title: Development of low methoxy amidated pectin-based mucoadhesive patches for buccal delivery of triclosan: effect of cyclodextrin complexation.
abstract: A novel mucoadhesive buccal patch formulation of triclosan (TR), a broad spectrum antibacterial agent, was developed using low methoxy amidated pectin (AMP). The integrity of AMP matrix was improved by addition of 20% (w/w) Carbopol (CAR). The efficiency of β-cyclodextrin-epichlorohydrin polymer (EPIβCD) and anionic carboxymethylated β-cyclodextrin-epichlorohydrin polymer (CMEPIβCD) in optimization of TR solubility and release from such a matrix was investigated and confronted to that of parent β-cyclodextrin (βCD). Loading of TR/βCD co-ground complex into AMP/CAR matrix resulted in a biphasic release profile which was sensitive upon the hydration degree of the matrix, due to lower solubilizing efficiency of βCD, while the drug release from patches loaded with TR/EPIβCD complex was significantly faster with a constant release rate. Microbiological studies evidenced faster onset and more pronounced antibacterial action of TR/EPIβCD loaded patches, clearly demonstrating their good therapeutic potential in eradication of Streptococcus mutans, a cariogenic bacteria, from the oral cavity.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovačića 1, Zagreb 10000, Croatia. mjug@pharma.hr
authors.forename: Mario
authors.initials: M
authors.lastname: Jug
authors.forename: Ivan
authors.initials: I
authors.lastname: Kosalec
authors.forename: Francesca
authors.initials: F
authors.lastname: Maestrelli
authors.forename: Paola
authors.initials: P
authors.lastname: Mura
mesh_terms: D000180:Acrylic Resins; D000268:Adhesiveness; D000278:Administration, Buccal; D000577:Amides / Q000737:chemistry*; D000818:Animals; D000891:Anti-Infective Agents, Local / Q000008:administration & dosage* / Q000494:pharmacology; D002610:Cheek; D004337:Drug Carriers; D016503:Drug Delivery Systems; D009061:Mouth Mucosa / Q000378:metabolism*; D010368:Pectins / Q000737:chemistry*; D010539:Permeability / Q000187:drug effects; D011145:Polyvinyls / Q000737:chemistry; D013295:Streptococcus mutans / Q000187:drug effects; D013552:Swine; D014260:Triclosan / Q000008:administration & dosage* / Q000494:pharmacology; D047392:beta-Cyclodextrins / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000180:Acrylic Resins; D000577:Amides; D000891:Anti-Infective Agents, Local; D004337:Drug Carriers; D011145:Polyvinyls; D047392:beta-Cyclodextrins; C006912:carboxypolymethylene; D014260:Triclosan; D010368:Pectins