MAO Xuhong, LIN Kunhua, ZHANG Liming, et al. Investigation of cationic glycogen derivatives conjugated with vitamin B12 residues[J]. Acta Scientiarum Naturalium Universitatis SunYatseni, 2019,58(4):68-77.
MAO Xuhong, LIN Kunhua, ZHANG Liming, et al. Investigation of cationic glycogen derivatives conjugated with vitamin B12 residues[J]. Acta Scientiarum Naturalium Universitatis SunYatseni, 2019,58(4):68-77. DOI: 10.13471/j.cnki.acta.snus.2019.04.007.
H 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%。GDVB12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。
Abstract
A cationic glycogen derivative conjugated with vitamin B12 (VB12) residues (GD-VB12) was synthesized and characterized using FTIR and
1
H 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
1
H 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
Keywords
glycogenglycogen derivativessynthesisstability in digestive tractbiodegradability