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    • 8. 发明授权
    • Polymer-lipid conjugate for fusion of target membranes
    • 用于融合靶膜的聚合物 - 脂质缀合物
    • US06224903B1
    • 2001-05-01
    • US09208684
    • 1998-12-10
    • Francis J. MartinSamuel Zalipsky
    • Francis J. MartinSamuel Zalipsky
    • A61K9127
    • A61K9/1272A61K9/1271
    • A fusogenic liposome composition for delivering a liposome-entrapped compound into the cytoplasm of a target cell is described. The liposomes have an outer surface coating of chemically releasable hydrophilic polymer chains which shield hydrophobic polymers on the liposome outer surface. Release of the hydrophilic polymer chains exposes the hydrophobic polymers for interaction with outer cell membranes of the target cells to promote fusion of the liposome with the target cells. Also disclosed is a polymer-lipid conjugate for use in promoting fusion between target membranes. The conjugate is composed of a first segment composed of a hydrophilic polymer and a second hydrophobic polymer segment. The second segment is joined to the first segment by a bond effective to release the first segment in response to an existing or an induced physiologic condition. Attached to the second segment is a vesicle-forming lipid member.
    • 描述了用于将脂质体包埋的化合物递送到靶细胞的细胞质中的融合脂质体组合物。 脂质体具有化学上可释放的亲水性聚合物链的外表面涂层,其在脂质体外表面上屏蔽疏水性聚合物。 亲水性聚合物链的释放使疏水性聚合物暴露于与靶细胞的外细胞膜相互作用,以促进脂质体与靶细胞的融合。 还公开了用于促进靶膜之间的融合的聚合物 - 脂质缀合物。 缀合物由由亲水性聚合物和第二疏水性聚合物链段构成的第一链段组成。 第二段通过有效释放第一段的键与第一段连接,以响应于现有或诱导的生理状况。 附着于第二段是形成囊泡的脂质成分。