Remote-controlled dexamethasone-duration on eye-surface with a micelle-magnetic nanoparticulate co-delivery system for dry eye disease  

作　　者：Qinxiang Zheng Chaoxiang Ge Kexin Li Longxin Wang Xiaoyu Xia Xiao Liu Rashid Mehmood Jianliang Shen Kaihui Nan Wei Chen Sen Lin 

机构地区：[1]National Engineering Research Center of Ophthalmology and Optometry,Eye Hospital,Wenzhou Medical University,Wenzhou 325027,China [2]National Clinical Research Center for Ocular Diseases,Eye Hospital,Wenzhou Medical University,Wenzhou 325027,China [3]Zhejiang Engineering Research Center for Tissue Repair Materials,Wenzhou Institute,University of Chinese Academy of Sciences,Wenzhou 325000,China [4]School of Chemical Engineering,UNSW Sydney,High Street,Building E10,Kensington,NSW 2052,Australia [5]Adult Cancer Program,Lowy Cancer Research Centre,UNSW Sydney,Corner Botany&High Streets,Kensington,NSW 2052,Australia

出　　处：《Acta Pharmaceutica Sinica B》2024年第8期3730-3745,共16页药学学报（英文版）

基　　金：supported by National Natural Science Foundation of China(No.82070932);the Zhejiang Provincial Natural Science Foundation of China(No.LY19H120002);the internal funding of Wenzhou Medical University(No.KYYW202020,China);The Project of Wenzhou Medical University Affiliated Eye Hospital(No.YNZD2201901,China);the integration project of State Key Laboratory of Ophthalmology,Optometry and Vision Science(No.J02-20190202,China).

摘　　要：Dexamethasone(DEX)is used to treat ocular surface diseases.However,regulating DEX duration in tears while preventing its absorption into the anterior chamber is critical for balancing its therapy effects and the side effects.In this study,a novel magnetic nanoparticle(MNP)-micelle(MC)codelivery system(MMDS)was developed.The MC moiety in the MMDS served as the carrier for DEX and the MNP part endowed the MMDS with magnetic-responsive properties.To extend its residency,the MMDS was magnetically attracted by an external magnet after instilling,which acted as a precorneal drug-depot enabling a sustainable release of DEX in tears.With combination of magnet treatment,the topical instillation of MMDS@DEX significantly prolonged the DEX-retention in tears and increased the DEX-concentration in the cornea and conjunctiva,as well as concurrently reduced the DEX-level in the aqueous humor,when compared with the commercial DEX eye drop treatment.The combination of MMDS@DEX and magnet treatment exerted significantly better therapeutic effects against DED with smaller side effects than conventional treatments including DEX suspension,commercial DEX eye drops,as well as the MMDS@DEX treatment alone.The present work provided a new method for the effective delivery of DEX to ocular surface tissues while reducing its side effects,which will be beneficial to the treatments of a wide range of ocular surface diseases.

关 键 词：Magnetic nanoparticle MICELLE DEXAMETHASONE Eye drop BIOAVAILABILITY Dry eye disease CORNEA CONJUNCTIVA 

分 类 号：R96[医药卫生—药理学]