期刊
DRUG DELIVERY
卷 25, 期 1, 页码 807-814出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/10717544.2018.1451935
关键词
Paclitaxel; albumin-conjugate; Ox; Re-sensitive release; maleimide; EPR effect
资金
- Innovative Research Team of the Ministry of Education
- Innovative Research Team in SYPHU by the Supporting Fund for Universities from the Chinese Central Government [51150039]
- Program for Liaoning Innovative Research Team in University
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.
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