白桦脂醇纳米乳的制备及其在S180荷瘤小鼠体内分布研究  

Preparation of betulin nanoemulsion and its distribution in S180 tumor-bearing mice

作　　者：王立鑫 李鑫[1] 蒙天琛 杨波[1] WANG Lixin;LI Xin;MENG Tianchen;YANG Bo(School of Pharmacy,Harbin University of Commerce,Harbin,Heilongjiang 150028,China)

机构地区：[1]哈尔滨商业大学药学院,黑龙江哈尔滨150028

出　　处：《湖南中医药大学学报》2024年第4期587-591,共5页Journal of Hunan University of Chinese Medicine

基　　金：中央支持地方高校改革发展资金人才培养项目。

摘　　要：目的制备白桦脂醇纳米乳,研究其在S180荷瘤小鼠体内的分布情况。方法通过相转变法制备白桦脂醇纳米乳,腹腔注射白桦脂醇纳米乳和白桦脂醇注射液,采用HPLC方法测定小鼠各组织中的药物浓度并计算药动学参数,分析比较两种制剂在小鼠体内组织分布情况。结果白桦脂醇纳米乳在各组织中Cmax和AUC依次为:肿瘤组织>肝>肾>脾>肺>心脏,且均高于白桦脂醇注射液组(P<0.05);肿瘤组织和肝脏的峰浓度比Ce分别为1.53和1.54;肿瘤的靶向效率Te值最大。结论与白桦脂醇注射液相比,白桦脂醇纳米乳在肿瘤组织和肝脏中的分布显著增加(P<0.01),白桦脂醇纳米乳对肿瘤组织具有明显的靶向性。Objective To prepare betulin nanoemulsion and study its distribution in S180 tumor-bearing mice.Methods Betulin nanoemulsion was prepared by phase transition method.After intraperitoneal injection of betulin nanoemulsion and betulin injection,HPLC method was used to determine the drug concentration in various tissues of mice and calculate the pharmacokinetic parameters.The tissue distribution of the two preparations in mice was analyzed and compared.Results The Cmax and AUC of betulin nanoemulsion in each tissue were as follows:tumor tissue>liver>kidney>spleen>lung>heart,all higher than those in betulin injection group(P<0.05);the peak concentration ratios(Ce)in tumor tissue and liver were 1.53 and 1.54,respectively;the tumor targeting efficiency(Te)value was the highest.Conclusion Compared with betulin injection,betulin nanoemulsion significantly increased distribution in tumor tissues and liver(P<0.01),and betulin nanoemulsion exhibited obvious targeting towards tumor tissues.

关 键 词：白桦脂醇 纳米乳 体内分布 靶向性 

分 类 号：R[医药卫生]