siRNA的PEG化脂质体的制备及处方的筛选
Preparation of PEGylated cationic liposome for siRNA delivery and formulation optimization
作者：张梦甜;韩剑锋;吴称玉;孙逊;
Author：
收稿日期： 年卷（期）页码：2014,29(04):-364-367
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：前体脂质体;PEG化阳离子脂质体;siRNA;处方筛选
Key words：
基金项目：
中文摘要
目的制备一种递送siRNA的PEG化脂质体,通过改变处方中PEG的比例来优化处方。方法采用前体脂质体的方法制备不同PEG含量的阳离子脂质体;用超速离心法分离脂质体siRNA复合物和游离siRNA;用荧光标记法检测siRNA,求得各处方脂质体对SiRNA的包封率;考察不同处方脂质体在血清中的稳定性;测定不同处方脂质体在A549细胞上的毒性和摄取效率;筛选最终脂质体处方并测定其粒径、电位,观察形状。结果选定5%PEG含量的脂质体为最终的处方,其在50%血清中的稳定性良好,在A549细胞上的摄取效率较高且无细胞毒性,siRNA与其的包封率为72.43%,siRNA形成复合物后的形态电镜结果显示良好。结论选定和制备了具有良好体外理化性质的PEG化脂质体递送siRNA。
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