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甘草次酸修饰海藻酸钠纳米给药系统的肝靶向性评估

DOI: 10.3724/SP.J.1105.2011.11086, PP. 817-823

Keywords: 甘草次酸,海藻酸盐,纳米给药系统,靶向效率

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Abstract:

通过EDC/NHS偶联反应将疏水性肝靶向小分子甘草次酸(GA)连接到天然多糖海藻酸钠(ALG)上,制备了具有双亲性肝靶向药物载体材料(GA-ALG).采用乳化法对广谱抗癌药物阿霉素(DOX)进行包载,得到肝靶向载药纳米粒子(DOX/GA-ALGNPs).利用单光子发射型计算机断层成像技术(SPECT)和药物体内分布实验对DOX/GA-ALGNPs的肝靶向性进行了评估.SPECT成像显示,99mTc标记空白纳米粒子(99mTc-GA-ALGNPs)主要集中在Wistar大鼠的肝脏部位,富集率达40.2%.药物体内组织分布结果显示,尾静脉注射3h后,DOX/GA-ALGNPs组小鼠肝脏中阿霉素浓度达到67.7μg/g,是DOX·HCl组的4.7倍.相对摄取率(re)、靶向效率(te)和加权平均靶向效率(te*)数据同样表明DOX/GA-ALGNPs具有显著肝靶向能力.研究表明甘草次酸修饰海藻酸钠纳米给药系统具有良好的肝靶向性.

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