Oral bioavailability of cantharidin-loaded solid lipid nanoparticles

Abstract

Background: The clinical application of cantharidin (CA) is limited by its insolubility, toxicity and short half-life in circulation. This study aims to achieve a steady and sustained blood concentration-time profile, using solid lipid nanoparticles (SLNs) as a drug carrier.Methods: CA-SLNs were prepared by a film dispersion-ultrasonication method. The physiochemical properties were studied by transmission electron microscopy. In vitro release and in vivo evaluation of CA-SLNs were studied by GC and GC-MS, while a comparison of the pharmacokinetic properties between CA-SLNs and free CA was performed in rats.Results: The mean size, drug content and encapsulation yield of CA-SLNs were 121 nm, 13.28 ± 0.12% and 93.83 ± 0.45%, respectively. The results show that CA-SLNs had a sustained release profile without a burst effect, a higher bioavailability than free CA after oral administration, and that the relative bioavailability of CA-SLNs to free CA was 250.8%.Conclusion: CA-SLNs could improve the solubility and oral bioavailability of CA. © 2013 Dang and Zhu; licensee BioMed Central Ltd.