Topical formulations and uses thereof

• US 9,937,225 B2
• Filed: 05/12/2016
• Issued: 04/10/2018
• Est. Priority Date: 08/24/2012
• Status: Active Grant

• Current Assignee: Sun Pharmaceutical Industries Limited
• Original Assignee: Sun Pharma Global Fze (Sun Pharmaceutical Industries Limited)
• Inventors: Mitra, Ashim K., Weiss, Sidney L.
• Primary Examiner(s): Bradley, Christina
• Application Number:
  US15/153,510
• Publication Number:
  US 20160256520A1
• Time in Patent Office: 698 Days
• CPC Class Codes: A61K 31/202 having three or more double bonds, e.g. linolenic eicosanoids, e.g. leukotrienes A61K31/557
• CPC Class Codes: A61K 38/13 Cyclosporins
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Provided herein include formulations for topical administration, such as ophthalmic formulations, and methods of using such formulations. In some aspects and embodiments the formulations may include a polyoxyl lipid or fatty acid, and or a polyalkoxylated alcohol and may include nanomicelles. Also include methods of treating or preventing diseases or conditions, such as ocular diseases or conditions.

Claims

1. An aqueous clear nanomicellar ophthalmic formulation comprising 0.05-0.5% by weight cyclosporine, a polyalkoxylated alcohol and one or more polymers comprising HCO-40, HCO-60, HCO-80, HCO-100, polyoxyl 35 castor oil or combinations thereof.

2. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polymer comprises HCO-40, HCO-60, HCO-80, HCO-100 or combinations thereof.

3. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polymer comprises polyoxyl 35 castor oil.

4. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polymer is HCO-40.

5. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polymer is 0.5-1.5% by weight of the formulation.

6. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polymer comprises HCO-40 HCO-60, HCO-80, or combinations thereof and is 0.5-1.5% by weight of the formulation.

7. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polyalkoxylated alcohol comprises Octoxynol-40.

8. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein the polyalkoxylated alcohol comprises Octoxynol-40 and is 0.02-4% by weight of the formulation.

9. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein the polyalkoxylated alcohol comprises Octoxynol-40 and is 0.02-0.1% by weight of the formulation.

10. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein the cyclosporine is 0.05-0.2% by weight of the formulation.

11. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polymer comprises HCO-40, HCO-60, HCO-80, HCO-100 or combinations thereof;

and wherein said polyalkoxylated alcohol is Octoxynol-40.

12. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polymer is 0.5-1.5% by weight of the formulation;

and said polyalkoxylated alcohol is Octoxynol-40 and is 0.02-0.1% of the formulation.

13. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said polymer is 0.5-1.5% of the formulation;

said polyalkoxylated alcohol comprises Octoxynol-40 and is 0.02-0.1% of the formulation; and

the cyclosporine is 0.05-0.2% of the formulation.

14. A method of treating or preventing an ocular disease or condition, said method comprising topically administering an aqueous clear nanomicellar formulation of claim 1.

15. A method of treating or preventing an ocular disease or condition, said method comprising topically administering an aqueous clear nanomicellar formulation of claim 13.

16. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said formulation provides higher average concentration of cyclosporine in cornea, conjunctiva and sclera in comparison to higher marketed strength.

17. The aqueous clear nanomicellar ophthalmic formulation of claim 1, wherein said formulation demonstrates mean cumulative inflammatory score of less than 2.