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目的制备吲哚美辛聚乳酸-羟基乙酸共聚物(PLGA)/Eudragit RS 100眼用缓释微球,并进行表征。方法采用O/W溶剂挥发法制备吲哚美辛PLGA/Eudragit RS 100微球,对微球的表面形态、载药量、包封率、体外释放特点、粒径、有机溶剂残留量、表面电位进行了表征分析,使用人视网膜色素上皮细胞(RPE cells)评估空白微球的细胞毒性。结果载体材料PLGA与Eudragit RS 100质量比为1∶3的吲哚美辛微球,电镜观察颗粒分布均匀,表面光滑;平均粒径为(1 676.4±739.5)nm;载药量为(18.79±0.19)%,包封率为(98.25±2.11)%,第1天存在突释,随后可以缓慢释放一个月左右;有机残留量平均为(267.33±13.57)ppm;空白微球表面电位为正电荷;空白微球无细胞毒性。结论吲哚美辛PLGA/Eudragit RS 100眼用缓释微球具有包封率高,粒径窄,体外释放缓慢,安全性好等特点,具有很好的临床应用前景。
Objective To prepare and characterize indomethacin PLGA / Eudragit RS 100 ocular sustained-release microspheres. Methods Indomethacin PLGA / Eudragit RS 100 microspheres were prepared by O / W solvent evaporation method. The morphology, drug loading, entrapment efficiency, in vitro release characteristics, particle size, residual organic solvent, surface potential Characterization analyzes were performed to evaluate the cytotoxicity of blank microspheres using human retinal pigment epithelial cells (RPE cells). Results The indometacin microspheres with the mass ratio of PLGA to Eudragit RS 100 was 1: 3. The particles were uniformly distributed and the surface was smooth under electron microscope. The average diameter was (1 676.4 ± 739.5) nm and the drug loading was (18.79 ± 0.19)%. The entrapment efficiency was (98.25 ± 2.11)%. There was a sudden release on the first day and then slowly released for about a month. The average residual organic content was (267.33 ± 13.57) ppm. Blank microspheres have no cytotoxicity. Conclusion Indomethacin PLGA / Eudragit RS 100 Ophthalmic sustained-release microspheres have the characteristics of high encapsulation efficiency, narrow particle size, slow release in vitro and good safety. It has good clinical application prospects.