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首页> 外文期刊>International Journal of Biological Macromolecules: Structure, Function and Interactions >Thermally self-assembled biodegradable poly(casein-g-N-isopropylacrylamide) unimers and their application in drug delivery for cancer therapy
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Thermally self-assembled biodegradable poly(casein-g-N-isopropylacrylamide) unimers and their application in drug delivery for cancer therapy

机译：热自组装可生物降解的聚（酪蛋白-G-N-异丙基丙烯酰胺）单层及其在药物递送中的癌症治疗的应用

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摘要

In this work, we report the synthesis of graft copolymers based on casein and N-isopropylacrylamide, which can self-assemble into biodegradable micelles of approximately 80 nm at physiological conditions. The obtained copolymers were degraded by trypsin, an enzyme that is overexpressed in several malignant tumors. Moreover, graft copolymers were able to load doxorubicin (Dox) by ionic interaction with the casein component. In vitro release experiments showed that the in situ assembled micelles can maintain the cargo at plasma conditions but release Dox immediately after their exposition at pH 5.0 and trypsin. Cellular uptake and cytotoxicity assays revealed the efficient delivery to the nucleus and antiproliferative efficacy of Dox in the breast cancer cell line MDA231. Both delivery and therapeutic activity were enhanced in presence of trypsin. Overall, the prepared micelles hold a great potential for their utilization as dual responsive trypsin/pH drug delivery system. (C) 2020 Elsevier B.V. All rights reserved.
机译：在这项工作中，我们报告基于酪蛋白和N-异丙基丙烯酰胺接枝共聚物的合成，其可以自组装成在生理条件下的约80nm可生物降解的微胶粒。将所得到的共聚物，通过胰蛋白酶，即在几个恶性肿瘤中过表达的酶降解。而且，接枝共聚物能够通过与酪蛋白组分离子相互作用多柔比星（DOX）加载。体外释放实验表明，在原位组装胶束可以维持在等离子体条件的货物但在pH 5.0胰蛋白酶和它们的阐述后立即释放的Dox。细胞摄取和细胞毒性测定法揭示的有效递送到在乳腺癌细胞系MDA231的Dox的细胞核和抗增殖功效。输送和治疗活性在胰蛋白酶存在下增强。总体而言，准备胶束保持其利用率双重响应胰蛋白酶/ PH值药物输送系统的巨大潜力。 （c）2020 Elsevier B.v.保留所有权利。

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