论文部分内容阅读
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: According to the demand of immunosuppressive therapy after corneal transplantation, we prepared the sustained-release microspheres containing cyclosporine A with small particle size for local ophthalmic administration and investigated its release in vitro. Methods: Sodium alginate and chitosan were used as carrier materials to prepare small particle size cyclosporin A microspheres by electrostatic droplet technology. Surfactant was added to the preparation system to optimize the formulation process and scan The morphology of microspheres was observed by electron microscopy and the release characteristics of microspheres in vitro were investigated by dynamic dialysis. Results: The prepared microspheres had good morphology, narrow particle size distribution, mean diameter of (12.4 ± 0.8) μm, entrapment efficiency of (82.8 ± 1.8)% and drug loading of (50.1 ± 1.2)% Higuchi equation fitted best. CONCLUSION: The chitosan-alginate containing cyclosporin A with good sphericity, small particle size, high entrapment efficiency and high drug loading was prepared by electrostatic droplet technology by reducing the surface tension of the prepared system. Release microspheres, the resulting drug release in vitro compliance with the proliferation mechanism.