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通过大分子引发剂ω-氨基-α-甲氧基聚乙二醇引发N-羧基-α-氨基环内酸酐开环聚合和水合肼侧基改性,制备了一系列聚乙二醇-聚氨基酸类三嵌段共聚物.其中聚氨基酸链段包括具有酰肼基的聚天冬氨酸衍生物(PAHy),以及疏水性的聚丙氨酸链段.引入具有pH响应性的腙键键合阿霉素,利用键合阿霉素与游离阿霉素之间的π-π叠合作用,在聚合物自组装形成胶束过程中通过化学键合+物理包埋的方式充分负载药物.该胶束以聚丙氨酸链段为核心,以PEG链段为冠层,以PAHy链段为包裹药物的壳层.载药胶束的粒径在170 nm左右.研究不同pH值条件下载药胶束的药物释放能力,随环境pH值的降低药物的释放速率显著增加.
A series of poly (ethylene glycol) -poly (ethylene glycol) -poly (ethylene glycol) -poly (ethylene glycol) -poly (ethylene glycol) Amino acid triblock copolymer wherein the polyamino acid segment comprises a polyaspartic acid derivative (PAHy) having a hydrazide group, and a hydrophobic polyalanine segment, wherein a hydrazone bond having a pH response is introduced Adriamycin, which utilizes the π-π lamination between the bound doxorubicin and the free doxorubicin, fully supports the drug through chemical bonding and physical embedding during the self-assembly of the polymer to form micelles. The bundle of polyalanine segments as the core, the PEG segment as the canopy, the PAHy segment as the drug-coated shell, and the size of the drug-loaded micelles was about 170 nm.The drug-loaded micelles Of the drug release capacity, with the environmental pH value of drug release rate increased significantly.