Effect of the chemically substituted L-histidine on the physio-chemical properties of Poly(L-histidine) based micelles

Triblock copolymer of poly(ethylene glycol)-poly(d,l-lactide)-poly(2,4-dinitrophenol-l-histidine)(mPEG-b-PLA-b-DNP-PHis) with DNP group substituted to the saturated nitrogen of l-histidine were synthesized.The pH sensitive properties of the copolymer micelles were characterized using an acid-base titration method,fluorescene probe technique, DLS observation and in vitro drug release, respectively.The results suggest that mPEG-b-PLA-b-DNP-PHis copolymers showed increased particle size, and similar pH responsive properties with mPEG-b-PLA-b-PHis copolymers.These results suggest that saturated nitrogen of PHis may serve as a valuable site for chemical modification of the PHis based copolymers because of the little effect on the pH responsive properties.However, selection of the substitution group needs to be considered due to the possible increase of micellar particle size of the micelles, leading to compromised passive targeting..
Mingxi Qiao Xiaojun Zhang Dawei Chen
School of Pharmacy, Shenyang Pharmaceutical University, P.O.Box 42, Wenhua Road 103, Shenyang,Liaoning Province 110016, PR China
国际会议
沈阳
英文
273-275
2016-04-28(万方平台首次上网日期,不代表论文的发表时间)