眼用伊曲康唑固体脂质纳米粒的制备及其体外释放  

Preparation and Characterization of Itraconazole Loaded Solid Lipid Nanoparticel for Ocular Topical Application and the in Vitro Drug Release

作　　者：王敬博 卢萍 梁珍 郭莹[1] 张振[1] 张俊杰[1] WANG Jing-bo;LU Ping;LIANG Zhen;GUO Ying;ZHANG Zhen;ZHANG Jun-jie(Henan Provincial People's Hospital,Henan Eye Institute,Henan University People's Hospital,Zhengzhou 450000,China)

机构地区：[1]河南省人民医院/河南省眼科研究所/河南大学人民医院,河南郑州450000

出　　处：《河南医学研究》2020年第6期972-975,共4页Henan Medical Research

基　　金：国家自然基金联合重点项目(U1704283);河南省科技厅基础与前沿(142300410057)。

摘　　要：目的为解决伊曲康唑(ITZ)的分散性,制备伊曲康唑固体脂质纳米粒(ITZ-SLN),并考察其体外释放规律。方法采用微乳法-低温固化法制备ITZ-SLN;用马尔文激光粒度仪测定纳米粒的Zeta电位与粒度分布,低温高速超滤离心分离SLN与未包封的药物,反相高效液相色谱法(RP-HPLC)测定包封率及其载药量,采用扩散法-超滤法测定纳米粒(ITZ-SLN)的体外释放行为。结果纳米粒的粒径为(15.23±2.10)nm,Zeta为(-22. 65±0.91)mV,包封率为(96.02±2.10)%,载药量为(0.15±0. 02)%,其体外释放规律符合一级释放动力学方程。结论该制剂处方设计和工艺方法可行,可达到缓释效果。Objective To develop solid lipid nanoparticles of itraconazole(ITZ-SLNs) and study itraconazole in vitro release characteristics from the ITZ-SLNs.Methods ITZ-SLN was prepared by microemulsion method and low temperature solidifying method. The particle size and zeta potential of the nanoparticles were evaluated. Entrapment efficiency and drug loading were determined by HPLC. In vitro release of ITZ from ITZ-SLNs was studied with direct dispersion-ultrafiltration method.Results The particles size of nanoparticles was(15.23±2.10) nm, zeta potential was(-22.65±0.91) mV, entrapment efficiency was(96.02±2.10)%, drug loading capacity was(0.15±0.02)%, and the in vitro release was fitted to the first-order model.Conclusion The preparation of ITZ-LSNs are practicable and the delivery systems can achieve sustained-release effects.

关 键 词：伊曲康唑 固体脂质纳米粒 体外释放 

分 类 号：R944.1[医药卫生—药剂学]