Method of coating fine particles with lipid film

• US 20040022938A1
• Filed: 07/03/2003
• Published: 02/05/2004
• Est. Priority Date: 10/04/2000
• Status: Active Grant

• Current Assignee: Kyowa Hakko Kirin Company Limited (Kirin Holdings Company Limited)
• Original Assignee: Kyowa Hakko Kirin Company Limited (Kirin Holdings Company Limited)
• Inventors: Kusano, Hiroko, Yamauchi, Masahiro, Kato, Yasuki, Iwata, Takeshi, Akinaga, Shiro, Uochi, Takaaki
• Granted Patent: US 7,678,415 B2
• Time in Patent Office: Days
• US Class Current: 427/212
• CPC Class Codes: A61K 31/7088 Compounds having three or more nucleosides or nucleotides
• CPC Class Codes: A61K 47/6911 the form being a liposome
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: A61K 9/1271 Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers liposome as conjugate A61K47/6911
• CPC Class Codes: A61K 9/1272 with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids with cholesterol as the only non-phosphatidyl surfactant A61K9/127; lipids as modifying agent A61K47/543
• CPC Class Codes: A61K 9/141 Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers (co) spray-dried products A61K9/16, (co) lyophilised products A61K9/19; the carrier being chemically bound to the active ingredient A61K47/50
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/5015 Organic compounds, e.g. fats, sugars
• CPC Class Codes: A61K 9/5123 Organic compounds, e.g. fats, sugars
• CPC Class Codes: A61K 9/5192 Processes
• CPC Class Codes: B01J 13/12 removing solvent from the wall-forming material solution

Abstract

An object of the present invention is to provide a safe, convenient and efficient method for coating fine particles with lipid membrane.

There is provided a method for coating fine particles with lipid membrane, characterized in that, the rate of a polar organic solvent in an aqueous solution containing the polar organic solvent where the fine particles are dispersed and lipid is dissolved, is decreased.

Claims

1. A method for coating fine particles with lipid membrane, which comprises coating fine particles with lipid membrane by decreasing the rate of a polar organic solvent in an aqueous solution containing the polar organic solvent where the fine particles are dispersed and lipid is dissolved.

7. The method for coating fine particles with lipid membrane according to any one of claims 1 to 6, wherein the fine particles are those containing a water-soluble polymer derivative which is the same as or different from the water-soluble polymer derivative (I) recited in claim 3.

8. The method for coating fine particles with lipid membrane according to any one of claims 1 to 7, wherein the fine particles are those containing one or more member(s) selected from a drug, lipid assembly, liposome, fine particles in the emulsion, natural polymer, synthetic polymer, metal colloid, cationic lipid, anionic lipid and a fine particle preparation.

9. The method for coating fine particles with lipid membrane according to any one of claims 1 to 7, wherein the fine particles are those containing a drug.

10. The method for coating fine particles with lipid membrane according to any one of claims 1 to 7, wherein the fine particles comprise a complex of a drug with one or more member(s) selected from lipid assembly, liposome, fine particles in the emulsion, natural polymer, synthetic polymer, metal colloid, cationic lipid, anionic lipid and a fine particle preparation.

11. The method for coating fine particles with lipid membrane according to any one of claims 1 to 7, wherein the fine particles comprise a complex of a drug with cationic lipid.

12. The method for coating fine particles with lipid membrane according to any one of claims 1 to 7, wherein the fine particles comprise a complex of a drug with anionic lipid.

13. The method for coating fine particles with lipid membrane according to any one of claims 1 to 7, wherein the fine particles comprise a complex of a drug, liposome containing phospholipid and a dextran sulfate sodium salt.

14. The method for coating fine particles with lipid membrane according to any one of claims 8 to 13, wherein the drug is a drug selected from a peptide, a protein, a nucleic acid, a low-molecular compound, a saccharide and a polymer compound.

15. The method for coating fine particles with lipid membrane according to any one of claims 1 to 14, wherein the polar organic solvent is one or more member(s) selected from an alcohol, a glycol and a polyalkylene glycol.

16. The method for coating fine particles with lipid membrane according to claim 15, wherein the alcohol is ethanol.

17. The method for coating fine particles with lipid membrane according to claim 15 or 16, wherein the glycol is a propylene glycol.

18. The method for coating fine particles with lipid membrane according to any one of claims 15 to 17, wherein the polyalkylene glycol is polyethylene glycol.

19. The method for coating fine particles with lipid membrane according to any one of claims 3 to 18, wherein the water-soluble polymer derivative is one or more member(s) selected from polyethylene glycolated lipid, a polyethylene glycol alkyl ether, a polyethylene glycol castor oil derivative, a polyethylene glycol sorbitan fatty acid ester, a polyethylene glycol stearate, a copolymer of ethylene glycol with propylene glycol and a glycerol ester.

2. A method for coating fine particles with lipid membrane, which comprises coating fine particles with lipid membrane by dispersing fine particles in an aqueous solution containing a polar organic solvent (liquid A), dissolving lipid in a polar organic solvent or an aqueous solution containing a polar organic solvent which is the same as or different from the above aqueous solution containing a polar organic solvent (liquid B), mixing the liquid A and the liquid B into liquid C, and decreasing the rate of a polar organic solvent in the liquid C to obtain liquid D.

3. The method for coating fine particles with lipid membrane according to claim 2, wherein the liquid B is a solution which is prepared by dissolving a water-soluble polymer derivative (I) together with the lipid.

4. The method for coating fine particles with lipid membrane according to claim 2 or 3, wherein the concentrations of the polar organic solvent in the liquid A and the liquid B are 30% or more.

5. The method for coating fine particles with lipid membrane according to claim 2 or 3, wherein the concentrations of the polar organic solvent in the liquid A and the liquid B are 60 to 90%.

6. The method for coating fine particles with lipid membrane according to claim 5, wherein the concentration of the polar organic solvent in the liquid D is 50% or less.