development of novel rosuvastatin nanostructured lipid carriers for oral delivery in an animal model

Jun Li,1,2,* Min Yang,2,* Wenrong Xu1 1School of Medical Science and Laboratory Medicine, Jiangsu University, Zhenjiang 212013, Jiangsu, China; 2Department of Intensive Care Unit, Chest Hospital Affiliated to Shanghai Jiaotong University, Shanghai 200030, China *These authors contributed equally to this work Objective: The aim of this study was to prepare rosuvastatin nanostructured lipid carriers (RST-NLCs) in order to increase the bioavailability of RST.Materials and methods: RST-NLCs were prepared by hot melt high-pressure homogenization method. The physicochemical parameters of RST-NLCs were characterized in terms of particle size, zeta potential, morphology, entrapment efficiency, and in vitro release behavior.Results: The mean particle size was found to be 98.4±0.3 nm. The entrapment efficiency was 84.3%±1.3%. The RST was slowly released from NLCs over a period of 48 h in the PBS. A similar phenomenon was also observed in a pharmacokinetic study in rats, in which the area under the curve of NLCs was 1.65-fold higher than that of tablet powder.Conclusion: The results of pharmacodynamics showed that the effective lipid-lowering activity of NLCs could be explained by the fact that NLCs resulted in sustained release of RST, which could have increased absorption and provided a higher bioavailability. Keywords: rosuvastatin, nanostructured lipid carriers, hot melt high-pressure homogenization, pharmacokinetic, pharmacodynamics