Method for coating fine particles with lipid membrane

• US 20100166847A1
• Filed: 02/01/2010
• Published: 07/01/2010
• Est. Priority Date: 10/04/2000
• Status: Active Grant

• Current Assignee: Hiroko Kusano, Masahiro Yamauchi, Shiro Akinaga, Takaaki Uochi, Takeshi Iwata, Yasuki Kato
• Original Assignee: Hiroko Kusano, Masahiro Yamauchi, Shiro Akinaga, Takaaki Uochi, Takeshi Iwata, Yasuki Kato
• Inventors: Kusano, Hiroko, Yamauchi, Masahiro, Kato, Yasuki, Iwata, Takeshi, Akinaga, Shiro, Uochi, Takaaki
• Granted Patent: US 9,757,344 B2
• Time in Patent Office: Days
• US Class Current: 514/1.100
• 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

1-19. -19. (canceled)

20. A coated fine particle comprising:

(i) a complex of a drug selected from a peptide, a protein and a nucleic acid and a liposome,

wherein (a) the drug is selected from an acidic peptide, an acidic protein, and a nucleic acid, the liposome comprises cationic lipid, and the complex is obtained by mixing the drug and the liposome in water, or (b) the drug is selected from a basic peptide and a basic protein, and the liposome comprises anionic lipid, and the complex is obtained by mixing the drug and the liposome in water,

wherein the complex has a diameter of 10 nm to 1,000 nm, and

(ii) closed vesicles of a lipid bilayer formed of lipid(s),

wherein the lipid(s) is selected from phospholipid, glyceroglycolipid, sphingoglycolipid, cholesterol and synthetic lipid,

wherein the complex is coated with the closed vesicles of the lipid bilayer.

21. The coated fine particle according to claim 20, wherein the complex contains a water-soluble polymer derivative.

22. The coated fine particle according to claim 20, wherein the liposome comprises a phospholipid and a dextran sulfate sodium salt.

23. The coated fine particle according to claim 21, wherein the water-soluble polymer derivative is one or more member(s) selected from a 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.

24. The coated fine particle according to claim 20, wherein the lipid(s) is one or more member(s) selected from phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidic acid, phosphatidylglycerol, phosphatidylinositol, lysophosphatidylcholine, sphingomyelin, polyethylene glycolated phospholipid, egg yolk lecithin, soybean lecithin and hydrogenated phospholipid.

25. The coated fine particle according to claim 20, wherein the lipid(s) is a mixture of egg yolk phosphatidylcholine (EggPC) and 1,2-distearoyl-sn-glycero-3-phosphatidylethanolamine-N-(polyethyleneglycol 2000) (PEG-DSPE).