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Interface cisplatin-crosslinked doxorubicin-loaded triblock copolymer micelles for synergistic cancer therapy.
Colloids and Surfaces B: Biointerfaces ( IF 5.4 ) Pub Date : 2020-08-26 , DOI: 10.1016/j.colsurfb.2020.111334
Xuedi Gao 1 , Yujie Lu 1 , Bin Wu 1 , Jibin Miao 1 , Peng Chen 1 , Bin Yang 1 , Jiasheng Qian 1 , Jingxing Si 2 , Ming Cao 1 , Ru Xia 1
Affiliation  

Combination chemotherapy is an effective way to improve the therapeutic efficiency in anticancer treatment. Herein, we synthesized a novel amphiphilic triblock copolymer via a two-step ring-opening polymerization (ROP) followed by post-modification. Doxorubicin (DOX) was encapsulated into the copolymeric micelles through hydrophobic interactions, cisplatin (CDDP) was employed to in situ crosslink the interface of DOX-loaded micelles through Pt-carboxyl coordination interaction. The CDDP-mediated crosslinking improved the stability of the micelles and also reduced the release of DOX at physiological pH. After being taken up into the endosome/lysosome, the low environmental pH weakened the Pt-carboxyl coordination interactions, resulting in the destruction of the micelles and the release of CDDP and DOX. Moreover, these micelles loaded with dual drugs enabled a synergistic anticancer effect, showing promise as a potential drug delivery platform for cancer therapy.



中文翻译:

界面顺铂交联的阿霉素三嵌段共聚物胶束,用于协同癌症治疗。

联合化疗是提高抗癌治疗效率的有效途径。本文中,我们通过两步开环聚合(ROP),然后进行后修饰,合成了一种新型的两亲性三嵌段共聚物。阿霉素(DOX)通过疏水相互作用被包裹在共聚物胶束中,顺铂(CDDP)用于原位通过Pt-羧基配位相互作用使DOX负载胶束的界面交联。CDDP介导的交联提高了胶束的稳定性,还减少了在生理pH下DOX的释放。低环境pH吸收到内体/溶酶体中后,削弱了Pt-羧基配位相互作用,导致胶束破坏以及CDDP和DOX释放。此外,这些载有双重药物的胶束具有协同的抗癌作用,显示出有望作为癌症治疗的潜在药物递送平台。

更新日期:2020-09-10
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