两性霉素B磁性脂质体的制备及磁靶向性研究  

Preparation and magnetic targeting of Amphotericin B magnetic liposomes

作　　者：赵梦玉[1] 张丽男[1] 孙勇军[1] 谢英花[1] 吴韶梅[1] 陈小龙[1] 高子彬[1] 

机构地区：[1]河北科技大学,河北石家庄050018

出　　处：《华西药学杂志》2014年第6期618-621,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81402886);河北省自然科学基金(H2014208004;H2012208080);河北省教育厅基金(QN2014093)

摘　　要：目的制备两性霉素B磁性脂质体(Am B-MLPs)并研究其在小鼠肺部的磁靶向性和组织分布。方法采用薄膜分散加超声的方法制备Am B-MLPs,并考察其性质。将小鼠随机均分为Am B注射液组、Am B-MLPs组及Am B-MLPs肺部加磁场组,各组小鼠均经尾静脉注射给药,测定不同时间点血浆中及组织中的药物浓度,比较各组织的药-时分布曲线、药时曲线下面积(AUC);采用DAS Ver1.0程序拟合求算药动学参数。结果所制备的Am B-MLPs平均粒径为246 nm,平均包封率为78.02%,有体外磁场响应性;Am B-MLPs加磁场组肺内的AUC是Am B注射液组的2.02倍,是Am B-MLPs组的1.47倍。Am B-MLPs加磁场组与Am B-MLPs组的靶向率比较,除肺部te值增大外,其他组织的te值均下降。结论制备的Am BMLPs在磁场作用下浓集于靶部位,具良好的磁靶向性。OBJECTIVE To prepare Amphotericin B magnetic liposomes（ Am B- MLPs） and investigate the magnetic targeting function of lung in mice and the tissue distribution. METHODS Am B- MLPs were prepared by means of film dispersion- ultrasonicationand its physical properties were studied. The rats were randomly divided into Am B injection group,Am B- MLPs group and Am B- MLPs in presence of magnetic field via lung group. The drug concentration in blood and other tissues were surveyed at predetermined time after intravenously administration. Drug- time distribution curves and AUC of tissues were compared. The pharmacokinetic parameters were calculated with DAS Ver1. 0. RESULTS The mean size of particles was 246 nm,and the mean encapsulation efficiency was 78. 02%,which has a good magnetic responsiveness. Compared with Am B injection group and Am B- MLPs group,the AUC of Am B- MLPs in presence of magnetic field of the lung group was improved 2. 02 and 1. 47 times,respectively. The targeting efficiency（ te） of other tissues in the Am B- MLPs in presence of magnetic field group was declined,while the teof lung was risen compared with the Am B- MLPs group. CONCLUSION The Am B- MLPs show the good targeting property when exposed in the magnetic field.

关 键 词：两性霉素B 磁性脂质体 药物动力学 组织分布 磁靶向性 

分 类 号：R94[医药卫生—药剂学]