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US 11,891,482 B2Granted
Polymer excipients for drug delivery applications
AssigneeTyndall Formulation Services, LLC
InventorsKevin N. Sill, Bradford T. Sullivan
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to the field of polymer chemistry and more particularly to multiblock copolymers comprising a poly(sarcosine) block and a D,L-mixed poly(amino acid) block and uses thereof.
Claims18
A method of increasing the solubility of a hydrophobic molecule in an aqueous solution comprising encapsulating the hydrophobic molecule in a multiblock copolymer of Formula I:
- wherein:
- R1a is H or an optionally substituted aliphatic group;
- R1b is H or an optionally substituted aliphatic group;
- R2 is H, an optionally substituted aliphatic group or an optionally substituted CO—(C1-C6) aliphatic group;
- each Ry is independently the side chain of γ-benzyl-D-glutamate, D-leucine, D-tyrosine, D-phenylalanine, D-alanine, D-valine, D-isoleucine, D-norleucine, O-acetyl-D-tyrosine, O-benzyl-D-tyrosine, or ε-benzyl-D-lysine;
- each Rz is independently the side chain of γ-benzyl-L-glutamate, L-leucine, L-tyrosine, L-phenylalanine, L-alanine, L-valine, L-isoleucine, L-norleucine, O-acetyl-L-tyrosine, O-benzyl-L-tyrosine, or ε-benzyl-L-lysine;
- x is 125-350;
- y is 5-35;
- z is 5-35.
6 more elements
A method of preparing a composition comprising a multiblock copolymer of Formula I:
- wherein:
- R1a is H or an optionally substituted aliphatic group;
- R1b is H or an optionally substituted aliphatic group;
- R2 is H, an optionally substituted aliphatic group or an optionally substituted CO—(C1-C6)aliphatic group;
- each Ry is independently the side chain of γ-benzyl-D-glutamate, D-leucine, D-tyrosine, D-phenylalanine, D-alanine, D-valine, D-isoleucine, D-norleucine, O-acetyl-D-tyrosine, O-benzyl-D-tyrosine, or ε-benzyl-D-lysine;
- each Rz is independently the side chain of γ-benzyl-L-glutamate, L-leucine, L-tyrosine, L-phenylalanine, L-alanine, L-valine, L-isoleucine, L-norleucine, O-acetyl-L-tyrosine, O-benzyl-L-tyrosine, or ε-benzyl-L-lysine;
- x is 125-350;
- y is 5-35;
- and
- z is 5-35,
- the method comprising dissolving a hydrophobic molecule, the copolymer of Formula I and, optionally, a cryoprotectant, in aqueous solution, to produce a mixed solution.
8 more elements
A method of preparing a composition comprising a multiblock copolymer of Formula I:
- wherein:
- R1a is H or an optionally substituted aliphatic group;
- R1b is H or an optionally substituted aliphatic group;
- R2 is H, an optionally substituted aliphatic group or an optionally substituted CO—(C1-C6)aliphatic group;
- each Ry is independently the side chain of γ-benzyl-D-glutamate, D-leucine, D-tyrosine, D-phenylalanine, D-alanine, D-valine, D-isoleucine, D-norleucine, O-acetyl-D-tyrosine, O-benzyl-D-tyrosine, or ε-benzyl-D-lysine;
- each Rz is independently the side chain of γ-benzyl-L-glutamate, L-leucine, L-tyrosine, L-phenylalanine, L-alanine, L-valine, L-isoleucine, L-norleucine, O-acetyl-L-tyrosine, O-benzyl-L-tyrosine, or ε-benzyl-L-lysine;
- x is 125-350;
- y is 5-35;
- and
- z is 5-35,
- the method comprising:
- a. dissolving a hydrophobic molecule in an organic solvent, to produce a hydrophobic molecule solution;
- b. dissolving a copolymer of Formula I and, optionally, a cryoprotectant, in an aqueous solution, to produce a copolymer solution;
- and
- c. mixing the hydrophobic molecule solution and the copolymer solution to produce a mixed solution, and optionally lyophilizing the mixed solution.
12 more elements
Dependencies are inferred from the claim text.