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    • 5. 发明公开
    • 약물 내포 액티브 타겟형 고분자 미셀, 의약 조성물
    • 活性靶向聚合物胶囊携带药物和药物组合物
    • KR1020100055498A
    • 2010-05-26
    • KR1020107006136
    • 2009-07-29
    • 나노캬리아 가부시키가이샤
    • 가토야스키하라다미츠노리사이토히로유키하야시타츠유키
    • A61K9/107A61K47/48A61P35/00A61P43/00
    • B82Y5/00A61K47/60A61K47/642A61K47/644A61K47/6845A61K47/6849A61K47/6905A61K47/6907A61K9/107A61K47/50
    • Provided is an active targeting type polymeric micelle carrying a drug enclosed therein wherein inappropriate drug release possibly impairing normal cells can be prevented. A polymeric micelle (100) which comprises a skeleton polymer unit (10) having a target-binding site (11) and a skeleton polymer unit (20) carrying a drug (14) but not having the target-binding site (11), wherein these units (10 and 20) are arranged radially with the target-binding site (11) outward and the drug (14) inside. In the case (i) wherein the polymeric micelle binds to a target (40) while sustaining the radial arrangement, the polymeric micelle is incorporated by endocytosis into a cell (50) providing the target (40) and then the radial arrangement is broken in the cell (50) so that the drug (14) is released within the cell (50). In the case (ii) wherein the radial arrangement is broken in the blood (60) before the binding to the target (40), the units (20) are discharged from the body by the metabolism so that the impairment of normal cells by the drug (14) can be prevented.
    • 提供了携带封闭在其中的药物的活性靶向型聚合物胶束,其中可以防止可能损害正常细胞的不适当的药物释放。 一种聚合物胶束(100),其包括具有靶结合位点(11)的骨架聚合物单元(10)和携带药物(14)但不具有靶结合位点(11)的骨架聚合物单元(20) 其中这些单元(10和20)与靶结合位点(11)径向排列并且药物(14)在内部。 在(i)其中聚合物胶束在维持径向排列的同时结合靶(40)的情况下,通过内吞将聚合物胶束引入到提供靶(40)的细胞(50)中,然后将径向布置破坏 细胞(50),使得药物(14)在细胞(50)内释放。 在与靶标(40)结合之前,血液(60)中的径向排列破裂的情况(ii)中,单位(20)通过代谢从身体排出,使得正常细胞受到 可以防止药物(14)。