Targeted compositions for diagnostic and therapeutic use
AssigneeImarx Therapeutics, Inc.
InventorsEvan C. Unger, Terry O. Matsunaga, Patricia A. Schumann
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Abstract
Novel targeted compositions which may be used for diagnostic and therapeutic use. The compositions may comprise lipid, protein or polymer gas-filled vesicles which further comprise novel compounds of the general formula L-P-T, wherein L comprises a hydrophobic compound, P comprises a hydrophilic polymer, and T comprises a targeting ligand which targets tissues, cells or receptors, including myocardial cells, endothelial cells, epithelial cells, tumor cells and the glycoprotein GPIIbIIIa receptor. The compositions can be used in conjunction with diagnostic imaging, such as ultrasound, as well as therapeutic applications, such as therapeutic ultrasound.
Claims70
A targeted vesicle composition for therapeutic or diagnostic use in vivo comprising, in an aqueous carrier, gas filled liposomes comprising a phosphatidylcholine selected from the group consisting of dioleoylphosphatidylcholine, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine, wherein said liposomes further comprise a compound having the formula
- wherein:
- X1 is a moiety selected from the group consisting of C(═X3), and C(═X3)—N(R8);
- X3 is O or S;
- R1 acyl having from 16 to 23 carbons;
- R2 is hydrogen or lower alkyl;
- R3 is a moiety having the structure (CH2)n, wherein n is an integer having the value between 1 and 10;
- R4 is acyl having from 16 to 23 carbons;
- R5 is hydrogen or lower alkyl;
- R7 is (CH2)—(CH2) or a direct bond;
- R8 is hydrogen or lower alkyl;
- P is PEG;
- and
- T is a targeting ligand comprising a peptide having the sequence CRGDC, wherein the two cysteines are linked together via a disulfide linkage.
A targeted vesicle composition for therapeutic or diagnostic use in vivo comprising, in an aqueous carrier, gas filled liposomes comprising a phosphatidylcholine selected from the group consisting of dioleoylphosphatidylcholine, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine, wherein said liposomes further comprise a compound having the formula
- wherein:
- each of R1 and R4 is acyl having 18 carbons;
- P is PEG-3400;
- and
- T comprises a peptide having the sequence CRGDC, wherein the two cysteines are linked together via a disulfide linkage.
A targeted vesicle composition for therapeutic or diagnostic use in vivo comprising, in an aqueous carrier, gas filled liposomes comprising a phosphatidylcholine selected from the group consisting of dioleoylphosphatidylcholine, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine, wherein said liposomes further comprise a compound having the formula
- wherein:
- each of R1 and R4 is acyl having 18 carbons;
- P is PEG-3400;
- and
- T comprises a peptide having the sequence CRGDC, wherein the two cysteines are linked together via a disulfide linkage.
Dependencies are inferred from the claim text.