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基于聚(2-乙基-2-恶唑啉)的可生物降解的还原和pH双重敏感聚合物胶束用于姜黄素的高效递送

Biodegradable reduction and pH dual-sensitive polymer micelles based on poly(2-ethyl-2-oxazoline) for efficient delivery of curcumin.

作者信息

Zhang Hena, Liu Xiaojun, Xu Ting, Xu Kang, Du Baixiang, Li Yuling

机构信息

School of Chemistry & Materials Science, Jiangsu Key Laboratory of Green Synthetic Chemistry for Functional Materials, Jiangsu Normal University Xuzhou 221116 China

出版信息

RSC Adv. 2020 Jul 6;10(43):25435-25445. doi: 10.1039/d0ra02779k. eCollection 2020 Jul 3.

Abstract

A series of disulfide-linked amphiphilic polymers polyoxaline-SS-poly(lactide) (PEtOx-SS-PLA) were prepared and self-assembled into nano-micelles in water. The anticancer drug curcumin (Cur) was selected as a model drug, the entrapment of Cur in PEtOx-SS-PLA micelles was investigated and the intracellular transport and release of Cur-loaded micelles was studied in C6 cells. The preparation of Cur-loaded polymer micelles showed that micelle size decreased after drug loading, favoring cell phagocytosis. MTT experiments showed that PEtOx-SS-PLA 52 micelles have a small IC (2.05 μg mL). The release behavior of PEtOx-SS-PLA 52 drug-loaded micelles in C6 cells showed that polymer micelle enhanced the intracellular release of Cur, and increased the inhibition effect of cancer cells. In a word, these reduction and pH-dual sensitive, biodegradable, hydrophilic shell-discarding PEtOx-SS-PLA micelles have great potential for future tumour administration.

摘要

制备了一系列二硫键连接的两亲性聚合物聚恶唑啉-SS-聚丙交酯(PEtOx-SS-PLA),并使其在水中自组装成纳米胶束。选择抗癌药物姜黄素(Cur)作为模型药物,研究了Cur在PEtOx-SS-PLA胶束中的包封情况,并在C6细胞中研究了载Cur胶束的细胞内转运和释放。载Cur聚合物胶束的制备表明,载药后胶束尺寸减小,有利于细胞吞噬。MTT实验表明,PEtOx-SS-PLA 52胶束的IC50较小(2.05 μg mL)。PEtOx-SS-PLA 52载药胶束在C6细胞中的释放行为表明,聚合物胶束增强了Cur的细胞内释放,并增强了对癌细胞的抑制作用。总之,这些具有还原和pH双重敏感性、可生物降解、亲水性外壳可丢弃的PEtOx-SS-PLA胶束在未来肿瘤给药方面具有巨大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18bb/9055264/d45530ebe237/d0ra02779k-s1.jpg

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