Design and characterization of nanoparticles containing ezetimibe and atorvastatin calcium

Abstract

Ezetimibe is a weak hypolipidemic drug with poor aqueous solubility; with bioavailability of only 12% therefore large dose is prescribed which leads to adverse effects on continuous usage. Combination of Ezetimibe and low dose of statins is as effective in lowering LDL-CH. Therefore Atorvastatin is used with Ezetimibe in this study. In the present study Atorvastatin calcium and Ezetimibe nanoparticles were prepared and characterized for particle size analysis, drug entrapment efficiency, scanning electron microscopy, Zeta potential and in vitro studies. All prepared formulations (F1 to F4) resulted in the nanosize range of 59.20 ± 11.75 nm to 92.10 ± 13.58 nm with spherical morphology. Drug entrapment efficiency and percentage yield were 37.01±0.12% to 62.00±0.29% and 43.88±0.77% to 64.41±0.55 % for Atorvastatin and Ezetimibe respectively. Nanoparticles of optimized formulation (F3) showed Zeta potential of 15.3 mV. In vitro release profile of nanoparticulate formulations F1 to F4 showed 79.95 to 84.60% of Atorvastatin Calcium and 79.09 to 85.09% of Ezetimibe drug release over a period of 240 min. The results indicated that formulation (F3) could be utilized as potential delivery system for the treatment of cardiovascular disease and an approach to reduce undue adverse effects of the drug due to over dosage.