Liposomes containing cationic lipids and vitamin D
AssigneeGen-Probe Incorporated
InventorsNanibhushan Dattagupta, Aditya Ranjan Das, C. Nagaraja Sridhar, Jasmin R. Patel
Life of this patent
Estimating the term…
Abstract
Lipid molecules bearing a cationic charge are described. These cationic lipids are useful in the delivery of biomolecules, such as oligonucleotides, nucleic acids, peptides, diagnostic imaging agents, proteins and drug molecules. In the form of liposomes, they can effectively be used for the intracellular delivery of biomolecules for therapeutic or diagnostic purposes.
Claims17
A formulation for introducing a biomolecule into a cell comprising a liposome, said liposome comprising a Vitamin D derivative, a pH sensitive amphiphile, a biomolecule and a thiocationic lipid of the formula:
- ##STR5## and optical isomers, salts, or a combination of optical isomers and salts thereof wherein:
- A.sup.1 and A.sup.2 are the same or different and are --O--CO--, --O--, --S--CO-- or --S--;
- A.sup.3 is --O--, --O--CO--, --CO--O--, --S--, --S--CO--, --CO--S--, --O--CS--, --CS--O--, --CO--NH--, --NH--CO--, --CS--NH--, --NH--CS--, --NH--CO--O--, --NH--CO--NH--, --O--CO--NH--, or is absent;
- R.sup.1 and R.sup.2 are the same or different and are H, or C.sub.1 to C.sub.23 saturated or partially unsaturated alkyl or aralkyl, with the proviso that at least one of R.sup.1 and R.sup.2 is not H;
- R.sup.3 is a C.sub.1 to C.sub.12 alkyl, aralkyl, alkaryl, heterocyclyl or heteroaryl;
- or
- R.sup.3 is an amino acid, a dipeptide, a tripeptide, a tetrapeptide or a pentapeptide;
- or
- R.sup.3 is --(CH.sub.2).sub.p --NR.sup.4 !.sub.q --R.sup.4,
- --(CH.sub.2).sub.p --NR.sup.4.sub.3.sup.+, ##STR6## wherein p is an integer from 1 to 5, q is an integer from 0 to 4, and R.sup.4 is H or a C.sub.1 to C.sub.4 alkyl, and each of m, n and o is an integer from 0 to 8, with the provisos that m.gtoreq.1 and (m+n+o).gtoreq.3.
Dependencies are inferred from the claim text.