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US 2014/0271822 A1Published application
Modified docetaxel liposome formulations
AssigneeMallinckrodt Inc.
InventorsWilliam McGhee, James Blackledge, Margaret Grapperhaus
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Abstract
The present invention provides compositions for the treatment of cancer. The compositions include liposomes containing a phosphatidylcholine lipid, a sterol, a PEG-lipid, and a taxane. The PEG-lipid constitutes from about 2 to about 8 mol % of the lipids in the liposome. The taxane is docetaxel esterified at the 2′-O position with a heterocyclyl-(C2-5alkanoic acid). Methods for preparation of liposomal taxanes and treatment of cancer with liposomal taxanes are also disclosed.
Claims31
A method for preparing a liposomal taxane, the method comprising:
- a) forming a first liposome having a lipid bilayer comprising a phosphatidylcholine lipid and a sterol, wherein the lipid bilayer encapsulates an interior compartment comprising an aqueous solution;
- b) loading the first liposome with a taxane, or a pharmaceutically acceptable salt thereof, to form a loaded liposome, wherein the taxane is docetaxel esterified at the 2′-O-position with a heterocyclyl-(C2-5alkanoyl) group;
- and
- c) forming a mixture comprising the loaded liposome and a poly(ethylene glycol)-phospholipid conjugate (PEG-lipid) under conditions sufficient to allow insertion of the PEG-lipid into the lipid bilayer;
- thereby forming the liposomal taxane.
2 more elements
31-40. (canceled)
Dependencies are inferred from the claim text.