Amphoteric liposomes comprising neutral lipids

摘要

Abstract An amphoteric liposome comprising neutral lipids wherein said neutral lipids are selected from the group comprising cholesterol or mixtures of cholesterol and at least one neutral or zwitterionic lipid and wherein K(neutral) of said mixtures is 0.3 or less. Said amphoteric liposome may encapsulate an active agent, such as nucleic acid therapeutics. Also disclosed are pharmaceutical compositions comprising said amphoteric liposomes as a carrier for the delivery or targeted delivery of active agents or ingredients. Figures: 1/17 lipid salt model lipid salt model K *100 -- 25 ---- 50 -A-75 *100 0 4 k 4,25 pH %Anion 100 3 4 5 pH 6 7 8 Fig. 1 lipid salt model lipid salt model Ic *100 4 + 25 -w-- 50 -a-7 *100x 30a 20 20 X /6,75 - 5.5 204,s p sog 3 10 , , % Anion 10D 3 4 5 pH 6 7 8 Fig. 2