# US 10,500,279 B2 · Low toxicity topical active agent delivery system > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,500,279 B2 - Document ID: US10500279B2 - Status: Granted - Kind: B2 - Application number: 15/890,408 - Filed: 2018-02-07 - Published: 2018-06-14 - Granted: 2019-12-10 - Earliest claimed: 2009-12-15 - Applicants: John E. Kulesza - Inventors: John E. Kulesza - Web page: https://patentgrep.com/patent/US10500279B2 ## CPC - A61K 47/08: containing oxygen, {e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides} - A61K 8/368: with carboxyl groups directly bound to carbon atoms of aromatic rings - A61K 8/38: Percompounds, e.g. peracids - A61K 8/585: {Organosilicon compounds} - A61K 8/671: {Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal} - A61K 8/69: containing fluorine - A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)} - A61K 31/07: Retinol compounds, e.g. vitamin A (retinoic acids A61K31/203) - A61K 31/194: having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid - A61K 31/203: Retinoic acids {; Salts thereof} - A61K 31/60: Salicylic acid; Derivatives thereof - A61P 17/00: Drugs for dermatological disorders - A61P 17/06: Antipsoriatics - A61P 17/16: Emollients or protectives, e.g. against radiation - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics - A61P 35/00: Antineoplastic agents - A61P 37/02: Immunomodulators - A61Q 15/00: Anti-perspirants or body deodorants (deodorisation of air A61L9/00) - A61Q 19/00: Preparations for care of the skin - A61Q 19/007: {Preparations for dry skin} - A61Q 19/08: Anti-ageing preparations - A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS ## Abstract An active agent delivery composition is provided that allows topical delivery of active agents including vitamin A and its derivatives. A polyhalogenic vehicle serves as a coupler for an active agent and a silicone carrier so as to allow solubilization of active agents not normally miscible in silicones and providing a moisture maintaining composition. ## Claims ### Claim 1 An active agent topical delivery composition comprising: an active agent present at a concentration between 0.001 to 0.5 weight percent, said active agent selected from the group consisting of vitamin A or its derivatives, salicylic acid, and benzoyl peroxide; a volatile linear organopolysiloxane carrier with 2 to 6 silicon atoms present at 10 percent to 75 percent by weight; a vehicle selected from the group consisting of methoxynonafluorobutane, ethoxynonafluorobutane, or a combination thereof, said vehicle present at from 5 percent to 40 percent by weight; and an alcohol at less than 5% by weight; said composition free of water and ethanol, wherein said active agent is insoluble at said concentration of active agent if in a fluid consisting of said active agent and said carrier or in a fluid consisting of said active agent and said vehicle, and wherein and the active agent fully soluble in the carrier and the vehicle combined at said concentration; and wherein the composition is clear liquid solution of said active agent at room temperature. ### Claim 2 (depends on 1) The composition of claim 1 wherein said alcohol is included and is ethoxydiglycol. ### Claim 3 (depends on 1) The composition of claim 1 wherein said active agent is a vitamin A derivative that is: retinal; retinoic acid; retinyl ester; retinol; tretinoin; isotretinoin; adapalene; tazarotene; or combinations thereof. ### Claim 4 (depends on 1) The composition of claim 1 wherein said active agent is vitamin A or its derivatives. ### Claim 5 (depends on 1) The composition of claim 1 wherein said agent is benzoyl peroxide, said benzyol peroxide present from 0.001 to 0.1 weight percent. ### Claim 6 (depends on 1) The composition of claim 1 wherein said volatile linear organopolysiloxane carrier is ethyl trisiloxane. ### Claim 7 (depends on 6) The composition of claim 6 wherein said ethyl trisiloxane is present at about 70 percent by weight. ### Claim 8 (depends on 1) The composition of claim 1 wherein said vehicle is present at 15 percent to 25 percent by weight. ### Claim 9 (depends on 1) The composition of claim 1 wherein said active agent is a retinoid. ### Claim 10 (depends on 1) The composition of claim 1, wherein said vehicle present at from 15 percent to 40 percent by weight. ### Claim 11 (depends on 1) The composition of claim 1, wherein the active agent is present at a concentration between 0.01 to 0.1 weight percent, wherein said volatile linear organopolysiloxane carrier is ethyl trisiloxane, and wherein said vehicle present at from 15 percent to 25 percent by weight. ### Claim 12 A skin care composition comprising: a vitamin A or vitamin A derivative at a concentration between 0.01 to 0.5 weight percent; a volatile linear organopolysiloxane carrier of 2 to 6 silicon atoms present at 10 percent to 75 percent by weight; a vehicle selected from the group consisting of methoxynonafluorobutane, ethoxynonafluorobutane, or a combination thereof, said vehicle having a boiling point less than 78 degrees Celsius, said vehicle present at from 5 percent to 40 percent by weight; and an alcohol at 0-5 percent by weight; wherein said active agent is insoluble at said concentration if in a fluid consisting of said active agent and said carrier or in a fluid consisting of said active agent and said vehicle, and wherein and the active agent fully soluble in the carrier and the vehicle combined at said concentration; said composition free of water and ethanol, and wherein the composition is clear liquid solution of said active agent at room temperature. ### Claim 13 (depends on 12) The composition of claim 12 wherein said active agent is vitamin A or its derivatives wherein said vitamin A or its derivatives are present at between 0.01 to 0.1 weight percent. ### Claim 14 (depends on 12) The composition of claim 12 wherein said volatile linear organopolysiloxane carrier is ethyl trisiloxane, or a combination of ethyl trisiloxane and disiloxane. ### Claim 15 (depends on 14) The composition of claim 14 wherein said ethyl trisiloxane is present at about 70 percent by weight. ### Claim 16 (depends on 12) The composition of claim 12 wherein said vehicle is present at 5 percent to 25 percent by weight. ### Claim 17 (depends on 12) The composition of claim 12, wherein said vehicle present at from 15 percent to 40 percent by weight. ### Claim 18 (depends on 12) The composition of claim 12, wherein the active agent is present at a concentration between 0.01 to 0.1 weight percent, wherein said volatile linear organopolysiloxane carrier is ethyl trisiloxane, and wherein said vehicle present at from 15 percent to 25 percent by weight. ### Claim 19 (depends on 1) The composition of claim 1 wherein said carrier is present at 70 percent by weight or greater, and said vehicle present at 15 to 25 percent by weight, said composition free of any additional agent capable of solublizing said active at said concentration.