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US 5,965,159 AGranted
Etherlipid-containing multiple lipid liposomes
AssigneeThe Liposome Company, Inc.
InventorsEric Mayhew, Andrew S. Janoff, Imran Ahmad, Suresh K. Bhatia
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Abstract
Described herein are liposomes containing etherlipids of the formula: ##STR1## as well as a phosphatidylcholine, a sterol, and a headgroup-derivatized lipid. These liposomes are useful in a variety of therapeutic regimens, including the treatment of cancers and inflammatory disorders.
Claims16
A liposome having a lipid bilayer which comprises:
- (a) a phosphatidylcholine;
- (b) a sterol;
- (c) a headgroup-derivatized lipid comprising a phosphatidylethanolamine linked at the ethanolamine group to a dicarboxylic acid;
- and, (d) an etherlipid having the formula:
- ##STR11## wherein R.sub.1 is Y.sub.1 Y.sub.2, Y.sub.2 is CH.sub.3 or CO.sub.2 H, Y.sub.1 is (CH.sub.2).sub.n1 (CH.dbd.CH).sub.n2 (CH.sub.2).sub.n3 (CH.dbd.CH).sub.n4 (CH.sub.2).sub.n5 (CH.dbd.CH).sub.n6 (CH.sub.2).sub.n7 (CH.dbd.CH).sub.n8 (CH.sub.2).sub.n9, the sum of n1+2n2+n3+2n4+n5+2n6+n7+2n8+n9 is an integer of from 3 to 23, n1 is zero or an integer of from 1 to 23, n3 is zero or an integer of from 1 to 20, n5 is zero or an integer of from 1 to 17, n7 is zero or an integer of from 1 to 14, n9 is zero or an integer of from 1 to 11, and each of n2, n4, n6 and 8 is independently zero or 1;
- wherein Z is oxygen or sulfur and R.sub.2 is CH.sub.3 ;
- wherein R.sub.3 is --O--P(O).sub.2 --O--CH.sub.2 CH.sub.2 N(CH.sub.3).sub.3 ;
- and wherein the phosphatidylethanolamine-dicarboxylic acid comprises from about 5 mole percent to about 20 mole percent of the lipid bilayer and the etherlipid comprises from greater than about 10 mole percent to less than about 30 mole percent of the lipid bilayer.
5 more elements
Dependencies are inferred from the claim text.