Bioresponsive albumin-conjugated paclitaxel prodrugs for cancer therapy. (1st January 2018)

• Record Type: Journal Article
• Authors: Yang, Jincheng; Lv, Qingzhi; Wei, Wei; Yang, Zhengtao; Dong, Jiajun; Zhang, Ruoshi; Kan, Qiming; He, Zhonggui; Xu, Youjun
• Is Part Of: Drug delivery. Volume 25:Number 1(2018)
• Page Start: 807
• Page End: 814
• Publication Date: 2018-01-01
• Subjects: Paclitaxel -- albumin-conjugate -- Ox/Re-sensitive release -- maleimide -- EPR effect; Drug delivery systems -- Periodicals; Drug targeting -- Periodicals; 615.05
• DOI: 10.1080/10717544.2018.1451935
• Languages: English
• ISSNs: 1071-7544

Abstract

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.