PCM和TAT双修饰脂质体的制备及心肌靶向性的初步评价
Preparation of PCM and TAT co-modified liposomes and evaluation of its myocardium targeting effect
作者：王欣;陈华黎;黄华;
Author：
收稿日期： 年卷（期）页码：2016,31(04):-342-345
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：PCM;TAT;香豆素-6;双修饰脂质体;心肌靶向性
Key words：
基金项目：
中文摘要
目的研究心肌特异性靶向肽PCM和穿膜肽TAT双修饰的载荧光探针香豆素-6脂质体的制备工艺,并初步考察其心肌靶向性。方法采用薄膜分散-超声法,以PCM和TAT为靶头,制备以大豆磷脂、胆固醇、DSPE-m PEG_(2000)为载体材料的载香豆素-6的双修饰脂质体;优化香豆素-6用量、靶头连接方法及靶头用量,以形态、粒径分布、电位、包封率及体外稳定性对脂质体进行表征;考察心肌细胞H_9C_2对双修饰脂质体的摄取能力,表征其心肌靶向性。结果 PCM和TAT通过插入法连接,当PCM的用量为脂质的3%、TAT的用量为脂质的1%、香豆素-6的用量为20μg时,所制得的双修饰脂质体的形态圆整,粒径分布为115.7±2.91 nm,Zeta电位为-13.1±1.81 m V,包封率为83.2%±3.1%,具有良好的体外稳定性,双修饰脂质体的心肌细胞摄取率明显高于未修饰和单修饰的脂质体。结论双修饰脂质体的制备工艺简单,PCM和TAT双修饰可提高脂质体的心肌细胞靶向性。
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