Semi-fluorinated block copolymers for delivery of therapeutic agents

摘要

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.

主权项

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.