1. Oral bioavailability of cantharidin-loaded solid lipid nanoparticles.
- Author
-
Yun-Jie Dang and Chun-Yan Zhu
- Subjects
- *
ANIMAL experimentation , *BIOAVAILABILITY , *CANTHARIDES , *DRUG delivery systems , *ELECTRON microscopy , *GAS chromatography , *MASS spectrometry , *NANOPARTICLES , *ORAL drug administration , *RATS , *DESCRIPTIVE statistics - 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. [ABSTRACT FROM AUTHOR]
- Published
- 2013
- Full Text
- View/download PDF