摘要
目的甘草酸表面镶嵌脂质体可增强药物载体对肝脏的趋靶性,拟采用酶促催化偶联法构建甘草酸修饰的脂质体药物载体。方法甘草酸和硬脂酸乙烯酯作为反应底物,丙酮作为反应介质,Novozym 435固定化脂肪酶作为催化剂,以甘草酸的转化率作为评价指标,对酶的加入量、底物摩尔比、反应温度、反应时间等因素进行了考察。结果当酶加入量为40 mg.mL-1,甘草酸和硬脂酸乙烯酯的摩尔比为1∶5,60℃下反应48 h,甘草酸转化率最大可达到60%以上。结论通过实验酶促构建载体修饰物工艺简单可行,有着潜在的应用前景。
Objective Liposome surface modified with glycyrrhizin can enhance liver targeting of the drug carrier. Therefore, we try to construct the liposome which surface was inlaid with glycyrrhizic acid by enzyme-catalyzed coupled reaction. Methods With glycyrrhizin and vinyl stearate as substrates, acetone as reaction medium and immobilized-lipase Novozym 435 as catalyst, we investigated effects of factors of the enzyme concentration, molar ratio of substrates, reaction temperature and reaction time on the reaction rate of glycyrrhizin. Results Under the condition of enzyme concentration at 40 mg·mL^-1, the molar ratio of glycyrrhizic acid to vinyl stearate being 1 ： 5, and reacting at 60℃ for 48 h, the reaction rate of glycyrrhizin was up more than 60 %. Conclusion Enzymatic synthesis of liposome surface modified with glycyrrhizin is simple and feasible, which has potential prospective application.
出处
《中药新药与临床药理》
CAS
CSCD
北大核心
2010年第4期431-434,共4页
Traditional Chinese Drug Research and Clinical Pharmacology
基金
高等学校博士学科点专项科研基金(20060572012)
国家自然科学基金(30772790)
关键词
甘草酸
硬脂酸乙烯酯
脂质体
酶促催化
Glycyrrhizic acid
Vinyl stearate
Liposome
Enzyme catalysis
作者简介
作者简介：程怡（1955-），女，教授，博士生导师，从事药剂学领域研究和教学工作。Email：ncchengyi@21cn.com。
