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 hydration 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 hydration step and fewer vesicles are substantially free of biologically active compound.
本发明公开了一种生产含有更多
生物活性化合物的多胶束凝聚囊泡 (MLCV) 的方法。该方法包括在
水性缓冲液中
水合至少一种粉末状脂质,
水合温度高于最高熔点脂质的相变温度,以形成多胶束囊泡,将多胶束囊泡的尺寸减小到约 20-400 纳米,以产生小单胶束囊泡(SUV)或大单胶束囊泡(LUV)或它们的混合物;将 SUVs、LUVs 或其混合物与
水溶液中的
生物活性化合物在充分条件下孵育,以形成含有
生物活性化合物的 MLCVs,而无需使用有机溶剂、冻融步骤或
水合步骤。与使用有机溶剂、冻融步骤或
水合步骤生产的现有技术脂质体相比,用这种方法生产的 MLCV 含有更多的
生物活性化合物,而且基本上不含
生物活性化合物的囊泡较少。