多西他赛皮下注射缓释凝胶的制备及其体外释放行为研究

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目的以pH/温度双重敏感嵌段共聚物OSM1-PCLA-PEG-PCLA-OSM1为载体,制备多西他赛缓释凝胶,并研究其体外释药行为。方法考察空白凝胶体外溶蚀情况;采用薄膜分散法制备多西他赛缓释凝胶,观察载药共聚物胶束形态,并进行体外释放考察。结果多西他赛缓释凝胶体外释放持续16d,不同共聚物浓度、不同载药量缓释凝胶中多西他赛第16天平均累积释放百分量分别为88.22%,84.06%,81.79%和78.78%,81.79%,87.51%。体外释放模型拟合符合零级释放动力学特征,满足以溶蚀、扩散相结合的释药模式。结论以pH/温度双重敏感嵌段共聚物OSM1-PCLA-PEG-PCLA-OSM1为载体制备的多西他赛缓释凝胶具有良好的缓释效果。 OBJECTIVE To prepare docetaxel sustained-release gel with pH / temperature dual-sensitive block copolymer OSM1-PCLA-PEG-PCLA-OSM1 and to study its in vitro release behavior. Methods The in vitro dissolution of blank gel was investigated. The docetaxel sustained-release gel was prepared by thin-film dispersion method. Morphology of drug-loaded copolymer micelles was observed and investigated in vitro. Results The sustained release of docetaxel sustained-release gel in vitro for 16 days showed that the average cumulative release percentage of docetaxel on the 16th day was 88.22%, 84.06% and 81.79% at different copolymer concentrations and sustained-release gels, respectively. And 78.78%, 81.79% and 87.51% respectively. The in vitro release model fit the zero-order release kinetics to meet the release mode combined with dissolution and diffusion. CONCLUSION Docetaxel sustained-release gel with pH / temperature dual-sensitive block copolymer OSM1-PCLA-PEG-PCLA-OSM1 as carrier has a good sustained release effect.
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