Oral bioavailability of cantharidin-loaded solid lipid nanoparticles

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.