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    • 5. 发明专利
    • Method for loading nucleic acid active substances within amphoteric liposomes, comprises: mixing lipid mixture solution and aqueous solution of nucleic acid active substances; and sterile filtrating the liposomes containing the substances
    • DE102006054192A1
    • 2007-09-20
    • DE102006054192
    • 2006-11-10
    • NOVOSOM AG
    • PANZNER STEFFENENDERT GEROLDRAUCHHAUS UNAHERZOG NATALIEMUELLER CLAUDIA
    • A61K48/00A61K9/127
    • Method for loading of nucleic acid active substances within amphoteric liposomes, comprises: (a) providing a lipid mixture solution; (b) providing an aqueous solution of the nucleic acid active substance; (c) mixing the two solutions by injecting the alcoholic solution of the lipid mixture into the nucleic acid solutions or vice versa; (f) separating the non-included active substance, saturation of the liposome suspension, exchange of the aqueous medium and/or separation of the water-miscible solvent, and (g) optionally sterile filtrating the liposomes containing the active substance. Method for loading of nucleic acid active substances within amphoteric liposomes, comprises: (a) providing a solution of a lipid mixture in a water-miscible solvent, preferably an alcohol that can be optionally acidified; (b) providing an aqueous solution of the nucleic acid active substance to be included that can be optionally acidified, where at least one of the two solutions in (a) and (b) has to be set to a pH value with the help of acids and/or buffer substances; (c) mixing the two solutions by injecting the alcoholic solution of the lipid mixture into the aqueous solution of the nucleic acids or vice versa or by combination of two partial flows of the provided lipid solution and nucleic acid solutions, optionally in one or more mixers; (d) optionally diluting the mixed solutions; (e) breaking up of the interactive forces between the amphoteric liposomes and the nucleic acids through an increase of the pH value to more than 7 or by an increase of the ionic strength and subsequent increase of the pH value to more than 7; (f) separating the non-included active substance and/or saturation of the liposome suspension and/or exchange of the aqueous medium and/or separation of the water-miscible solvent, where each of these steps is independently optional; and (g) optionally sterile filtrating the liposomes containing the active substance, where between the steps (c) and (d) and/or between (d) and (e) and/or between (e) and (f) and/or between (f) and (g), an extruding step can take place and/or between the steps (e) and (f) and/or between (f) and (g), one or more freezing/thawing cycle(s) can take place and/or after step (e), (f) or (g), one or more freezing/thawing cycle(s) and/or a lyophilization of the liposomes containing the active substance can take place. An independent claim is included for the amphoteric liposomes comprising the nucleic acids obtained by the above method. ACTIVITY : None given. MECHANISM OF ACTION : Gene therapy.