Development, optimization, and evaluation of emulsion‐gelled floating beads using natural polysaccharide‐blend for controlled drug release

Abstract

Abstract This article describes the development, optimization, and evaluation of groundnut oil‐entrapped tamarind seed polysaccharide (TSP)‐alginate floating beads containing diclofenac sodium by emulsion‐gelation method for gastroretentive delivery. The effect of polymer to drug ratio, groundnut oil to water ratio, and sodium alginate to TSP ratio on drug entrapment, density, and drug release of floating beads was optimized using three‐factor and two‐level factorial design. The optimized floating beads showed drug entrapment efficiency of 82.48% ± 2.34%, density of 0.88 ± 0.07 g/cm 3 , cumulative drug release of 41.02% ± 0.86% after 8 h and floated well over 8 h in simulated gastric fluid (pH 1.2) with 8.25 min floating lag‐time. The in vitro drug release from these floating beads containing diclofenac sodium was followed controlled‐release pattern (zero‐order kinetics) with case‐II transport mechanism. The average bead size was ranged from 1.07 ± 0.03 to 1.94 ± 0.09 mm. The floating beads were characterized by SEM, FTIR, and 1 H NMR. The optimized floating beads showed excellent anti‐inflammatory activity in carrageenan‐induced rats over prolonged period after oral administration. POLYM. ENG. SCI., 2013. © 2012 Society of Plastics Engineers