Polyanionic polymers which enhance fusogenicity
First Claim
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1. A compound of the formula wherein:
- R1 is a member selected from the group consisting of hydrogen, hydroxyl, amino, optionally-substituted alkyl and a ligand;
Y is a member selected from the group consisting of hydrogen, optionally-substituted alkyl, optionally-substituted cycloalkyl, optionally-substituted aryl and optionally-substituted heteroaryl;
X is a member selected from the group consisting of optionally-substituted amino, oxygen, sulfur and a carbon single bond;
R2 is a member selected from the group consisting of C6–
C26 alkyl, C6–
C26 alkenyl, dialkylglycerolyl, dialkenylglycerolyl, diacylglycerolyl, 1,2-diacyl-sn-glycero-3-phosphoethylenyl, 1,2-dialkoxy-3-aminopropanyl and 1,2-diacyloxy-3-aminopropanyl;
R3 is a member selected from the group consisting of hydrogen, hydroxyl, amino, optionally-substituted alkyl and a ligand;
n is greater than 1; and
i is greater than 1.
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Abstract
The present invention relates generally to the amphiphilic polyelectrolyte, poly(2-ethylacrylic acid) and covalently bonded lipids to generate Lipo-PEAA. These Lipo-PEAA are then used to make pH-sensitive liposomes which become unstable, permeable or fusogenic with certain pH changes. In addition, this invention generally describes methods for delivering therapeutic compounds and drugs to target cells by administering to a host the pH-sensitive liposomes of the present invention.
50 Citations
46 Claims
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1. A compound of the formula
wherein: -
R1 is a member selected from the group consisting of hydrogen, hydroxyl, amino, optionally-substituted alkyl and a ligand; Y is a member selected from the group consisting of hydrogen, optionally-substituted alkyl, optionally-substituted cycloalkyl, optionally-substituted aryl and optionally-substituted heteroaryl; X is a member selected from the group consisting of optionally-substituted amino, oxygen, sulfur and a carbon single bond; R2 is a member selected from the group consisting of C6–
C26 alkyl, C6–
C26 alkenyl, dialkylglycerolyl, dialkenylglycerolyl, diacylglycerolyl, 1,2-diacyl-sn-glycero-3-phosphoethylenyl, 1,2-dialkoxy-3-aminopropanyl and 1,2-diacyloxy-3-aminopropanyl;R3 is a member selected from the group consisting of hydrogen, hydroxyl, amino, optionally-substituted alkyl and a ligand; n is greater than 1; and i is greater than 1. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
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13. A pH-sensitive liposome, said liposome comprising a lipid and a compound of the formula
wherein: -
R1 is a member selected from the group consisting of hydrogen, hydroxyl, amino, optionally-substituted alkyl and a ligand; Y is a member selected from the group consisting of hydrogen, optionally substituted alkyl, optionally-substituted cycloalkyl, optionally-substituted aryl and optionally-substituted heteroaryl; X is a member selected from the group consisting of optionally-substituted amino, oxygen, sulfur a carbon single bond; R2 is a member selected from the group consisting of C6–
C26 alkyl, C6–
C26 alkenyl, dialkylglycerolyl, dialkenylglycerolyl, diacylglycerolyl, 1,2-diacyl-sn-glycero-3-phosphoethylenyl, 1,2-dialkoxy-3-aminopropanyl and 1,2-diacyloxy-3-aminopropanyl;R3 is a member selected from the group consisting of hydrogen, hydroxyl, amino, optionally-substituted alkyl and a ligand; n is greater than 1; and i is greater than 1. - View Dependent Claims (14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46)
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Specification