Submitted to: Meeting Abstract
Publication Type: Abstract Only
Publication Acceptance Date: 10/19/2003
Publication Date: 11/20/2003
Citation: Liu, L.S., Fishman, M.L., Hicks, K.B., Kende, M. 2003. An in vitro study of mucoadhesive properties of pectin and pectin derivatives. Meeting Proceedingsj7th US-Japan Symposium on Drug Delivery Systems, Maui, Hawaii, USA December 14-19, 2003, Part 1, p.16. Interpretive Summary:
Technical Abstract: Pectins are plant cell wall polysaccharides, mainly consisting of galacturonic acid and their methyl ester units in the backbone with inserted or attached neutral sugars. The most important properties of pectins for pharmaceutical preparations are their ability to gel and form films and their unique ability, by which pectins remain intact in the upper gastrointestinal tract and degrade in the lower gastrointestinal tract by colon microflora. These properties offer distinct advantages of pectins over other polysaccharides in the preparation of transmucosal delivery systems of bioactive materials. Due to the rich blood supply and relatively good permeability, mucosa is an attractive route for systemic delivery of bioactive materials. Mucosal adhesion of a delivery systems of bioactive materials will facilitate their release and enhance their uptake due to increased residence time and bioavailability in the nasal or in the intestinal tract. In the present study, pectin gels prepared from citrus fruit pectins with various degrees of esterification (D.E.) and pectin derivatives carrying primary amine and/or quaternary ammonium groups were examined for in vitro assessment of mucoadhesion. Pectin formulations were labeled with fluoresceinamine and loaded on porcine intestinal membrane. The pectins uptake by the membrane were measured by a fluorimeter at the excitation of 490 nm and the emission of 530 nm. The results showed that the low D.E. pectins had higher mucoadhesive activity than high D.E. pectins. Introduction of primary amine or quaternary ammonium groups also enhanced the mucoadhesivness. To investigate the interaction of pectin with mucin, the pectin formulations were examined for rheological synergism by dynamic oscillatory rheology and for morphology by laser scanning confocal microscopy. It was concluded that mucoadhesiveness of pectins is determined by the number and availability of hydrogen bond-forming groups in the pectin backbone.