Semi-fluorinated block copolymers for delivery of therapeutic agents
First Claim
1. A therapeutic formulation for delivering a hydrophobic drug or fluorophilic therapeutic agent to a patient, said formulation comprising:
- said hydrophobic drug or fluorophilic therapeutic agent; and
semi-fluorinated block copolymers, wherein each of said semi-fluorinated block copolymers comprises a hydrophilic block, a fluorophilic block, and a hydrophobic group;
wherein said fluorophilic block of each of said semi-fluorinated block copolymers is positioned between said hydrophilic block and said hydrophobic group,wherein said hydrophobic group is a distearoyl-glycero-phosphoethanolamine;
wherein said hydrophilic block is a poly(ethylene glycol) block having a molecular weight selected over the range of 1000 g mol−
1 to 12,000 g mol−
1; and
wherein said fluorophilic block is a perfluorinated alkyl chain having a length of 6 to 20 carbons.
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Abstract
The present invention provides semi-fluorinated block copolymers and related methods of synthesizing and using semi-fluorinated block copolymers for drug delivery and drug formulation applications. Semi-fluorinated block copolymers of this aspect of the invention include block copolymers having discrete hydrophilic, fluorophilic and hydrophobic structural domains that are capable of forming supramolecular structures in aqueous solutions, such as micelles, for encapsulating hydrophobic and/or fluorophilic therapeutic agents. Encapsulation by semi-fluorinated block copolymers of the present invention allows for enhanced solubilization and stabilization of hydrophobic and/or fluorophilic therapeutic agents relative to conventional drug delivery compositions and methods.
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Citations
25 Claims
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1. A therapeutic formulation for delivering a hydrophobic drug or fluorophilic therapeutic agent to a patient, said formulation comprising:
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said hydrophobic drug or fluorophilic therapeutic agent; and
semi-fluorinated block copolymers, wherein each of said semi-fluorinated block copolymers comprises a hydrophilic block, a fluorophilic block, and a hydrophobic group;
wherein said fluorophilic block of each of said semi-fluorinated block copolymers is positioned between said hydrophilic block and said hydrophobic group,wherein said hydrophobic group is a distearoyl-glycero-phosphoethanolamine; wherein said hydrophilic block is a poly(ethylene glycol) block having a molecular weight selected over the range of 1000 g mol−
1 to 12,000 g mol−
1; andwherein said fluorophilic block is a perfluorinated alkyl chain having a length of 6 to 20 carbons. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 22, 23, 24, 25)
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17. A method of administering a hydrophobic drug or fluorophilic therapeutic agent to a patient in need of treatment;
- said method comprising the steps of;
providing a therapeutic formulation comprisingsaid hydrophobic drug or fluorophilic therapeutic agent, and semi-fluorinated block copolymers in an aqueous solution, wherein each of said semi-fluorinated block copolymers comprise a hydrophilic block, a fluorophilic block, and a hydrophobic group;
wherein said fluorophilic block of each of said semi-fluorinated block copolymers is positioned between said hydrophilic block and said hydrophobic group,wherein said hydrophobic group is 1,2-distearoyl-S,N-glycero-3-phosphoethanolamine; wherein said hydrophilic block is a poly(ethylene glycol) block having a molecular weight selected over the range of 1000 g mol−
1 to 12,000 g mol−
1; andwherein said fluorophilic block is a perfluorinated alkyl chain having a length of 6 to 20 carbons; and delivering said therapeutic formulation to said patient.
- said method comprising the steps of;
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18. A method of solubilizing a hydrophobic drug or fluorophilic therapeutic agent, said method comprising the steps of:
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providing said hydrophobic drug or fluorophilic therapeutic agent, and semi-fluorinated block copolymers in an aqueous solution, wherein each of said semi-fluorinated block copolymers comprises a hydrophilic block, a fluorophilic block, and a hydrophobic group;
wherein said fluorophilic block of each of said semi-fluorinated block copolymers is positioned between said hydrophilic block and said hydrophobic group,wherein said hydrophobic group is 1,2-distearoyl-S,N-glycero-3-phosphoethanolamine; wherein said hydrophilic block is a poly(ethylene glycol) block having a molecular weight selected over the range of 1000 g mol−
1 to 12,000 g mol−
1; andwherein said fluorophilic block is a perfluorinated alkyl chain having a length of 6 to 20 carbons; and
wherein said semi-fluorinated block copolymers self assemble in said aqueous solution to form a supramolecular structure that at least partially encapsulates said hydrophobic drug or fluorophilic therapeutic agent, thereby solubilizing said hydrophobic drug or fluorophilic therapeutic agent.
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19. A method of decreasing the toxicity of a hydrophobic drug or fluorophilic therapeutic agent, said method comprising the steps of:
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providing said hydrophobic drug or fluorophilic therapeutic agent, and semi-fluorinated block copolymers in an aqueous solution, wherein each of said semi-fluorinated block copolymers comprises a hydrophilic block, a fluorophilic block, and a hydrophobic group;
wherein said fluorophilic block of each of said semi-fluorinated block copolymers is positioned between said hydrophilic block and said hydrophobic group,wherein said hydrophobic group is 1,2-distearoyl-S,N-glycero-3-phosphoethanolamine; wherein said hydrophilic block is a poly(ethylene glycol) block having a molecular weight selected over the range of 1000 g mol−
1 to 12,000 g mol−
1; andwherein said fluorophilic block is a perfluorinated alkyl chain having a length of 6 to 20 carbons; and
wherein said semi-fluorinated block copolymers self assemble in said aqueous solution to form a supramolecular structure that at least partially encapsulates said hydrophobic drug or fluorophilic therapeutic agent, thereby decreasing the toxicity of said hydrophobic drug or fluorophilic therapeutic agent.
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- 20. A semi-fluorinated block copolymer having the chemical formula:
Specification