公开(公告)号：US4310506A

公开(公告)日：1982-01-12

申请号：US123162

申请日：1980-02-20

申请人： John D. Baldeschwieler ,  Ronald C. Gamble ,  Marcia R. Mauk

发明人： John D. Baldeschwieler ,  Ronald C. Gamble ,  Marcia R. Mauk

IPC分类号： A61K9/127 ,  A61K51/12 ,  A61K49/00 ,  A61K43/00 ,  B01J13/00

CPC分类号： A61K51/1234 ,  A61K9/1278 ,  A61K2123/00 ,  Y10T428/2984

摘要： Unilamellar vesicles comprising a lipid bilayer, an ionophore being incorporated in said lipid bilayer, a chelating agent entrapped within the vesicles, and an effective amount of physiologically compatible cation bound to said chelating agent within the vesicles. Unilamellar vesicles are loaded by incubating the vesicles with the cation, terminating the incubation and recovering the loaded vesicles by chromatography. In some applications of the invention, the cation may be a radioactive tracer, in which case the vesicles can be administered to the human host and observed by scintillation techniques to produce a radioimage which is useful for diagnostic purposes.

摘要翻译： 包含脂质双层的单层囊泡，掺入所述脂质双层中的离子载体，包封在囊泡内的螯合剂，以及与囊泡内的所述螯合剂结合的有效量的生理上相容的阳离子。 通过将囊泡与阳离子孵育来加载单层囊泡，终止孵育并通过色谱法回收加载的囊泡。 在本发明的一些应用中，阳离子可以是放射性示踪剂，在这种情况下，囊泡可以施用于人宿主并通过闪烁技术观察以产生可用于诊断目的的放射性图像。

公开(公告)号：US4310505A

公开(公告)日：1982-01-12

申请号：US92342

申请日：1979-11-08

申请人： John D. Baldeschwieler ,  Ronald C. Gamble ,  Marcia R. Mauk ,  Tsung-Ying Shen ,  Mitree M. Ponpipom

发明人： John D. Baldeschwieler ,  Ronald C. Gamble ,  Marcia R. Mauk ,  Tsung-Ying Shen ,  Mitree M. Ponpipom

IPC分类号： A61K51/00 ,  A61K9/127 ,  A61K47/00 ,  A61K49/00 ,  A61K43/00 ,  B01J13/00

CPC分类号： A61K9/1272 ,  A61K9/127 ,  A61K9/1271 ,  Y10T428/2984

摘要： 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.

摘要翻译： 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。