环孢素A-pH敏感性纳米粒的制备工艺和体外释药特性  

Study on preparation and releasing characteristics of Cyclosporin A pH sensitive nanoparticles in vitro

作　　者：杨志强[1] 许洁[1] 潘萍[1] 张学农[1] 王毅[1] 

机构地区：[1]苏州大学药学院,苏州215123

出　　处：《中国新药杂志》2008年第20期1783-1786,共4页Chinese Journal of New Drugs

基　　金：江苏省科技厅社会发展项目资助(BS200522);江苏省高校高新技术产业发展项目资助(JHB05-46);江苏省卫生厅招标课题(H200630)

摘　　要：目的:研究环孢素A-pH敏感性纳米粒的制备方法和体外释药特性。方法:采用乳化-溶剂扩散技术结合正交实验设计制备了环孢素A-pH敏感性纳米粒;超速离心法测定纳米粒的包封率,并对其粒径、表面形态、体外释药和稳定性影响因素进行考察。结果:环孢素A-pH敏感性纳米粒的包封率为99.7%;平均粒径为44.8 nm;透射电镜下呈均匀规则的圆球型;体外释放实验中,当pH>6时,药物能迅速的释放出来。结论:pH敏感性纳米粒有望开发成为一种新型环孢素A纳米制剂。Objective：To study the preparation and releasing characteristics of cyclosporine A-Eudragit S100-Nanoparticles （CyA-NP） in vitro. Methods：Ethanol-injection technique and orthogonal experimental design was introduced to prepare CyA-NP. The encapsulation efficiency was determined by separating nanoparticles from dispersed aqueous medium by ultracentrifugation. The particle size,superficial appearance and drug release profile of CyA-NP in vitro were measured while the stability was investigated. Results：The particles exhibited satisfied mean particle size of 44.8 nm with the encapsulation efficiency over 99.7%. The load-drug nanoparticles was spherical observed by the transmission electric microscope （TEM）. The drug released from nanoparticles was burst when the medium pH was above 6.0. Conclusion：pH-sensitive Eudragit S100 was a potential drug vehicle for developing a high performance CyA nanoparticle carrier system.

关 键 词：环孢素A pH敏感性纳米粒 体外释放 

分 类 号：R943.41[医药卫生—药剂学] R979.5[医药卫生—药学]