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    • 90. 发明申请
    • CELL TRANSPORT COMPOSITIONS AND USES THEREOF
    • 细胞运输组合物及其用途
    • WO2004012672A2
    • 2004-02-12
    • PCT/US2003/024323
    • 2003-08-01
    • MANNKIND CORPORATION
    • GELBER, CohavaROUSSEAU, Kathleen
    • A61K
    • A61K9/0075A61K9/1641A61K9/167A61K9/1676A61K47/545A61K47/6927
    • Compositions and methods have been developed for transporting compounds across membranes with little or no toxicity and, when targeted through the appropriate routes of administration (i.e., lung, gastrointestinal (GI) tract), little or no immune stimulation. The compositions can mediate cellular delivery of compounds that would otherwise not enter cells and enhance the intracellular delivery of compounds that would otherwise enter cells inefficiently. The methods are carried out by contacting a proximal face of a lipid bilayer or membrane (e.g. the surface of an intact cell) with a complex containing a compound (e.g., a therapeutic agent) and a diketopiperazine (DKP). DKP and the compound are non-covalently associated with each other or covalently bound to each other .
    • 开发了用于将化合物跨越膜转运而几乎没有或没有毒性的组合物和方法,并且当通过适当的给药途径(即肺,胃肠道(GI)道)靶向时,很少或没有免疫 刺激。 所述组合物可以介导化合物的细胞递送,否则所述化合物不会进入细胞并且增强化合物的细胞内递送,否则所述化合物将无效地进入细胞。 通过使脂质双分子层或膜的近侧面(例如完整细胞的表面)与含有化合物(例如治疗剂)和二酮哌嗪(DKP)的复合物接触来进行所述方法。 DKP和化合物彼此非共价缔合或彼此共价结合。