Block copolymers and uses thereof
AssigneeEcole Polytechnique Federale De Lausanne (Epfl)
InventorsJames Brandon DIXON, Jeffrey A. HUBBELL, Conlin P. O'NEIL, Melody SWARTZ, Diana VELLUTO
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Abstract
Block copolymers containing charged blocks or chemical moieties sensitive to oxidation or hydrolysis have been developed. We describe the use of such block copolymers in supramolecular structures, e.g., micelles or vesicles, and pharmaceutical compositions and in methods of preparing the supramolecular structures and pharmaceutical compositions. The invention is particularly useful for the delivery of pharmaceutical agents, e.g., nucleic acids, to cells.
Claims50
A block copolymer comprising a hydrophilic block and a hydrophobic block, wherein said hydrophilic or hydrophobic block is interrupted with a hydrolysable chemical moiety,
- wherein said hydrophilic block comprises poly(ethylene glycol), poly(ethylene oxide)-co-poly(propylene oxide) di- or multiblock copolymers, poly(ethylene oxide), poly(vinvl alcohol), poly(ethylene-co-vinyl alcohol), poly(N-vinyl pyrrolidone), poly(acrylic acid), poly(ethvloxazoline), poly(alkvlacrvlates), poly(acrvlamide), poly(N-alkylacrylamides), polysaccharide, poly(N,N-dialkylacrylamides), hyaluronic acid, or poly (N-acryloylmorpholine), and
- said hydrophobic block comprises poly(propylene sulfide), Poly(Propylene glycol), esterified poly(acrylic acid), esterified poly(glutamic acid), or esterified poly(aspartic acid).
-7. (canceled)
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-17. (canceled)
The supramolecular structure of claim, wherein said pharmaceutical agent is a polypeptide that is an antibody or an antigen-binding fragment thereof.
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-22. (canceled)
-25. (canceled)
-29. (canceled)
A method of encapsulating a pharmaceutical agent in a supramolecular structure comprising
- a. applying heat to a mixture of (i) a block copolymer comprising a hydrophilic block and a hydrophobic block, (ii) an excipient, and (iii) a pharmaceutical agent in an amount sufficient to homogenize said mixture, and
- b. diluting said mixture in an aqueous solution.
-33. (canceled)
A method of making a vesicle comprising:
- a. forming micelles from a block copolymer comprising a hydrophilic block and a hydrophobic block, wherein vesicles of said block copolymer are thermodynamically more stable than micelles;
- and
- b. heating said micelles to form said vesicle.
-40. (canceled)
A dry formulation comprising micelles comprising a block copolymer comprising a hydrophilic block and a hydrophobic block, wherein said formulation comprises less than 5% water by weight.
-46. (canceled)
A supramolecular structure comprising a (i) a block copolymer comprising a positively charged block, and (ii) a nucleic acid, wherein said supramolecular structure has a maximal diameter of 60 nm or less.
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A block copolymer comprising PEG-PPS-PEI.
-71. (canceled)
A supramolecular structure comprising block copolymers comprising a hydrophilic block and a hydrophobic block, wherein said block copolymers comprise a charged chemical moiety and wherein 5-25% of said block copolymers have the charged chemical moiety disposed at the outer surface of said structure.
(canceled)
Dependencies are inferred from the claim text.