偶联维生素B12基团的阳离子糖原衍生物  

Investigation of cationic glycogen derivatives conjugated with vitamin B12 residues

作　　者：毛旭宏 林坤华 张黎明 杨立群 MAO Xuhong;LIN Kunhua;ZHANG Liming;YANG Liqun(School of Materials Science and Engineering∥School of Chemistry∥Key Laboratory for PolymericComposite and Functional Materials of Ministry of Education∥Guangdong Provincial Key Laboratory forHigh Performance Polymer-based Composites, Sun Yat-sen University, Guangzhou 510275, China)

机构地区：[1]中山大学材料科学与工程学院//中山大学化学学院//聚合物复合材料及功能材料教育部重点实验室//广东省高性能树脂基复合材料重点实验室

出　　处：《中山大学学报（自然科学版）》2019年第4期68-77,共10页Acta Scientiarum Naturalium Universitatis Sunyatseni

基　　金：广东省自然科学基金重点项目(2017B030311007);广东省公益研究与能力建设专项(2016A020222017);广州市科技计划(201607010249)

摘　　要：以糖原为原料合成偶联VB12基团的阳离子糖原衍生物(GD-VB12),将作为口服纳米药物的载体材料。FTIR和 1H NMR结果证实二乙烯三胺阳离子基团和VB12基团均与糖原分子发生偶联,它们的取代度分别为0.9%和0.6%。GD-VB12衍生物在水中能形成纳米粒,粒径约为200 ~ 300 nm。GD-VB12衍生物在模拟胃液和小肠液中稳定性较高,有利于携带口服药物安全地通过消化道。GD-VB12衍生物在1 h内能快速被糖原磷酸化酶a降解。因此,GD-VB12衍生物将有可能作为口服药物的纳米传输载体被小肠吸收而进入体循环后,在肝脏和肌肉定位释放药物。A cationic glycogen derivative conjugated with vitamin B12 (VB12) residues (GD-VB12) was synthesized and characterized using FTIR and 1H NMR spectroscopy, which could be used as a nano-carrier for oral delivery of drugs. The degree of distribution of diethylenetriamine and VB12 residues were determined to be 0.9% and 0.6% using 1H NMR integral method and UV-vis spectroscopy, respectively. The GD-VB12 derivative was observed as particles with irregular shape in the sizes ranging from 200 to 300 nm. It exhibited a high stability in the simulated gastric medium and the simulated small intestinal medium, and is beneficial for safe delivery of drugs through the digestive tract. The GD-VB12 derivative could be rapidly degraded by glycogen phosphorylase a within 1 h. Therefore, the GD-VB12 derivative possesses potential as a carrier for oral delivery of drugs safely and targeted release of drugs in the liver and muscle.

关 键 词：糖原 糖原衍生物 合成 消化道稳定性 生物降解性能 

分 类 号：O636.12[理学—高分子化学]