公开(公告)号：US20150283246A1

公开(公告)日：2015-10-08

申请号：US14438409

申请日：2013-09-22

申请人： Ke LIU ,  Feirong GONG ,  Hui XU ,  Yuewu LANG ,  Huaying FAN ,  Fei HAN ,  Xin CHE

发明人： Ke Liu ,  Feirong Gong ,  Hui Xu ,  Yuewu Lang ,  Huaying Fan ,  Fei Han ,  Xin Che

IPC分类号： A61K47/34 ,  C08G63/82 ,  A61K9/19 ,  A61K31/337 ,  A61K31/09 ,  A61K31/704 ,  C08G63/664 ,  A61K9/107

CPC分类号： A61K47/34 ,  A61K9/107 ,  A61K9/1075 ,  A61K9/19 ,  A61K31/09 ,  A61K31/337 ,  A61K31/704 ,  A61K47/42 ,  C08G63/664 ,  C08G63/6852 ,  C08G63/823 ,  C08G63/912 ,  C08G64/183

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.

摘要翻译： 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物形成的胶束药物负载体系。 所述两亲嵌段共聚物包含亲水链段和疏水链段，并且所述疏水片段的端基用疏水性基团封端。 将已知安全性的甲氧基聚乙二醇（或聚乙二醇） - 聚酯嵌段共聚物用作本发明的两亲性嵌段共聚物的基本材料，并且用疏水基团改性聚酯链段的末端羟基， 在药物分子和嵌段共聚物的疏水链段之间改善，并且其间的相互作用增强。 此外，提供了用于容纳药物分子的更大的空间。 所述胶束在限制胶束核内的药物分子和防止药物从胶束中溶解更有效。 因此，获得了具有高稳定性的药物负载型胶束。