增溶瑞香素稳定囊泡作为药物载体探究.docVIP

增溶瑞香素稳定囊泡作为药物载体探究 　 作者：胡长刚 王仲妮 李干佐 谢辉 安娅 张笑一 廖莉玲 【摘要】 目的 探讨增溶瑞香素的稳定囊泡作为药物载体的优越性。方法 选择生理上能接受的2种表面活性剂，即仿生磷酯阳离子表面活性剂PTA与阴离子表面活性剂SDS，按一定比例复配能自发形成稳定性囊泡，用负染色透射电镜和动态光散射对其进行表征，并以其作为药物瑞香素的载体开展其组成、温度对包封率的影响，以及在模拟胃液及模拟肠液中的释放情况的研究。结果 在表面活性剂总浓度为5.0×10-3mol/L，PTA/SDS=3∶7时，囊泡粒径最大为151.1nm，包封率最高为28.2%。它们在模拟胃液和模拟肠液中释放75%的时间分别为240min和340min。结论 本研究对于阴阳离子表面活性剂复配自发形成囊泡作为药物载体进行了探索性工作，并对实验现象和结果从理论上进行讨论，为今后的研究指出方向。 【关键词】 囊泡 瑞香素 粒径 包封率 释放分数 药物载体 【Abstract】 Objective To study drug delivery of the stable vesicles with daphnetin solubilization.Methods Stable vesicles were formed from mixed solution of cation surfactant PTA and anion surfactant SDS at proper proportions. The formation and characters of the vesicles were demonstrated by negative-staining TEM and dynamic light scattering. Using the vesicles as the delivery of daphnetin， we carried out the research on the effect of formation and temperature upon entrapment efficiency. Research had also been carried out upon the release circumstance of daphnetin contained in the vesicles in simulated gastric and intestinal fluid.Results The results showed that entrapment efficiency of the vesicles reached a max of 28.2%， and the diameter reached a max of 151.1nm when the total concentration of surfactants were 5.0×10-3mol/L，PTA/SDS=3∶7. In simulated gastric and intestinal fluid ，the time for the release rate of daphnetin containing vesicles reaching 75% were respectively 240 minutes and 340 minutes.Conclusion This study has made an exploration research on utilizing vesicles spontaneously-formed from mixed solution of cation surfactant and anion surfactant as drug delivery， and a theoretical exploration is also presented in this paper about the phenomena and results of experiment. 【Key words】 vesicle daphnetin diameter entrapment efficiency release percent drug delivery 由于阴阳离子表面活性剂复配必然产生强烈的电性作用，因而使表面活性大大提高，显示出极大的增效作用，因此渐渐地应用于实际［1］。囊泡作为分子有序组合体的一个重要分支，被广泛地应用于模拟生物膜［2］，合成纳米材料［3］、作为微反应器［4］和药物载体［5］等科技领域。囊泡作为药物载体具有防止药物降解失活，延长药物的作用时间以及降低毒副作用等特点，因而囊泡包