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Bioresponsive albumin-conjugated paclitaxel prodrugs for cancer therapy

Journal 2018 · IF 3.095 · 发表于 2018 年 3 月 19 日
作者: Jincheng Yang,Qingzhi Lv,Wei Wei,Zhengtao Yang,Jiajun Dong,Ruoshi Zhang,Qiming Kan,Zhonggui He,Youjun Xu
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摘要

The efficacy of traditional chemotherapy often suffers from rapid clearance and off-target toxicity. Drug delivery systems and controlled release are applied to improve the therapeutic efficiencies of small-molecule drugs. In this work, two novel oxidative/reductive (Ox/Re) -sensitive and one non-sensitive Paclitaxel (PTX) prodrugs were synthesized with a maleimide group, which rapidly conjugates with albumin in vivo. Albumin serves as a good vehicle to deliver more prodrug to tumors due to the enhanced permeation and retention (EPR) effect. PTX was then released from the prodrugs in glutathione(GSH)/ reactive oxygen species(ROS)-rich tumor microenvironments. This bioresponsive prodrug strategy demonstrates potent chemotherapeutic efficiency in vivo and may be utilized in clinical cancer therapy.