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).