US2016338956A1PendingUtilityA1

Liposomes Useful for Drug Delivery

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Assignee: MERRIMACK PHARMACEUTICALS INCPriority: May 3, 2004Filed: Aug 3, 2016Published: Nov 24, 2016
Est. expiryMay 3, 2024(expired)· nominal 20-yr term from priority
Inventors:Keelung HongDaryl C. DrummondDmitri B. Kirpotin
A61P 35/00A61P 43/00A61P 31/04A61P 31/12A61K 9/127A61K 47/60Y10S977/773A61K 47/26A61K 31/4745C07H 13/12A61K 47/50Y10S977/906A61K 9/1278A61K 31/475A61K 47/28A61K 31/337A61K 47/10A61K 31/704A61K 31/4375Y10S977/907A61K 9/1277A61K 47/24A61K 9/0019A61K 9/1271A61K 47/6913C07K 14/245C07K 7/08A61K 38/00A61P 1/00A61K 38/10C07K 7/06A61P 35/04A61P 35/02A61P 29/00A61P 27/16A61P 25/28A61P 25/24A61P 25/22A61P 25/20A61P 25/18A61P 25/04A61P 25/00A61P 15/10A61P 13/12A61P 13/08A61P 13/00A61P 11/06A61P 11/00A61P 9/10A61P 9/04A61P 9/00A61P 7/10A61P 5/50A61P 3/12A61P 3/10A61P 3/04A61P 3/00A61P 1/18A61P 1/16A61P 1/14A61P 1/12A61P 1/10A61P 1/08A61P 1/04A61K 47/36A61K 9/50A61K 47/30A61K 45/06
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Claims

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.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         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.

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