Mebeverine HCl-loaded sodium carboxymethyl gum ghatti-chitosan microparticles: In vitro-in vivo evaluations

Abstract

The current research attempted to design a sustained releasing microparticles made of chitosan and carboxymethylated derivative of gum ghatti (CMGG) via polyelectrolyte complexation. CMGG was synthesized by conventional Williamson ether synthesis method, where degree of substitution was found 0.40 ± 0.04%. The synthesized CMGG and chitosan was used to formulate mebeverine HCl (M-HCl) loaded CMGG-chitosan microparticles by means of crosslinking using glutaraldehyde (covalent crosslinker). The particle sizes and DEE (%) of these M-HCl loaded microparticles were within 34.40 ± 1.06 to 46.00 ± 1.05 μm and 75.85 ± 1.20% to 51.44 ± 0.25%, respectively. The formulated M-HCl loaded CMGG-chitosan microparticles were instrumentally characterized using SEM, DSC and FTIR analyses. In vitro, M-HCl loaded microparticles in gastric pH were observed to have a greater M-HCl releasing rate than those at alkaline pH. Korsmeyer–Peppas model with the Fickian diffusion phenomena were found to be followed by these newly developed microparticles in in vitro drug releasing. In addition, in vivo pharmacodynamic activity of M-HCl loaded CMGG-chitosan microparticles in healthy rabbits was evaluated and a higher correlation coefficient indicated the existence of excellent in vitro-in vivo correlation.