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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-ALG NPs).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-ALG NPs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-ALG NPs)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3 h后,DOX/GA-ALG NPs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-ALG NPs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.
Hydrophilic liver-targeting small molecule glycyrrhetinic acid (GA) was linked to natural polysaccharide sodium alginate (ALG) by EDC / NHS coupling reaction to prepare amphipathic liver targeting drug carrier material (GA-ALG). (DOX) was encapsulated by emulsion method to obtain liver-targeting drug-loaded nanoparticles (DOX / GA-ALG NPs) .Using single photon emission computed tomography (SPECT) and drug The liver targeting of DOX / GA-ALG NPs was evaluated by in vivo distribution.SPECT imaging showed that 99mTc-labeled blank nanoparticles (99mTc-GA-ALG NPs) were mainly localized in the liver of Wistar rats, 40.2% .The results of tissue distribution showed that the adriamycin concentration in liver of DOX / GA-ALG NPs group reached 67.7μg / g after 3 h of tail vein injection, which was 4.7 times higher than DOX.HCl group.The relative uptake rate (re), targeting efficiency (te) and weighted average targeting efficiency (te *) data also showed that DOX / GA-ALG NPs had significant liver targeting ability.Research shows that glycyrrhetinic acid modified sodium alginate nano-drug delivery system has Good liver targeting.