CMCT-FA修饰阿霉素纳米脂质体的制备与体外pH敏感释放

Preparation and in Vitro pH-Sensitive Release of CMCT-FA Modified Doxorubicin Nanoliposomes

利用1-乙基-3-(3-二甲基丙基)-碳二亚胺(EDC)介导反应合成了叶酸偶联的羧甲基壳聚糖(CMCT-FA),以阿霉素为模型药物,采用薄膜分散-pH梯度法制备CMCT-FA修饰的阿霉素纳米脂质体。考察了CMCT-FA修饰阿霉素纳米脂质体的包封率、粒径、ζ电位以及在不同pH释药介质中的释放特性。结果表明:CMCT-FA修饰阿霉素纳米脂质体的ζ电位较未修饰脂质体明显减小,但较CMCT修饰阿霉素纳米脂质体无明显差别;与阿霉素纳米脂质体和CMCT修饰的阿霉素纳米脂质体相比,CMCT-FA修饰的阿霉素纳米脂质体在酸性条件下的药物释放速率和药物释放量均有明显提高。

Folate-coupled carboxymethyl chitosan（CMCT-FA）was synthesized through the 1-ethyl-3-（3-dimethylaminopropyyl）-carbodiimide-mediated reaction.CMCT-FA modified pH-sensitive nanoliposomes were prepared by the film-pH gradient method using doxorubicin（DOX） as a model drug.The encapsulation efficiency,particle size distribution,ζ potential and drug release character of the nanoliposomes were investigated.The results showed that the ζ potential of CMCT-FA modified DOX nanoliposomes decreased significantly compared with unmodified DOX nanoliposomes,while changed slightly in comparison with CMCT modified DOX nanoliposomes.The release rate and cumulative release amount of DOX from nanoliposomes in acidic condition increased significantly after CMCT-FA modification.