Autocatalytic strategy for tuning drug release from peptide-drug supramolecular hydrogel  

作　　者：Yuqin Wu Tian Xia Xiaohui Ma Lei Lei Lulu Du Xiaoning Xu Xiangyi Liu Yueting Shi Xingyi Li Deqing Lin 

机构地区：[1]Institute of Biomedical Engineering,School of Ophthalmology&Optometry and Eye Hospital,Wenzhou Medical University,Wenzhou 325027,China

出　　处：《Chinese Chemical Letters》2023年第10期204-208,共5页中国化学快报（英文版）

基　　金：financially supported by the Natural Science Foundation of Zhejiang Province(No.LY20H180012);。

摘　　要：Peptide-drug conjugates(PDCs) composed of peptide, spacer and drug have gained extensive attention in the field of drug delivery owing to its precise control over the drug payload and architecture. However,the achievement of controllable and rapid drug release at targeted site by PDCs is still a great challenge for pharmaceutist. Herein, we introduced the histidine residue into PDCs to generate a supramolecular hydrogel via a p H-trigger strategy, which exhibited an autocatalytic effect to precisely tune drug release from PDCs hydrogel. Using indomethacin(Idm) as model drug, various PDCs(Y(Idm)EEH, Y(Idm)EEK and Y(Idm)EER) were synthesized and their self-assembling properties were investigated in terms of critical aggregation concentration(CAC), transmission electron microscopy(TEM) and rheometer. Introduction of histidine residue into PDCs presented a robust catalytic activity on the ester hydrolysis of p-nitrophenyl acetate in aqueous solution, as well conferred the autocatalytic capacity to hydrolyze the PDCs into active parent drug(Idm). Overall, we reported an autocatalytic activity of histidine residue to precisely tune drug release from PDCs hydrogels.

关 键 词：Peptide-drug conjugates Supramolecular hydrogel AUTOCATALYSIS HYDROLYSIS Drug release 

分 类 号：TQ460.1[化学工程—制药化工] TQ427.26