Oral bioavailability of cantharidin-loaded solid lipid nanoparticles
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, No. 151 Malianwa North Road, Haidian District, Beijing, 100094, P. R. China
Chinese Medicine 2013, 8:1 doi:10.1186/1749-8546-8-1Published: 8 January 2013
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.
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.
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%.
CA-SLNs could improve the solubility and oral bioavailability of CA.