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Amphiphilic block copolymer, method for preparing the same, and micellar drug encapsulation system formed of the copolymer and an antitumor agent

机译:两亲性嵌段共聚物,其制备方法以及由该共聚物和抗肿瘤剂形成的胶束药物包封系统

摘要

The present invention relates to a novel amphiphilic block copolymer and the preparation method thereof, as well as a micellar drug-loaded system formed by said copolymer and an anti-tumor drug. Said amphiphilic block copolymer comprises a hydrophilic segment and a hydrophobic segment, and the end group of said hydrophobic segment is end-capped with a hydrophobic group. Methoxypolyethylene glycol (or polyethylene glycol)-polyester block copolymer which has recognized safety is used as a fundamental material of the amphiphilic block copolymer of the present invention, and the terminal hydroxyl group of the polyester segment is modified with a hydrophobic group, whereby the compatibility between the drug molecule and the hydrophobic segments of the block copolymer is improved, and the interaction therebetween is enhanced. Moreover, a larger space for accommodating the drug molecules is provided. Said micelles are more effective in restricting the drug molecules inside the micellar core and preventing the drug from dissolved out of the micelles. Therefore, a drug-loaded micelle with high stability is obtained.
机译:本发明涉及新型两亲嵌段共聚物及其制备方法,以及由所述共聚物和抗肿瘤药形成的胶束载药体系。所述两亲嵌段共聚物包含亲水链段和疏水链段,并且所述疏水链段的端基被疏水基团封端。已被确认安全的甲氧基聚乙二醇(或聚乙二醇)-聚酯嵌段共聚物被用作本发明的两亲嵌段共聚物的基本材料,并且聚酯链段的末端羟基被疏水基团改性,从而相容性改善了药物分子与嵌段共聚物的疏水链段之间的相互作用,并增强了它们之间的相互作用。而且,提供了更大的用于容纳药物分子的空间。所述胶束在限制胶束核心内的药物分子和防止药物从胶束中溶出方面更有效。因此,获得了具有高稳定性的载药胶束。

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