Utilization of H-bond interaction of nucleobase Uralic with antitumor methotrexate to design drug carrier with ultrahigh loading efficiency and pH-responsive drug release

利用核碱基乌拉酸与抗肿瘤甲氨蝶呤的氢键相互作用设计超高载药效率和pH响应药物释放的药物载体

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作者:Teng-Teng Cai, Qi Lei, Bin Yang, Hui-Zhen Jia, Hong Cheng, Li-Han Liu, Xuan Zeng, Jun Feng, Ren-Xi Zhuo, Xian-Zheng Zhang

Abstract

A novel Uralic (U)-rich linear-hyperbranched mono-methoxy poly (ethylene glycol)-hyperbranched polyglycerol-graft-Uralic (mPEG-HPG-g-U) nanoparticle (NP) was prepared as drug carrier for antitumor methotrexate (MTX). Due to the H-bond interaction of U with MTX and hydrophobic interaction, this NP exhibited high drug loading efficiency of up to 40%, which was significantly higher than that of traditional NPs based on U-absent copolymers (<15%). In addition, MTX-loaded mPEG-HPG-g-U NPs also demonstrated an acidity-accelerated drug release behavior.

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