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Bioresponsive albumin-conjugated paclitaxel prodrugs for cancer therapy.


ABSTRACT: 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.

SUBMITTER: Yang J 

PROVIDER: S-EPMC6058529 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature

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Bioresponsive albumin-conjugated paclitaxel prodrugs for cancer therapy.

Yang Jincheng J   Lv Qingzhi Q   Wei Wei W   Yang Zhengtao Z   Dong Jiajun J   Zhang Ruoshi R   Kan Qiming Q   He Zhonggui Z   Xu Youjun Y  

Drug delivery 20181101 1


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  ...[more]

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