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    • 112. 发明公开
    • Solid core liposomes
    • Liposome mit harten Kernen。
    • EP0277776A2
    • 1988-08-10
    • EP88300750.2
    • 1988-01-28
    • THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
    • Huang, Leaf
    • A61K9/50
    • B82Y30/00A61K9/1277Y10S436/829Y10S514/963Y10T428/2984
    • Preferred solid core liposomes are prepared in four major steps:

      (1) Preparation of prevesicles with encapsulated solid cores of agarose-gelatin by emulsification of agarose-gelatin sol in organic solvent containing emulsifiers followed by cooling;
      (2) Extraction of lipophilic components from prevesicles to obtain microspherules of agarose - ­gelatin;
      (3) In an optional step, colloidal gold particles are introduced into the microspherules, which are then coated with a protein or peptide molecule layer;
      (4) Encapsulation of the microspherules is conducted using a modified organic solvent spherule evaporation method for the formation of the liposomes.

      Electron micrographs indicate that if liposomes are prepared by using a lipid mixture containing dioleoyl phosphatidyl choline, cholesterol, dioleoylphosphatidylglycerol, and triolein (molar ratio 4.5:4.5:1:1), there is only a single continuous bilayer membrane for each solid core liposome.
    • 优选的固体核脂质体以四个主要步骤制备:(1)通过在含有乳化剂的有机溶剂中乳化琼脂糖凝胶溶胶随后冷却来制备具有封装的琼脂糖凝胶固体核心的前囊泡; (2)从前囊中提取亲脂性成分,得到琼脂糖凝胶微珠; (3)在任选的步骤中,将胶体金颗粒引入微球体中,然后用蛋白质或肽分子层包被; (4)使用用于形成脂质体的改性有机溶剂微球蒸发法进行微球的封装。 电子显微照片表明,如果通过使用含有二油酰磷脂酰胆碱,胆固醇,二油酰磷脂酰甘油和三油酸甘油酯(摩尔比为4.5:4.5:1:1)的脂质混合物制备脂质体,则每个固体核脂质体仅存在单个连续双层膜。