Formulation and evaluation of dabigatran loaded microballoons for prolonged drug release

Abstract

The objective of the present investigation was to formulate microballoons loaded with dabigatran in the polymeric core for achieving sustained release and hence improved bioavailability. Microballoons loaded with dabigatran in the polymer shell were prepared by simple solvent evaporation method using either ethyl cellulose alone or a blend of ethyl cellulose with HPMC/PVP-K30/Eudragit S100/Methyl cellulose in a fixed ratio. The percent yield of the microballoons ranged from 38.7 to 62.4% with highest yield obtained in F3. The particle size was measured using optical microscopy and the particles were observed to be spherical in shape. The particle size ranged from 28.50 ± 16.378 µm (F3) to 48.14 ± 16.748 µm (F1). The angle of repose ranged from 26.37° to 28.09° and the Carr’s index and Hausner’s ratio were in between 6.38 to 19.95 and 1.07 to 1.25 respectively. It was found that all the formulations exhibited buoyancy in the range of 61.42 to 71.71% over a period of 8h. This suggests that the formulations were able to float for sufficient time and would be able to control the release of dabigatran for longer duration. The in vitro drug release study depicted that the highest amount of drug was released from F3 (66.79%) while the lowest was released from F1 (50.27%) at the end of 8 hours of study.