Penetrating efficiency of supramolecular hydrogel eye drops:Electrostatic interaction surpasses ligand-receptor interaction  

作　　者：Zhibin Ren Shan Li Xiaoying Liu Guanghao Lv Lei Chen Jingli Wang Xingyi Li Jiaqing Wang 

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

出　　处：《Chinese Chemical Letters》2024年第11期419-422,共4页中国化学快报（英文版）

基　　金：supported by National Natural Science Foundation of China(Nos.82102215 and 82372129);Wenzhou Medical University Scientific Research Fund(No.KYQD20210602)。

摘　　要：The low drug bioavailability of eye drops challenges the therapy of ocular disorders with high efficacy.One of solutions is to extend the corneal retention and enhance the penetration of drug into cornea.Here we synthesize two fluorophore-conjugated peptide based analogs rich in positive charges(i.e.,NBDFFKK)and with a specific ligand(i.e.,NBD-FFRGD),respectively,to visualize their performances in vitro and in vivo.The peptides both can self-assemble into supramolecular hydrogels with the microstructure of nanofibers.The in vitro experiments exhibit that two peptides are both uniformly distributed in cytoplasm,and the intracellular amount of peptide rich in positive charges is significantly larger than that of peptide with a specific ligand.The living corneal fluorescence shows that two peptides enter the corneal stroma within 15 min,and the peptide rich in positive charges is accumulated more extensively throughout the entire cornea,revealing that the supramolecular hydrogel eye drops penetrate the cornea more efficiently via electrostatic interaction than that via ligand-receptor interaction.This work,as a comparative study of supramolecular hydrogel eye drops on penetrating efficiency,indicates a possible direction for the design of eye drops with efficient corneal penetration.

关 键 词：Supramolecular hydrogel Eye drop Electrostatic interaction Ligand-receptor interaction Corneal penetration 

分 类 号：R77[医药卫生—眼科] O648.17[医药卫生—临床医学]