逐层自组装微囊对甲氨蝶呤的体外可控释放研究  

Controlled release of methotrexate drug in vitro via layer-by-layer self-assembled vesicles

作　　者：白志军[1] 刘雨双 郭俊[1] 侯静[1] 赵欣敏 张峰[1] 

机构地区：[1]内蒙古农业大学生命科学学院,呼和浩特010018

出　　处：《中国科学：化学》2015年第8期836-842,共7页SCIENTIA SINICA Chimica

基　　金：国家自然科学基金(21171086;81160213);内蒙古自治区草原英才工程项目(108-108038);内蒙古科技厅(211-202077);内蒙古农业大学(109-108040;211-109003;211-206038)资助

摘　　要：高装载率和可控释放的药物传送系统具有很好的生物医学应用前景.本文研究了逐层自组装技术对抗肿瘤药物甲氨蝶呤(MTX)的装载与控释.利用不同颜色的发光量子点将甲氨蝶呤与高分子聚电解质进行标记后,通过添加Tween 80一锅法制备出平均粒径约500 nm,装载率为54.82%的MTX碳酸钙颗粒,并以此为模板制备出了可酸度控释的MTX药物微囊.探讨了酸度、逐层自组装层数、药物分子的标记等因素与可控释放的密切关系及相关机理.此项研究可为MTX药物微囊的细胞内实验及生物体内的应用奠定实验基础.Drug delivery systems with high loading and controllable release hold promises for biomedical applications. Here in this paper, we studied on the loading and controlled release of methotrexate（MTX） by using layer-by-layer self-assembly technology. After labeling MTX and the polyelectrolyte by photoluminescent quantum dots with different colors, MTX-calcium carbonate particles with an average diameter of 500 nm and 54.82% MTX loading rate were prepared by one-pot synthesis with the addition of Tween 80, which subsequently acted as the templates for preparing the p H-controlled-release MTX drug vesicles. We also discussed how the factors such as pH, layers of polyelectrolytes and the labeling of MTX influence the controllable release and the corresponding mechanisms. The information might provide some experimental basis for the future intracellular trials and in vivo applications of MTX drug vesicles.

关 键 词：碳酸钙颗粒 甲氨蝶呤 逐层自组装 药物微囊 可控释放 

分 类 号：TQ460.1[化学工程—制药化工]