Liposomal lupeol acetate and the use thereof in preparing drugs for rheumatoid arthritis

• US 10,441,540 B2
• Filed: 11/07/2014
• Issued: 10/15/2019
• Est. Priority Date: 03/14/2014
• Status: Active Grant

• Current Assignee: National Yang-Ming University
• Original Assignee: National Yang-Ming University
• Inventors: Hwang, Jeng-Jong, Wang, Wei-Hsun
• Primary Examiner(s): Kishore, Gollamudi S
• Application Number:
  US14/536,336
• Publication Number:
  US 20150258025A1
• Time in Patent Office: 1,803 Days
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 19/10 for osteoporosis

Abstract

The present invention relates to a liposomal lupeol acetate (Lipo-LA) and its use in the treatment or prevention of rheumatoid arthritis (RA). The liposomal lupeol acetate of the present invention especially inhibits inflammatory responses and osteoclast generation (osteoclastogenesis) in the progression of rheumatoid arthritis (RA) at a half dose of the un-capsulated lupeol acetate, which may significantly reduce the incidence of RA and improve the therapeutic efficacy of lupeol acetate.

Claims

1. A pharmaceutical composition comprising:

a liposomal lupeol acetate for use of inhibiting osteoclastogenesis;

wherein the liposomal lupeol acetate consists of;

lupeol acetate;

an aqueous core; and

a lipid bilayer having an inner space in which the lupeol acetate is located is constructed by a phosphatidylcholine (PC) and polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE) and wherein the molecular ratio of the phosphatidylcholine and polyethylene glycol-distearoylphosphatidylethanolamine is 20;

1 to 35;

1.

2. The pharmaceutical composition of claim 1, wherein the phosphatidylcholine comprises egg phosphatidylcholine (EPC).

3. The pharmaceutical composition of claim 1, wherein the molecular ratio of the phosphatidylcholine (PC) and polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE) in the lipid bilayer is 30:

1.

4. The pharmaceutical composition of claim 1, further comprising a steroid anti-inflammatory agent.

5. The pharmaceutical composition of claim 4, wherein the liposomal lupeol acetate is used to reduce osteoporosis caused by the steroid anti-inflammatory agent.