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Open Access Research

Oral bioavailability of cantharidin-loaded solid lipid nanoparticles

Yun-Jie Dang and Chun-Yan Zhu*

Author Affiliations

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

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Chinese Medicine 2013, 8:1  doi:10.1186/1749-8546-8-1

Published: 8 January 2013

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.