首页> 外国专利> PH SENSITIVE LIPOSOME COMPOSITIONS FOR CONTROLLING SURFACE TOPOGRAPHY AND BINDING REACTIVITY IN FUNCTIONALIZED LIPOSOMES

PH SENSITIVE LIPOSOME COMPOSITIONS FOR CONTROLLING SURFACE TOPOGRAPHY AND BINDING REACTIVITY IN FUNCTIONALIZED LIPOSOMES

机译:用于控制功能性脂质体的表面敏感性和结合反应性的PH敏感脂质体组合物

摘要

Methods for controlling surface topography and binding reactivity in functionalized lipid layers, including in the form of liposomes, using pH-dependent processes. During direct cell-to-cell communication, lipids on the extracellular side of plasma membranes reorganize, and membrane associated communication-related molecules co-localize. At co-localization sites, sometimes identified as rafts, the local cell surface topography and reactivity are altered. Integration of these processes on nanometer-sized lipid vesicles used as drug delivery carriers would precisely control their interactions with diseased cells minimizing toxicities. Included are pH-dependent processes on functionalized lipid bilayers demonstrating reversible sharp changes in binding reactivity within a narrow pH window. Cholesterol enables tuning of the membrane reorganization to occur at pH values not necessarily close to the reported pKa's of the constituent titratable lipids. One illustrative function of the invention is to use liposomes to deliver bioactive agents to cancer or tumor cells and compositions of specific lipids that form liposomes to deliver a biologically active agent.
机译:使用pH依赖过程控制功能化脂质层(包括脂质体形式)中的表面形貌和结合反应性的方法。在直接的细胞间通信过程中,质膜细胞外侧的脂质重新组织,并且与膜相关的通信相关分子共定位。在共定位位点,有时被确定为筏,局部细胞表面的形貌和反应性发生了变化。将这些过程整合到用作药物传递载体的纳米级脂质囊泡上将精确控制它们与患病细胞的相互作用,从而将毒性降至最低。包括在功能化脂质双层上的pH依赖性过程,该过程证明了在狭窄的pH窗口内可逆的结合反应性急剧变化。胆固醇使膜重组的调节发生在不一定接近所报告的可滴定脂质的pKa的pH值时。本发明的一种说明性功能是使用脂质体将生物活性剂递送至癌细胞或肿瘤细胞,以及形成脂质体的特定脂质的组合物以递送生物活性剂。

著录项

  • 公开/公告号US2010047334A1

    专利类型

  • 公开/公告日2010-02-25

    原文格式PDF

  • 申请/专利权人 SOFOU STAVROULA;

    申请/专利号US20090511110

  • 发明设计人 SOFOU STAVROULA;

    申请日2009-07-29

  • 分类号A61K9/127;A61K47/44;

  • 国家 US

  • 入库时间 2022-08-21 18:52:33

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