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二碲化物桥联的聚乙二醇-聚己内酯共聚物作为叶酸靶向和氧化还原响应性纳米颗粒用于增强癌症治疗

Ditelluride-Bridged PEG-PCL Copolymer as Folic Acid-Targeted and Redox-Responsive Nanoparticles for Enhanced Cancer Therapy.

作者信息

Pang Zekun, Zhou Jiayan, Sun Chunyang

机构信息

Department of Radiology and Tianjin Key Laboratory of Functional Imaging, Tianjin Medical University General Hospital, Tianjin, China.

出版信息

Front Chem. 2020 Feb 28;8:156. doi: 10.3389/fchem.2020.00156. eCollection 2020.

Abstract

The development of the nanosized delivery systems with targeting navigation and efficient cargo release for cancer therapy has attracted great attention in recent years. Herein, a folic acid (FA) modified PEGylated polycaprolactone containing ditelluride linkage was synthesized through a facile coupling reaction. The hydrophobic doxorubicin (DOX) can be encapsulated into the polymeric micelles, and such nanoparticles (F-TeNP) exhibited redox-responsive drug release under abundant glutathione (GSH) condition due to the degradation of ditelluride bonds. In addition, flow cytometric analyses showed that the FA ligands on F-TeNP could facilitate their cellular uptake in 4T1 breast cancer cells. Therefore, F-TeNP led to the promoted drug accumulation and enhanced growth inhibition on 4T1 tumor . The obtained results suggest F-TeNP excellent potential as nanocarriers for anticancer drug delivery.

摘要

近年来,用于癌症治疗的具有靶向导航和高效药物释放功能的纳米递送系统的开发备受关注。在此,通过简便的偶联反应合成了一种含有二碲键的叶酸(FA)修饰的聚乙二醇化聚己内酯。疏水性阿霉素(DOX)可被包封到聚合物胶束中,由于二碲键的降解,这种纳米颗粒(F-TeNP)在丰富的谷胱甘肽(GSH)条件下表现出氧化还原响应性药物释放。此外,流式细胞术分析表明,F-TeNP上的FA配体可促进其在4T1乳腺癌细胞中的细胞摄取。因此,F-TeNP导致4T1肿瘤上药物积累增加和生长抑制增强。所得结果表明F-TeNP作为抗癌药物递送的纳米载体具有优异的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dc91/7059598/7d796400dbe3/fchem-08-00156-g0001.jpg

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