Oral bioavailability of cantharidin-loaded solid lipid nanoparticles.
Oral bioavailability of cantharidin-loaded solid lipid nanoparticles.
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DOI：
10.1186/1749-8546-8-1
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发表时间：
2013-01-08
期刊：
影响因子：
4.9
通讯作者：
Zhu CY
中科院分区：
文献类型：
--
作者：
Dang YJ;Zhu CY
由于其难溶性、毒性和在循环中半衰期短等原因，限制了其临床应用。本研究旨在以固体脂质纳米粒（SLNs）为药物载体，获得稳定、持续的血药浓度-时间曲线。采用薄膜分散-超声法制备CA-SLN。用透射电子显微镜研究了其理化性质。采用GC和GC-MS法研究了CA-SLN的体外释放和体内评价，并比较了CA-SLN和游离CA在大鼠体内的药代动力学特性。CA-SLN的平均粒径为121 nm，载药量为13.28 ± 0.12%，包封率为93.83 ± 0.45%。结果表明，CA SLN具有缓释作用，无突释效应，口服后的生物利用度高于游离CA，CA SLN相对于游离CA的相对生物利用度为250.8%。CA-SLNs可提高CA的溶解度和口服生物利用度。
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. 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. 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%. CA-SLNs could improve the solubility and oral bioavailability of CA.
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影响因子：
--
作者：
CRAVEN, JD;POLAK, A
通讯作者：
POLAK, A
DOI：
10.1358/mf.2010.32.3.1423886
发表时间：
2010-04-01
影响因子：
--
作者：
Dang, Y. J.;Hu, C. H.;Zhu, C. Y.
通讯作者：
Zhu, C. Y.
影响因子：
6.4
作者：
Zhang, JP;Ying, K;Rui, YC
通讯作者：
Rui, YC
影响因子：
--
作者：
OAKS, WW;DITUNNO, JF;MILLS, LC
通讯作者：
MILLS, LC
影响因子：
6.1
作者：
MATSUZAWA, M;GRAZIANO, MJ;CASIDA, JE
通讯作者：
CASIDA, JE