叶酸修饰的苦参总黄酮固体自微乳的制备  

Preparation of Total Flavonoids of Sophora Flavescens Solid Self-Microemulsion Modified by Folic Acid

作　　者：杨志欣[1] 刘天教 卞士嘉 王楠[1] 王鑫[1] 王艳宏[1] YANG Zhixin;LIU Tianjiao;BIAN Shijia;WANG Nan;WANG Xin;WANG Yanhong(Key Laboratory of Chinese Materia Medica(Ministry of Education),Heilongjiang University of Chinese Medicine,Harbin 150040 Heilongjiang,China)

机构地区：[1]黑龙江中医药大学北药基础与应用研究教育部重点实验室,黑龙江哈尔滨150040

出　　处：《中药新药与临床药理》2023年第2期256-262,共7页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：黑龙江省自然科学基金项目(H2016057,H2017066);黑龙江中医药大学“优秀创新人才支持计划”项目(2012,2018)。

摘　　要：目的 制备叶酸修饰的苦参总黄酮固体自微乳,评价其理化性质及细胞毒性。方法 以苦参酮、槐属二氢黄酮G、异黄腐醇的吸收率为指标,采用大鼠在体结肠循环试验筛选叶酸修饰的苦参总黄酮自微乳的处方;以粒径和Zeta电位为指标,单因素考察确定叶酸修饰的苦参总黄酮固体自微乳处方的吸附材料种类和用量。考察优选后的自微乳对人结肠癌细胞(HT-29细胞)的细胞毒性。结果 当叶酸-聚乙二醇-二硬脂酰磷脂酰乙醇胺与乳化剂的比值为3∶100时,能显著提高结肠组织对苦参酮、槐属二氢黄酮G、异黄腐醇的吸收(P<0.05);叶酸修饰的苦参总黄酮自微乳∶α-乳糖质量最佳比例为1∶2;制备的叶酸修饰的苦参总黄酮固体自微乳透射电镜下呈现类球的实体粒子,粒径为(38.5±1.0) nm,Zeta电位为-(32.1±1.1) mV;细胞毒性实验表明叶酸修饰的苦参总黄酮固体自微乳对HT-29细胞具有显著的抑制作用(P<0.05)。结论 该研究成功制备了叶酸修饰的苦参总黄酮固体自微乳,其对HT-29具有较好的抑制作用。Objective To prepare total flavonoids of Sophora Flavescens solid self-microemulsion modified by folic acid(TF-S-FSMEDDS), and to evaluate its physicochemical properties and cytotoxicity. Methods Taking the absorption rate of kurarinone,sophoraflavanone G and isoxanthohumol as indicators,we screened the formulation of TF-S-FSMEDDS by colonic circulation test in rats. Moreover, the particle size and Zeta potential were used as indicators,the single factor investigation was used to determine the type and dosage of adsorbents for the formulation of TF-S-FSMEDDS. The cytotoxicity of the optimized self-microemulsion against HT-29 cell lines was investigated.Results When the ratio of folic acid-polyethylene glycoldistearoyl phosphatidylethanolamine(FA-PEG-DSPE) to emulsifier was 3∶100, it could significantly improve the colonic absorption of kurarinone, sophoraflavanone G,isoxanthohumol(P<0.05). The optimum mass ratio of TF-S-FSMEDDS to α-lactose was 1∶2. The prepared TF-SFSMEDDS showed uniform spherical-like solid particles under transmission electron microscope,and the particle size was(38.5±1.0)nm,and the Zeta potential was-(32.1 ± 1.1) mV. The cytotoxicity experiment showed that TF-S-FSMEDDS has a significant inhibitory effect on HT-29 cells(P<0.05). Conclusion In this study,TF-SFSMEDDS was successfully prepared,which showed a good inhibitory effect on HT-29 cells.

关 键 词：苦参总黄酮 自微乳系统 叶酸受体 制备工艺 

分 类 号：R283.6[医药卫生—中药学]