Cationic lipids for intracellular delivery of biologically activ

Details Cationic lipids for intracellular delivery of biologically activ Cationic lipids for intracellular delivery of biologically activ

1991-04-16

1993-11-23

Killos, Paul J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

560155, 560252, 530323, 554227, 554224, 554223, 564292, 574549, 574552, C07C 6952

Patent

active

052646181

ABSTRACT:
Disclosed are cationic lipids capable of facilitating transport of biologically active agents into cells, including the transfection of cells by therapeutic polynucleotides, the delivery of antiviral drugs, and the introduction of immunogenic peptides. The cationic lipids, comprising an ammonium group, have the general structure ##STR1## Also disclosed are adducts of these compounds comprising additional cationic sites that enhance the transfective or transport activity. Structure-activity correlations provide for the selection of preferred compounds to be synthesized for this purpose. Compositions disclosed for use of these cationic lipid include formulations for in vitro transfection and pharmaceutical formulations for parenteral and topical administration of therapeutic agents.

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