Preparation and evaluation of glibenclamide-loaded biodegradable nanoparticles

Abstract

Purpose: To formulate and evaluate glibenclamide (GB)-loaded poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) for controlled release. Methods: GB-loaded PLGA NPs were prepared by solvent evaporation technique using methanol/dichloromethane (2:1) and characterized by transmission electron microscopy (TEM), and differential scanning calorimetry (DSC). The effect of stirring speed (250, 1000, 1500 and 2500 rpm) and drug: polymer ratio (1:1, 1: 2, 1:3 and 2:1) on particle size, size distribution, zeta potential, drug loading, encapsulation efficiency and drug release was also studied. Results: Stable NPs were successfully prepared without any incompatibility, as indicated by TEM and DSC studies, respectively. As polymer and drug concentrations, and stirring speed increased, particle size, drug loading and encapsulation efficiency also increased. Increase in polymer concentration sustained drug release but reverse was obtained as drug concentration increased. Conclusion: Controlled release biodegradable glibenclamide NPs can be efficiently prepared by emulsification solvent evaporation method suitably modulating processing variables. © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria.