Abstract
Current study explores the potential of nanostructured lipid carriers (NLCs) for bioavailability enhancement of ezetimibe on oral administration. Microemulsion technique was employed for the development of NLCs. Along with NLC, a nanoemulsion of ezetimibe was also prepared and compared with optimized NLC for morphology and in vitro release. An aqueous dispersion of the optimized NLC was transformed into a stable free-flowing solidified-NLC (S-NLC) by adsorbing it on Neusilin® US2. The S-NLC was evaluated for differential scanning calorimetry (DSC), X-ray diffraction (XRD), scanning electron microscopy (SEM), drug content, dissolution profile, pharmacodynamics and pharmacokinetics in rats. DSC and XRD studies showed reduced crystallinity of ezetimibe in the form of S-NLC. SEM study supports these results, as no drug precipitation was observed on the carrier surface. Dissolution study exhibited a notable rise in the dissolution of the drug from S-NLC as compared to pure drug and marketed tablet. In vivo evaluation in rats revealed a significant reduction in the level of total cholesterol as compared to positive control and drug suspension group, whereas for high-density lipoprotein, non-significant change was observed. Pharmacokinetics study showed a significant rise in the bioavailability of ezetimibe using NLC formulation as compared to the suspension and marketed tablet.
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