载siRNA的PLGA-b-PEG纳米粒制备及初步体外评价  

Preparation and in Vitro Evaluation of PLGA-b-PEG Nanoparticles Loading siRNA

作　　者：纪刚剑 林雯[2] 史琼枝 李银科 JI Gangjian;LI Wen;SHI Qiongzhi;LI Yinke(Wuhan Third Hospital·Tongren Hospital of Wuhan University,Wuhan,Hubei,China 430060;Huangshi Love&Health Hospital,Huangshi,Hubei,China 435000;General Hospital of Central Theater Command of Chinese PLA,Wuhan,Hubei,China 430070)

机构地区：[1]湖北省武汉市第三医院·武汉大学附属同仁医院,湖北武汉430060 [2]黄石爱康医院,湖北黄石435000 [3]中国人民解放军中部战区总医院,湖北武汉430070

出　　处：《中国药业》2022年第17期33-37,共5页China Pharmaceuticals

基　　金：湖北省自然科学基金[2019CFC886];湖北省科技计划项目[2020CFB569];湖北省卫生和计划生育委员会2018年联合基金[WJ2018H0116]。

摘　　要：目的 探讨载小干扰核糖核酸(siRNA)的聚乳酸-羟基乙酸共聚物-b-聚乙二醇(PLGA-b-PEG)纳米粒的制备工艺,并对其进行表征及初步体外评价。方法 采用复乳法制备含药纳米粒。通过透射电子显微镜、原子力显微镜观察形态,Zeta电位/粒度分析仪测定Zeta电位及其粒径,计算包封率,考察稳定性、体外释药,并进行细胞增殖检测。结果 制备的纳米粒呈球形,粒径均匀,平均粒径为(101.5±6.3)nm,Zeta电位为-(31.7±4.5)mV,包封率为(57.6±4.8)%;在4℃条件下放置30 d,粒径和Zeta电位分别为(103.3±5.7)nm和-(32.5±5.2)mV;纳米粒体外可持续释药48 h以上,且超声可加速药物释放;siRNA纳米粒具有较强的肿瘤细胞活性抑制作用。结论 制备的纳米粒理化特性良好,性质稳定,具有一定的超声刺激释药特性。Objective To investigate the preparation and characterization of poly (lactic-co-glycolic acid)-b-polyethylene glycol(PLGA-b-PEG) nanoparticles loading the small interfering RNA (siRNA),and to evaluate them preliminarily in vitro.MethodsThe nanoparticles containing drugs were prepared by the double emulsion method.The morphology of nanoparticles was observed by the transmission electron microscope (TEM) and the atomic force microscope (AFM).The Zeta potential and particle size of nanoparticles were measured by the Zeta potential/particle size analyzer.The entrapment efficiency of nanoparticles was calculated.The stability and in vitro drug release of nanoparticles were investigated.The cell proliferation was tested.ResultsThe prepared nanoparticles were spherical and uniform with the average particle size of (101.5±6.3)nm,the Zeta potential of-(31.7±4.5)mV and the entrapment efficiency of (57.6±4.8)%.Placed at 4℃for 30 d,the particle size and Zeta potential of nanoparticles were (103.3±5.7)nm and-(32.5±5.2)mV,respectively.The nanoparticles could release drugs constantly for more than 48 h in vitro,and the ultrasound could stimulate the drug release.The nanoparticles loading the siRNA had a strong inhibitory effect on tumor cell viability.ConclusionThe prepared nanoparticles have good physical and chemical characteristics,stable properties,and a certain characteristic of drug release stimulated by the ultrasound.

关 键 词：聚乳酸-羟基乙酸共聚物-b-聚乙二醇 纳米粒 超声 小干扰核糖核酸 

分 类 号：R979.1[医药卫生—药品] TQ460.6[医药卫生—药学]