Invisible patch for the controlled delivery of cosmetic, dermatological, and pharmaceutical active ingredients onto the skin

• US 20030175333A1
• Filed: 02/28/2003
• Published: 09/18/2003
• Est. Priority Date: 03/06/2002
• Status: Abandoned Application

• Current Assignee: Adi Shefer, Samuel Shefer
• Original Assignee: Adi Shefer, Samuel Shefer
• Inventors: Shefer, Samuel, Shefer, Adi
• Application Number:
  US10/376,736
• Publication Number:
  US 20030175333A1
• Time in Patent Office: Days
• US Class Current: 424/449
• CPC Class Codes: A61K 2800/244 Endothermic; Cooling; Cooling sensation
• CPC Class Codes: A61K 36/185 Magnoliopsida (dicotyledons)
• CPC Class Codes: A61K 36/258 Panax (ginseng)
• CPC Class Codes: A61K 36/28 Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
• CPC Class Codes: A61K 36/38 Clusiaceae, Hypericaceae or Guttiferae (Hypericum or Mangosteen family), e.g. common St. Johnswort
• CPC Class Codes: A61K 36/49 Fagaceae (Beech family), e.g. oak or chestnut
• CPC Class Codes: A61K 36/53 Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
• CPC Class Codes: A61K 36/537 Salvia (sage)
• CPC Class Codes: A61K 36/84 Valerianaceae (Valerian family), e.g. valerian
• CPC Class Codes: A61K 8/0208 Tissues; Wipes; Patches
• CPC Class Codes: A61K 8/35 Ketones, e.g. benzophenone
• CPC Class Codes: A61K 8/368 with carboxyl groups directly bound to carbon atoms of aromatic rings
• CPC Class Codes: A61K 8/44 Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
• CPC Class Codes: A61K 8/671 Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
• CPC Class Codes: A61K 8/676 Ascorbic acid, i.e. vitamin C
• CPC Class Codes: A61K 8/678 Tocopherol, i.e. vitamin E
• CPC Class Codes: A61K 8/731 Cellulose; Quaternized cellulose derivatives
• CPC Class Codes: A61K 8/8129 Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by an alcohol, ether, aldehydo, ketonic, acetal or ketal radical; Compositions of hydrolysed polymers or esters of unsaturated alcohols with saturated carboxylic acids; Compositions of derivatives of such polymers, e.g. polyvinylmethylether
• CPC Class Codes: A61K 8/8176 Homopolymers of N-vinyl-pyrrolidones. Compositions of derivatives of such polymers
• CPC Class Codes: A61K 8/9789 Magnoliopsida [dicotyledons]
• CPC Class Codes: A61K 8/9794 : Liliopsida [monocotyledons]
• CPC Class Codes: A61K 9/7007 : Drug-containing films, membranes or sheets A61K9/0041, A61K9/0043, A61K9/006, A61K9/0063 take precedence
• CPC Class Codes: A61K 9/7053 : obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61L 15/44 : Medicaments
• CPC Class Codes: A61L 2300/602 : Type of release, e.g. controlled, sustained, slow
• CPC Class Codes: A61P 17/00 : Drugs for dermatological disorders
• CPC Class Codes: A61P 17/02 : for treating wounds, ulcers, burns, scars, keloids, or the like
• CPC Class Codes: A61P 17/10 : Anti-acne agents
• CPC Class Codes: A61P 17/12 : Keratolytics, e.g. wart or anti-corn preparations
• CPC Class Codes: A61P 17/16 : Emollients or protectives, e.g. against radiation
• CPC Class Codes: A61Q 19/00 : Preparations for care of the skin
• CPC Class Codes: A61Q 19/02 : for chemically bleaching or whitening the skin
• CPC Class Codes: A61Q 19/04 : for chemically tanning the skin topical sun or radiation screening or tanning preparations A61Q17/04
• CPC Class Codes: A61Q 19/08 : Anti-ageing preparations
• CPC Class Codes: A61Q 9/04 : Depilatories

Abstract

The present invention relates to a patch for controlled topical or transdermal delivery of effective levels of cosmetic, dermatological, and pharmaceutical active ingredients onto the skin, hair follicles, and sebaceous glands, with minimal discomfort and ease of use. The patch can be transparent or clear and comprises a rate-controlling matrix layer. The matrix layer comprises water-sensitive, bioadhesive, film forming polymers, a water soluble oligomer, and a surfactant. The cosmetic, dermatological, and pharmaceutical active ingredients are soluble or dispersed in the matrix. The patch becomes tacky when wetted and adheres onto the skin. The adhesive properties of the patch are sufficient to maintain the patch in place on the skin for the recommended treatment period while allowing the patch to be readily removed without causing skin irritation or leaving adhesive residue on the skin.

Claims

1. A patch for controlled topical or transdermal delivery of effective levels of cosmetic, dermatological, or pharmaceutical active ingredients onto the skin, hair follicles, or sebaceous glands comprising a single matrix layer formed of a bioadhesive water-sensitive polymer, a water soluble oligomer, a surfactant and one or more cosmetic, dermatological, or pharmaceutical active ingredients.

2. The patch according to claim 1 wherein said patch dissolves or disintegrates upon contact with moisture.

3. The patch according to claim 1 wherein the bioadhesive water-sensitive polymer comprises one or more materials selected from the group consisting of:

a carbohydrate, starch, starch derivatives, starch hydrolyzate, modified starches, modified starch derivatives, hydroxyalkyl starches, hydroxypropyl cellulose, alkyl and carboxyalkyl cellulose, alkali metal salts of carboxyalkyl cellulose, polyvinyl alcohol, cellulose derivatives, polysaccharide, gum arabic and their derivatives, polyethylene glycol, water soluble acrylic, water soluble polyester, polyvinyl pyrrolidone, polyvinyl pyrrolidone cellulose derivatives, casein, gelatin, solubilized proteins, polyacrylamide, polyamine, polyquaternary amine, styrene maleic anhydride resins, polyethylene amine, ethylene maleic anhydride copolymer, methylvinyl ether maleic anhydride copolymer, acrylic acid copolymers, anionic polymers of methacrylic acid and methacrylate, cationic polymers with dimethyl-aminoethyl ammonium functional groups, polyethylene oxide and water soluble polyamide.

4. The patch according to claim 1 wherein the bioadhesive water-sensitive polymer comprises one or more materials selected from the group consisting of polyvinyl alcohol, polyvinyl pyrrolidone, modified starch derivatives and hydrolyzed starches.

5. The patch according to claim 1 wherein the oligomer comprises one or more materials selected from the group consisting of xylose, ribose, glucose, mannose, galactose, fructose, dextrose, polydextrose, sucrose, maltose, corn syrup solids, palatin, sorbitol, xylitol, mannitol, maltitol, lactitol, xanthan, maltodextrin, galactomanan, tragacanth, manitol, lactitol, oligisaccharides and hydrocolloids.

6. The patch according to claim 1 wherein the surfactant has an HLB of at least about 10.

7. The patch according to claim 1 wherein the surfactant comprises one or more materials selected from the group consisting of anionic, cationic, nonionic, amphoteric, zwitterionic and combinations thereof.

8. The patch according to claim 1 wherein the surfactant comprises one or more materials selected from the group consisting of sodium lauryl sulfate, cocoamidopropylbetaine, lauroamphoacetate, dialkylamine oxide, alkyl polyglycoside, methyl glucamide, sarcosinate, taurate, cocoyl isethionate, sucrose distearate, diglyceryldistearate, tetraglyceryl tristearate, decaglyceryl decastearate, diglyceryl monostearate, hexaglyceyl tristearate, decaglyceryl pentastearate, sorbitan monostearate, sorbitan tristearate, diethylene glycol monostearate, ester of glycerol and of palmitic acid, ester of glycerol and stearic acid, monostearate polyoxyethylenated containing 2 oxyethylene units, glyceryl mono- and dibehenate and pentaerythrityl tetrastearate, alkyl carboxylates, acyl lactylates, alkyl ether carboxylates, N-acyl sarcosinates, polyvalent alkyl carbonates, N-acyl glutamates, fatty acid, polypeptide condensates, sulfuric acid esters, polyoxyethylene, lecithin, ethoxylated alcohols, ethoxylated esters, ethoxylated amides, polyoxypropylene, propoxylated alcohol, ethoxylated/propoxylated block polymers, propoxylated esters, alkanolamides, amine oxides, fatty acid esters of polyhydric alcohols, ethylene glycol esters, diethylene glycol esters, propylene glycol esters, glycerol esters, polyglycerol fatty acid esters, sorbitan esters, sucrose esters, glucose esters and simethicone.

9. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, and pharmaceutical active ingredients are uniformly distributed throughout the matrix layer.

10. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are selected from the group consisting of anti-oxidant;

free radical scavenger;

moisturizer;

depigmentation agent;

liporegulator;

reflectant;

humectant;

antimicrobial agent;

allergy inhibitor;

anti-acne agent;

anti-aging agent;

anti-wrinkling agent;

antiseptic agent;

analgesic;

antitussive;

antipruritic;

local anesthetic;

anti-hair loss agent;

hair growth promoting agent;

hair growth inhibitor agent;

anti-dandruff agent;

antihistamine;

keratolytic agent;

anti-inflammatory agent;

freshener;

healing agent;

anti infective;

inflammation inhibitor;

anti-emetic;

anticholinergic;

vasoconstrictor;

vasodilator;

wound healing promoter;

peptide, polypeptide;

protein;

deodorant;

antiperspirant;

skin emollient;

skin moisturizer;

softener;

hair conditioner;

hair softener;

hair moisturizer;

tanning agent;

skin lightening agent;

antifungal;

depilating agent;

external analgesic;

counterirritant;

hemorrhoidal;

insecticide;

poison ivy treatment agent;

poison oak treatment agent;

burn treatment agent;

anti-diaper rash agent;

prickly heat agent;

make-up preparation;

vitamin;

amino acid;

amino acid derivative;

herbal extract;

retinoid;

flavoid;

sensory marker;

anti-oxidant;

skin conditioner;

hair lightener;

chelating agent;

cell turnover enhancer;

coloring agent;

sunscreen;

anesthetic;

immunomodulator, nourishing agent;

moisture absorber;

sebum absorber and mixtures thereof.

11. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are anti-septic agents selected from the group consisting of triclosan povidone, iodine, resorcinol, phenoxy, isopropanol and chlorhexidine.

12. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are anti-microbial agents selected from the group consisting of erythromyxin, tetracycline, cephalosporin and clindamycin.

13. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are keratolytic agents of salicylic acid.

14. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are topical antiseptics selected from the group consisting of iodine, mercury, silver, phenol, and nitrofurazone and combinations thereof.

15. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are anti-inflammatory agents chosen from the group consisting of aspirin and ibuprofen.

16. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are anti-irritant compositions selected from the group consisting of an antihistamine and calamine.

17. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are counter-irritant compositions selected from the group consisting of capsaicin, menthol, and clove oil.

18. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are moisturizers.

19. The patch according to claim 18 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are moisturizers selected from the group consisting of aloe, lanolin, glycerin, mineral oil, and combinations thereof.

20. The patch of claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are permeation enhancers.

21. The patch of claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients selected from the group consisting of an anti-inflammatory analgesic agent, a steroid hormone, a steroidal anti-inflammatory agent, an antihistamine, a local anesthetic, a bactericide, a disinfectant, a vasoconstrictor, a hemostatic, a chemotherapeutic drug, an antibiotic, a keratolytic, a cauterizing agent, an antiviral drug, and combinations thereof.

22. The patch of claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are anti-aging active agents.

23. The patch of claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are depigmentation active agents.

24. The patch of claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are anti-acne agents.

25. The patch of claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are tanning agents of dihydroxyacetone.

26. The patch according to claim 1 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are effervescent agents selected from the group consisting of sodium bicarbonate and sodium carbonate.

27. A patch according to claim 1 wherein said one or more dermatological active ingredients are selected from the group consisting of anti-oxidants, free radical scavengers, moisturizers, depigmenting agents, liporegulators, anti-acne agents, anti-dandruff agents, anti-aging agents, softeners, anti-wrinkle agents, keratolytic agents, anti-inflammatory agents, fresheners, healing agents, vascular protectors, antibacterial agents, antifungal agents, antiperspirants, deodorants, skin conditioners, anesthetics, immunomodulators and nourishing agents, moisture absorbers, and sebum absorbers.

28. A patch according to claim 1 further comprising a solubilizer selected from the group consisting of glycerol, propylene glycol, polyalcohol, sorbitol and sorbitol derivatives.

29. The patch according to claim 1 wherein said matrix is transparent.

30. The patch according to claim 1 wherein said matrix has a color.

31. The patch according to claim 1 having a size in the range of about 0.25 cm² to about 500 cm², and a shape to match the shape of a region to be treated.

32. The patch according to claim 1 wherein the matrix layer has a thickness from about 0.0001 mm to about 1.0 mm.

33. The patch according to claim 1 wherein said patch further comprises a detachable protective layer.

34. The patch according to claim 1 wherein said one or more cosmetic, dermatological, or pharmaceutical active ingredients are encapsulated in one or more of hydrophobic nanospheres, microspheres or hydrophobic nanospheres encapsulated in microspheres.

35. The patch according to claim 34 wherein said microsphere is formed of a moisture sensitive, water sensitive or pH sensitive material.

36. The patch according to claim 34 wherein said one or more of said cosmetic, dermatological and pharmaceutical active ingredients are encapsulated in said hydrophobic nanospheres of said hydrophobic nanospheres encapsulated in microspheres, in said microsphere of said hydrophobic nanospheres encapsulated in microspheres or in both said hydrophobic nanospheres of said hydrophobic nanospheres encapsulated in microspheres and said microspheres of said hydrophobic nanospheres encapsulated in microspheres.

37. The patch according to claim 34 wherein said microsphere is formed of a water-sensitive material comprising one or more materials selected from water soluble and water dispersible natural oligomers, synthetic oligomers, natural polymers, synthetic polymers and copolymers, starch derivatives, oligosaccharide, polysaccharides, hydrocolloids, natural gums, proteins, xylose, ribose, glucose, mannose, galactose, fructose, dextrose, polydextrose, sucrose, maltose, or corn syrup solids, palatin, sorbitol, xylitol, mannitol, maltitol, lactitol, xanthan, maltodextrin, galactomanan or tragacanth, polyvinyl pyrrolidone, water soluble celluloses, polyvinyl alcohol, ethylene maleic anhydride copolymer, methylvinyl ether maleic anhydride copolymer, acrylic acid copolymers, anionic polymers of methacrylic acid and methacrylate, cationic polymers with dimethyl-aminoethyl ammonium functional groups, polyethylene oxides, water soluble polyamide or polyester, water soluble hydroxyalkyl and carboxyalkyl celluloses.

38. The patch according to claim 34 wherein said microsphere has a size from about 0.5 microns to about 300 microns.

39. The patch according to claim 34 wherein said hydrophobic nanosphere is formed of a lipid or wax.

40. The patch according to claim 34 wherein said nanosphere has an average sphere size in the range from about 0.01 micron to about 5 microns.

41. A method for treating the skin comprising the step of:

applying to a surface of the skin to be treated the patch according to claim 1.

42. The method of claim 41 further comprising the step of:

moistening a surface of the skin before the step of applying the patch.

43. The method of claim 41 wherein the one or more of said cosmetic, dermatological, or pharmaceutical active ingredients are selected from the group consisting of anti-oxidants, free radical scavengers, moisturizers, depigmenting agents, liporegulators, anti-acne agents, anti-dandruff agents, anti-aging agents, softeners, anti-wrinkle agents, keratolytic agents, anti-inflammatory agents, fresheners, healing agents, vascular protectors, antibacterial agents, antifungal agents, antiperspirants, deodorants, skin conditioners, anesthetics, immunomodulators and nourishing agents, moisture absorbers, and sebum absorbers.

49. An article of manufacture applied to the skin comprising the patch of claim 1.

50. The article of claim 49 wherein said article is an invisible bandage.

44. A method for adhering a patch onto the skin, hair follicles or sebaceous glands comprising the steps of:

wetting an area of said skin hair follicles or sebaceous glands; and

affixing the patch to the skin, hair follicles or sebaceous glands, said patch comprising a single matrix layer formed of a bioadhesive water-sensitive polymer, a water soluble oligomer, and a surfactant.

45. The method of claim 44 wherein said patch further comprises one or more cosmetic, dermatological, or pharmaceutical active ingredients which are selected from the group consisting of anti-oxidant;

free radical scavenger;

moisturizer;

depigmentation agent;

liporegulator;

reflectant;

humectant;

antimicrobial agent;

allergy inhibitor;

anti-acne agent;

anti-aging agent;

anti-wrinkling agent;

antiseptic agent;

analgesic;

antitussive;

antipruritic;

local anesthetic;

anti-hair loss agent;

hair growth promoting agent;

hair growth inhibitor agent;

anti-dandruff agent;

antihistamine;

keratolytic agent;

anti-inflammatory agent;

freshener;

healing agent;

anti infective;

inflammation inhibitor;

anti-emetic;

anticholinergic;

vasoconstrictor;

vasodilator;

wound healing promoter;

peptide, polypeptide;

protein;

deodorant;

antiperspirant;

skin emollient;

skin moisturizer;

softener;

hair conditioner;

hair softener;

hair moisturizer;

tanning agent;

skin lightening agent;

antifungal;

depilating agent;

external analgesic;

counterirritant;

hemorrhoidal;

insecticide;

poison ivy treatment agent;

poison oak treatment agent;

burn treatment agent;

anti-diaper rash agent;

prickly heat agent;

make-up preparation;

vitamin;

amino acid;

amino acid derivative;

herbal extract;

retinoid;

flavoid;

sensory marker;

anti-oxidant;

skin conditioner;

hair lightener;

chelating agent;

cell turnover enhancer;

coloring agent;

sunscreen;

anesthetic;

immunomodulator, nourishing agent;

moisture absorber;

sebum absorber and mixtures thereof.

46. A method of using a patch comprising the step of:

applying a patch to the skin, hair follicles or sebaceous glands for a period of application in a range of about one minute to about 12 hours, said patch comprising a single matrix layer formed of a bioadhesive water-sensitive polymer, a water soluble oligomer, and a surfactant.

47. The method of claim 46 wherein said patch further comprises one or more pharmaceutical active ingredients selected from the group consisting of an anti-inflammatory analgesic agent, a steroidal anti-inflammatory agent, an antihistamine, a local anesthetic, a bactericide, a disinfectant, a vasoconstrictor, a hemostatic, a chemotherapeutic drug, an antibiotic, a keratolytic, a cauterizing agent, an antiviral drug, and a combination thereof.

48. A patch for controlled topical or transdermal delivery of effective levels of cosmetic, dermatological, or pharmaceutical active ingredients onto the skin, hair follicles, or sebaceous glands comprising a matrix layer which comprises one or more materials selected from the group consisting of polyvinyl alcohol, polyvinyl pyrrolidone, modified starch derivatives and hydrolyzed starches and a combination thereof, an oligomer selected from the group consisting of xylose, ribose, glucose, mannose, galactose, fructose, dextrose, polydextrose, sucrose, maltose, corn syrup solids, palatin, sorbitol, xylitol, mannitol, maltitol, lactitol, xanthan, maltodextrin, galactomanan, tragacanth, manitol, lactitol, oligisaccharides and hydrocolloids, a surfactant, and one or more of said cosmetic, dermatological, and pharmaceutical active ingredients uniformly distributed throughout the polymeric water-soluble matrix layer.