摘要
目的:针对角膜移植术后免疫抑制治疗需求,制备眼部局部给药的小粒径载环孢素A缓释微球,并进行体外释放考察。方法:以海藻酸钠、壳聚糖为载体材料,采用静电液滴工艺,通过向制备体系添加表面活性剂,制备小粒径载环孢素A微球,设计正交试验优化处方工艺,扫描电镜观察微球表面形态,动态透析法考察微球的体外释放特性。结果:所制微球形态良好,粒径分布窄,平均粒径为(12.4±0.8)μm,包封率为(82.8±1.8)%,载药量为(50.1±1.2)%,体外释放行为用Higuchi方程拟合效果最好。结论:采用静电液滴工艺,通过减小制备体系的表面张力,制备了球形度优良、粒径小、包封率和载药量较高的载环孢素A的壳聚糖-海藻酸盐缓释微球,所得制剂的体外释药规律服从扩散机制。
OBJECTIVE To prepare microspheres loaded cyclosporin A for corneal transplantation immunosuppressive thera pies and investigate the drug release behavior in vitro. METHODS The small particle size microspheres were prepared with alginate and ehitosan as carrier through impulsive electrostatic technique by adding surface active agent to the preparation system which was optimized by orthogonal design. The morphology of microspheres was observed by SEM and the drug-release behav iour in vitro was conducted with dynamic dialysis. RESULTS The optimized microspheres assumed a good sphericity and uniformly particle size distribution. The average diameter, entrapment efficiency and drug loading of the microspheres were （12. 4 ±0. 8） m, （82. 8 ±1.8）% and （50. 1 ±1.2）%, respectively. The behavior of drug release was accorded with the Higuchi ki netics equation. CONCLUSION The calcium alginate-chitosan microspheres with good sphericity, small size, high encapsulation efficiency and drug loading which obey the diffusion mechanism in vitro release were successfully prepared by impulsive electrostatic technique through reducing the surface tension of preparation system.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2011年第17期1424-1429,共6页
Chinese Journal of Hospital Pharmacy
基金
陕西省"13115"科技创新工程重大科技专项(编号:2008ZDKG-58)
关键词
环孢素A
海藻酸盐
壳聚糖
微球
静电液滴工艺
体外释放
cyclosporin A
sodium alginate
chitosan
microsphere
electrostatic droplet generation technique
in vitro release
