Ophthalmic formulation comprising citicoline carried by liposome for the treatment of glaucoma

• US 10,576,039 B2
• Filed: 10/16/2017
• Issued: 03/03/2020
• Est. Priority Date: 10/17/2016
• Status: Active Grant

• Current Assignee: Omikron Italia Srl
• Original Assignee: Omikron Italia Srl
• Inventors: Virno, Cristiano, Malizia, Marco
• Primary Examiner(s): Holloman, Nannette
• Application Number:
  US16/342,261
• Publication Number:
  US 20190321292A1
• Time in Patent Office: 869 Days
• Field of Search: None
• CPC Class Codes: A61K 31/7068 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics

Abstract

The present invention relates to an ophthalmic formulation comprising citicoline and liposomes to be used in treating glaucoma. The inventors have found that the liposomes result to be particularly effective in carrying citicoline in the posterior segment of the eye (vitreous chamber) and in reaching the retina and the optic nerve head.

Claims

1. A composition for ophthalmic use comprising liposomes that include citicoline or salts thereof.

2. The composition according to claim 1 wherein said liposomes comprise a double layer of phospholipids and an aqueous core.

3. The composition according to claim 1 wherein said liposomes are composed of hydrogenated phospholipids.

4. The composition according to claim 1 further comprising hyaluronic acid and/or stearylamine.

5. The composition according to claim 1 wherein said citicoline has a concentration between 0.5 and 3% by weight.

6. The composition according to claim 1 which is a solution, ointment, suspension, eye drops, gel, cream, foam, spray, or ointment.

7. The composition according to claim 1 which has a pH between 7 and 7.4 and an osmolarity between 280 and 300 mOsml/kg.

8. The composition according to claim 1 wherein said liposomes have a size between 25 nm and 1 μ

m.

9. The composition according to claim 1 further comprising one or more active agents for topical use in treating glaucoma.

10. The composition according to claim 1 wherein the composition does not comprise benzalchonium chloride (BAK).

20. The composition for use according to claim 9 wherein said agents are topical anti-hypertensive drugs.

21. A method of treating glaucoma in a subject in need thereof comprising topically administering a pharmaceutically effective amount of the composition of claim 1 to said subject.

11. A composition for ophthalmic use comprising liposomes, hyaluronic acid, and/or stearylamine, wherein the liposomes include citicoline or salts thereof.

12. The composition according to claim 11 wherein said liposomes comprise a double layer of phospholipids and an aqueous core.

13. The composition according to claim 11 wherein said liposomes consist of hydrogenated phospholipids.

14. The composition according to claim 11 wherein the composition does not contain benzalchonium chloride (BAK).

15. The composition according to claim 11 wherein said citicoline has a concentration between 0.5 and 3% by weight.

16. The composition according to claim 11 which is a solution, ointment, suspension, eye drops, gel, cream, foam, spray, or ointment.

17. The composition according to claim 11 which has a pH between 7 and 7.4 and an osmolarity between 280 and 300 mOsml/kg.

18. The composition according to claim 11 wherein said liposomes have a size between 25 nm and 1 μ

m.

19. The composition according to claim 11 further comprising one or more active agents for topical use in treating glaucoma.