雷公藤甲素叶酸-壳聚糖纳米粒的制备及其释药性能考察  

Preparation and in vitro Release Investigation of Triptolide-Folic Acid Chitosan Nanoparticle

作　　者：童文婷[1] 刘波[1] 张睿 徐彭[1] 管咏梅[1] 聂斌[1] 谈伟锋[1] 

机构地区：[1]江西中医学院,南昌330004 [2]江西工程职业学院,南昌330006

出　　处：《中国实验方剂学杂志》2012年第22期49-52,共4页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：江西省教育厅科学技术研究项目(GJJ11543);江西省卫生厅科技计划项目(20112026)

摘　　要：目的:制备具有靶向性的雷公藤甲素叶酸-壳聚糖纳米粒,并考察其体外释药性能。方法:以粒径和PDI为指标,采用单因素试验和正交试验法,考察溶液pH值、反应温度、壳聚糖和多聚磷酸钠的比例及质量浓度对壳聚糖纳米粒的制备工艺的影响;通过雷公藤甲素与壳聚糖的偶联比及雷公藤甲素、叶酸活性酯和壳聚糖上的氨基反应确定最佳制备工艺,采用离子交联法制备雷公藤甲素叶酸-壳聚糖纳米粒。采用HPLC考察其体外释药特性。结果:最佳制备工艺为反应温度25℃,溶液pH 3.5,壳聚糖-多聚磷酸3∶1,壳聚糖与多聚磷酸钠的质量分数均为0.3%,制得的纳米粒平均粒径约170 nm,粒子分散指数(PDI)约0.21。载药纳米粒的释放率于4 h后达平衡,最大释药率约68%。结论:按优选工艺制备的雷公藤甲素叶酸-壳聚糖纳米粒质量稳定可靠,优选的工艺简便易行。Objective： To prepare triptolide- folic acid chitosan nanoparticle with targeting, and study on its in vitro release property. Method： With particle size and PDI as indexes, influence of solution pH, reaction temperature, proportion and mass concentration of chitosan and sodium polyphosphate on preparation technology of chitosan nanoparticle were investigated by single factor test and orthogonal design; Optimum preparation technology was selected by coupling ratio of triptolide and chitosan, amino reaction of triptolide, folie acid active ester and chitosan, triptolide-folic acid chitosan nanoparticle was prepared by ionic crosslinking method. In vitro release property was examined by HPLC. Result： Optimum preparation technology was as following： reaction temperature 25 ~C , solution pH of 3.5, chitosan-sodium polyphosphate 3： 1, the mass concentration of chitosan and sodium polyphosphate of all 0. 3%. Average particle size of prepared nanoparticle was about 170 nm, PDI was about 0.21. Release rate of drug-loading nanoparticle reached equilibrium after 4 h, the maximum release rate was about 68%. Conclusion： Quality of triptolide-folie acid chitosan nanoparticle was stable and reliable, which was prepared by optimized preparation technology, and optimized technology was simple.

关 键 词：雷公藤甲素 叶酸 壳聚糖 纳米粒 正交设计 体外释放 

分 类 号：R283.6[医药卫生—中药学]