论文部分内容阅读
目的:制备重组人血管内皮抑制素(恩度)缓释微球,并对微球理化性质及体外释放行为进行初步考察。方法:采用乳化溶剂挥发法(W/O/O)制备恩度载药微球;对微球载药量、粒径、突释、体外释放速率及降解行为进行考察,同时利用凝胶电泳初步评价体外释放过程中恩度的完整性。结果:增加聚乳酸-羟基乙酸嵌段共聚物(PLGA)中羟基乙酸的比例、提高PLGA浓度、降低内水相体积、提高理论载药量均增加微球载药能力;降低内水相体积、提高分散速度均减小突释。增加PLGA中羟基乙酸的比例,30 d时累积释放可增加到65%。降解实验说明释放初期微球主要以扩散方式释放恩度,释放后期主要表现为微球的降解。凝胶电泳结果表明微球制备过程对蛋白质聚集性的影响不大。结论:用PLGA作为载体材料制备微球,可以延缓恩度的释放。
OBJECTIVE: To prepare sustained-release microspheres with recombinant human endostatin (Endostar) and to investigate the physico-chemical properties and in vitro release behavior of the microspheres. Methods: Endemic drug-loaded microspheres were prepared by emulsion solvent evaporation (W / O / O) method. The drug loading, particle size, burst release, in vitro release rate and degradation behavior of microspheres were investigated. To evaluate the integrity of grace during in vitro release. Results: Increasing the proportion of glycolic acid in PLGA, increasing the concentration of PLGA, decreasing the volume of inner aqueous phase and increasing the theoretical drug loading all increased the drug loading ability of microspheres; decreasing the volume of inner aqueous phase, Increase the speed of dispersion are reduced burst. Increasing the proportion of glycolic acid in PLGA increased the cumulative release to 65% at 30 days. Degradation experiments showed that the initial release of microspheres mainly by the release of the proliferation of grace, the latter part of the release of microspheres mainly for the degradation. The results of gel electrophoresis showed that the microsphere preparation process had little effect on the protein aggregation. Conclusion: Preparation of microspheres using PLGA as a carrier material can delay the release of grace.