公开(公告)号：EP1027033A2

公开(公告)日：2000-08-16

申请号：EP98921310.3

申请日：1998-05-14

申请人： Inex Pharmaceuticals Corp.

发明人： SEMPLE, Sean, C. ,  KLIMUK, Sandra, K. ,  HARASYM, Troy ,  HOPE, Michael, J. ,  ANSELL, Steven, M. ,  CULLIS, Pieter ,  SCHERRER, Peter ,  DEBEYER, Dan

IPC分类号： A61K9/00

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 %.