# US 10,441,540 B2 · Liposomal lupeol acetate and the use thereof in preparing drugs for rheumatoid arthritis

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- Number: US 10,441,540 B2
- Document ID: US10441540B2
- Status: Granted
- Kind: B2
- Application number: 14/536,336
- Filed: 2014-11-07
- Published: 2015-09-17
- Granted: 2019-10-15
- Earliest claimed: 2014-03-14
- Assignees: National Yang-Ming University
- Applicants: National Yang-Ming University
- Inventors: Jeng-Jong Hwang; Wei-Hsun Wang
- Web page: https://patentgrep.com/patent/US10441540B2

## CPC

- A61K 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/10: for osteoporosis
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 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.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 1)

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.

### Claim 4 (depends on 1)

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

### Claim 5 (depends on 4)

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