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