An Investigation on Liver-Targeting Microemulsions of Norcantharidin
An Investigation on Liver-Targeting Microemulsions of Norcantharidin
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DOI：
10.1080/10717540500176829
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发表时间：
2005-01
期刊：
影响因子：
6
通讯作者：
Li Zhang;Xun Sun;Zhirong Zhang
中科院分区：
文献类型：
--
作者：
Li Zhang;Xun Sun;Zhirong Zhang
针对去甲斑泻素(NCTD)注射剂常引起泌尿器官损害的临床事实，我们制备了NCTD w/o微乳，以改善其溶解度，提高NCTD的活体摄取。最佳微乳配方为：7%水、45%大豆卵磷脂/乙醇(2：1)、油酸乙酯，微乳粒径为44.5±8.6 nm。药代动力学研究表明，NCTD微乳在小鼠体内的循环时间相对较长，单次静脉注射5 mg/kg后，NCTD微乳的循环时间较NCTD注射剂长。肝脏的整体靶向效率由3.66%提高到6.10%。这些结果表明NCTD微乳系统是治疗肝源性疾病的一种有前途的候选药物。
Based on the clinical fact that norcantharidin (NCTD) injection frequently causes urinary organ damnification, we prepared a NCTD w/o microemulsion as an alternative to improve the solubility and enhance the live uptake of NCTD. The optimal microemulsion formulation consisted of 7% water, 45% soybean lecithin/ethanol (2:1), and ethyl oleate, with the droplet size of 44.5 ± 8.6 nm. Pharmacokinetics study showed that NCTD microemulsion had relatively longer circulating time in mice than NCTD injection after a single intravenous injection at a dose of 5 mg/kg. Moreover, the overall drug targeting efficiency of liver was enhanced from 3.66% to 6.10%. These results suggest that a NCTD microemulsion system is a promising candidate for the treatment of hepatogenic diseases.