Amphiphilic block copolymers for nucleic acid delivery
AssigneeBiocompatibles UK Limited
InventorsAndrew Lennard LEWIS, Giuseppe BATTAGLIA, Irene CANTON, Peter William STRATFORD
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Abstract
The present invention provides a composition comprising vesicles and encapsulated within the vesicles, nucleic acid comprising less than 1000 nucleotides, wherein the vesicles comprise an amphiphilic block copolymer having a hydrophilic and a hydrophobic block. Methods of forming vesicles and methods of delivering nucleic acid, in particular, iRNA into cells, are also provided.
Claims25
A composition comprising nanovesicles having an aqueous core and encapsulated within the aqueous core of the nanovesicles, nucleic acid comprising less than 1000 nucleotides, wherein the nanovesicles comprise an amphiphilic block copolymer having a hydrophilic and a hydrophobic block, wherein the ratio of the degree of polymerization of the hydrophilic to hydrophobic block is in the range of 1:2.5 to 1:8,
- wherein the hydrophobic block has a degree of polymerization in the range 50 to 250 and the hydrophilic block has a degree of polymerization of at least 15, the hydrophilic block comprises ethylenically unsaturated radically polymerizable monomers comprising a zwitterionic monomer, and wherein the hydrophobic block comprises (diisopropylamino)ethyl methacrylate or (diethylamino)ethyl methacrylate monomers.
A composition comprising nanovesicles having an aqueous core and encapsulated within the aqueous core of the nanovesicles, nucleic acid comprising less than 1000 nucleotides, wherein the nanovesicles have a diameter in the range 50-5000 nm and comprise an amphiphilic block copolymer having a hydrophilic and a hydrophobic block, wherein the ratio of the degree of polymerization of the hydrophilic to hydrophobic block is in the range of 1:2.5 to 1:8,
- wherein the hydrophobic block has a degree of polymerization in the range 50 to 250 and the hydrophilic block has a degree of polymerization of at least 15, the hydrophilic block is formed from ethylenically unsaturated radically polymerizable monomers comprising a zwitterionic monomer, and
- wherein the hydrophobic block comprises (diisopropylamino)ethyl methacrylate monomers.
A composition comprising nanovesicles and encapsulated within the aqueous core of the nanovesicles, nucleic acid comprising less than 1000 nucleotides, wherein the nanovesicles have a diameter in the range 50-1000 nm and comprise an amphiphilic block copolymer having a hydrophilic block comprising 2-methacryloyloxy ethyl phosphorylcholine and a hydrophobic block comprising 2-(diisopropyl)amino ethyl methacrylate, wherein the degree of polymerisation of the hydrophilic block is 20 to 25 and the degree of polymerisation of the hydrophobic block is 70 to 75, and wherein the nucleic acid is siRNA.
Dependencies are inferred from the claim text.