Key Laboratory of Mesoscopic Chemistry of MOE, Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210023, China.
College of Materials Science and Technology, Nanjing University of Aeronautics and Astronautics, Nanjing 211106, China.
ACS Appl Bio Mater. 2022 Jul 18;5(7):3320-3328. doi: 10.1021/acsabm.2c00318. Epub 2022 Apr 29.
Supramolecular prodrug vesicles with efficient property for dual chemotherapy have been successfully constructed based on the orthogonal self-assembly between a water-soluble pillar[5]arene host () and a betulinic acid guest () as well as doxorubicin (DOX). Under the acidic microenvironment of cancer cells, both the encapsulated anticancer drug DOX and prodrug can be effectively released from DOX-loaded ⊃ prodrug vesicles for combinational chemotherapy. Furthermore, bioexperiments indicate that DOX-loaded prodrug vesicles can obviously enhance the anticancer efficiency based on the cooperative effect of DOX and , while remarkably reducing the systematic toxicity in tumor-mice, displaying great potential applications in combinational chemotherapy for cancer treatments.
基于水溶性杯[5]芳烃主体（）与白桦脂酸客体（）以及阿霉素（DOX）之间的正交自组装，成功构建了具有高效双重化疗性能的超分子前药囊泡。在癌细胞的酸性微环境下，包封的抗癌药物 DOX 和前药都可以从 DOX 负载的⊃前药囊泡中有效释放出来，进行联合化疗。此外，生物实验表明，载 DOX 的前药囊泡可以通过 DOX 和的协同作用明显提高抗癌效率，同时显著降低肿瘤小鼠的系统毒性，在癌症联合化疗中具有很大的应用潜力。
