Preparation and Drug Release Properties of a Novel PLA-PEG-PTX Pro-Drug
Lactide (LA) and PEG as raw materials, 2,2-Dimethylol Propionic Acid (DMPA) as initiator, hexamethylene diisocyanate (HDI) as coupling agent, amphiphilic block copolymer PLA-PEG with side carboxyl group was synthesized.A novel PLA-PEG-PTX pro-drug was prepared through the esterification reaction between the side carboxyl group on copolymer and hydroxyl group on paclitaxel.Its structure was characterized with 1H-NMR and FT-IR.The pro-drug micelles were prepared by solvent evaporation method.The particle size of the micelles was determined by nano particle tracking analyzer, the micro structure of the micelles was determined by TEM, and the drug release properties were investigated by dialysis experiments.Results showed that the pro-drug micelles are spherical with core-corona structure and major particles size in 55-85nm.The PLA-PEG750-PTX (molar ratio of LA to DMPA as 40 to 1) pro-drug micelles released paclitaxel slowly and steadily without obvious burst release in buffer solution with pH=7.0, and its cumulative release rate reached to 36% in 10 hours.PLA-PEG750-PTX pro-drug micelles have a certain sustained-release effect, which is beneficial to improve the anti-tumor effect of paclitaxel.
Amphiphilic block copolymer Chemical bond Self-assembly Drug release
Chong-chong Bian Yu-shun Jin Jun-jie Zhang
Department of Materials Science and Engineering, Beijing Institute of Petrochemical Technology, Beij Department of Materials Science and Engineering, Beijing Institute of Petrochemical Technology, Beij
国际会议
The 2016 China Functional Materials Technology and Industry Forum (2016中国国际功能材料大会暨第九届中国功能材料及其应用学术会议)
重庆
英文
793-800
2016-07-25（万方平台首次上网日期，不代表论文的发表时间）