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    • 1. 发明授权
    • Lipid vesicles bearing carbohydrate surfaces as lymphatic directed
vehicles for therapeutic and diagnostic substances
    • 含有碳水化合物表面的脂质囊泡作为治疗和诊断物质的淋巴导向载体
    • US4310505A
    • 1982-01-12
    • US92342
    • 1979-11-08
    • John D. BaldeschwielerRonald C. GambleMarcia R. MaukTsung-Ying ShenMitree M. Ponpipom
    • John D. BaldeschwielerRonald C. GambleMarcia R. MaukTsung-Ying ShenMitree M. Ponpipom
    • A61K51/00A61K9/127A61K47/00A61K49/00A61K43/00B01J13/00
    • A61K9/1272A61K9/127A61K9/1271Y10T428/2984
    • Lipid vesicles comprising a lipid bilayer which includes analogs of cell-surface receptors such as dicetyl phosphate; stearylamine; 6-(5-cholesten-3.beta.-yloxy) hexyl 1-thio-.beta.-L-fucopyranoside; 6-(5-cholesten-3.beta.-yloxy) hexyl 1-thio-.beta.-D-galactopyranoside; 6-(5-cholesten-3.beta.-yloxy)hexyl 1-thio-.alpha.-D-mannopyranoside; 6-(5-cholesten-3-yloxy)hexyl 2-acetamido-2-deoxy-1-thio-.beta.-D-galactopyranoside; 6-(5-cholesten-3.beta.-yloxy)hexyl 6-amino-6-deoxy-1-thio-.beta.-D-galactopyranoside; or 6-(5-cholesten-3.beta.-yloxy)hexyl 6-amino-6-deoxy-1-thio-.alpha.-D-mannopyranoside; cholesterol and distearoyl phospatidylcholine, and an effective amount of physiologically compatible radioactive tracer, cytotoxic or therapeutic agent as a part of the vesicles. The vesicles of this invention can be administered to the human host and have been found to release the contents of the vesicles in a predetermined manner, i.e., controlled release, and in some cases, to be rapidly concentrated in the lymphatic system and/or liver, lungs or spleen of the host.
    • 包含脂质双层的脂质囊泡,其包括细胞表面受体的类似物,例如磷酸二鲸蜡酯; 硬脂胺 6-(5-胆甾烯-3β-氧代)己基1-硫代-β-L-吡喃葡萄糖苷; 6-(5-胆甾烯-3β-氧基)己基1-硫代-β-D-吡喃半乳糖苷; 6-(5-胆甾烯-3β-氧基)己基1-硫代-α-D-吡喃甘露糖苷; 6-(5-胆甾烯-3-基氧基)己基2-乙酰氨基-2-脱氧-1-硫代-β-D-吡喃半乳糖苷; 6-(5-胆甾烯-3β-氧基)己基6-氨基-6-脱氧-1-硫代-β-D-吡喃半乳糖苷; 或6-(5-胆甾烯-3β-氧基)己基6-氨基-6-脱氧-1-硫代-α-D-吡喃甘露糖苷; 胆固醇和二硬脂酰磷脂酰胆碱,以及有效量的生理相容的放射性示踪剂,细胞毒性剂或治疗剂作为囊泡的一部分。 本发明的囊泡可以施用于人宿主,并且已经被发现以预定的方式(即控制释放)释放囊泡的内容物,并且在一些情况下快速浓缩在淋巴系统和/或肝脏中 ,肺或脾脏的主机。