Schiff连接的聚乙二醇化阿霉素前药形成pH响应性纳米粒子，具有高载药量和有效的*癌治疗

标题：Schiff连接的聚乙二醇化阿霉素前药形成pH响应性纳米粒子，具有高载药量和有效的*癌治疗

Schiff-Linked PEGylated Doxorubicin Prodrug Forming pH-Responsive Nanoparticles With High Drug Loading and Effective Anticancer Therapy

作者：Jian Song, Bingbing Xu, Hui Yao, Xiaofang Lu, Yang Tan, Bingyang Wang, Xing Wang, Zheng Yang

链接：[https://www.frontiersin.org/articles/10.3389/fonc.2021.656717/full](https://www.frontiersin.org/articles/10.3389/fonc.2021.656717/full)

摘要：

该研究设计了一种通过酸敏感的Schiff碱键连接PEG和DOX的前药系统，能够在酸性肿瘤微环境中响应性释放DOX。该纳米粒子在正常生理条件下保持稳定，而在pH 5.0的环境中迅速释放DOX。体外实验表明，该系统在乳腺癌细胞（MCF-7）中显示出优良的*肿瘤活性，优于游离DOX，表明其在癌症化疗中的应用前景。

Developing efficacious drug delivery systems for targeted cancer chemotherapy remains a major challenge. Here we demonstrated a kind of pH-responsive PEGylated doxorubicin (DOX) prodrug via the effective esterification and Schiff base reactions, which could self-assemble into the biodegradable micelles in aqueous solutions. Owing to low pH values inside the tumor cells, these PEG-Schiff-DOX nanoparticles exhibited high drug loading ability and pH-responsive drug release behavior within the tumor cells or tissues upon changes in physical and chemical environments, but they displayed good stability at physiological conditions for a long period. CCK-8 assay showed that these PEGylated DOX prodrugs had a similar cytotoxicity to the MCF-7 tumor cells as the free DOX drug. Moreover, this kind of nanoparticle could also encapsulate small DOX drugs with high drug loading, sufficient drug release and enhanced therapeutic effects toward MCF-7 cells, which will be benefited for developing more drug carriers with desirable functions for clinical anticancer therapy.

结论：

Schiff碱连接的PEG-DOX前药纳米粒子具有pH响应性和高载药量，显示出在肿瘤靶向治疗中的潜力。([patrinum.ch][3])