Li Yang, Yuan Xinchao, Yu Jialin, Fan Yiqi, He Tian, Lu Shuai, Li Xiaopeng, Qiu Huayu, Yin Shouchun
College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou, 311121, P. R. China.
College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen, 518055, P. R. China.
ACS Appl Bio Mater. 2020 Nov 16;3(11):8061-8068. doi: 10.1021/acsabm.0c01163. Epub 2020 Oct 28.
Synergistic therapy with nanocarriers is a promising strategy for effective cancer treatment. Here, we synthesized an amphiphilic rhomboidal metallacycle M, in which a glucose-modified pyridine ligand was used to improve water-solubility and an organoplatinum(II) receptor acted as a platinum-based anticancer agent. Moreover, because of the amphiphilic properties, M self-assembled into micelles or nanobelts at different concentrations, and a drug delivery system (DDS) was developed by encapsulating the anticancer drug doxorubicin (DOX) into the micelles. The morphology, cell uptake, cytotoxicity, internalization, and antitumor effect of the DDS were investigated. Under low intracellular pH conditions, the DDS disassembled to release the loaded DOX in situ. The designed DDS exhibited good biocompatibility, synergistic antitumor efficacy, and negligible adverse effects in a U87 tumor-bearing mice model.
纳米载体协同治疗是一种很有前景的有效癌症治疗策略。在此，我们合成了一种两亲性菱形金属环M，其中使用葡萄糖修饰的吡啶配体来提高水溶性，有机铂（II）受体作为铂类抗癌剂。此外，由于具有两亲性，M在不同浓度下自组装成胶束或纳米带，并通过将抗癌药物阿霉素（DOX）包封到胶束中开发了一种药物递送系统（DDS）。研究了DDS的形态、细胞摄取、细胞毒性、内化和抗肿瘤作用。在低细胞内pH条件下，DDS分解以原位释放负载的DOX。所设计的DDS在U87荷瘤小鼠模型中表现出良好的生物相容性、协同抗肿瘤疗效和可忽略不计的不良反应。
