聚天冬氨酸-酪氨酸纳米胶束载体的制备及载药性能研究

Study on preparation and drug loading property of polyaspartic acid-tyrosine nano micelle carrier

聚天冬氨酸接枝酪氨酸可形成具有较强载药能力的自组装纳米胶束载体,以此为研究对象探讨了碳二亚胺盐酸盐/N-羟基琥珀酰亚胺(EDC/NHS)催化体系对酰胺化反应的影响以及疏水段酪氨酸接枝率对胶束载体载药率的影响。结果表明,EDC/NHS催化体系比例的增加会提高反应的接枝率,而疏水段酪氨酸接枝率的增加可以提高对疏水性药物的负载能力,接枝率从0升高到26%的过程中可以使载药率从4.0%提高至58.16%。利用具有肿瘤靶向性能的叶酸对载体进行化学修饰得到兼具pH响应性和体内主动靶向能力的多重响应性高载药率纳米胶束载体。

Graft of tyrosine onto polyaspartic acid formed self-assembled micelle carriers with strong drug loading ability.The effect of EDC/NHS catalytic system on amidation reaction and the effect of tyrosine grafting rate on drug loading rate were investigated.Finally,it was concluded that under certain conditions,the increase of EDC/NHS usage increased the graft rate of the reaction,while the increase of tyrosine graft rate of hydrophobic segment improved the loading capacity of hydrophobic drugs,and the drug loading rate increased from 4.0%to 58.16%when the graft rate increased from 0 to 26%.In addition,folic acid,a recognized target ligand,was used to chemically modify the carrier with the aim to obtain multiple responsive nano micellar carriers with high drug loading,evident pH responsiveness and in vivo active targeting ability.