Felodipine loaded PLGA nanoparticles: preparation, physicochemical characterization and in vivo toxicity study

Felodipine, a calcium channel blocker has been widely used for the treatment of hypertension and cardiovascular diseases; but the frequent dosing is needed for its poor solubility and variable bioavailability. In present study an attempt has been made to overcome the problems through nanoparticulate delivery system using poly (D, L-lactic-co-glycolic acid) polymer keeping in the view to get better sustainability of the formulation. The nanoparticles were prepared by single emulsion solvent evaporation technique and the physico-chemical characterization of prepared nanoparticles confirmed the particles were nanosize range with smooth and spherical morphology. Further, the compatibility of drug-polymer combination was analyzed by FTIR and DSC study. The in vitro drug release study of PLGA nanoparticles showed longer duration of drug release with reduced burst release compared with pure felodipine. The in vitro drug release data were fitted with various mathematical models to establish the drug release mechanism from the nanoparticles and found to follow mixed order kinetics. The in vivo toxicity study in albino mice showed no noticeable change in biochemical parameters and histopathology of organs. Hence, the developed felodipine nanoparticles were prepared, characterized and could possibly be advantageous for prolonged drug release and improving the antihypertensive effect. © 2014, Jana et al.; licensee Springer.