An amphiphilic dendritic drag carrier compound, 6-Ann 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. 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 O. 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 concentrations. And it was interested that the aggregates morphological characteristics was changed from tubes to niosomes along with the addition of various contents of water.%以苯甲酸为模型药物分子,设计合成了两亲性树枝状药物载体化合物6.Arm MPEG-Drug conjugate.采用1H NMR和13 C NMR谱对其结构进行了表征.1H NMR结果表明,载体化合物在有机溶剂和水中表现出不同的聚集行为,在水中可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了该化合物在水中的胶束化行为.结果显示,该化合物具有很低的临界胶束浓度[2.5×10-2 mg/mL(5.3×10-6moL/L)];它在水溶液中浓度为1.0mg/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,初始浓度不同时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.
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