# US 10,869,822 B2 · Compositions for treatment of dermatological diseases and conditions and methods of use thereof

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- Number: US 10,869,822 B2
- Document ID: US10869822B2
- Status: Granted
- Kind: B2
- Application number: 15/962,436
- Filed: 2018-04-25
- Published: 2018-08-23
- Granted: 2020-12-22
- Earliest claimed: 2007-10-10
- Assignees: DermaMedics, LLC
- Applicants: DermaMedics, LLC
- Inventors: Bryan B. Fuller
- Web page: https://patentgrep.com/patent/US10869822B2

## CPC

- A61K 8/37: Esters of carboxylic acids
- A61K 8/25: Silicon; Compounds thereof
- A61K 8/33: containing oxygen
- A61K 8/34: Alcohols
- A61K 8/347: {Phenols}
- A61K 8/35: Ketones, e.g. benzophenone
- A61K 8/368: with carboxyl groups directly bound to carbon atoms of aromatic rings
- 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 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 9/2063: {Proteins, e.g. gelatin}
- A61K 31/085: having an ether linkage to aromatic ring nuclear carbon
- A61K 31/11: Aldehydes
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 31/222: with compounds having aromatic groups, e.g. dipivefrine, ibopamine
- A61K 31/60: Salicylic acid; Derivatives thereof
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/06: Antipsoriatics
- A61P 17/10: Anti-acne agents
- A61Q 19/02: for chemically bleaching or whitening the skin
- A61Q 19/08: Anti-ageing preparations
- 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
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

Compositions containing an effective dermatological disease-treating or dermatological condition-treating active agent and a pharmaceutically-acceptable carrier or vehicle are disclosed. Methods of using the compositions are also disclosed.

## Claims

### Claim 1

A transdermal composition for topical administration to a subject having a dermatological disease or dermatological condition, comprising:
an effective dermatological disease-treating or dermatological condition-treating amount of an active agent comprising soluble ethyl vanillin and/or a salt thereof, wherein the soluble ethyl vanillin retains its stability in the transdermal composition for at least 3 months, and wherein the soluble ethyl vanillin and/or a salt thereof is formed by dissolving solid ethyl vanillin and/or a salt thereof in non-aqueous solvent; and
a pharmaceutically-acceptable carrier or vehicle effective in carrying or enabling passage of the active agent into the epidermis or dermis of the skin of the subject where the active agent has its effect on the dermatological disease or dermatological condition; and
wherein the transdermal composition is non-aqueous and is absent emulsifiers.

### Claim 2 (depends on 1)

The transdermal composition of claim 1, wherein the transdermal composition inhibits production of at least one matrix metalloproteinase (MMP) in the treated skin.

### Claim 3 (depends on 1)

The transdermal composition of claim 1, wherein the transdermal composition reduces MMP-9 levels in the treated skin.

### Claim 4 (depends on 1)

The transdermal composition of claim 1, wherein the active agent further comprises at least one of:
(a) dihydroeugenol and/or a salt thereof and/or an ester thereof; and
(b) isoeugenol and/or a salt thereof and/or an ester thereof.

### Claim 5 (depends on 1)

The transdermal composition of claim 1, wherein the pharmaceutically-acceptable carrier or vehicle comprises at least one of a penetration enhancer and a silicone.

### Claim 6 (depends on 5)

The transdermal composition of claim 5, wherein the pharmaceutically-acceptable carrier or vehicle primarily comprises 20% to 90% by weight of a silicone.

### Claim 7 (depends on 1)

The transdermal composition of claim 1, further comprising at least one of cinnamaldehyde and salicylic acid.

### Claim 8 (depends on 1)

The transdermal composition of claim 1, further defined as being effective in percutaneous transmission such that the active agent can be maintained in the epidermis or dermis in the treated skin at a concentration in a range of from 1 μM to 1000 μM.

### Claim 9 (depends on 1)

The transdermal composition of claim 1, wherein the active agent composition stimulates dermal production of at least one of collagen, elastin, tissue inhibitors of metalloproteinases (TIMPs), and Hyaluronic Acid Synthase-2 (HAS-2) in the treated skin.

### Claim 10

A method of inhibiting production of at least one matrix metalloproteinase (MMP) in a subject's skin, the method comprising:
topically administering an effective amount of a transdermal composition to a portion of the subject's skin, wherein the transdermal composition comprises:
an active agent comprising at least one of soluble ethyl vanillin and a salt thereof, wherein the at least one of soluble ethyl vanillin a salt thereof is formed by dissolving at least one of solid ethyl vanillin and a salt thereof in non-aqueous solvent; and
a pharmaceutically-acceptable carrier or vehicle effective in carrying or enabling passage of the active agent into the epidermis or dermis of the skin of the subject where the active agent has its effect on the at least on MMP; and
wherein the transdermal composition is non-aqueous and is absent emulsifiers.

### Claim 11 (depends on 10)

The method of claim 10, wherein the transdermal composition reduces MMP-9 levels in the treated skin.

### Claim 12

A method of treating a dermatological condition in a subject's skin, the method comprising:
topically administering an effective amount of a transdermal composition to a portion of the subject's skin which is affected by a dermatological condition, wherein the transdermal composition comprises:
an active agent comprising at least one of soluble ethyl vanillin and a salt thereof, wherein the at least one of soluble ethyl vanillin and a salt thereof is formed by dissolving at least one of solid ethyl vanillin and a salt thereof in non-aqueous solvent; and
a pharmaceutically-acceptable carrier or vehicle effective in carrying or enabling passage of the active agent into the epidermis or dermis of the skin of the subject where the active agent has its effect on the at least one dermatological condition; and
wherein the transdermal composition is non-aqueous and is absent emulsifiers; and
wherein the dermatological condition is selected from the group consisting of inflammation, rosacea, allergic contact dermatitis, irritant contact dermatitis, seborrheic dermatitis, radiation dermatitis, erythema, psoriasis, atopic dermatitis, eczemas, actinic keratosis, acne, scarring, aging, and alopecia areata.

### Claim 13 (depends on 12)

The method of claim 12, wherein the at least one of the soluble ethyl vanillin and the salt thereof retains its stability in the transdermal composition for at least 3 months.

### Claim 14 (depends on 12)

The method of claim 12, wherein the active agent further comprises at least one of:
(a) dihydroeugenol and/or a salt thereof and/or an ester thereof; and
(b) isoeugenol and/or a salt thereof and/or an ester thereof.

### Claim 15 (depends on 14)

The method of claim 14, wherein the ester of isoeugenol comprises isoeugenyl acetate.

### Claim 16 (depends on 12)

The method of claim 12, wherein the transdermal composition further comprises at least one of cinnamaldehyde and salicyclic acid.

### Claim 17 (depends on 12)

The method of claim 12, wherein the pharmaceutically-acceptable carrier or vehicle of the transdermal composition comprises at least one of a penetration enhancer and a silicone.

### Claim 18 (depends on 12)

The method of claim 12, wherein the active agent is maintained in the epidermis or dermis of the treated skin at a concentration in a range from 1 μM to 1000 μM.

### Claim 19 (depends on 12)

The method of claim 12, wherein the transdermal composition stimulates dermal production of at least one of collagen, elastin, tissue inhibitors of metalloproteinases (TIMPs), and Hyaluronic Acid Synthase-2 (HAS-2) in the treated skin.

### Claim 20 (depends on 12)

The method of claim 12, wherein the transdermal composition inhibits production of at least one matrix metalloproteinase (MMP) in the treated skin.
