mPEG接枝葡聚糖偶联肉桂醛的合成及pH敏感释放  

Synthesis and pH Sensitive Release of Conjugate of Dextran Coupled with Cinnamyl Aldehyde and Grafted with mPEG

作　　者：陶丽[1] 姚日生[1,2] 刘璐[1] 李曼曼[1] 

机构地区：[1]合肥工业大学化学工程学院,安徽合肥230009 [2]农产品生物化工教育部工程研究中心,安徽合肥230009

出　　处：《安徽化工》2009年第4期22-26,共5页Anhui Chemical Industry

摘　　要：采用高碘酸钠氧化葡聚糖制成聚醛基葡聚糖，以己二酰肼为间隔臂，通过生成腙键分别偶联肉桂醛，接枝醛化mPEG。透射电镜观察该偶联物在水相中可自组装成粒径为200～300nm的纳米胶束。紫外跟踪检测在pH为5．4、6．8、7．4缓冲液中的释放行为，显示肉桂醛的释放速率v（pH=5．4）〉〉v（pH=6．8）〉v（pH=7．4）。所制该载药隐形纳米粒将可借助EPR效应被动靶向富集于肿瘤组织；在拟肿瘤细胞溶酶体pH≈5．4环境下可敏感释药，因而将具备一定的肿瘤靶向释药性能。A new drug delivery system of Dextran coupled with Cinnamyl aldehyde and grafted with mPEG, by the bond of hydrazone which was sensitive to pH=5.4 weak acidic environment was designed and prepared. The conjugate could assemble to nanoparticle with the diameter of 200-300nm in water, and then might beneficiate passively to tumor tissue through the effect of EPR. The release rate of cinnamyl aldehyde from the conjugate showed the tendency of v （pH=5.4） 〉〉v（pH=6.8）〉v（pH=7.4）. It meant that the prepared structure of conjugate might be unstable to the acidic environment of tumor cell and the drug would be released sensitively.

关 键 词：肉桂醛 葡聚糖 单甲氧基聚乙二醇 肿瘤靶向 

分 类 号：R914.4[医药卫生—药物化学] R979.1[医药卫生—药学]