Submicron-liposome containing triterpenoid and a method for preparing the same

• US 20040180082A1
• Filed: 10/02/2003
• Published: 09/16/2004
• Est. Priority Date: 10/09/2002
• Status: Abandoned Application

• Current Assignee: Amorepacific Corporation
• Original Assignee: Amorepacific Corporation
• Inventors: Han, Sang-Hoon, Nam, Gae-Won, Chang, Ih-Seop, Kang, Hyung-seok
• Application Number:
  US10/676,260
• Publication Number:
  US 20040180082A1
• Time in Patent Office: Days
• US Class Current: 424/450
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 9/1277 Processes for preparing; Proliposomes

Abstract

Disclosed herein is submicron-liposome containing highly concentrated triterpenoid prepared by using non-toxic solvent without intense mechanical treatment and a method for preparing the same.

Claims

1. A method for preparing triterpenoid liposome, which comprises the following steps of:

(a) dispersing triterpenoid in a polyol while heating up to 60˜

70°

C. to prepare dispersion;

(b) adding a base into the dispersion of step (a) to prepare low viscosity dispersion;

(c) dissolving phospholipid in ethanol of a room temperature to prepare ethanol solution of phospholipid;

(d) adding the ethanol solution of step (c) into the dispersion of step (b);

(e) adding the mixture of step (d) into distilled water and then emulsifying to prepare emulsion; and

(f) adding an acid to the emulsion of step (e) to prepare submicron-liposome.

2. The method according to claim 1, wherein said polyol of step (a) is selected from the group consisting of pentylene glycol, butylene glycol and propylene glycol.

3. The method according to claim 1, wherein said base of step (b) is selected from the group consisting of triethanolamine, triisopropanolamine, potassium hydroxide, 2-aminobutanol, sodium hydroxide, ammonium hydroxide and calcium hydroxide.

4. The method according to claim 3, wherein said base is the same normality as that of the triterpenoid of step (a) and added in an amount of 0.001˜

0.5% by weight based on the total weight of the liposome.

5. The method according to claim 3, wherein said base is added in an amount to maintain pH of the dispersion of step (b) to a range of 10˜

11.

6. The method according to claim 1, wherein said acid of step (f) is selected from the group consisting of adipic acid, boric acid, citric acid, acetic acid, formic acid, fumaric acid, lactic acid, glycolic acid, succinic acid, propionic acid, pyruvic acid and phosphoric acid.

7. The method according to claim 6, wherein said acid is the same normality as that of the base of step (b).

8. The method according to claim 6, wherein said acid is added in an amount to maintain pH of the liposome of step (f) in a range of 5˜

8.

9. The method according to claim 1, wherein said phospholipid of step (c) has 0˜

3 of double bonds.

10. The method according to claim 1, wherein said phospholipid of step (c) contains 70˜

95 wt % of phosphatidylcholine.

11. Triterpenoid liposome prepared by the method according to any one of claims 1 having triterpenoid loaded therein at a high concentration.

12. Triterpenoid liposome according to claim 11, wherein is the diameter of the liposome is in a range of 0.001˜

10 μ

m.

13. Triterpenoid liposome according to claim 11, wherein said triterpenoid is selected from the group consisting of ursolic acid, oleanolic, centella asiatica extract, betulinic acid, β

-boswellic acid and their admixture.

14. Triterpenoid liposome according to claim 11, wherein the content of said phospholipid in triterpenoid liposome is in a range of 0.001˜

15% by weight based on the total weight of liposome.

15. Triterpenoid liposome according to claim 11, wherein the content of said triterpenoid in triterpenoid liposome is in a range of 0.001˜

5% by weight based on the total weight of liposome.

16. A skin-care composition containing triterpenoid liposome according to claim 11.

17. The skin-care composition according to claim 16, wherein the composition has a formulation of skin softener, toilet water, nutrition toilet water, nutrition cream, massage cream, essence, eye cream, eye essence, cleansing cream, cleansing foam, cleansing water, pack, powder, body lotion, body oil, body essence, make-up base, foundation, hairdyes, shampoo, body cleaner, tooth paste, oral cleaner, patch or sprays.