Liposomes Useful for Drug Delivery
AssigneeMerrimack Pharmaceuticals, Inc.
InventorsKeelung Hong, Daryl C. Drummond, Dmitri Kirpotin
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Abstract
The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.
Claims16
An irinotecan liposome composition comprising irinotecan and a sulfated sugar encapsulated in a lipid vesicle, wherein the composition is obtainable by a process comprising the steps of:
- (a) forming the lipid vesicle encapsulating the sulfated sugar and one or more substituted ammonium compounds selected from the group consisting of diethylammonium and triethylammonium in a lipid composition comprising one or more lipid components forming the lipid vesicle;
- (b) contacting the lipid vesicle with irinotecan at a temperature above the phase transition temperature of the lipid vesicle, to load at least 85% of the irinotecan into the lipid vesicle.
An irinotecan liposome composition comprising irinotecan and a sulfated sugar selected from the group consisting of sucrose hexasulfate, sucrose heptasulfate, and sucrose octasulfate encapsulated in a lipid vesicle, wherein the composition is obtained by a process comprising the steps of:
- (a) forming the lipid vesicle encapsulating the sulfated sugar and one or more substituted ammonium compounds selected from the group consisting of:
- diethylammonium and triethylammonium in a lipid composition comprising one or more lipid components forming the lipid vesicle;
- (b) contacting the lipid vesicle with irinotecan at a temperature above the phase transition temperature of the lipid vesicle, to load at least 85% of the irinotecan into the lipid vesicle.
An irinotecan liposome composition comprising irinotecan and a sulfated sugar selected from the group consisting of sucrose hexasulfate, sucrose heptasulfate, and sucrose octasulfate encapsulated in a lipid vesicle, wherein the composition is obtainable by a process comprising the steps of:
- (a) forming the lipid vesicle encapsulating the sulfated sugar having a pKa of 3 or less at a concentration of 1.2-2.5N, and one or more substituted ammonium compounds selected from the group consisting of diethylammonium and triethylammonium at a concentration of 0.55-0.65 M in a lipid composition comprising DSPC, cholesterol and PEG-DSPE in a 3:2:0.015 molar ratio forming the lipid vesicle;
- (b) contacting the lipid vesicle with irinotecan at a temperature above the phase transition temperature of the lipid vesicle, to load at least 85% of the irinotecan into the lipid vesicle.
Dependencies are inferred from the claim text.