The preparation and characteristics of sterically stabilized liposomes containing paclitaxel and super-paramagnetic iron oxide nanoparticles  

包载超顺磁性氧化铁纳米粒和紫杉醇长循环脂质体的构建及表征（英文）

作　　者：任伟 张爽 钟婷[1,2] 黄丹 姚鑫 郭阳 段晓川 殷一凡 张漱石 张烜 

机构地区：[1]北京大学医学部药学院分子药剂学与新释药系统北京市重点实验室,北京100191 [2]北京大学医学部天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2016年第8期570-575,共6页中国药学（英文版）

基　　金：Specialized Research Fund for the Doctoral Program of Higher Education(Grant No.20120001110012)

摘　　要：Theranostics, combining therapy and diagnosis, is an appealing approach for chemotherapy. In the present study, we selected paclitaxel （PTX） as a therapeutic agent, super-paramagnetic iron oxide nanoparticles （SPIO） as a diagnostic agent and sterically stabilized liposomes as a carrier to prepare theranostic liposomes. The SPIO were prepared and characterized. Moreover, the sterically stabilized liposomes containing PTX and SPIO （PTX/SPIO-SSL） were prepared. The characteristics of PTX/SPIO-SSL were investigated. The results indicated that prepared SPIO exhibited super-paramagnetic and could be used for MRI. The average particle size of PTX/SPIO-SSL was about 170 rim, with a polydispersity index （PDI） less than 0.3. The zeta potential of PTX/SPIO-SSL was negative. The PTX entrapment efficiency of PTX/SPIO-SSL was more than 98%. The TEM results indicated the spherical structure and dense SPIO content in PTX/SPIO-SSL. The in vitro release of PTX from PTX/SPIO-SSL and PTX-SSL was almost identical at both pH 6.8 and 7.4. In conclusion, the PTX/SPIO-SSL were prepared and characterized in vitro. The anti-tumor and diagnostic activity of PTX/SPIO-SSL should be investigated deeply in future study.诊疗结合是目前抗肿瘤研究的一个新方向。在本文的研究中,我们制备超顺磁性氧化铁纳米粒(SPIO),随后,将SPIO和抗肿瘤药物紫杉醇(PTX)共包载于脂质体中,制备了兼具诊断与治疗功能的纳米给药系统(PTX/SPIO-SSL)。对制备的SPIO及PTX/SPIO-SSL进行表征,对PTX/SPIO-SSL的体外药物释放进行评价。实验结果显示,SPIO粒径均一,外观圆整,具备超顺磁性可用于MR成像。PTX/SPIO-SSL可成功包封SPIO,其粒径为170 nm左右,PDI小于0.3,粒径分布均匀,表面荷负电,紫杉醇的包封率均大于98%。体外药物释放试验表明,PTX/SPIO-SSL中紫杉醇的释放与PTX-SSL相似。有关PTX/SPIO-SSL的诊断与治疗作用将在后期的研究进行。

关 键 词：PACLITAXEL Super-paramagnetic iron oxide nanoparticles Sterically stabilized liposomes THERANOSTICS 

分 类 号：R943[医药卫生—药剂学]