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 sucrose octasulfate precipitated in a matrix comprising one or more phospholipids, wherein the matrix has a size of approximately 110 nm and comprises a total of 500-550 mg irinotecan base per mmol of total phospholipids.
2 . The liposome composition of claim 1 , wherein the matrix comprises DSPC and cholesterol.
3 . The liposome composition of claim 2 , wherein the matrix comprises DSPC, cholesterol, and PEG-DSPE in a molar ratio of 3:2:0.015.
4 . The liposome composition of claim 1 , wherein the matrix comprises a total of 500 mg irinotecan base per mmol of total DSPC and PEG-DSPE.
5 . The liposome composition of claim 4 , wherein the matrix comprises DSPC, cholesterol, and PEG-DSPE in a molar ratio of 3:2:0.015.
6 . The liposome composition of claim 1 , wherein the matrix comprises a PEGylated lipid.
7 . A pharmaceutical composition comprising irinotecan sucrose octasulfate within a matrix comprising one or more phospholipids and having a size of approximately 110 nm, wherein the composition comprises a total of 500-550 mg irinotecan base per mmol of total phospholipids in the matrix, wherein at least 90% of the irinotecan in the pharmaceutical composition is in the irinotecan sucrose octasulfate within the matrix.
8 . The liposome composition of claim 7 , wherein the matrix comprises a PEGylated lipid.
9 . The composition of claim 8 , wherein the irinotecan sucrose octasulfate is precipitated within the matrix from irinotecan hydrochloride and sucrose octasulfate triethylammonium.
10 . The composition of claim 9 , wherein the irinotecan sucrose octasulfate is precipitated within the matrix.
11 . The liposome composition of claim 10 , wherein the matrix comprises DSPC and cholesterol.
12 . The liposome composition of claim 11 , wherein the matrix comprises DSPC, cholesterol, and PEG-DSPE in a molar ratio of 3:2:0.015.
13 . The liposome composition of claim 11 , wherein the matrix comprises a total of 500 mg irinotecan base per mmol of total DSPC and PEG-DSPE.
14 . The liposome composition of claim 8 , wherein the PEGylated lipid is PEG-DSPE.
15 . The liposome composition of claim 7 , wherein the composition comprises a total of 500 mg irinotecan base per mmol of total DSPC and PEG-DSPE.
16 . A pharmaceutical composition comprising irinotecan sucrose octasulfate salt precipitated within a lipid matrix comprising DSPC, cholesterol, and PEG2000-DSPE and having a size of approximately 110-120 nm, wherein the composition comprises a total of 500 mg irinotecan base per mmol of total DSPC and PEG2000-DSPE in the matrix, and wherein at least 90% of the irinotecan in the pharmaceutical composition is in the irinotecan sucrose octasulfate within the matrix.
17 . The composition of claim 16 , wherein the matrix consists of DSPC, cholesterol, and PEG2000-DSPE in a molar ratio of 3:2:0.015.
18 . The composition of claim 16 , wherein the irinotecan sucrose octasulfate is precipitated as a salt in the matrix.
19 . The composition of claim 16 , wherein the irinotecan sucrose octasulfate is formed in the matrix from irinotecan hydrochloride and sucrose octasulfate triethylammonium.
20 . The composition of claim 17 , wherein the irinotecan sucrose octasulfate is precipitated within the matrix.