中国药理学通报2012，Vol.28Issue(9)：1314-1318,5.DOI:10.3969/j.issn.1001-1978.2012.09.030
盐酸小檗碱纳米脂质体的优化制备方法及其体外细胞毒性研究
The optimized preparative method of berberine hydrochloride nanoliposome and its in vivo cytotoxicity
摘要
Abstract
Aim To optimize the preparation conditions of berberine hydrochloride liposome, in order to improve its bioavail-ability and to alleviate its toxicity. Methods The BH nanoliposome were prepared by optimized active loading method. Furthermore, the entrapment efficiency, partical size and shape of those liposome were investigated. The biological safety of the liposome was evaluated by MTT assay. Results The optimized preparative protocol of BH nanoliposome was that the ratio of the quantity of Lecithin and Cholesterol was 3 to 1, the BH content of those nanoliposome was 0. 8 g · L-1 , and the hatch temperature was 60℃. The cell survival rate was maintained at more than 80% 48 hours after treated by low concentration ( ≤20 mg · L-1 ) BH nanoliposome sample. Conclusions The entrapment efficiency of the liposome prepared by the optimized process is 83 % and the partical size ( 90 nm or thereabouts ) becomes smaller than that of the reported which can improve the bioavailability of drugs. The toxic effects of the BH nanoliposome on Hela cells is less than that of the pure berberine within 48 hours, which indicates that this improved preparative method of the nanoliposome may help to improve the safety of the drug.关键词
主动载药法/盐酸小檗碱/纳米脂质体/生物安全性/生物利用度/细胞毒Key words
active loading method/ berberine hydrochloride/ nanoliposome/ biological safety/ bioavailability/ cytotoxicity分类
医药卫生引用本文复制引用
李彩虹,王俊玲,周克元..盐酸小檗碱纳米脂质体的优化制备方法及其体外细胞毒性研究[J].中国药理学通报,2012,28(9):1314-1318,5.基金项目
广东省中医药局科研项目(No ZY1008) （No ZY1008）
湛江市科技攻关计划项目(No 2009C3106013) （No 2009C3106013）
东莞市科技计划项目(No 200910815261) （No 200910815261）
广东医学院青年基金项目(No XQ0816) （No XQ0816）
