眼用环孢霉素A缓释超微粒的制备及眼内分布研究  

Preparation of nanoparticles of chitosan loaded with cyclosporine A and distribution in the eye

作　　者：原艳波 原续波[2] 李弘[3] 苗春秀[1] 王来好[1] 常津[2] 盛京[2] 

机构地区：[1]山西长治医学院附属医院,长治046000 [2]天津大学材料科学与工程学院 [3]南开大学吸附与分离功能高分子材料国家重点实验室

出　　处：《中国中医眼科杂志》2005年第1期20-22,共3页China Journal of Chinese Ophthalmology

基　　金：山西省教委高校科技开发项目(200214);国家自然科学基金青年基金项目(50301008)

摘　　要：目的探讨壳聚糖-胆固醇双亲性聚合物包载环孢霉素A的缓释性及超微粒制备及眼内分布。方法壳聚糖-胆固醇双亲性聚合物与环孢霉素A共溶于溶剂中,对水透析形成超微载药微粒,37℃条件下测试超微粒体外释放状态。以放射性99锝标记壳聚糖超微粒,制成滴眼剂,以SPECT测试超微粒在兔眼中的滞留时间。结果壳聚糖载药超微粒可在6小时内缓释环孢霉素A,超微粒在给药后4小时在眼表具有良好的滞留性。结论以壳聚糖双亲性聚合物包载环孢霉素A对干眼症的治疗具有潜在的应用价值。OBJECTIVE To assess the control release of cyclosporine A from nanoparticles composed of chitosan-g-cholesterol amphiphilic polymer,and the distribution of nanoparticles in the eye.METHODS Nanoparticles loading cyclosporine A were prepared by added chitosan amphiphilic polymer and cyclosporine A into co-solvent,and then dialyzed against water,the control releasing behavior in-vitro were studied at 37℃.Chitosan nanoparticles were labelled with 99Te,and the distribution of nanoparticles were studied by SPECT technology.RESULTS The releasing of cyclosporine A can be control by chitosan nanoparticles within 6 hours,and the nanoparticles showed prolonged percorneal residence time within experiment time(4 hours).CONCLUSION Chitosan nanoparticle is a potential vehicle for the improvement of the delivery of cyclosporine A to the ocular mucosa.

关 键 词：壳聚糖 超微粒 环孢霉素A 干眼症 

分 类 号：R979.5[医药卫生—药品] R988.1[医药卫生—药学]