β-环糊精-聚乙二醇-α-常春藤皂苷自组装胶束的制备和抗肿瘤活性研究  

Preparation of β-CD-PEG-α-hederin self-assembly micelle and its anti-tumor activity

作　　者：周军[1] 刘健 ZHOU Jun;LIU Jian(Department of Pharmacy,Jiangxi Breast Hospital,Nanchang 330006,China)

机构地区：[1]江西省胸科医院药剂科,江西南昌330006

出　　处：《现代药物与临床》2021年第7期1375-1378,共4页Drugs & Clinic

基　　金：江西省卫生计生委中医药科研课题(2017B096)。

摘　　要：目的研究β-环糊精-聚乙二醇-α-常春藤皂苷自组装胶束的制备、溶血性和体内外抗肿瘤活性。方法采用自组装方法制备了β-环糊精-聚乙二醇-α-常春藤皂苷的纳米胶束,考察了胶束在大鼠全血中的溶血性,研究了胶束在不同细胞上的体外活性,以荷HT29肿瘤细胞的小鼠为模型,研究了胶束的体内抗肿瘤活性。结果β-环糊精-聚乙二醇-α-常春藤皂苷在水性介质中能自组装成粒径较小的纳米胶束。该胶束能显著降低α-常春藤皂苷的溶血性;在体外细胞实验中,胶束的抗肿瘤活性明显低于α-常春藤皂苷,这可能与在体外环境中α-常春藤皂苷不能从胶束中释放出来有关。β-环糊精-聚乙二醇-α-常春藤皂苷自组装胶束在HT29荷瘤小鼠体内显示非常好的抗肿瘤活性。结论β-环糊精-聚乙二醇-α-常春藤皂苷自组装胶束为皂苷的减毒增效提供了一个非常好的研究模式。Objective To prepare β-CD-PEG-α-hederin self-assembly micelle, and to study its preparation, hemolytic activity and the anti-tumor in vitro and in vivo. Methods The micelle was prepared with the self-assembly method. The hemolytic activity was studied with the rat blood. The in vitro and in vivo pharmacological activity was studied with cancer cell and tumor xenograft mice,respectively. Results The micelle was self-assembled in the aqueous solvent with small diameter. The hemolytic activity of β-CD-PEG-α-hederin micelle could be negligible when compared with α-hederin. The in vitro cytotoxicity of β-CD-PEG-α-hederin micelle was very low which may be related to the inability of α-hederin to be released from micelles in the in vitro environment. The micelle displayed a high anti-tumor activity in HT29-bearing mice. Conclusion The study of β-CD-PEG-α-hederin self-assembly micelle provides a basis for attenuation and enhancement of saponins.

关 键 词：α-常春藤皂苷 β-环糊精-聚乙二醇-α-常春藤皂苷自组装胶束 制备 溶血性 抗肿瘤 

分 类 号：R944[医药卫生—药剂学]