title: Mucoadhesive properties of cross-linked high amylose starch derivatives.
abstract: Acetate (Ac-), aminoethyl (AE-) and carboxymethyl (CM-)derivatives of cross-linked high amylose starch (HASCL-6) were previously shown to control, over more than 20h, the release of drugs from highly loaded (up to 60% drug) monolithic tablets. It was now of interest to evaluate their mucoadhesive characteristics in view of further utilization in buccal or vaginal transmucosal delivery. The present study shows that ionic AE-HASCL-6 and CM-HASCL-6 derivatives exhibit higher mucoadhesive properties than neutral HASCL-6 and Ac-HASCL-6, suggesting that the ionic groups introduced on cross-linked starch chains play a role in the bioadhesion process. The adhesiveness seemed related to capillary attraction forces. Surface adhesion parameters were calculated for slabs based on the mentioned polymers and corroborated with their swelling behavior at various pH changes. The positively charged AE-derivatives presented a higher adhesion at acidic pH, being thus recommended for vaginal delivery, whereas the negatively charged derivatives (CM-HASCL-6) exhibited a better adhesion at neutral pH, being thus more appropriate for buccal delivery.
authors.affiliation: Department of Chemistry and Biochemistry, Centre BioMed, Université du Québec à Montréal, CP 8888, Succ. Centre-Ville, Montréal, Québec H3C 3P8, Canada.
authors.forename: Jérôme
authors.initials: J
authors.lastname: Mulhbacher
authors.forename: Pompilia
authors.initials: P
authors.lastname: Ispas-Szabo
authors.forename: Mathieu
authors.initials: M
authors.lastname: Ouellet
authors.forename: Serge
authors.initials: S
authors.lastname: Alex
authors.forename: Mircea Alexandru
authors.initials: MA
authors.lastname: Mateescu
mesh_terms: D000268:Adhesiveness; D000688:Amylose / Q000737:chemistry*; D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D009077:Mucins; D009092:Mucous Membrane; D013213:Starch / Q000737:chemistry*; D013607:Tablets
chemical_list: D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D009077:Mucins; D013607:Tablets; D013213:Starch; D000688:Amylose