Engineering Research Center for Biomedical Materials, School of Life Sciences, Anhui Key Laboratory of Modern Biomanufacturing, Anhui University, 111 Jiulong Road, Hefei, Anhui Province 230601, PR China.
Engineering Research Center for Biomedical Materials, School of Life Sciences, Anhui Key Laboratory of Modern Biomanufacturing, Anhui University, 111 Jiulong Road, Hefei, Anhui Province 230601, PR China.
Mater Sci Eng C Mater Biol Appl. 2019 Jan 1;94:169-178. doi: 10.1016/j.msec.2018.09.029. Epub 2018 Sep 11.
Triblock copolymer PEG-block-poly(ortho ester urethane)-block-PEG (PEG-POEU-PEG) was conveniently prepared via polycondensation reaction between the ortho ester-containing diol and hexamethylene diisocyanate (HDI) at varying reaction time followed by termination with polyethylene glycol monomethyl ether (mPEG). PEG-POEU-PEG could further self-assemble into nano-scaled micelles. Ortho ester degradation in these micelles was significantly accelerated at pH 5.0 due to its pH sensitivity. In vitro drug release profiles showed that only a small amount of the loaded DOX was released in PBS solution at pH 7.4, while DOX could be quickly released at pH 5.0. MTT assay reveals that the micelles were completely nontoxic to cultured cells. Moreover, DOX-loaded micelles exhibited efficient antitumor efficiency against cancer cells. Therefore, the micelles may be potential drug carriers in cancer therapy.
三嵌段共聚物聚乙二醇嵌段-聚（原酸酯氨酯）嵌段-聚乙二醇（PEG-POEU-PEG）通过含原酸酯二醇与六亚甲基二异氰酸酯（HDI）在不同反应时间下的缩聚反应方便地制备，然后用聚乙二醇单甲醚（mPEG）终止。PEG-POEU-PEG 可以进一步自组装成纳米级胶束。由于其 pH 敏感性，这些胶束在 pH 5.0 时原酸酯的降解明显加快。体外药物释放曲线表明，在 pH 7.4 的 PBS 溶液中只有少量负载的 DOX 释放，而在 pH 5.0 时 DOX 可以快速释放。MTT 测定表明，胶束对培养细胞完全无毒。此外，载 DOX 的胶束对癌细胞表现出高效的抗肿瘤活性。因此，胶束可能是癌症治疗中的潜在药物载体。
