Stabilized all-aqueous emulsions and methods of making and using thereof

Patent metadata

Field	Value
Publication number	US-9757333-B2
Application number	US-201414564365-A
Country	US
Kind code	B2
Filing date	Dec 9, 2014
Priority date	Dec 9, 2013
Publication date	Sep 12, 2017
Grant date	Sep 12, 2017

Abstract

Methods for preparing all-aqueous emulsions, including stable emulsions or emulsions having high viscosity and/or ultra-low interfacial tension are described. The method includes mixing, combining, or contacting a first electrically charged phase containing a first solute (e.g., dispersed phase) with at least a second phase containing a second solute (e.g., continuous phase). The solutes are incompatible with each other. The electrostatic forces between the two phases induce the formation of droplets of a dispersed phase in a continuous phase. The dispersed and continuous phases contain oppositely charged molecules, such as surfactants or other macromolecules and colloids which stabilize the drops of the dispersed phase. Complex coacervation of the oppositely charged molecules or colloids at the interface of the two aqueous phases results in formation of a membrane or barrier which prevents coalescence or aggregation of the droplets. The membrane also prevents leakage of any encapsulated agents from the droplets.

First claim

We claim:

1. A method for preparing a stabilized all-aqueous emulsion, the method comprising contacting an electrically charged first aqueous phase containing a first solute and one or more charged surfactants with an optionally charged second aqueous phase containing a second solute and one or more charged surfactants which has a charge opposite to the charge of the surfactant in the first aqueous phase, wherein the solutes are incompatible and induce formation of droplets of a dispersed phase in a continuous phase wherein the first aqueous phase and second aqueous phase are contacted using electrospraying.

2. The method of claim 1 , wherein the emulsion has a dynamic viscosity of >100 mPa·s or an interfacial tension of <0.1 mN/m.

3. The method of claim 1 , wherein the first and second solutes are selected from the group consisting of polyethylene glycol (PEG), dextran, methyl cellulose, sodium dextran sulfate, polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP); tripotassium phosphate, sodium citrate, sodium sulfate, and disodium phosphate.

4. The method of claim 3 , wherein the first solute is PEG and the second solute is dextran.

5. The method of claim 4 , wherein the molecular weight of PEG is about 8,000-20,000 Daltons and the concentration of PEG is 8% and the molecular weight of dextran is about 500,000 Daltons and the concentration of dextran is about 5-15%.

6. The method of claim 1 , wherein the first aqueous phase and/or the second aqueous phase further contains one or more therapeutic, prophylactic, and/or diagnostic agents that are encapsulated in the droplets of the dispersed phase.

7. The method of claim 1 , wherein the first aqueous phase and/or the second aqueous phase further contains cells that are encapsulated in the droplets of the dispersed phase.

8. An emulsion prepared by the method of claim 1 .

9. The emulsion of claim 8 , wherein the droplets comprise a membrane on the surface of the droplets which prevents coalescence of the droplets and/or prevent leakage of the contents of the droplets.

10. The emulsion of claim 9 , wherein the diameter of the droplets is from about 100 microns to about 1000 microns.

11. A pharmaceutical composition comprising the emulsion of claim 8 and one or more pharmaceutically acceptable carriers.

12. A method for administering one or more therapeutic, prophylactic, and/or diagnostic agent to a patient in need thereof, the method comprising administering the emulsion of claim 8 .

13. The method of claim 12 , wherein the agent is a biomolecule, a small molecule, or combinations thereof.

14. The method of claim 12 , wherein the emulsion is administered orally.

15. The method of claim 12 , wherein the emulsion is administered parenterally.

16. A method for administering cells to a patient in need thereof, the method comprising administering the emulsion of claim 8 .

17. The method of claim 16 , wherein the emulsion is administered parenterally.

Assignees

• Versitech Ltd

Inventors

• Shum Ho Cheung
• Song Yang
• Liu Zhou

Classifications

• A61K9/0019

  Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00) · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K9/107 Primary

  Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)} · CPC title

• A61K47/36

  Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin · CPC title

• B01F3/0803

  Operations & Transport · mapped topic