膜修饰脂质体的制备及对心肌细胞的靶向作用

Preparation of surface-modified liposome and its targeting for cardiomyocytes in vitro

目的制备 3- {4 - [2- 羟基 (1- 甲基乙胺基 )丙氧基 ]辛基 }丙酸十六醇酯 (PAC)膜修饰脂质体 ,并对其体外心肌细胞靶向性进行研究。方法合成 β1 受体配体亲脂性化合物 (PAC)并制备PAC膜修饰的脂质体 (PAC- L) ;将荧光标记的脂质体加入体外培养的心肌细胞中 ,分别在常氧及缺氧条件下共同培养一定时间后 ,用荧光分光光度计测定心肌细胞摄取荧光脂质体的量。结果体外心肌靶向性研究表明PAC- L与心肌细胞有较强的亲和力 ,在常氧状态下心肌细胞对PAC L的摄取较Plain -L高约 3. 2倍 ,而在缺氧状态下心肌细胞对PAC- L的摄取较Plain- L高达 5 1倍。

Objective To prepare the liposomes surface-modified with 3-{4-[2-hydroxyl-(1-methyl ethylamino)propoxy]phenyl} propionic acid cetylester(PAC) and investigate the cardiomyocyte targeting in vitro.Method PAC was synthesized,and the liposomes surface-modified with PAC were prepared(PAC-L);The uptake of PAC-L by cardiomyocytes was studied by incubating fluorescence labeled liposomes with cardiomyocytes in vitro and measuring the association of liposomes by a fluorescence spectrophotometer.Result A high affinity of PAC-L to the cardiomyocytes was observed,the amount of cell uptake of PAC-L under the normoxic condition was 3.2-fold higher than that of plain-L(P<0.001),and the increase was 5.1-fold when hypoxia happened(P<0.001). Conclusion It indicates that PAC-L was a potential drug carrier for targeting to ischemic myocardium.