# US 11,026,902 B2 · Topical composition and delivery system and its use

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- Number: US 11,026,902 B2
- Document ID: US11026902B2
- Status: Granted
- Kind: B2
- Application number: 16/291,221
- Filed: 2019-03-04
- Published: 2019-08-22
- Granted: 2021-06-08
- Earliest claimed: 2012-12-07
- Assignees: Sambria Pharmaceuticals, LLC
- Applicants: Sambria Pharmaceuticals, LLC
- Inventors: Michael Harvey Greenspan
- Web page: https://patentgrep.com/patent/US11026902B2

## CPC

- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- 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 9/127: Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
- A61K 31/08: acyclic, e.g. paraformaldehyde
- A61K 31/10: Sulfides; Sulfoxides; Sulfones
- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- A61K 31/245: Amino benzoic acid types, e.g. procaine, novocaine (salicylic acid esters A61K31/60)
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/08: containing oxygen, {e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61P 23/02: Local anaesthetics
- 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

## Abstract

The described invention provides a topical delivery system comprising a pharmaceutical composition for application directly to a skin of a subject in need thereof comprising (a) an effective therapeutic amount of an active therapeutic agent; (b) chemical drivers comprising an amino benzoate local anesthetic, ethoxydiglycol and methylsulfonylmethane (MSM) that in combination are effective to synergistically deliver the therapeutic agent; and (c) a depot component for keeping the pharmaceutical composition in the skin. Methods for delivering an active therapeutic agent into skin, for keeping it in the skin, for reducing systemic side effects attributable to entry of the active agent into the blood stream, and a method for treating a condition, disease or disorder of skin topically also are described in accordance with the embodiments of the described invention.

## Claims

### Claim 1

A topical delivery system comprising a pharmaceutical composition formulated for application directly to a skin of a subject in need thereof, comprising:
(a) a therapeutic amount of an amino benzoate local anesthetic agent;
(b) chemical drivers comprising ethoxydiglycol, propylene glycol, and methylsulfonylmethane (MSM), wherein the chemical drivers are cooperatively effective to deliver the amino benzoate local anesthetic agent into skin; and
(c) a depot component that is effective to keep the aminobenzoate local anesthetic agent locally in the skin and to reduce distribution of the aminobenzoate local anesthetic agent to the blood stream, wherein the depot component is selected from the group consisting of a liposome, a polymer, a polymersome, and a combination thereof.

### Claim 2 (depends on 1)

The topical delivery system according to claim 1, wherein the amino benzoate local anesthetic agent is selected from the group consisting of benzocaine, lidocaine, tetracaine or a combination thereof.

### Claim 3 (depends on 1)

The topical delivery system according to claim 1, wherein the pharmaceutical composition is in an administration form selected from the group consisting of a cream, a gel, or a spray.

### Claim 4 (depends on 1)

The topical delivery system according to claim 1, further comprising a vasoconstrictor.

### Claim 5 (depends on 4)

The topical delivery system according to claim 4, wherein the vasoconstrictor is nonirritating when applied to skin.

### Claim 6 (depends on 4)

The topical delivery system according to claim 4, wherein the vasoconstrictor is phenylephrine.

### Claim 7 (depends on 1)

The topical delivery system according to claim 1, wherein the liposome comprises a phosphatidyl choline, cholesterol, and at least one anionic or cationic phospholipid.

### Claim 8 (depends on 1)

The topical delivery system according to claim 1, wherein the liposome comprises a pharmaceutically acceptable salt of an active therapeutic agent.

### Claim 9 (depends on 8)

The topical delivery system according to claim 8, wherein the active therapeutic agent is selected from the group consisting of a steroidal analgesic agent, a non-steroidal analgesic agent, a wound healing agent, an anti-inflammatory agent, an antihistamine agent, an anti-neoplastic agent, or a combination thereof.