US 2003.0175333A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0175333 A1 Shefer et al. (43) Pub. Date: Sep. 18, 2003 (54) INVISIBLE PATCH FOR THE CONTROLLED Publication Classification DELIVERY OF COSMETIC, DERMATOLOGICAL AND (51) Int. Cl." .......................... A61K 31/715; A61K 9/70 PHARMACEUTICALACTIVE INGREDIENTS (52) U.S. Cl. .............................................. 424/449; 514/61 ONTO THE SKN (76) Inventors: Adi Shefer, East Brunswick, NJ (US); (57) ABSTRACT Samuel Shefer, East Brunswick, NJ (US) The present invention relates to a patch for controlled topical Correspondence Address: or transdermal delivery of effective levels of cosmetic, Diane Dunn McKay dermatological, and pharmaceutical active ingredients onto Mathews, Collins, Shepherd & McKay, P.A. the skin, hair follicles, and Sebaceous glands, with minimal Suite 306 discomfort and ease of use. The patch can be transparent or 100 Thanet Circle clear and comprises a rate-controlling matrix layer. The matrix layer comprises water-Sensitive, bioadhesive, film Princeton, NJ 08540 (US) forming polymers, a water Soluble oligomer, and a Surfac (21) Appl. No.: 10/376,736 tant. The cosmetic, dermatological, and pharmaceutical active ingredients are Soluble or dispersed in the matrix. The (22) Filed: Feb. 28, 2003 patch becomes tacky when wetted and adheres onto the skin. The adhesive properties of the patch are Sufficient to main Related U.S. Application Data tain the patch in place on the skin for the recommended treatment period while allowing the patch to be readily (63) Continuation-in-part of application No. 10/091,935, removed without causing skin irritation or leaving adhesive filed on Mar. 6, 2002. residue on the skin. US 2003/0175333 A1 Sep. 18, 2003 INVISIBLE PATCH FOR THE CONTROLLED 0008 U.S. Pat. No. 6,280,764 discloses a patch for DELIVERY OF COSMETIC, DERMATOLOGICAL, topical application of an anti-acne formulation has in various AND PHARMACEUTICALACTIVE INGREDIENTS embodiments a backing film, a release layer and at least one ONTO THE SKN adhesive polymeric matrix layer located between the back 0001. This application is a continuation in part of U.S. ing film and the release layer. The anti-acne formulation is application Ser. No. 10/091,935, filed Mar. 6, 2002, entitled uniformly distributed throughout one or more polymeric “A Patch for Controlled Delivery of Cosmetic, Dermato matrix layers and has an anti-acne effective amount of at logical, and Pharmaceutical Active Ingredients into the least two agents Selected from the group of an anti-micro Skin,” the contents of which are each incorporated by bial, an antiseptic, an anti-irritant, a keratolytic agent, a reference into this application. hormone, a hormone agonist and a hormone antagonist. BACKGROUND OF THE INVENTION 0009 U.S. Pat. No. 6,296,869 discloses a dermal patch which includes a substrate formed of a hydrophobic and 0002) 1. Field of the Invention hydrophilic fiber mixture, and a hydrogel adhesive deposited 0003. The present invention relates to an invisible patch onto the Substrate. The adhesive contains an alpha or beta for the controlled delivery of cosmetic, dermatological, and hydroxy acid. The patch is applied to skin for treating the pharmaceutical active ingredients onto the skin which is Signs of aging, especially around areas of the eye. formed of a Single matrix layer. The patch is applied onto the 0010 U.S. Pat. No. 6,280,765 discloses patch comprising skin by Wetting or moistening the target area. Upon appli a hydrophobic polymer layer bound to a Support layer and cation onto the Skin Surface, the patch dissolves or disinte containing: a) first particles of at least one water-soluble grates and provides a Substantive therapeutic layer to the active compound, b) second particles of oil, c) at least one treatment Site over an extended period of time. liposoluble active compound, d) third particles of a water 0004 2. Description of the Related Art absorbing agent all of which are dispersed homogeneously 0005 The localized treatment of body tissues, diseases, in the polymer layer. This patch allows the packaging and and wounds requires that the particular active ingredient be controlled administration of an assembly of skin-nourishing maintained at the Site of treatment for an effective period of and/or skin-repairing Substances of different nature, and also time. Transdermal patches for the administration of active has excellent adhesive power on the skin. ingredients onto the skin have become very popular in recent 0011 U.S. Pat. No. 5,232,702 describes a patch structure years. These patches adhere to the targeted area and the consisting of an occlusive Support layer and a polymer layer active ingredient is continually absorbed through the skin bound to the Support layer. The polymer layer is formed of into the bloodstream for systemic distribution. a matrix of a Silicone polymer including, in the dispersed 0006 The term “transdermal” as used herein, means State, fatty Substances and hydrophilic active compounds. transdermal or percutaneous administration, i.e. application This form of patch is more particularly suitable for deliv of the skin treating composition directly to the skin to be ering water-Soluble active compounds of lipophilic nature. treated. Hence the terms “skin,”“derma,”“epidermis,” and 0012 U.S. Pat. No. 5,976,565 discloses a patch for the like Shall also be used interchangeably unless Specifi topical application of an anti-acne formulation has in various cally Stated otherwise. embodiments a backing film, a release layer and at least one 0007 Transdermal patches, which permit the controlled adhesive polymeric matrix layer located between the back release of the active ingredients onto the skin, are known ing film and the release layer. The anti-acne formulation is from the literature. Two types of patches for skin applica uniformly distributed throughout one or more polymeric tions are described in the literature. The first type of patches matrix layers and has an anti-acne effective amount of at has a multilayer Structure, where the active ingredients are least two agents Selected from the group consisting of an dissolved or dispersed in the various layers. The Second type anti-microbial, an antiseptic, an anti-irritant, a keratolytic of patch is a pressure-Sensitive adhesive patch, where the agent, a hormone, a hormone agonist and a hormone antago active is dissolved or dispersed in the patch adhesive layer. nist. Multilayer patches normally have a structure comprising Several Successive layers in the following order: a first 0013 U.S. Pat. No. 5,100,672 discloses a pressure sen Support layer, which is typically occlusive, Such as, com Sitive adhesive transdermal patch having a composite adhe posed of a material impermeable to the active compound, So sive layer reinforced with a web layer. Cosmetically bioac as to prevent the evaporation thereof and facilitate transder tive Substances used in the patch include water Soluble mal migration; a Second storage layer fastened to the Support Vitamins Such as Vitamin C, and lipoSoluble Vitamins A and layer and containing the active compound and capable of E or their derivatives. placement directly in contact with the skin; a layer of an 0014 U.S. Pat. No. 6,180,133 discloses an anti-wrinkle adhesive material applied to the Surface of the Storage layer skin treating composition comprises a pressure Sensitive and permeable to the active compound to facilitate attach matrix patch having dissolved in the adhesive a mixture of ment of the patch to the skin; and a detachable protective antioxidants in the form of a Vitamins C ester and Vitamin E. layer which hermetically covers the Storage layer So as to Also preferably dissolved in the adhesive are glycerine and protect it from any external contamination during Storage a polydiorganosiloxane adhesion-adjusting agent. Option prior to use of the patch. In the preSSure Sensitive adhesive ally dissolved in the adhesive is also one or more members patches, the bioactive Substances are mixed with and for Selected from the group consisting of moisturizing agents, mulated into a pressure Sensitive adhesive matrix which may skin collagen Synthesis promoting agents and exfoliating be Subsequently coated as a single pressure Sensitive adhe agents. When applied to a wrinkled skin area the composi Sive layer. tion acts to diminish fine wrinkles and improves the overall US 2003/0175333 A1 Sep. 18, 2003 thickness, elasticity, firmness and Smoothness of the skin. DETAILED DESCRIPTION OF THE The modified adhesive properties of the patch are sufficient INVENTION to maintain the patch in place on the skin for the recom 0019. The present invention relates to a novel patch to mended treatment period while allowing the patch to be deliver cosmetic, dermatological, and pharmaceutical active readily removed without causing skin irritation or leaving ingredients onto the Skin, hair follicles, and Sebaceous adhesive residue on the Skin. glands. The patch can be translucent or invisible. Upon 0015 EP-A-0346211 describes the use of a copolymer application and adherence of the patch to the Surface of skin, of 2-ethyl-hexyl acrylate and N-vinyl-2-pyrrolidone without the cosmetic, dermatological, and pharmaceutical active ingredients, diffuse, or penetrate the Surrounding tissues, and absorption promoters. EP-A-0 272918 describes the use of provide effective delivery to the treatment site. The patch of a macroporous foam in which active ingredient is present in the present invention offers the advantages of an effective immobilized form. EP-A-0 409 383 describes an estrogen residence time with minimal discomfort and ease of use, and containing patch in the concentration range from 0.01 to 1% is an appropriate vehicle for local as well as Systemic of an estrogen in combination with a water-insoluble vinyl delivery of active ingredients. pyrrollidone for retarded release of the active ingredient to the skin.