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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

The preparation and characteristics of sterically stabilized liposomes containing paclitaxel and super-paramagnetic iron oxide nanoparticles
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摘要 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。 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.
作者 Wei Ren Shuang Zhang Ting Zhong Dan Huang Xin Yao Yang Guo Xiaochuan Duan Yifan Yin Shushi Zhang Xuan Zhang Wei Ren;Shuang Zhang;Ting Zhong;Dan Huang;Xin Yao;Yang Guo;Xiaochuan Duan;Yifan Yin;Shushi Zhang;Xuan Zhang;Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University Health Science Center;Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center
出处 《中国药学:英文版》 CAS CSCD 2016年第8期570-575,共6页 Journal of Chinese Pharmaceutical Sciences
基金 Specialized Research Fund for the Doctoral Program of Higher Education(Grant No.20120001110012)
关键词 紫杉醇 超顺磁性氧化铁纳米粒 脂质体 诊疗结合 Paclitaxel, Super-paramagnetic iron oxide nanoparticles, Sterically stabilized liposomes, Theranostics
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