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Home Nonmetallic Processes Hydrocarbon-oil-fluorochemical-preparations-and-methods-of-use

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 Hydrocarbon oil/fluorochemical preparations and methods of use

Details
Inventors: Trevino, Leo A.; Riess, Jean G.; Dellamary, Luis A.; Krafft, Marie-Pierre; Tarara, Thomas E.;
Assignee: Alliance Pharmaceutical Corp. (San Diego, CA)
Primary Examiner: Hollinden; Gary E.
Assistant Examiner: Hartley; Michael G.
Attorney, Agent or Firm: Knobbe, Martens Olson & Bear, LLP

Novel hydrocarbon oil/fluorochemical preparations and methods for their use are provided. The preparations, which preferably comprise a fluorophilic dispersing agent, may be in the form of hydrocarbon oil-in-fluorochemical dispersions or in the form of a multiple emulsion comprising a polar liquid continuous phase and are particularly useful for administering bioactive agents. In particular the preparations of the present invention may be used to control the bioavailability and improve the efficacy of lipophilic bioactive agents having limited solubility in an aqueous physiological environment.

DETAILED DESCRIPTION OF THE PRESENT INVENTION In a broad aspect the present invention provides hydrocarbon oil/fluorochemical (HO/FC) preparations that may be used for controlled administration of bioactive agents.
Preferred embodiments of the present invention comprise hydrocarbon oil-in-fluorochemical (HO/FC) dispersions and hydrocarbon oil-in-fluorochemical-in-polar liquid (HO/FC/W) multiple emulsions.
The HO/FC dispersions typically comprise a fluorochemical continuous phase into which a hydrocarbon oil is dispersed.
In select embodiments the dispersed hydrocarbon oil may comprise a bioactive agent.
These dispersions are preferably stabilized through the use of a fluorophilic dispersing agent.
Preferably, the HO/FC/W multiple emulsions comprise a disperse phase (or HO/FC phase) comprising hydrocarbon oil particulates, or droplets, at least partially encapsulated in fluorochemical.
In such embodiments the fluorochemical encapsulated hydrocarbon oil droplets are dispersed in a continuous polar liquid phase comprising a hydrophilic emulsifying agent.
A fluorinated surfactant or a fluorocarbon-hydrocarbon diblock compound and natural phospholipids can be used, for example, as the fluorophilic and as the emulsifying agents, respectively.
HO/FC preparations, both in the form of HO/FC dispersions and HO/FC/W emulsions, have utility as vehicles and controlled release systems for bioactive agents, and lipophilic material in general.
With the HO/FC dispersions and HO/FC/W multiple emulsions of the present invention, the diffusion of a lipophilic drug, comprising or associated with the encapsulated hydrocarbon oil droplet may be significantly retarded by the fluorochemical shell.
These properties allow for controlled drug release and prolonged delivery profiles, particularly for lipophilic bioactive agents.
The fluorochemical barrier can also act to protect the encapsulated substances from body fluids and vice-versa, thus reducing the toxicity of the incorporated substances.
The partially fluorinated or perfluorinated compounds comprising the fluorochemical component of the disclosed preparations, both HO/FC and HO/FC/W, are typically chosen for their low toxicity, gas dissolving capacity, surface tension and spreading coefficient



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