Chen Kuo-Yu, Zeng Si-Ying
Department of Chemical and Materials Engineering, National Yunlin University of Science and Technology, Yunlin 64002, Taiwan.
Polymers (Basel). 2017 Jun 7;9(6):210. doi: 10.3390/polym9060210.
In this study, 2-[(Acryloyloxy)ethyl]trimethylammonium chloride was graft polymerized onto chitosan (CS) to form quaternary ammonium CS (QAC) by using ammonium persulfate as a redox initiator. Alginate (ALG) microspheres loaded with a water-soluble macromolecular model drug, blue dextran (BD), were obtained by corporation of coaxial gas-flow method and ionic gelation process. CS and QAC were then coated on the surfaces of ALG microspheres to generate core/shell structured CS/ALG and QAC/ALG microspheres, respectively. The experiment result showed that QAC/ALG microspheres had a smaller particle size due to the stronger electrostatic interactions between QAC and ALG molecules. In vitro drug release studies at pH 7.4 and pH 9.0 exhibited that the release rate of BD was significantly decreased after ALG microspheres coating with CS and QAC. Moreover, ALG microspheres coated with QAC showed a prolonged release profile for BD at pH 9.0. Therefore, QAC/ALG microspheres may be a promising hydrophilic macromolecular drug carrier for a prolonged and sustained delivery.
在本研究中,以过硫酸铵作为氧化还原引发剂,将2-[(丙烯酰氧基)乙基]三甲基氯化铵接枝聚合到壳聚糖(CS)上,形成季铵化壳聚糖(QAC)。通过同轴气流法和离子凝胶化过程相结合,获得了负载水溶性大分子模型药物蓝色葡聚糖(BD)的海藻酸钠(ALG)微球。然后将CS和QAC分别包覆在ALG微球表面,制备出核/壳结构的CS/ALG和QAC/ALG微球。实验结果表明,由于QAC与ALG分子之间较强的静电相互作用,QAC/ALG微球具有更小的粒径。在pH 7.4和pH 9.0条件下的体外药物释放研究表明,用CS和QAC包覆ALG微球后,BD的释放速率显著降低。此外,用QAC包覆的ALG微球在pH 9.0时对BD显示出延长的释放曲线。因此,QAC/ALG微球可能是一种有前景的亲水性大分子药物载体,可实现延长和持续给药。