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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 Glycyrrhizic acid surface inlaid liposomes can enhance the drug targeting target of the liver, intends to use enzymatic coupling method to construct glycyrrhizic acid modified liposome drug carrier. Methods Glycyrrhizic acid and vinyl stearate were used as reaction substrates and acetone as reaction medium. Novozym 435 immobilized lipase was used as catalyst, and the conversion of glycyrrhizic acid was used as the evaluation index. The amount of enzyme, substrate molar ratio, reaction Temperature, reaction time and other factors were investigated. Results When the enzyme dosage was 40 mg.mL-1, the molar ratio of glycyrrhizic acid to vinyl stearate was 1: 5, the reaction was carried out at 60 ℃ for 48 h, the conversion of glycyrrhizic acid reached 60%. Conclusion The process of enzymatic construction of carrier modification is simple and feasible, and has potential application prospects.