title: 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%.
  
  
  CONCLUSIONS
  CA-SLNs could improve the solubility and oral bioavailability of CA.
authors.affiliation: 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. cuzhu@implad.ac.cn.
authors.forename: Yun-Jie
authors.initials: YJ
authors.lastname: Dang
authors.forename: Chun-Yan
authors.initials: CY
authors.lastname: Zhu