Effect of varying drug loading on particle size distribution and drug release kinetics of verapamil hydrochloride microspheres prepared with cellulose esters

Abstract

Microspheres containing two different drug loadings of a calcium channel blocker, verapamil hydrochloride, were prepared with three different cellulose esters namely cellulose acetate (CA), cellulose acetate propionate (CAP) and cellulose acetate butyrate (CAB) of approximately similar molecular weights using the emulsion-solvent evaporation method. Increasing the drug loading from 33.3 to 50% w/w increased the geometric mean diameter of the microspheres as well as the T_50% values, i.e. time required to release 50% of the drug from microspheres prepared with all the three cellulose esters. Drug release from the microspheres was affected by the nature of polymer. Mathematical modelling of drug release data by fitting the data to various equations revealed that the data did not fit the conventional Higuchi's and Baker-Lonsdale's models for drug release from spherical matrices. Instead, the data fitted the log-probability and the Weibull models quite well.

Key Words:

• Verapamil
• cellulose ester
• emulsion
• solvent evaporation
• microsphere