pH敏感型mPEG-Hz-PLA聚合物纳米载药胶束的制备

发布时间：2018-06-11 13:34

  本文选题：mPEG-Hz-PLA聚合物 + 胶束　； 参考：《高分子学报》2017年03期

【摘要】：以合成的含有腙键的聚乙二醇大分子(mPEG-Hz-OH)为引发剂,以丙交酯为单体引发开环聚合反应,并通过调整投料比,制备出3种不同分子量的含腙键的生物可降解嵌段聚合物(mPEG-Hz-PLA).将腙键引入到聚合物的骨架中,以此构建聚合物胶束并作为pH敏感型纳米药物载体.制备的pH敏感型胶束的CMC值等于或低于5.46×10-4 mg/m L,DLS和TEM显示粒径均小于100 nm,且粒径分布均匀.非pH敏感型胶束在不同pH下的粒径变化不明显,而pH敏感型胶束在酸性环境下(pH=4.0和pH=5.0)胶束粒径出现了明显变化.以阿霉素为模型药物制备了pH敏感型载药胶束,其粒径比空白胶束大(100~200 nm),且粒径分布均匀.药物释放实验表明pH敏感型载药胶束随着释放介质pH降低累积释药量增高.MTT实验表明空白胶束对HeLa细胞和RAW264.7细胞几乎没有抑制作用,而载阿霉素的胶束对2种细胞的抑制作用都随着剂量的增大和时间的延长而增强.
[Abstract]:Three kinds of biodegradable block polymers containing Hydrazone bond were prepared by using poly (ethylene glycol) macromolecule containing Hydrazone bond as initiator, lactide as monomer to initiate ring-opening polymerization, and by adjusting the feed ratio. Hydrazone bond was introduced into the framework of polymer to construct polymer micelle and used as pH sensitive drug carrier. The mg/m values of pH sensitive micelles were equal to or less than 5.46 脳 10-4 mg/m DLS and Tem showed that the particle size of the prepared micelles was less than 100nmand the particle size distribution was uniform. The particle size of non-pH sensitive micelles did not change obviously at different pH values, but the particle size of pH sensitive micelles changed obviously in acidic environment (pH 4. 0 and pH 5. 0). The pH-sensitive drug loaded micelles were prepared using adriamycin as the model drug. The particle size of the micelles was larger than that of the blank micelles, and the particle size distribution was uniform. Drug release assay showed that pH-sensitive drug carrier micelles increased with the decrease of release medium pH. MTT assay showed that the blank micelles had little inhibitory effect on HeLa cells and RAW264.7 cells. The inhibitory effects of adriamycin-loaded micelles on both cells increased with the increase of dose and time.
【作者单位】： 河南大学药物研究所;
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