Fine particles coated with lipid membrane

• US 9,757,344 B2
• Filed: 02/01/2010
• Issued: 09/12/2017
• Est. Priority Date: 10/04/2000
• Status: Expired due to Fees

• Current Assignee: Kyowa Hakko Kirin Company Limited (Kirin Holdings Company Limited)
• Original Assignee: Kyowa Hakko Kirin Company Limited (Kirin Holdings Company Limited)
• Inventors: Kato, Yasuki, Yamauchi, Masahiro, Kusano, Hiroko, Iwata, Takeshi, Uochi, Takaaki, Akinaga, Shiro
• Primary Examiner(s): Le, Holly
• Application Number:
  US12/656,487
• Publication Number:
  US 20100166847A1
• Time in Patent Office: 2,780 Days
• Field of Search: 436 13, 436 86, 424474, 424475, 424477, 424490, 424491, 424498, 428403, 428407
• 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

A coated fine particle comprisisng: (i) a complex of a drug and a cationic lipid, wherein (a) the drug is a nucleic acid and the complex is obtained by mixing the drug and the cationic lipid in water, wherein the complex has a diameter of 10 nm to 1,000 nm, and (ii) a lipid layer 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 lipid layer.

Claims

1. A coated fine particle comprising:

(i) a complex containing a drug, a cationic lipid, and a water-soluble polymer derivative,

wherein the drug is a nucleic acid and the complex is obtained by mixing the drug ,the water-soluble polymer derivative, and the cationic lipid in water,

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

wherein the water-soluble polymer derivative is one or more member(s) selected from a copolymer of ethylene glycol with propylene glycol, and a glycerol ester, and

(ii) a lipid membrane formed of lipid(s),

wherein the lipid(s) is selected from phosphatidylserine, phosphatidylglycerol, lysophosphatidylcholine, polyethylene glycolated phospholipid, egg yolk lecithin, soybean lecithin and hydrogenated phospholipid, and

wherein the complex is coated with the lipid membrane.