RDP多肽修饰的姜黄素隐形脂质体脑靶向作用的研究  

Brain targeting effect of PEGylated liposomes modified with RDP peptide

作　　者：项松涛[1] 赵明[1] 史现勋 付爱玲[1] 

机构地区：[1]西南大学药学院,重庆400716

出　　处：《中国药理学通报》2015年第8期1136-1141,共6页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 81273416);教育部高校基本科研业务费(No XDJK2013A030);教育部回国人员启动基金[教外司留(2012)940号];教育部新世纪优秀人才支持计划资助

摘　　要：目的以源于狂犬病毒糖蛋白的新型衍生肽(RVGderived peptide,RDP)为靶向载体,研究其修饰的姜黄素隐形纳米脂质体的特征和脑靶向作用。方法薄膜分散法制备出脂质体。体外释放实验考察释药情况。小鼠经尾静脉注射姜黄素混悬液(CUR)、姜黄素脂质体(CUR-L)、RDP修饰的姜黄素隐形脂质体(RDP-CUR-L),分别在不同时间点取小鼠组织器官,HPLC法检测姜黄素在各组织的分布。结果制备的隐形纳米脂质体粒径在100 nm左右,分散性良好,包封率大于85%,制备重现性较好。小鼠经尾静脉分别注射CUR、CUR-L和RDP-CUR-L后,CUR组并未在脑中检测到姜黄素,CUR-L组仅在脑中检测到少量姜黄素,而RDP-CUR-L组小鼠脑内检测到了较高浓度的姜黄素。结论RDP能够引导脂质体入脑,这将为治疗脑部疾病提供新的方法。Aim Targeted drug delivery in the brain is the necessary way for the treatment of brain diseases. In our study, a new peptide derived from the rabies vi- rus glycoprotein （RVG-derived peptide, RDP） was used as a targeted carrier to modify the curcumin stealth liposomes, and their characteristics and brain targeting effect were studied. Methods The curcumin liposomes were prepared by thin film dispersion. The release test in vitro was conducted to investigate their drug release. Curcumin distribution in several organs of mice was investigated by caudal vein injection of curcumin suspension liquid （CUR）, curcumin lipo- somes （CUR-L）, RDP modified curcumin stealth lipo- somes （RDP-CUR-L） via HPLC assay at different timepoints. Results The prepared stealth nano liposomes had a size of around 100 nm, and also had a good dis- persion and reproducibility. The entrapment efficiency was larger than 85%. After caudal vein injection of CUR, CUR-L and RDP-CURoL in mice respectively, no curcumin was detected in brain of CUR group, and only a little was detected in CUR-L group. Neverthe- less, high concentration of curcumin was detected in RDP-CUR-L group. Conclusion RDP can deliver li- posome into the brain, which may provide a new meth- od for the treatment of brain diseases.

关 键 词：姜黄素 RDP 脂质体 体内分布 细胞穿膜肽 脑靶向 

分 类 号：R-332[医药卫生] R282.71