US2021205245A1PendingUtilityA1

Liposomal anticancer compositions

50
Assignee: IRISYS LLCPriority: Sep 9, 2016Filed: Feb 11, 2021Published: Jul 8, 2021
Est. expirySep 9, 2036(~10.2 yrs left)· nominal 20-yr term from priority
Inventors:Igor NikoulinGerald J. YakatanYevgeniya PlekhovRobert P. Giannini
A61K 31/704A61K 31/136A61K 9/127A61P 35/00A61K 47/12A61K 47/24A61K 31/122A61K 47/10A61K 31/198A61K 31/4745A61K 47/34A61K 45/06A61K 31/375A61K 47/28A61K 9/10A61K 31/194A61K 9/0019A61K 9/19
50
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

Provided herein includes methods and compositions for the treatment of cancer. Described herein are liposome encapsulated chemotherapeutic agents and methods for preparing and utilizing the same.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A pharmaceutical composition comprising a liposome, wherein the liposome comprises a plurality of lipids; a weakly basic anticancer compound; and oxalic acid or a salt of oxalic acid; wherein the weight ratio of the plurality of lipids to the weakly basic anticancer compound is from about 20:1 to about 50:1. 
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the weight ratio of the plurality of lipids to the weakly basic anticancer compound is from 20:1 to 50:1. 
     
     
         3 . The pharmaceutical composition of  claim 1 , wherein the weight ratio of the plurality of lipids to the weakly basic anticancer compound is from about 30:1 to about 50:1. 
     
     
         4 . The pharmaceutical composition of  claim 1 , wherein the weight ratio of the plurality of lipids to the weakly basic anticancer compound is from 30:1 to 50:1. 
     
     
         5 . The pharmaceutical composition of  claim 1 , wherein the weight ratio of the plurality of lipids to the weakly basic anticancer compound is from about 30:1 to about 40:1. 
     
     
         6 . The pharmaceutical composition of  claim 1 , wherein the weight ratio of the plurality of lipids to the weakly basic anticancer compound is from about 40:1 to about 50:1. 
     
     
         7 . The pharmaceutical composition of  claim 1 , wherein the weight ratio of the plurality of lipids to the weakly basic anticancer compound is about 40:1. 
     
     
         8 . The pharmaceutical composition of  claim 1 , wherein the plurality of lipids comprise a plurality of free cholesterols or a plurality of phospholipids. 
     
     
         9 . The pharmaceutical composition of  claim 1 , wherein the plurality of lipids comprise a plurality of free cholesterols and a plurality of phospholipids. 
     
     
         10 . The pharmaceutical composition of  claim 9 , wherein the molar ratio of the plurality of phospholipids to the plurality of free cholesterols is at least 0.5 to 1 to about 4 to 1. 
     
     
         11 . The pharmaceutical composition of  claim 9 , wherein the molar ratio of the plurality of phospholipids to the plurality of free cholesterols is from about 0.86:1 to about 3.68:1. 
     
     
         12 . The pharmaceutical composition of  claim 1 , wherein the weakly basic anticancer compound is doxorubicin, irinotecan, mitoxantrone, or a combination of two or more thereof. 
     
     
         13 . The pharmaceutical composition of  claim 1 , wherein the weakly basic anticancer compound has a pKa from about 7.5 to about 9.0. 
     
     
         14 . The pharmaceutical composition of  claim 1 , wherein the liposome comprises about 500 μg/mL to about 1,000 μg/mL of the weakly basic anticancer compound. 
     
     
         15 . The pharmaceutical composition of  claim 14 , wherein the liposome comprises about 750 μg/mL to about 850 μg/mL of the weakly basic anticancer compound. 
     
     
         16 . The pharmaceutical composition of  claim 1 , wherein the plurality of lipids comprise a poloxamer. 
     
     
         17 . The pharmaceutical composition of  claim 16 , wherein the poloxamer is poloxamer 188. 
     
     
         18 . The pharmaceutical composition of  claim 1 , further comprising ascorbic acid, N-acetylcysteine, ascorbyl palmitate, ubiquinone, or ethylenediaminetetraacetic acid. 
     
     
         19 . The pharmaceutical composition of  claim 1 , wherein:
 (i) at least 40% to 80% of the weakly basic anticancer compound is released from the liposome at pH 5 under standard assay conditions; wherein the standard assay conditions comprise 20 times or 50 times dilution in phosphate buffered saline at pH 5.0 for 2 hours, 4 hours, 6 hours, or 8 hours at 37° C.;   (ii) at least 10% to 50% of the weakly basic anticancer compound is released from the liposome at pH 6.0 under standard assay conditions; wherein the standard assay conditions comprise 20 times or 50 times dilution in phosphate buffered saline at pH 6.0 for 2 hours, 4 hours, 6 hours, or 8 hours at 37° C.;   (iii) at least 7% to 30% of the weakly basic anticancer compound is released from the liposome at pH 6.7 under standard assay conditions; wherein the standard assay conditions comprise 20 times or 50 times dilution in phosphate buffered saline at pH 6.7 for 2 hours, 4 hours, 6 hours, or 8 hours at 37° C.; or   (iv) less than 5% of the weakly basic anticancer compound is released from the liposome at pH 7.4 under standard assay conditions; wherein the standard assay conditions comprise 20 times or 50 times dilution in phosphate buffered saline at pH 7.4 for 2 hours, 4 hours, 6 hours, or 8 hours at 37° C.   
     
     
         20 . The pharmaceutical composition of  claim 1 , wherein the pharmaceutical composition comprises a plurality of the liposome having a mean longest dimension of about 40 nm to about 100 nm determined by the intensity-averaged particle diameters measured by dynamic light scattering; 
       or wherein the pharmaceutical composition comprises a plurality of the liposome having a mean longest dimension from about 1 nm to about 50 nm determined by cryo-transmission electron microscopy.

Cited by (0)

No later patents cite this yet.

References (0)

No backward citations on record.