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.
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基金资助
山西省自然科学基金(201701D121030,201701D121044,201901D211091)