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中国药学(英文版) ›› 2016, Vol. 25 ›› Issue (8): 570-575.DOI: 10.5246/jcps.2016.08.063

• 【研究论文】 • 上一篇    下一篇

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

任伟1,2, 张爽1,2, 钟婷1,2, 黄丹1,2, 姚鑫1,2, 郭阳1,2, 段晓川1,2, 殷一凡2, 张漱石2, 张烜1,2*   

  1. 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
  • 收稿日期:2016-05-15 修回日期:2016-05-29 出版日期:2016-09-01 发布日期:2016-06-12
  • 通讯作者: Tel.: +86-010-82805928, E-mail: xuanzhang@bjmu.edu.cn
  • 基金资助:
    Specialized Research Fund for the Doctoral Program of Higher Education (Grant No. 20120001110012).

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

Wei Ren1,2, Shuang Zhang1,2, Ting Zhong1,2, Dan Huang1,2, Xin Yao1,2, Yang Guo1,2, Xiaochuan Duan1,2, Yifan Yin2, Shushi Zhang2, Xuan Zhang1,2*   

  1. 1. Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
    2. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2016-05-15 Revised:2016-05-29 Online:2016-09-01 Published:2016-06-12
  • Contact: Tel.: +86-010-82805928, E-mail: xuanzhang@bjmu.edu.cn
  • Supported by:
    Specialized Research Fund for the Doctoral Program of Higher Education (Grant No. 20120001110012).

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, 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SPIOPTX/SPIO-SSL进行表征, PTX/SPIO-SSL的体外药物释放进行评价。实验结果显示, SPIO粒径均, 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: 紫杉醇, 超顺磁性氧化铁纳米粒, 脂质体, 诊疗结合

Abstract:

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 nm, 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. 

Key words: Paclitaxel, Super-paramagnetic iron oxide nanoparticles, Sterically stabilized liposomes, Theranostics

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