高等学校化学学报 ›› 2011, Vol. 32 ›› Issue (6): 1389.

• 研究论文 • 上一篇    下一篇

用于纳米载药系统的两亲性聚乙二醇-药物分子偶联体的合成及胶束化性质

梁海岩, 吴学, 金慧娟   

  1. 延边大学长白山生物资源与功能分子教育部重点实验室, 延吉 133002
  • 收稿日期:2010-08-11 修回日期:2010-12-08 出版日期:2011-06-10 发布日期:2011-05-10
  • 通讯作者: 金慧娟 E-mail:jinhj@ybu.edu.cn
  • 基金资助:

    国家自然科学基金(批准号: 20762011)资助.

Synthesis and Micelle Characterization of Amphiphilic MPEG-Drug Conjugate Used in Drug Delivery System 

LIANG Hai-Yan, WU Xue, JIN Hui-Juan*   

  1. Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education,  Yanbian University, Yanji 133002, China
  • Received:2010-08-11 Revised:2010-12-08 Online:2011-06-10 Published:2011-05-10
  • Contact: JIN Hui-Juan E-mail:jinhj@ybu.edu.cn
  • Supported by:

    国家自然科学基金(批准号: 20762011)资助.

摘要: 设计和合成了两亲性树枝状药物载体化合物6-Arm MPEG-Drug Conjugate,其中所使用的模型药物分子为苯甲酸.用1H NMR和13C NMR测试对结构进行了表征. 1H NMR谱图表明载体化合物在有机溶剂和水中表现不同的聚集行为,在水中自组装形成纳米微粒.利用荧光探针技术、动态激光光散射和扫描电镜研究其在水中的胶束化行为.结果显示,该药物载体化合物具有很低的临界胶束浓度,2.5×10-2 mg/mL (5.3×10-6 mol/L);在水溶液中浓度为1.0 mg/mL时的流体力学直径为67.4 nm,多分散指数为0.106;通过扫描电镜观察发现,初始浓度不同形成的聚集体形态也不同,得到了管状和方形结构胶束,而且随着不同水量的加入,聚集态从管状转变为囊泡状结构.

关键词: 药物载体, 胶束, 囊泡, 两亲性, 聚乙二醇单甲醚

Abstract: An amphiphilic dendritic drug carrier compound 6-Arm MPEG-Drug Conjugate was designed and synthesized in which benzoic acid was used as model drug. The molecular structure was characterized by means of 1H NMR and 13C NMR spectroscopy. 1H NMR verified that 6-Arm MPEG-Drug Conjugate changed conformation in organic solvent and in aqueous solution. It assembled to nano-sized particle in aqueous solution. So the micelle characteristics of 6-Arm MPEG-Drug Conjugate in water were investigated by fluorescence spectroscopy, dynamic light scattering (DLS) and scanning electron microscopy (SEM). The critical micelle concentration (CMC) was determined by a fluorescence technique to be 2.5×10-2 mg/mL (5.3×10-6 mol/L); The hydrodynamic diameter of micelle was measured to be 67.4 nm at the concentration of 1.0 mg/mL by DLS and the polydispersity index (PDI) was estimated to be 0.106. In addition, 6-Arm MPEG-Drug Conjugate exhibited different aggregation behavior. It was found that tubes and microcubic particles could be formed at the different initial concentration. And it was interested that the aggregates morphological characteristics was changed from tubes to niosomes along with the addition of various contents of water.

Key words: drug carrier, micelle, niosome, amphiphilic, MPEG

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