Pentoxifylline Loaded Floating Microballoons: Design, Development and Characterization.

Abstract

The floating microballoons have been utilized to obtain prolonged and uniform release in the stomach. The objective of the present study involves design, development, and characterization of pentoxifylline loaded floating microballoons to prolong their gastric residence time. Pentoxifylline (trisubstituted xanthine derivative) loaded microballoons were prepared by the solvent evaporation technique using different concentrations of polymers like HPMC K4M and ethyl cellulose (EC) in ethyl alcohol and dichloromethane organic solvent system. Microballoons were characterized for their particle size, surface morphology, production yield, loading efficiency, buoyancy percentage, and in vitro drug release studies. From the characterization it was observed that increases in amount of polymers (HPMC K4M and EC) led to increased particle size, loading efficiency, and buoyancy percentage, and retarded drug release. The particle size, particle yield, loading efficiency, buoyancy percentage and in vitro drug release for optimized formulation (F3) were found to be 104.0 ± 2.87 µm, 80.89 ± 2.24%, 77.85 ± 0.61%, 77.52 ± 2.04%, and 82.21 ± 1.29%, respectively. The data was fitted to different kinetic models to illustrate its anomalous (non-Fickian) diffusion. The in vitro result showed that formulations comprised of varying concentrations of ethyl cellulose in higher proportion exhibited much retarded drug release as compared to formulations comprised of higher proportion of varying concentrations of HPMC K4M.