Wisconsin Alumni Research Foundation

Sandro Mecozzi

Robert A Pearce

Glen S Kwon

Jonathan P Fast

William Tucker

Moira Esson

The present invention discloses an ionic liquid composition comprising an at least partially hydrophobic ionic liquid, wherein the at least partially hydrophobic ionic liquid comprises a di cation comprising two monocationic groups linked by a bridging group wherein the bridging group provides an at least partially hydrophobic character. The composition may also include a hydrophilic ionic liquid. The hydrophobic ionic liquid may include a quaternary ammonium group which may be substituted or unsubstituted, saturated or unsaturated, linear, branched, cyclic or aromatic and the bridging group is a unsubstituted or substituted C-Calkylene or C-Calkoxy alkyl. Also disclosed is a nanoemulsion formulation which includes the ionic liquid compositions, at least one polymer, a hydrophobic liquid, an aqueous liquid, and a hydrophobic or hydrophilic therapeutic agent. Methods to deliver a therapeutic agent by delivering a nanoemulsion and methods to make a nanoemulsion are also disclosed.

Ionic liquid-based nanoemulsion formulation for the efficient delivery of hydrophilic and hydrophobic therapeutic agents

The present invention provides therapeutic formulations, including therapeutic nanoemulsions, and related methods for the in vivo delivery of hydrophobic compounds, including an important class of hydrophobic anesthetics. Formulations and methods of the invention include semifluorinated block copolymers and perhalogenated fluorous compounds, such as perfluorooctyl bromide or perfluorodecalin, capable of forming a stable nanoemulsion without the need of conventional lipid components that support bacterial and/or fungal growth (e.g., soybean oil and similar lipids). In certain embodiments, emulsion-based formulations are provided that are capable of formulating, delivering and releasing amounts of hydrophobic drugs effective for a range of clinical applications, including inducing and maintaining anesthesia in patients. In certain embodiments, emulsion-based formulations are provided that are capable of supporting controlled release, for example, over a range of rates useful for clinical applications including rapid and sustained release.

Fluoropolymer emulsions with perhalogenated stabilizer for the delivery of hydrophobic drugs

The present invention provides therapeutic formulations, including therapeutic nanoemulsions, and related methods for the in vivo delivery of hydrophobic compounds, including an important class of hydrophobic anesthetics. Formulations and methods of the invention include semifluorinated block copolymers, and optionally phospholipid surfactants, capable of forming a stable nanoemulsion without the need of conventional lipid components that support bacterial and/or fungal growth (e.g., soybean oil and similar lipids). In certain embodiments, emulsion-based formulations are provided that are capable of formulating, delivering and releasing amounts of hydrophobic drugs effective for a range of clinical applications, including inducing and maintaining anesthesia in patients. In certain embodiments, emulsion-based formulations are provided that are capable of supporting controlled release, for example, over a range of rates useful for clinical applications including rapid and sustained release.

Fluoropolymer emulsions with branched semifluorinated block copolymer or phospholipid surfactant for the delivery of hydrophobic drugs

The present invention provides therapeutic formulations, including therapeutic emulsions and nanoemulsions, and related methods for the delivery of fluorinated therapeutic compounds, including an important class of low boiling point perfluorinated and/or perhalogenated volatile anesthetics. Emulsion-based fluorinated volatile anesthetic formulations compatible with intravenous administration are provided that are capable of delivering and releasing amounts of fluorinated volatile anesthetic compounds effective for inducing and maintaining anesthesia in patients. Intravenous delivery of the present emulsion-based fluorinated volatile anesthetic formulations permits anesthetic levels in a patient to be selectively adjusted very rapidly and accurately without the need to hyperventilate patients and without the use of irritating agents.

Fluoropolymer-based emulsions for the intravenous delivery of fluorinated volatile anesthetics

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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Madison, WI, United States of America

Sandro Mecozzi