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多臂两亲嵌段共聚物和生育酚聚乙二醇 1000 琥珀酸酯的血清稳定胶束增强药物耐药性抑制

Enhanced drug resistance suppression by serum-stable micelles from multi-arm amphiphilic block copolymers and tocopheryl polyethylene glycol 1000 succinate.

机构信息

School of Health Science & Engineering, University of Shanghai for Science & Technology, Shanghai,  200093, China.

Department of Nanomedicine & Shanghai Key Lab of Cell Engineering, Naval Medical University, Shanghai,  200433, China.

出版信息

Nanomedicine (Lond). 2024;19(14):1297-1311. doi: 10.1080/17435889.2024.2347197. Epub 2024 May 30.

DOI:10.1080/17435889.2024.2347197
PMID:39046514
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11285239/
Abstract

To develop a robust drug-delivery system using multi-arm amphiphilic block copolymers for enhanced efficacy in cancer therapy. Two series of amphiphilic polymer micelles, PEG-b-PCL and PEG-b-PCL/TPGS, were synthesized. Doxorubicin (DOX) loading into the micelles was achieved via solvent dialysis. The micelles displayed excellent biocompatibility, narrow size distribution, and uniform morphology. DOX-loaded micelles exhibited enhanced antitumor efficacy and increased drug accumulation at tumor sites compared with free DOX. Additionally, 4A-PEG-b-PCL/TPGS micelles effectively suppressed drug-resistant MCF-7/ADR cells. This study introduces a novel micelle formulation with exceptional serum stability and efficacy against drug resistance, promising for cancer therapy. It highlights innovative strategies for refining clinical translation and ensuring sustained efficacy and safety .

摘要

利用多臂两亲嵌段共聚物开发一种稳健的药物输送系统,以提高癌症治疗的疗效。 合成了两种两亲聚合物胶束,PEG-b-PCL 和 PEG-b-PCL/TPGS。 通过溶剂透析将阿霉素(DOX)载入胶束中。 胶束表现出良好的生物相容性、窄的粒径分布和均匀的形态。与游离 DOX 相比,载 DOX 的胶束显示出增强的抗肿瘤功效和增加的肿瘤部位药物积累。此外,4A-PEG-b-PCL/TPGS 胶束有效地抑制了耐药 MCF-7/ADR 细胞。 本研究介绍了一种具有出色血清稳定性和抗耐药性的新型胶束制剂,有望用于癌症治疗。它突出了用于确保持续疗效和安全性的创新策略的重要性。

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