Rosuvastatin loaded nanostructured lipid carrier: For enhancement of oral bioavailability

Abstract

Rosuvastatin is a lipid lowering agent, which has low solubility and low bioavailability of 20% with oral administration. Therefore the present study was undertaken to improve solubility and bioavailability of Rosuvastatin by formulating it into Nano structured lipid carriers (NLCs) by using stearic acid and Compritol ATO 888 as solid-lipid, Oleic acid as liquid-lipid and Poloxamer 188 as a surfactant. Rosuvastatin loaded NLCs were prepared by high shear homogenisation followed by Ultra sonication technique. In this study two solid lipids (stearic acid and Compritol ATO 888) were compared with liquid lipid in different concentration in order to select suitable solid liquid lipid for Rosuvastatin to achieve particle size in nano range. The prepared NLCs were evaluated for particle size and size distribution, Poly dispersity index, drug content, entrapment efficiency, zeta potential, In-vitro drug release, In-vivo bioavailability study in rat. The drug content for the formulation F1 to F8 was found to be in the range of 83.18 to 96.59%. The formulation F3 was optimised based on the mean particle size, poly dispersity index, entrapment efficiency and zeta potential which showed 213.26 nm, 0.22, 89.1% and -50.6 respectively. Transmission electron microscopy (TEM) studies on formulation F3 revealed that all the particles were within the nano size range. Formulation F3 showed In-vitro drug release of 76.22% at the end of 12 hrs with a sustained release. HPLC method was developed for determination of Rosuvastatin calcium in rat plasma for bioavailability and pharmacokinetic evaluation. The relative bioavailability of NLC formulation F3 showed an enhanced bioavailability with two folds as compared to the marketed conventional tablet. The stability study was carried at 4ºC with 65% RH for 30 days showed no change in the particle size, entrapment efficiency and In-vitro drug release.