Liposomes Useful for Drug Delivery
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.
1 . A pharmaceutical composition comprising irinotecan within a lipid matrix as irinotecan sucrose octasulfate, wherein the lipid matrix has a size of approximately 110 nm and comprises one or more phospholipids, and wherein the composition comprises a total of 500 mg of irinotecan base per mmol of total lipid matrix phospholipids.
2 . The composition of claim 1 , wherein the lipid matrix comprises a neutral phospholipid and cholesterol.
3 . The composition of claim 1 , wherein the lipid matrix comprises a lecithin and cholesterol.
4 . The composition of claim 1 , wherein the lipid matrix comprises a lecithin, a PEGylated lipid, and cholesterol.
5 . The composition of claim 1 , wherein the lipid matrix comprises DSPC, cholesterol, and PEG-DSPE in a molar ratio of 3:2:0.015.
6 . The composition of claim 1 , wherein the lipid matrix forms a vesicle encapsulating the irinotecan sucrose octasulfate.
7 . The composition of claim 6 , wherein the vesicle comprises DSPC, cholesterol, and PEG-DSPE in a molar ratio of 3:2:0.015.
8 . The composition of claim 1 , wherein the composition comprises a total of 500 mg of irinotecan base per mmol of total DSPC and PEG-DSPE.
9 . The composition of claim 8 , wherein the lipid matrix forms a vesicle encapsulating the irinotecan sucrose octasulfate.
10 . The composition of claim 9 , wherein the vesicle comprises DSPC, cholesterol, and PEG-DSPE in a molar ratio of 3:2:0.015.
11 . A pharmaceutical composition comprising irinotecan within a lipid matrix as irinotecan sucrose octasulfate, wherein the lipid matrix has a size of approximately 110 nm and comprises cholesterol and one or more phospholipids, and wherein the composition comprises a total of 500 mg of irinotecan base per mmol of total lipid matrix phospholipids, and wherein at least 90% of the irinotecan in the pharmaceutical composition is within the lipid matrix.
12 . The composition of claim 11 , wherein at least 90% of the irinotecan in the pharmaceutical composition is irinotecan sucrose octasulfate in the lipid matrix.
13 . The composition of claim 11 , wherein the lipid matrix forms a vesicle encapsulating the irinotecan sucrose octasulfate.
14 . The composition of claim 13 , wherein the vesicle comprises a lecithin, a PEGylated lipid, and cholesterol.
15 . The composition of claim 14 , wherein the vesicle comprises DSPC, cholesterol, and PEG-DSPE in a molar ratio of 3:2:0.015.
16 . The composition of claim 15 , wherein the lipid matrix comprises a total of 500 mg of irinotecan base per mmol of total DSPC and PEG-DSPE.
17 . The composition of claim 11 , wherein the composition comprises a total of 500 mg of irinotecan base per mmol of total DSPC and PEG-DSPE.
18 . A pharmaceutical composition comprising irinotecan within a lipid matrix as irinotecan sucrose octasulfate, wherein the lipid matrix has a size of approximately 110 nm and comprises DSPC, cholesterol, and PEG-DSPE, and wherein the composition comprises a total of 500 mg of irinotecan base per mmol of total DSPC and PEG-DSPE, and wherein at least 90% of the irinotecan in the pharmaceutical composition is in the irinotecan sucrose octasulfate within the lipid matrix.
19 . The composition of claim 18 , wherein the lipid matrix forms a vesicle encapsulating the irinotecan sucrose octasulfate.
20 . The composition of claim 19 , wherein the vesicle comprises DSPC, cholesterol, and PEG-DSPE in a molar ratio of 3:2:0.015.