原创力文档oral bioavailability of cantharidin-loaded solid lipid nanoparticles口服生物利用度cantharidin-loaded固体脂质纳米粒.pdf
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oral bioavailability of cantharidin-loaded solid lipid nanoparticles口服生物利用度cantharidin-loaded固体脂质纳米粒
Dang and Zhu Chinese Medicine 2013, 8:1
/content/8/1/1
RESEARCH Open Access
Oral bioavailability of cantharidin-loaded solid
lipid nanoparticles
*
Yun-Jie Dang and Chun-Yan Zhu
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.
Background There are many kinds of Mylabris-based pharmaceut-
Mylabris, the dry body of Mylabris phalerata Pallas or ical preparations on the Chinese market, such as com-
Mylabris cichorii Linnaeus , is recorded in the People’s pound Mylabris injection (Aidi injection, State Permit
Republic of China Pharmacopoeia as having an antican- No. and compound Mylabris capsules (State
cer
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