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    • 2. 发明申请
    • LIPID CARRIER COMPOSITIONS WITH PROTECTED SURFACE REACTIVE FUNCTIONS
    • 具有保护表面反应功能的脂质载体组合物
    • WO0141738A3
    • 2001-11-29
    • PCT/CA0001494
    • 2000-12-11
    • CELATOR TECHNOLOGIES INCMAYER LAWRENCE DCHIU GIGIBALLY MARCEL B
    • MAYER LAWRENCE DCHIU GIGIBALLY MARCEL B
    • A61K9/127
    • A61K9/1271
    • The liposomes of the invention have a reactive surface that demonstrates reduced interaction with macromolecules and increased blood circulation time. The reactive surface may comprise phosphatidylserine. The liposomes are protected by the presence of high levels of a hydrophilic polymer conjugated to a lipid. The invention further provides means for adjusting the appropriate ratio of hydrophilic polymer to a reactive lipid by a) determining the reactivity of the lipid; b) determining the time required for the carrier to reach its desired target location; c) determining the affinity of desired interactions with the reactive surface; and d) incorporating in the liposome or lipid carrier the amount of polyethylene glycol required to protect the reactive surface.
    • 本发明的脂质体具有反应性表面,其表现出与大分子减少的相互作用和增加的血液循环时间。 反应性表面可以包含磷脂酰丝氨酸。 通过存在高水平的与脂质缀合的亲水性聚合物来保护脂质体。 本发明还提供了通过以下方法来调节亲水性聚合物与活性脂质的适当比例:a)确定脂质的反应性; b)确定承运人达到其所需目标位置所需的时间; c)确定与反应性表面的所需相互作用的亲和力; 和d)在脂质体或脂质载体中掺入保护反应性表面所需的聚乙二醇的量。