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mPEG接枝葡聚糖偶联肉桂醛的合成及pH敏感释放
引用本文:陶丽,姚日生,刘璐,李曼曼.mPEG接枝葡聚糖偶联肉桂醛的合成及pH敏感释放[J].安徽化工,2009,35(4):22-26.
作者姓名:陶丽  姚日生  刘璐  李曼曼
作者单位:合肥工业大学化学工程学院,安徽,合肥,230009;合肥工业大学化学工程学院,安徽,合肥,230009;农产品生物化工教育部工程研究中心,安徽,合肥,230009
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。

关 键 词:肉桂醛  葡聚糖  单甲氧基聚乙二醇  肿瘤靶向

Synthesis and pH Sensitive Release of Conjugate of Dextran Coupled with Cinnamyl Aldehyde and Grafted with mPEG
TAO Li,YAO Ri-sheng,LIU Lu,LI Man-man.Synthesis and pH Sensitive Release of Conjugate of Dextran Coupled with Cinnamyl Aldehyde and Grafted with mPEG[J].Anhui Chemical Industry,2009,35(4):22-26.
Authors:TAO Li  YAO Ri-sheng    LIU Lu  LI Man-man
Affiliation:TAO Li1,YAO Ri-sheng1,2,LIU Lu1,LI Man-man1 (1. Chemical Engineering College,Hefei University of Technology,Hefei 230009,China,2. Engineering Research Center of Bio-process of Ministry of Education,China)
Abstract: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.
Keywords:Cinnamyl aldehyde  Dextran  Monomethoxypoly(ethylene glycol)  tumor-targeted  
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