# US 8,771,649 B2 · Inducible release vehicles > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,771,649 B2 - Document ID: US8771649B2 - Status: Granted - Kind: B2 - Application number: 10/558,816 - Filed: 2004-05-28 - Published: 2007-04-26 - Granted: 2014-07-08 - Earliest claimed: 2003-05-30 - Assignees: Nederlandse Organisatie voor toegepast-natuurwetenschappelijk onderzoek TNO - Applicants: Henricus Matheus Wilhelmus Maria Thijssen; Roy Christiaan Montijn; Johannes Wilhelmus Timmermans; Theodoor Maximiliaan Slaghek; Jacobus Johannes Frederick van Veen; Johannes Wilhelmus Leonardus Boumans - Inventors: Henricus Matheus Wilhelmus Maria Thijssen; Roy Christiaan Montijn; Johannes Wilhelmus Timmermans; Theodoor Maximiliaan Slaghek; Jacobus Johannes Frederick van Veen; Johannes Wilhelmus Leonardus Boumans - Web page: https://patentgrep.com/patent/US8771649B2 ## CPC - A61L 15/46: Deodorants or malodour counteractants, e.g. to inhibit the formation of ammonia or bacteria - A01N 25/10: Macromolecular compounds - A61P 17/10: Anti-acne agents - A61L 2300/208: Quaternary ammonium compounds - A61L 2300/404: Biocides, antimicrobial agents, antiseptic agents - A61L 2300/604: Biodegradation - A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K) - A01N: PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF (preservation of food or foodstuff A23); BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES (preparations for medical, dental or toiletry purposes which kill or prevent the growth or proliferation of unwanted organisms A61K); PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract This invention relates to inducible release vehicle comprised of crosslinked carbohydrates or proteins and an active ingredient. The release is induced by an external stimulus, e.g. an enzyme such as amylase. Such a vehicle can particularly be used in applications for preventing microbial decay or combating microbial infections. Other uses are for oral applications such as providing antdaries or flavoring compounds and for pharmaceutical and/or nutraceutical applications. ## Claims ### Claim 1 Inducible release vehicle comprising a charged cross-linked polymer and an active component, wherein release of the active component does not occur in an aqueous medium until release is initiated by contact of the vehicle with a stimulus external to the vehicle, wherein said polymer is a carbohydrate consisting of only C-, O- and H-atoms, and wherein the stimulus external to the vehicle is an enzyme with specificity for the degradation of said polymer. ### Claim 2 (depends on 1) Vehicle according to claim 1 wherein the active ingredient is incorporated after the vehicle has been isolated. ### Claim 3 (depends on 2) Vehicle according to claim 2 wherein the carbohydrate polymer is modified by oxidation, substitution with carboxymethyl groups, or esterification. ### Claim 4 (depends on 1) Vehicle according to claim 1 wherein the release of the active ingredient is induced by change of electrostatic interaction. ### Claim 5 (depends on 1) Vehicle according to claim 1 wherein the polymer is chosen from the group consisting of starch, cellulose, and pectin. ### Claim 6 (depends on 1) Vehicle according to claim 1 wherein the cross linker is chosen from the group consisting of a divinyl sulphone, a epichlorohydrin, a di-epoxide, a sodium trimetaphosphate and an adipic acid. ### Claim 7 (depends on 1) Vehicle according to claim 1 wherein the polymer is cross-linked by means of a cross-linking enzyme chosen from the group consisting of peroxidases, laccases, polyphenol oxidases, and lipoxygenases. ### Claim 8 (depends on 1) Vehicle according to claim 1 wherein the vehicle is loaded with a charged compound. ### Claim 9 (depends on 1) Vehicle according to claim 1 wherein the vehicle is loaded with a hydrophobic compound. ### Claim 10 (depends on 8) Vehicle according to claim 8 wherein the vehicle is loaded with a protein or an anti microbial compound. ### Claim 11 (depends on 1) A pharmaceutical and/or nutraceutical composition comprising a vehicle according to claim 1. ### Claim 12 (depends on 1) A cosmetic composition comprising a vehicle according to claim 1, wherein the active component is an anti acne agent. ### Claim 13 (depends on 1) A cosmetic composition comprising a vehicle according to claim 1, wherein the active component is a deodorant. ### Claim 14 (depends on 1) A fungicidal paint comprising a vehicle according to claim 1, wherein the active component is a fungicide. ### Claim 15 (depends on 1) An antifouling paint composition comprising a vehicle according to claim 1, wherein the active component is an antifouling component. ### Claim 16 (depends on 1) A dressing means comprising a vehicle according to claim 1, wherein the dressing means is a wound dressing means or a sanitary dressing means and wherein the active component is an antimicrobial compound. ### Claim 17 (depends on 1) A medicine containing a vehicle according to claim 1, wherein the active component is an antimicrobial compound. ### Claim 18 (depends on 1) A medicine containing a vehicle according to claim 1, wherein the active component is a cytostatic agent. ### Claim 19 (depends on 1) A coating comprising a vehicle according to claim 1, wherein the active component is an antimicrobial compound. ### Claim 20 (depends on 1) A vehicle according to claim 1 which contains a flavoring agent. ### Claim 21 (depends on 1) A method for producing a vehicle according to claim 1 comprising: a) providing a polymer and a cross-linker or cross-linking enzyme; b) activating the cross-linking by addition of base or acid; c) allowing for cross-linking and gelation of the cross-linked polymer to occur; d) breaking the gel resulting from step c) into smaller particles; e) drying the particles from step d) and optionally grinding these into finer particles; f) loading said particles with an active component. ### Claim 22 (depends on 9) Vehicle according to claim 9 wherein the vehicle is loaded with a protein or an anti microbial compound. ### Claim 23 (depends on 8) Vehicle according to claim 8, wherein the charged compound has a molecular weight below 50 kD. ### Claim 24 (depends on 3) Vehicle according to claim 3, wherein the carbohydrate polymer is modified by esterification by acetyl groups. ### Claim 25 (depends on 4) Vehicle according to claim 4, wherein the change of electrostatic interaction is induced by a change in pH. ### Claim 26 (depends on 4) Vehicle according to claim 4, wherein the change of electrostatic interaction is induced by a change in the salt concentration. ### Claim 27 (depends on 20) Vehicle according to claim 20, wherein the flavoring agent is for a chewing gum. ### Claim 28 (depends on 1) Vehicle according to claim 1, wherein said enzyme is selected from the group consisting of amylase, hemicellulase, xylanase, glucanase, pullulanase, arabinodase, cellulase, pectinase, and mannanase, and wherein said polymer comprises glucose, fructose, sucrose, maltose, arabinose, mannose, galactose, lactose, cellulose, dextrin, agarose, amylose, amylopectin, or gum, or oligomers or polymers thereof. ### Claim 29 (depends on 6) Vehicle according to claim 6, wherein the di-epoxide is selected from the group consisting of glycerol diglycidyl ether and butanedioldiglycidyl ether. ### Claim 30 (depends on 1) Vehicle according to claim 1, wherein in a moist environment, the active component exists in an intact form within the vehicle until release of the active component from the vehicle is initiated by contact of the vehicle with the stimulus external to the vehicle.