心肌细胞靶向脂质体的制备及体外靶向性研究  

Preparation of cardiomyocyte-targeting liposomes and their targeting ability in vitro

作　　者：陈妍[1] 邓英杰[1] 郝艳丽[1] 王振远[2] 盛军[2] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]长春生物制品研究所,吉林长春130062

出　　处：《药学学报》2005年第6期568-572,共5页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(30271548).

摘　　要：目的　制备心肌细胞靶向脂质体,并对其体外心肌细胞靶向性进行研究。方法　选用与β1 受体阻滞剂艾司洛尔结构类似的亲脂性化合物PAC修饰脂质体(PAC- L);将荧光标记的普通脂质体(Plain- L)与PAC L加入体外培养的心肌细胞中,在特定实验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　PAC -L与心肌细胞有较强的亲和力,且心肌细胞对PAC L的摄取显著高于非心肌细胞(P<0 .001);常氧条件下2h心肌细胞对PAC L的摄取较Plain- L高约2 9倍,而在缺氧条件下则高出5 2倍;心肌细胞对Plain -L的摄取约11%是以内吞方式摄取的,而对PAC- L则约有56%是以内吞方式进行的。结论　本文制备的PAC -L具有较强的心肌细胞特异靶向性,有可能成为一种有效的缺血心肌靶向性药物载体。Aim To prepare the cardiomyocyte-targeting liposomes and investigate their cardiomyocyte targetability in vitro. Methods Liposomes modified with compound 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. Results A high affinity of PAC-L to the cardiomyocytes was observed, the amount of cell uptake of ~PAC-L by cardiomyocytes was higher than that by nonmyocyte (P<0.001); The amount of cardiomyocyte uptake of PAC-L on the normoxia condition 2 h was 2.9-fold higher than that of plain-L, and the increase was 5.2-fold when hypoxia occured; The form of liposome uptake changed, the amount of cardiomyocyte uptake of Plain-L by internalization was only 11%, while that of PAC-L was 56%. Conclusion It is indicated that PAC-L was a potential drug carrier for targeting to ischemic myocardium.

关 键 词：心肌细胞 脂质体 靶向性 

分 类 号：R943.4[医药卫生—药剂学] R943.42[医药卫生—药学]