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公开(公告)号:EP1027033B1
公开(公告)日:2009-07-22
申请号:EP98921310.3
申请日:1998-05-14
发明人: SEMPLE, Sean, C. , KLIMUK, Sandra, K. , HARASYM, Troy , HOPE, Michael, J. , ANSELL, Steven, M. , CULLIS, Pieter , SCHERRER, Peter , DEBEYER, Dan
CPC分类号: A61K9/1277 , A61K9/1272 , Y10T428/2984
摘要: Methods for the preparation of a lipid-nucleic acid composition are provided. According to the methods, a mixture of lipids containing a protonatable or deprotonatable lipid, for example an amino lipid and a lipid such as a PEG- or polyamide oligomer-modified lipid is combined with a buffered aqueous solution of a charged therapeutic agent, for example polyanionic nucleic acids, to produce particles in which the therapeutic agent is encapsulated in a lipid vesicle. Surface charges on the lipid particles are at least partially neutralized to provide surface-neutralized lipid-encapsulated compositions of the therapeutic agents. The method permits the preparation of compositions with high ratios of therapeutic agent to lipid and with encapsulation efficiencies in excess of 50 %.