离子诱导结合化学交联法制备壳聚糖纳米粒及其作为药物靶向-Core.PDF

1, 2 1 1 1* 陈娟 , 胡权 , 侯振清, 张其清 ( 1, 361005; 2, 361004) : 制备粒径相对可控的壳聚糖纳米粒, 探索其在药物缓释体 中的应用 以多聚磷酸钠为离子诱导剂戊 二醛为化学交联剂, 通过离子诱导结合化学交联法, 制备壳聚糖纳米粒; 在 1乙基( 3二甲氨基丙基)碳二亚胺盐酸盐( EDC ) 作用下, 分别进行丝裂霉素载药以及聚乙二醇( PEG), 叶酸修饰; 另外, 对载药纳米粒子进行不同 pH 条件下的体外释药实验; 对PEG, 叶酸修饰的壳聚糖纳米粒罗丹明 B荧光标记后, 进行激光共聚焦以及活体成像实验 离子诱导交联法可以获 得粒径范围在 200~ 500 nm 的壳聚糖纳米粒; 丝裂霉素载药量可以达到 25% , 包封率为 50% , 体外释药呈现突释和缓释双相 特征, 并且随着 pH 的升高释药明显加快; 未经修饰的叶酸修饰的以及 PEG和叶酸修饰的纳米粒都能有效的进入H ela细胞, 而单独 PEG修饰的却很少进入细胞内; 叶酸修饰的纳米粒有明显的靶向作用, PEG修饰的纳米粒可以明显延长实验裸鼠血液 中循环时间 采用离子诱导结合化学交联法可以获得粒径可控稳定适合于主动靶向给药的壳聚糖纳米粒 : 壳聚糖; 离子诱导交联法; 制备; 丝裂霉素; 靶向缓释 : R944 : A : 100 1- 2494( 2010) 18- 1400- 04 Preparation of Chitosan Nanoparticles for Targeting and SustainedDrug Delivery System by Ioninduced Combinedwith Chem icalCrosslinking 1, 2 1 1 1* CHEN Juan , HU Quan , HOU Zhenqing , ZHANG Q iq ing ( 1R esearch Center of B iomed icalEng ineering, X iamen University,X iamen 361005, China; 2ZhongshanH osp ital, X iamen University,X iamen 361004, China) ABST ACT: OBJECTIVE T o prepare hitosan nanoparti le w ith ontrollab le size and investigate its appli ations to targeting and sustained drug delivery systemMETHODS The omb ination of an ionindu ed and hem i al rosslinking m ethod w as used to pre pare hitosan nanoparti les, and m itom y in C, PEG and foli a id w ere bound ovalently on the surfa e of hitosan nanoparti les in the presen e of 1ethyl3( 3d mi ethyllam inopropyl) arbod imi ide hydro h loride ( EDC ), respe tivelyIn vitro drug release testw as arried out in different pH PBS solution Con fo al laser s anning m i ros ope of H ela ell and in vivo mi aging test were arried out using PEG and foli a idm odified hitosan nanoparti les labeled by Rhodam ine B ESULTS The d iam eter was in the range