文献类型：期刊文献

中文题名：马钱子碱脂质体透皮制剂的安全性及药效学研究

英文题名：Study on Safety and Pharmacodynamic Action of Transdermal Liposomal Brucine

作者：秦湘奇[1];袁媛[1];刘昌胜[1];王秋云[2];沈晰[1];杨柏灿[2]

机构：[1]教育部生物医用材料工程中心,华东理工大学生物材料研究所,上海200237;[2]上海中医药大学中药学院中药教研室,上海201203

年份：2008

卷号：25

期号：6

起止页码：1358

中文期刊名：生物医学工程学杂志

外文期刊名：Journal of Biomedical Engineering

收录：MEDLINE(收录号：19166209);CSTPCD;;Scopus;北大核心:【北大核心2004】；CSCD:【CSCD2011_2012】；PubMed;

基金：上海市纳米专项资助课题(0352nm115,0552nm007)

语种：中文

中文关键词：马钱子碱脂质体;急性毒性;过敏性;镇痛;抗炎

外文关键词：Liposomal Brucine（LB） Acute toxicity Allergic Analgesic Anti-inflammatory

摘要：采用乙醇滴入法制备平均粒径为54 nm、包封率为72%的马钱子碱脂质体;以同剂量纯马钱子碱为对照,考察马钱子碱脂质体透皮制剂的皮肤急性毒性,皮肤过敏性,镇痛抗炎效果以及在240 min内的作用持续性。结果显示:所制备的透皮制剂无皮肤急性毒性、无皮肤致敏性,毒性显著低于普通马钱子碱;镇痛抗炎效果好于同剂量的马钱子碱溶液,且呈现良好的剂量相关性,相同时间内本制剂比同剂量马钱子碱药效更持久。由此可见,脂质体包覆能有效降低马钱子碱的毒性,提高其镇痛抗炎疗效,同时实现药物的长效作用。
Liposomal Brucine （LB） with high encapsulation efficiency （72 % ） and small particle diameter （mean particle diameter, 54 nrn） was prepared by ethanol-dripping method. The safety and pharmacodynamic action of LB,a new transdermal preparation, were investigated in details with the use of white rabbits, guinea-pigs and mice, respectively. The tests revealed that LB had no acute toxicity to integral and broken skin, and had no allergic effects on skin. In writhing test, the analgesic effect of LB was higher than that of free brucine. The anti-inflammatory activity of LB was significantly higher than that of free brucine （P〈 0.01）. Meanwhile, LB exhibited a better dose-response manner and a longer duration of analgesic effects. In conclusion, LB could reduce the toxicity of brucine, enhance the analgesic and antiinflammatory effects of brucine, and achieve its sustained-release.