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

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.