Self-assembled H-shaped pegylated methotrexate conjugates with high drug-carrying capability for intracellular drug delivery
A novel prodrug of pegylated methotrexate conjugates (PMC) with high drug-carrying capability and redox sensitive drug release mechanism was reported for intracellular drug delivery.PMC was structured by a H-shape with four anticancer drug methotrexate (MTX) linked to both ends of PEG main chain via disulfide linkers, resulting in the conjugates with a high and constant drug loading efficiency up to 30%.The amphiphilic property of PMC enables them to self-assemble into nanomicelles in aqueous solution, while the cleavable disulfide linkers allow conjugated MTX to exert its therapeutic activity due to the fast cleavage of disulfide linkers when exposed to the intracellular concentration of glutathione (GSH).Cell proliferation assays performed with HepG2 cancer cells confirmed the pharmacological efficacy.
Prodrug Methotrexate conjugate Redox sensitive Drug delivery
Haiqing Dong Wenjuan Xia Tianbin Ren
The Institute for Biomedical Engineering & Nano Science, Tongji University, Shanghai 200092
国内会议
2013年中国药物制剂大会——中国药学会药剂专业委员会2013年学术年会暨国际控释协会中国分会2013年学术年会
武汉
英文
312-314
2013-10-26（万方平台首次上网日期，不代表论文的发表时间）