Bioresponsive albumin-conjugated paclitaxel prodrugs for cancer therapy

Drug Delivery

Youjun Xu¹  Qingzhi Lv¹  Jiajun Dong¹  Zhengtao Yang¹  Ruoshi Zhang¹  Qiming Kan¹  Wei Wei¹  Zhonggui He¹  Jincheng Yang¹ 

[1] Shenyang Pharmaceutical University;

关键词: paclitaxel;    albumin-conjugate;    ox/re-sensitive release;    maleimide;    epr effect;   

DOI  :  10.1080/10717544.2018.1451935

来源: DOAJ

【 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.

【 授权许可】

Unknown