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

作　　者：王丽丹[1] 钱秀珍[1] 杨善祥[1] 徐云龙[1] 

机构地区：[1]华东理工大学材料科学与工程学院,超细材料制备与应用教育部重点实验室,上海200237

出　　处：《华东理工大学学报（自然科学版）》2012年第2期176-180,共5页Journal of East China University of Science and Technology

基　　金：上海市重点学科建设项目;上海市纳米科技专项(0952nm06000)

摘　　要：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.

关 键 词：阿霉素 纳米脂质体 羧甲基壳聚糖 叶酸 PH敏感 EDC 

分 类 号：R944.1[医药卫生—药剂学]