穿膜肽修饰盐霉素胶束的制备与表征  

Preparation and properties of salinomycin micelles modified by tumor-penetrating peptide

作　　者：毛骁丽[1] 张翮[2] 俞媛[2] 鲁莹[2] 解方园 巩志荣[2] 孙治国[2] 何文婷[1] 钟延强[1,2] 

机构地区：[1]福建中医药大学药学院,福州350108 [2]第二军医大学药学院药剂学教研室,上海200433

出　　处：《中国新药杂志》2014年第23期2812-2816,共5页Chinese Journal of New Drugs

摘　　要：目的:制备靶向穿膜肽修饰的小粒径胶束,负载抗肿瘤干细胞药物盐霉素,构建具有肿瘤组织高渗透性的载药系统。方法:采用薄膜分散法制备盐霉素胶束,并以粒径、包封率、载药量、累积释放量等为指标综合考察其相关性质,CCK-8法考察体外抗肿瘤干细胞活性。结果:制备的盐霉素胶束粒径为13 nm,包封率为62.08%,载药量为5.72%,48 h累积释放量达62%,对Hep G2肝癌干细胞具有显著的抑制作用。结论:经优化制备的盐霉素胶束具有较小的粒径,较高的包封率和载药量,并具有一定的缓释作用,为进一步研究奠定了基础。Objective： To prepare salinomycin-loaded DSPE-PEG2000 micelles modified by CRGDK, a tumor-penetrating peptide. Methods： Salinomycin micelles were prepared by a thin-film utrasonieation method; and the morphology, particle size, the entrapment efficacy and drug loading were also investigated. In vitro antitumour effect was evaluated by CCK-8 methods. Results： The particle size, the entrapment efficacy and drug loading of salinomycin mieelles were 13 nm, 62.08% and 5.72% , respectively. The micelles released 62% of total drug during the first 24 h. In vitro antitumour effect was confirmed in HepG2 cells. Conclusion： Thin-film utrasonication is convenient to prepare salinomycin micelles. The micelles show the properties of small particle size, high entrapment efficiency and loading with the advantages of sustained release, which is useful for the further studies.

关 键 词：盐霉素 胶束 薄膜分散法 肿瘤干细胞 

分 类 号：R943.42[医药卫生—药剂学]