Mucoadhesive beads of gliclazide: Design, development, and evaluation

Abstract

Novel mucoadhesive beads were developed and evaluated for oral controlled release of the hypoglycaemic agent gliclazide. Various formulations of mucoadhesive beads were prepared using two different natural polymers, alginate and ispaghula, in various stoichiometric proportions with CaCl2 as a source of counter ions. The mucoadhesive beads were characterized for entrapment efficiency, particle size, surface morphology, and swelling index. The kinetics of drug release and their mucoadhesive nature in vitro using goat intestinal mucosa was also investigated at various physiological pH conditions. The effects of various proportions of the two polymers along with the effect of various percentages of counter ions on mucoadhesion property, size, entrapment efficiency, and drug release behaviour were studied. The effective mucoadhesion property with sustained release profile was observed from optimized mucoadhesive beads consisting of alginate and ispaghula husk (1:1) and polymer (2:1) with 5-10% w/v counter ions (CaCl2). These formulations showed optimum mucoadhesion behaviour having more than 70% w/v of drug entrapment and particle sizes of 896.7 0.8 and 920.6 1.2 µm, respectively.