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LIPID ASSEMBLIES COMPRISING NON-LIPOSOME FORMING AMPHIPHILES

机译:包含非脂质体形成性两亲化合物的脂质组合

摘要

The present invention concerns a stable lipid assembly comprising a biologically active lipid having a hydrophobic region and a polar headgroup, wherein the atomic mass ratio between the headgroup and hydrophobic region is less than 0.3, and a lipopolymer having a hydrophobic lipid region and a polymer headgroup, wherein the atomic mass ratio between the headgroup and hydrophobic region is at least 1.5 and optionally a lipid matrix composed of liposome forming lipids. Specific lipid assemblies according to the invention comprise the biologically active lipid, ceramide, a lipid derivatized with polyethylene glycol (lipopolymer) and optionally in combination with a phospholipid (e.g. Egg phosphatidylcholine (EPC) and hydrogenated soybean phosphatidylcholine (HSPC)). The lipid assemblies of the invention exhibited a therapeutic effect in vitro in tumor cells as well as in vivo in animal models and they deliver the biologically active lipid to the disease site.
机译:本发明涉及一种稳定的脂质组装体,其包括具有疏水性区域和极性头基的生物活性脂质,其中所述头部基团和疏水性区域之间的原子质量比小于0.3,以及具有疏水性脂质区域和聚合物头基的脂聚合物。 ,其中头基和疏水区之间的原子质量比为至少1.5,并且任选地由形成脂质体的脂质组成的脂质基质。根据本发明的特定脂质组装物包括生物活性脂质,神经酰胺,用聚乙二醇(脂聚合物)衍生的脂质以及任选地与磷脂(例如蛋磷脂酰胆碱(EPC)和氢化大豆磷脂酰胆碱(HSPC))组合。本发明的脂质组装体在肿瘤细胞中以及在动物模型中在体内均显示出治疗效果,并且它们将生物活性脂质递送至疾病部位。

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