Multilamellar coalescence vesicles (MLCV) containing biologically active compounds
    1.
    发明授权
    Multilamellar coalescence vesicles (MLCV) containing biologically active compounds 有权
    含有生物活性化合物的多层聚结囊泡(MLCV)

    公开(公告)号:US06544549B1

    公开(公告)日:2003-04-08

    申请号:US09164350

    申请日:1998-10-01

    IPC分类号: A61K9127

    摘要: A method for producing multilamellar coalescence vesicles (MLCVs) containing increased amounts of biologically active compound is disclosed. The method involves hydrating at least one powdered lipid in an aqueous buffer at a temperature above the phase transition temperature of the highest melting lipid to form multilamellar vesicles, reducing the size of the multilamellar vesicles to about 20-400 nm to produce small unilamellar vesicles (SUVs) or large unilamellar vesicles (LUVs) or a mixture thereof; and incubating the SUVs, LUVs or mixture thereof with a biologically active compound in an aqueous solution under sufficient conditions to form MLCVs containing the biologically active compound without the use of an organic solvent, a freeze-thawing step or a dehydration step. MLCVs produced by this method contain increased amounts of biologically active compound over prior art liposomes produced with an organic solvent, a freeze-thawing step or a dehydration step and fewer vesicles are substantially free of biologically active compound

    摘要翻译: 公开了一种生产含有增加量的生物活性化合物的多层聚结囊泡(MLCV)的方法。 该方法包括在高于最高熔融脂质的相变温度的温度下在水性缓冲液中水合至少一种粉状脂质以形成多层囊泡,将多层囊泡的尺寸减小到约20-400nm,以产生小的单层囊泡( SUV)或大单层囊泡(LUV)或其混合物; 以及在足够的条件下在水溶液中将SUV,LUV或其混合物与生物活性化合物一起孵育以形成含有生物活性化合物的MLCV,而不使用有机溶剂,冻融步骤或脱水步骤。 通过该方法制备的MLCV含有比现有技术的有机溶剂脂质体增加量的生物活性化合物,冻融步骤或脱水步骤,较少的囊泡基本上不含生物活性化合物