T.T.T.T.T. W. T% to t es wale . 3 So 8O O. SO. SO. &O. S.O. O. O. N9W Dep U.S. Patent Jan. 5, 1999 Sheet 6 of 6 5,855,897 T % %H2 a E N On S. s O 2ŽS O 2 d O 4 2 al - 2. 2 d L?o o LO Co LO Co Ltd CN A9W Dep 5,855,897 1 2 TOPCAL COMPOSITION AND METHOD occurring Stratum corneum lipid components, as well as FOR ENHANCING LIPID BARRIER increasing the Stratum corneum per se. There is thus pro SYNTHESIS Vided a new type of cosmetic or pharmaceutical composition which functions by enhancing the Skin's own functions, FIELD OF THE INVENTION resulting in a more natural means of preventing dry skin and The present invention relates to topically applied compo other undesirable results of a deficient lipid barrier. Sitions which increase lipid Synthesis in skin. More Specifically, the invention relates to compositions compris BRIEF DESCRIPTION OF THE FIGURES ing cafestol as a lipid barrier enhancer. FIG. 1 is photograph of a TLC plate showing the results of dose-variable (left) and time-variable (right) application BACKGROUND OF THE INVENTION of cafestol acetate to living skin models. Each shows an Skin is typically characterized as consisting of three increase in ceramide production with increasing dosage and distinct layers, namely the Stratum corneum, the epidermis time. and the dermis. The Stratum corneum, the Outermost layer, FIG. 2 is a photograph of a TLC plate showing the results is made up of keratinized cells, Surrounded by intercellular 15 of a comparison between application of cafestol acetate and Space filled with lipids. The Stratum corneum provides a coffee bean oil to living skin models, with respect to Substantial physical barrier to penetration of most Substances dose-dependent increase in ceramide production. to the lower layers of the skin. In addition to preventing FIG. 3 is a graphic representation of densitometric analy transport of Substances to the other skin layers, however, this sis of the TLC plate shown in FIG. 2, showing the effect of barrier also aids in prevention of water loSS from the skin. each treatment on ceramide content of skin relative to Both functions are primarily attributable to the presence of dosage. the lipids in the Stratum corneum. FIG. 4 is a graphic representation of the effect of cafestol There are two Sources of the Skin Surface lipids making up this important barrier: Sebaceous glands and the epidermis. acetate and cafestol palmitate on barrier Strength measured The lipids are a diverse group of compounds, comprising 25 via tape stripping and TEWL. triglycerides, diglycerides, ceramides, free fatty acids, wax FIG. 5 is a graphic representation of the effect of cafestol esters, cholesterol and cholesterol esters, and Squalene. The on ceramide production in Skin over time. quantity and composition of the skin Surface lipids differ FIG. 6 is a graphic representation of a dose-dependent from place to place on the body, and may to Some extent be effect of cafestol on ceramide production in Skin related to the number of Sebaceous glands in a given area of the skin. The condition of the skin Surface lipids may also be SUMMARY OF THE INVENTION affected by an essential fatty acid deficiency. Additionally, The present invention relates to topical compositions the lipid barrier is easily diminished by exposure to harsh comprising as an active component an effective amount of detergents or Soaps. It is apparent, then, that the quality of 35 cafestol, or derivatives thereof, in combination with a cos the skin lipid barrier can vary widely, depending on a metically or pharmaceutically acceptable carrier. The inven number of different factors, and therefore, may not always tion also relates to a method for increasing lipid Synthesis in be adequate to perform its protective function optimally. the skin which comprises applying to the skin an effective AS an attempt to compensate for what may be a less than amount of cafestol or a derivative thereof. As the lipid adequate lipid barrier, cosmetic compositions frequently 40 barrier is a key factor in maintaining the quality and mois incorporate components which compensate for water loSS. ture of skin, the topical application of cafestol or its deriva Examples of Such materials are hygroscopic humectants, tives is thus also useful in improving overall skin condition, e.g., urea or propylene glycol, or emollients, e.g., oleyl and in the prevention or treatment of a variety of dry skin alcohol or caprylic/capric triglycerides. Certain cosmetic generally, and Specific skin conditions in which the natural components may be occlusive skin conditioners, which are 45 lipid barrier is compromised or absent. used to provide an “artificial” barrier, Such compounds are frequently lipids which remain on the Skin Surface, and DETAILED DESCRIPTION OF THE include various hydrogenated oils, waxes and butters. INVENTION Although many of these products provide an effective means Cafestol is a diterpene which occurs naturally in, among of Stemming water loSS from the Skin, they do have to be 50 other Sources, coffee bean oil. Cafestol has the following reapplied frequently to maintain the effect, and do not chemical formula: generally constitute a natural-occurring component of the Stratum corneum, potentially giving rise to an unnatural, greasy feel to the skin. In addition, various pharmaceutical or cosmetic active agents are also frequently used to treat the 55 Symptoms of dry skin-associated conditions; however, in many cases, particularly with pharmaceutical agents, the treatments themselves may cause undesirable Side effects in the individual being treated, while ultimately resulting in no actual repair of the lipid barrier. 60 The present invention now provides a useful substitute for the daily application of Skin conditioning agents, or harsh It is available commercially in esterified form as cafestol topical active agents. It has now been discovered that it is acetate. Diverse biological activities have been attributed to possible to actually amplify the production of the skin's cafestol and related compounds. For example, coffee bean natural lipid barrier. Specifically, it has been found that 65 oil, which contains cafestol, has been said to be useful as a cafestol, when applied topically to the skin, is capable of sun filter (U.S. Pat. No. 4,793.990). An extract of essential Stimulating the production of one or more of the naturally oils of coffee has been used, in combination with numerous 5,855,897 3 4 other components, including cocoa butter and antioxidants, maceutical” or "cosmetic' will be understood to encompass in toilet Soap compositions, the components are Said to both human and animal pharmaceuticals or cosmetics. Use Synergistically interact to provide a "monomolecular film' ful carriers include, for example, water, acetone, ethanol, on the skin (SU 1770352). Further, cafestol itself, in com ethylene glycol, propylene glycol, butane-1,3-diol, isopro bination with another coffee bean oil component, kahweol, pyl myristate, isopropyl palmitate, or mineral oil. Method has been Suggested as having a protective effect against ology and components for formulation of cosmetic and carcinogens in animal Subjects (Miller et al., Nutr. Cancer pharmaceutical compositions are well known, and can be 15:41-46, 1991; Huggett and Schilter, Colloq. Sci. Int. Cafe found, for example, in Remington's Pharmaceutical C.R. 16(1): 65–72, 1995. Cafestol and kahweol have also Sciences, Eighteenth Edition, A.
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