Core-shell lipid-polymer nanoparticles as a promising ocular drug delivery system to treat glaucoma

作     者：Yang Zhou Aiping Fang Fazhan Wang Huili Li Quansheng Jin Lingjing Huang Chunmei Fu Jun Zeng Zhaohui Jin Xiangrong Song Yang Zhou;Aiping Fang;Fazhan Wang;Huili Li;Quansheng Jin;Lingjing Huang;Chunmei Fu;Jun Zeng;Zhaohui Jin;Xiangrong Song

作者机构：State Key Laboratory of Biotherapy and Cancer Center/Department of PharmacyWest China Hospitaland Collaborative Innovation Center for BiotherapySichuan UniversityChengdu 610041China West China School of PharmacySichuan UniversityChengdu 610041China 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2020年第31卷第2期

页      面：494-500页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 0703[理学-化学] 10[医学] 

基　　金：financially supported by Sichuan Province Science and Technology Support Program(Nos.16ZC2698 and 2018JY0582) the National Natural Science Foundation of China(No.81872821)。 

主　　题：Core-shell lipid-polymer nanoparticles Ocular drug delivery system Sustained release Corneal permeation Intraocular pressure 

摘      要：Nowadays,tremendous researches have been focused on the core-shell lipid-polymer nanoparticles(LPNs) due to the advantages of both liposomes and polymer nanoparticles.In this work,LPNs were applied to encapsulate brinzolamide(Brz-LPNs) for achieving sustained drug release,improving drug corneal permeation and enhancing drug topical therapeutic effect.The structure of Brz-LPNs was composed of poly(lactic-co-glycolic) acid(PLGA) nanocore which encapsulated Brz(Brz-NPs) and lipid shell around the core.Brz-LPNs were prepared by a modified thin-film dispersion method.With the parameters optimization of Brz-LPNs,optimal Brz-LPNs showed an average particle size of151.23±1.64 nm with a high encapsulation efficiency(EE) of 86.7%±2.28%.The core-shell structure of Brz-LPNs were confirmed by transmission electronic microscopy(TEM).Fourier transformed infrared spectra(FTIR) analysis proved that Brz was successfully entrapped into Brz-LPNs.Brz-LPNs exhibited obvious sustained release of Brz,compared with AZOPT^■ and Brz-LPs.Furthermore,the corneal accumulative permeability of Brz-LPNs significantly increased compared to the commercial available formulation(AZOPT^■) in vitro.Moreover,Brz-LPNs(1 mg/mL Brz) showed a more sustained and effective intraocular pressure(IOP) reduction than Brz-LPs(1 mg/mL) and AZOPT^■(10 mg/mL Brz) in vivo.In conclusion,Brz-LPNs,as promising ocular drug delivery systems,are well worth developing in the future for glaucoma treatment.