MODIFICATIONS OF SOLID 3-sn-PHOSPHOGLYCERIDES

Abstract

Methods for hydrolyzing solid ungranulated lysophosphatidylcholine with phospholipase A 2 are provided. Also disclosed are methods for making a lipid matrix of lysophosphatidylcholine, monoglyceride and fatty acid, and lipid matrices of particular structure.

1 . A drug delivery composition comprising a lipid matrix and a pharmaceutically acceptable carrier, wherein at least part of the lipid matrix is in a phase other than a lamellar phase, hexagonal phase or inverse hexagonal phase, wherein the lipid matrix comprises lysophosphoglyceride, monoglyceride and fatty acid, wherein the molar ratio of lysophosphoglyceride:the sum of monoglyceride and fatty acid in the lipid matrix is between 1:3 and 1:12. 
     
     
         2 . The drug delivery composition of  claim 1 , wherein the lipid matrix comprises from about 0 to about 8 moles of water per mole of lipid. 
     
     
         3 . The drug delivery composition of  claim 2 , wherein the lipid matrix comprises at least about 1 moles of water per mole of lipid. 
     
     
         4 . The drug delivery composition of  claim 2 , wherein the lipid matrix comprises at least about 3 moles of water per mole of lipid. 
     
     
         5 . The drug delivery composition of  claim 2 , wherein the lipid matrix comprises at least about 8 moles of water per mole of lipid. 
     
     
         6 . The drug delivery composition of  claim 1  wherein the molar ratio of lysophosphoglyceride:the sum of monoglyceride and fatty acid in the lipid matrix is between 1:5 and 1:6. 
     
     
         7 . The drug delivery composition of  claim 6  wherein the lipid matrix has a lysophosphoglyceride:monoglyceride:fatty acid molar ratio between 1:4:2 and 1:2:4. 
     
     
         8 . The drug delivery composition of  claim 7  wherein the lipid matrix has a lysophosphoglyceride:monoglyceride:fatty acid molar ratio selected from the group consisting of 1:4:2, 1:3:3 and 1:3:2. 
     
     
         9 . The drug delivery composition of  claim 1 , wherein the lysophosphoglyceride is lysophosphatidylcholine. 
     
     
         10 . The drug delivery composition of  claim 1 , further comprising one or more water soluble or water insoluble pharmaceutical compounds. 
     
     
         11 . A nutritional supplement for the treatment of cystic fibrosis comprising an effective amount of the drug delivery composition of  claim 1 . 
     
     
         12 . A nutritional supplement comprising the drug delivery composition of  claim 1 .