ADM-PBCA载药纳米微球的制备及其界面Tf靶向载体的修饰  

Preparation and transferrin surface modification of PBCA ADM-loaded nanospheres

作　　者：曾竞[1] 李周明[1] 杨培慧[1] 蔡继业[1] 

机构地区：[1]暨南大学化学系,广东广州510632

出　　处：《东南大学学报（医学版）》2011年第1期18-23,共6页Journal of Southeast University(Medical Science Edition)

基　　金：国家自然科学基金资助项目(21071064);科技部973项目(2010CB833603)

摘　　要：为了提高临床抗肿瘤药物的疗效,降低其毒副作用,本研究探讨以阿霉素(ADM)为模型药物,以聚氰基丙烯酸正丁酯(PBCA)为载体,通过乳化聚合法制备PBCA载药纳米微球并对其表征;利用红外光谱探讨载药纳米微球的结合机理,检测了PBCA载药纳米微球的体外释药性能;最后将PBCA载药纳米微球经十六烷基三甲基溴化铵对其表面改性后,利用化学键合方法在其表面修饰上转铁蛋白(Tf),旨在实现药物的主动靶向性。通过L9(33)正交设计实验发现,优化后的载药纳米微球平均粒径为276.7 nm,平均包封率为(54.74±1.52)%,平均载药量为(26.07±1.63)%,分散性及成球性良好。另外体外释药实验表明,PBCA载药纳米微球具有良好的缓释性能和双相释药特性,符合双相动力学方程:Q=0.516 1+36.02e(-t/6.151 2)+5.87e(-t/1.61)(r=0.989 5)。In the interests of advancing clinical curative effect and reducing side-effect of antitumor drugs,this paper described adriamycin（ADM） as model drug,polybutylcyanoacrylate（PBCA） as drug delivery material,drug-loaded PBCA nanospheres was synthesized in emulsified solution and then characterizated.The conjunct mechanism of nanospheres were studied by FT-IR.The controlled-release of PBCA drug-loaded nanospheres in vitro were investigated as well.Furthermore,ADM-PBCA were surface modified by CTAB,and then targeted by transferrin via chemical bonding.The measurements of ADM-PBCA nanospheres were： the mean diameter was 276.7 nm,the mean encapsulation rate was（54.74±1.52）%,the mean loading was（26.07±1.63）%,the dispersancy and conglobation of nanospheres were fine.The release in vitro showed that,the PBCA drug-loaded nanospheres possessed the characterization of sustained-release and biophases-release,in accordance with the biophases kinetic equation： Q=0.516 1＋36.02e（-t/6.151 2）＋ 5.87e（-t/1.61）（r=0.989 5）.

关 键 词：聚氰基丙烯酸正丁酯 阿霉素 载药微球 体外释药 转铁蛋白靶向 

分 类 号：R313[医药卫生—基础医学]