Development, in-vitro and in-vivo evaluation of ezetimibe-loaded solid lipid nanoparticles and their comparison with marketed product

Abstract

This study aims to develop ezetimibe-loaded solid lipid nanoparticles (SLNs) and compare them with marketed product and drug suspension for dissolution and bioavailability. Ezetimibe-loaded SLNs were fabricated using high pressure homogeniser (HPH). The content of SLNs were (drug, solid lipid and surfactant; 50/300/25 mg/ml of distilled water). They were characterized through particle size, poly dispersive index (PDI), zeta potential and entrapment efficiency (EE). Moreover, dynamic scattering calorimetry (DSC) and powder x-ray diffraction (PXRD) were also performed. Furthermore, in-vitro release study was performed followed by pharmacokinetics study in rats after oral administration of ezetimibe-loaded SLNs and compared with marketed product and powder drug suspension. The mean particle size, PDI and zeta potential of ezetimibe-loaded SLNs were 156.9 nm, 0.125 and −20.5 mV, respectively with 90.7% EE. DSC and PXRD study exhibited that the drug was crystalline in powder form, however converted into amorphous form when entrapped in SLNs. Enhanced dissolution and bioavailability of ezetimibe was observed from ezetimibe-loaded SLNs as compared to marketed product and drug suspension. Stability studies revealed that the formulation remains unchanged for 3 months. Thus SLN is a suitable carrier for ezetimibe with enhanced dissolution and bioavailability as compared to the marketed product.