去唾液酸糖蛋白受体介导甘草次酸壳聚糖微球的质量评价  

Quality Evaluation of Glycyrrhetinic Acid Chitosan Microspheres Mediated by Asialogycoprotein Receptor

作　　者：黄敏敏 郑品劲 孔松芝 廖铭能 吴伟枝 周雨蕾 Huang Minmin;Zheng Pinjin;Kong Songzhi;Liao Mingneng;Wu Weizhi;Zhou Yulei(Faculty of Chemistry and Environmental Science,Guangdong Ocean University,Zhanjiang 524000,China)

机构地区：[1]广东海洋大学化学与环境学院,广东湛江524000

出　　处：《山东化工》2023年第9期20-23,共4页Shandong Chemical Industry

基　　金：广东省普通高校青年创新人才类项目(230419089);广东海洋大学科研启动经费资助项目(R20034)。

摘　　要：目的:甘草次酸具有多种药理作用,如抗肿瘤、抗炎和抗病毒等。对甘草次酸进行修饰,制成靶向缓释制剂可以使药物准确到达作用部位,降低对其他组织的伤害。实验制备去唾液酸糖蛋白受体介导的甘草次酸壳聚糖微球,并对所制备的微球进行表征和质量评价。方法:采用乳化交联法制备,并对壳聚糖微球的粒径、Zeta电位、红外光谱图、包封率和载药量、体外释放度及稳定性等方面进行考察。结果:制备的微球粒径为1.106~1.718μm,Zeta电位为(15.13±1.76)mV,包封率为82.4%,载药量为1.02%,24 h体外释放度为77.09%,稳定性有待提高。结论:去唾液酸糖蛋白受体介导的甘草次酸壳聚糖微球,可为研制靶向肝药物提供一定的理论依据和实践基础。Objective:Glycyrrhetinic acid has a variety of pharmacological effects,such as anti-tumor,anti-inflammatory and anti-virus.The modification of glycyrrhetinic acid to make targeted sustained-release preparations can make the drug reach the site of action accurately and reduce the damage to other tissues.Glycyrrhetinic acid chitosan microspheres mediated by asialoglycoprotein receptor were prepared,and the prepared microspheres were characterized and evaluated.Methods:The chitosan microspheres were prepared by emulsion crosslinking method.The particle size,Zeta potential,infrared spectrum,encapsulation efficiency and drug loading,in vitro release and stability of chitosan microspheres were investigated.Results:The particle size of the prepared microspheres was 1.106~1.718μm,the Zeta potential was(15.13±1.76)mV,the encapsulation efficiency was 82.4%,the drug loading was 1.02%,and the 24 h in vitro release was 77.09%.The stability needs to be improved.Conclusion:The prepared asialoglycoprotein receptor-mediated chitosan microspheres can provide a theoretical basis and practical basis for the development of targeted liver drugs.

关 键 词：去唾液酸糖蛋白受体 甘草次酸 壳聚糖微球 质量评价 

分 类 号：TQ464.54[化学工程—制药化工] R285[医药卫生—中药学]