Liposomal peptide-lipid conjugates and delivery using same
AssigneeThe Liposome Company, Inc.
InventorsPaul R. Meers, Charles Pak, Shaukat Ali, Andrew Janoff, J. Craig Franklin, Ravi K. Erukulla, Donna Cabral-Lilly
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Abstract
Peptide-lipid conjugates are incorporated into liposomes so as to selectively destabilize the liposomes in the vicinity of target peptidase-secreting cells, and hence, to deliver the liposomes to the vicinity of the target cells, or directly into the cells. The liposomes can thus be used to treat mammals for diseases, disorders or conditions, e.g., tumors, microbial infection and inflammations, characterized by the occurrence of peptidase-secreting cells.
Claims14
A liposome having a bilayer comprising a lipid component which comprises a peptide-lipid conjugate having the formula:
- ##STR6## wherein:
- X is a linker selected from the group consisting of a single bond and the group R.sup.3 ;
- each of R.sup.1, R.sup.2 and R.sup.3 is independently a group having the formula --OC(O)(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 CH.sub.3 ;
- n1 is equal to zero or an integer of from 1 to 22, n3 is equal to zero or an integer of from 1 to 19, n5 is equal to zero or an integer of from 1 to 16, n7 is equal to zero or an integer of from 1 to 13, n9 is equal to zero or an integer of from 1 to 10;
- for each of R.sup.1 and R.sup.2 independently the sum of n1+2n2+n3+2n4+n5+2n6+n7+2n8+n9 is an integer equal to from 12 to 22;
- for R.sup.3 the sum of n1+2n2+n3+2n4+n5+2n6+n7+2n8+n9 is zero or an integer equal to from (0) 1 to 22;
- each of n2, n4, n6 and n8 is independently equal to 0 or 1;
- and,
- Y is an enzyme cleavable peptide comprising an amino acid sequence which is the substrate of a cell-secreted peptidase.
Dependencies are inferred from the claim text.