硫酸铵梯度法提高双重载药纳米粒中小檗碱的载药量与包封率  

Study on increasing drug loading and encapsulation rate of berberine in dual drug-loading nanoparticles via ammonium sulfate gradient method

作　　者：姜爱玲 吴敏 JIANG Ailing;WU Min(Pharmacy Teaching and Research Office,School of Pharmacy,Chengdu Medical College,Chengdu 610500,China)

机构地区：[1]成都医学院药学院药剂学教研室,成都610500

出　　处：《西北药学杂志》2020年第4期554-560,共7页Northwest Pharmaceutical Journal

基　　金：四川省教育厅自然科学重点项目(编号:17ZA0110);成都医学院应用开发与成果转化培育项目(编号:CYCG17-01);成都医学院2017年国家级大学生创新创业项目(编号:201713705026)。

摘　　要：目的采用硫酸铵梯度法制备脂质膜(LB)包裹的中空介孔二氧化硅纳米粒(LB-HMSNS),将小檗碱(BBR)负载到HMSNs内,提高BBR的载药量和包封率。方法用薄膜水化法制备LB-HMSNs,通过马尔文激光粒度仪和透射电镜(TEM)表征其粒径、表面电荷和形态;通过被动载药法和硫酸铵梯度法将BBR负载到HMSNs内;用HPLC法测定2种方法BBR的含量;通过单因素实验对硫酸铵梯度法主动负载BBR进行优化,并探究吴茱萸碱(EVO)负载到LB上对BBR含量的影响。结果成功制备了LB-HMSNs,其最佳粒径为345 nm,多分散性指数(PDI)为0.199,Zeta电位为-27 mV;被动载药法最大载药量和包封率分别为8.41%和56.22%,硫酸铵梯度法在药脂比为1∶4时其载药量达10.3%,包封率为92%;优化结果显示,硫酸铵梯度法可将BBR载药量提高到被动载药的1倍以上(16.5%),包封率与被动载药基本一致;EVO的负载对BBR载药量和包封率的影响可忽略。结论硫酸铵梯度法可有效提高BBR的载药量和包封率。Objective To prepare lipid-coated hollow mesoporous silica nanoparticles(LB-HMSNs)for berberine(BBR)by ammonium sulfate gradient method,and to improve the drug loading capacity and encapsulation efficiency of BBR.Methods LB-HMSNs was prepared by dispersion film assay.The size,Zeta potential,shape were determined by laser particle analyzer and transmission electron microscope(TEM).BBR was loaded by passive drug loading and ammonium sulfate gradient method,and the contents were determined by HPLC.The ammonium sulfate gradient method was optimized by single factor experiment to improve the influence of evodiamine(EVO)to BBR.Results LB-HMSNs was successfully developed,and the optimal particle size was 345 nm,polydispersity index(PDI)was 0.199,Zeta potential was-27 mV.The largest drug loading and encapsulation efficiency of the passive loading method were 8.41%and 56.22%respectively.However when the ratio of drug to lipid was 1∶4,the drug loadings reached 10.3%and the envelopment rate increased to 92%.The results of optimization showed that the ammonium sulfate gradient method could improve BBR loading once more than the method of passive drug loading(16.5%),and the envelopment rate was basically identical.The effect of EVO load on the drug loading and encapsulation efficiency of BBR can be ignored.Conclusion The BBR drug loading and encapsulation rate could be improved by ammonium sulfate gradient method.

关 键 词：小檗碱 硫酸铵梯度法 被动载药法 中空介孔二氧化硅纳米粒 吴茱萸碱 

分 类 号：R944[医药卫生—药剂学]