LIPID-POLYMER CONJUGATES, THEIR PREPARATION AND USES THEREOF
This invention provides low molecular weight lipid-GAG and phospholipids-GAG conjugates and methods of use thereof in suppressing, inhibiting, preventing, or treating a pathogenic effect on a cell, including, inter alia, infection with intracellular pathogens.
1 . A lipid-polymer conjugate comprising a glycosaminoglycan (GAG) conjugated to a phospholipid (PL) wherein said conjugate is prepared by reacting said GAG with said PL in a mass PL to mass GAG ratio from about 0.25:15 to about 5:15, respectively.
2 . The lipid-polymer conjugate of claim 0 , wherein said mass PL to mass GAG ratio is about 0.25:15.
3 . The lipid-polymer conjugate of claim 0 , wherein said mass PL to mass GAG ratio is about 0.5:15.
4 . The lipid-polymer conjugate of claim 0 , wherein said mass PL to mass GAG ratio is about 1:15.
5 . The lipid-polymer conjugate of claim 0 , wherein said mass PL to mass GAG ratio is about 2:15.
6 . The lipid-polymer conjugate of claim 0 , wherein said mass PL to mass GAG ratio is about 5:15.
7 . The lipid-polymer conjugate of claim 0 , wherein said GAG is hyaluronic acid, heparin, heparan sulfate, chondroitin, chondroitin sulfate, dermatan sulfate or keratan sulfate.
8 . The lipid-polymer conjugate of claim 0 , wherein said PL is a phosphatidylethanolamine, a phosphatidylserine, a phosphatidylcholine, a phosphatidylinositol, a phosphatidic acid or a phosphatidylglycerol.
9 . The lipid-polymer conjugate of claim 0 , wherein said PL comprises the residue of palmitic acid or myristic acid.
10 . The lipid-polymer conjugate of claim 0 , wherein said PL is dimyristoyl phosphatidylethanolamine or dipalmitoyl phosphatidylethanolamine.
11 . The lipid-polymer conjugate of claim 0 , wherein the polydispersity of said GAG is from about 1 to 1.75.
12 . The lipid-polymer conjugate of claim 11 , wherein the polydispersity of said GAG is from about 1.25 to 1.5.
13 . The lipid-polymer conjugate of claim 0 , wherein the average molecular weight of said GAG is between 5 KD to 90 KD.
14 . The lipid-polymerconjugate of claim 13 , wherein the average molecular weight of said GAG is between 5 KD to 20 KD.
15 - 23 . (canceled)
24 . A lipid-polymer conjugate comprising a glycosaminglycan (GAG) conjugated to a phospholipid (PL) via an amide or ester linkage wherein the molecular weight of said GAG is between 5 to 20 KD and wherein the polydispersity of said GAG is from about 1 to 1.75.
25 . The lipid-polymer conjugate of claim 24 , wherein the polydispersity of said GAG is from about 1.25 to 1.5.
26 . The lipid-polymer conjugate of claim 24 , wherein said GAG is hyaluronic acid, heparin, heparan sulfate, chondroitin, chondroitin sulfate, dermatan sulfate or keratan sulfate.
27 . The lipid-polymer conjugate of claim 24 , wherein said PL is a phosphatidylethanolamine, a phosphatidylserine, a phosphatidylcholine, a phosphatidylinositol, a phosphatidic acid or a phosphatidylglycerol.
28 . The lipid-polymer conjugate of claim 24 , wherein said PL comprises the residue of palmitic acid or myristic acid.
29 . The lipid-polymer conjugate of claim 24 , wherein said PL is dimyristoyl phosphatidylethanolamine or dipalmitoyl phosphatidylethanolamine.
30 . A pharmaceutical composition comprising the lipid-polymer conjugate of claim 1 .
31 . A pharmaceutical composition comprising the lipid-polymer conjugate of claim 24 .