title: Mucoadhesive, triclosan-loaded polymer microspheres for application to the oral cavity: preparation and controlled release characteristics.
abstract: The aim of this study was to develop mucoadhesive microspheres that can be utilised for the controlled release of triclosan in oral-care formulations, specifically dental pastes. Using a double-emulsion solvent evaporation technique, triclosan was incorporated into microspheres that were prepared from Gantreztrade mark MS-955, Carbopol 974P, polycarbophil or chitosan and the profiles for its release were established under simulated 'in use' conditions. Triclosan was rapidly released into a sodium lauryl sulphate containing buffer from all but the chitosan microspheres. The release of triclosan from microspheres suspended in a non-aqueous paste, was found to be sustained over considerable time-periods, which were influenced strongly by the nature of the polymeric carrier. For microspheres that were fabricated from Gantrez, Carbopol or polycarbophil, the release appeared to obey zero-order kinetics whereas in the case of chitosan-derived vehicles, the release profile fitted the Baker and Lonsdale model. The work has demonstrated that these polymeric microspheres, particularly those of chitosan, are promising candidates for the sustained release of triclosan in the oral cavity.
authors.affiliation: Lilly Forschung GmbH, Hamburg, Germany.
authors.forename: Sandra
authors.initials: S
authors.lastname: Kockisch
authors.forename: Gareth D
authors.initials: GD
authors.lastname: Rees
authors.forename: John
authors.initials: J
authors.lastname: Tsibouklis
authors.forename: John D
authors.initials: JD
authors.lastname: Smart
mesh_terms: D000269:Adhesives / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D000284:Administration, Oral; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D008863:Microspheres; D009055:Mouth / Q000187:drug effects / Q000378:metabolism; D011108:Polymers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D014260:Triclosan / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D000269:Adhesives; D003692:Delayed-Action Preparations; D011108:Polymers; D014260:Triclosan