# US 12,213,963 B2 · Topical formulation of disease-modifying antirheumatic drug (DMARDs) for the treatment of rheumatoid arthritis, melanoma, squamous cell carcinoma, atopic dermatitis, and psoriasis

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- Number: US 12,213,963 B2
- Document ID: US12213963B2
- Status: Granted
- Kind: B2
- Application number: 18/047,707
- Filed: 2022-10-19
- Published: 2024-04-25
- Granted: 2025-02-04
- Earliest claimed: 2022-10-19
- Assignees: Manoj Jadhav
- Applicants: Manoj Purushottam Jadhav
- Inventors: Manoj Purushottam Jadhav; Mangal Shailesh Nagarsenkar; Supriya Shrihari Shidhaye; Shivali Hargovind Tank; Bhagyashri Surendra Parab; Pradnya Nikhil Korlekar; Anita Pandurang Ayre; Palak Karia
- Web page: https://patentgrep.com/patent/US12213963B2

## CPC

- A61K 31/42: Oxazoles
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 31/277: having a ring, e.g. verapamil
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- 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)
- 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)

## Abstract

The present invention relates to a composition of disease-modifying antirheumatic drugs (DMARDs) for treatment of auto-immune diseases. More particularly, the invention relates to the microemulsion based emulgel composition of DMARD-leflunomide or its derivatives for treatment of auto-immune diseases such as rheumatoid arthritis, atopic dermatitis, psoriasis and skin cancer such as melanoma, squamous cell carcinoma. The invention also discloses a method for preparation of microemulsion based emulgel composition with improved physicochemical, pharmacokinetic properties of leflunomide to be used in pharmaceutical compositions. This invention discloses the delivery of leflunomide across human skin for the treatment of autoimmune and oncological conditions. The unique delivery of leflunomide in the form of microemulsion based emulgel composition is disclosed.

## Claims

### Claim 1

A topical microemulsion-based emulgel composition comprising:
a. 0.5-1.0 (% w/v) leflunomide;
b. 5 (% w/v) propylene glycol monocaprylate;
c. 3.75 (% w/v) polysorbate 20;
d. 3.75 (% w/v) polyoxyl 40 hydrogenated castor oil;
e. 7.5 (% w/v) polyethylene glycol 400;
f. 2.5 (% w/v) carbomer; and
g. q.s. water.

### Claim 2 (depends on 1)

The topical microemulsion-based emulgel composition of claim 1, wherein the composition consists of:
a. 1.0 (% w/v) leflunomide;
b. 5 (% w/v) propylene glycol monocaprylate;
c. 3.75 (% w/v) polysorbate 20;
d. 3.75 (% w/v) polyoxyl 40 hydrogenated castor oil;
e. 7.5 (% w/v) polyethylene glycol 400;
f. 2.5 (% w/v) carbomer; and
g. q.s. water.

### Claim 3

A topical microemulsion-based emulgel composition comprising:
a. 0.5-1.0 (% w/v) leflunomide;
b. 5 (% w/v) propylene glycol dilaurate;
c. 3.75 (% w/v) polysorbate 20;
d. 3.75 (% w/v) polyoxyl 40 hydrogenated castor oil;
e. 7.5 (% w/v) polyethylene glycol 400;
f. 2.5 (% w/v) carbomer; and
g. q.s. water.

### Claim 4 (depends on 3)

The topical microemulsion-based emulgel composition of claim 3, wherein the composition consists of:
a. 1.0 (% w/v) leflunomide;
b. 5 (% w/v) propylene glycol dilaurate;
c. 3.75 (% w/v) polysorbate 20;
d. 3.75 (% w/v) polyoxyl 40 hydrogenated castor oil;
e. 7.5 (% w/v) polyethylene glycol 400;
f. 2.5 (% w/v) carbomer; and
g. q.s. water.