# US 12,214,071 B2 · Topical composition containing antioxidants

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- Number: US 12,214,071 B2
- Document ID: US12214071B2
- Status: Granted
- Kind: B2
- Application number: 18/371,619
- Filed: 2023-09-22
- Published: 2024-02-29
- Granted: 2025-02-04
- Earliest claimed: 2014-09-17
- Applicants: Alps South Europe
- Inventors: Aldo Laghi; Nathaniel Vint
- Web page: https://patentgrep.com/patent/US12214071B2

## CPC

- 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 8/062: {Oil-in-water emulsions}
- A61K 8/31: Hydrocarbons
- A61K 8/345: {containing more than one hydroxy group}
- A61K 8/361: {Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof}
- A61K 8/37: Esters of carboxylic acids
- A61K 8/375: {the alcohol moiety containing more than one hydroxy group}
- A61K 8/4946: {Imidazoles or their condensed derivatives, e.g. benzimidazoles}
- A61K 8/678: {Tocopherol, i.e. vitamin E}
- A61K 8/922: {of vegetable origin}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 31/235: having an aromatic ring attached to a carboxyl group
- A61K 31/355: Tocopherols, e.g. vitamin E
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/18: Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- 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)
- A61Q 19/00: Preparations for care of the skin
- A61K 2800/522: Antioxidants; Radical scavengers
- A61K 2800/524: Preservatives
- 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)
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

Compositions for topical application that effectively deliver antioxidants across the epidermis, dermis, or a combination thereof into cells and/or the bloodstream while concurrently maintaining chemical activity of the antioxidants. In certain aspects, these formulations include emulsions and balms each having a lipophilic carrier and a lipophilic antioxidant solubilized by the lipophilic carrier. Also disclosed herein are methods for making these compositions for topical application.

## Claims

### Claim 1

A topical composition comprising:
30-75 percent by weight water;
3-6 percent by weight surfactant;
1-50 percent by weight lipophilic carrier having a molecular weight between 150 and 600;
0.25-4 percent by weight lipophilic antioxidant having a formula:
wherein:
R1 represents a C1 to C9 linear or branched alkyl group or styrene;
R2 is optional and represents a C1 to C6 linear or branched alkyl group or styrene;
Y1 represents a C1 to C6 linear or branched alkyl group, styrene, —SR5, or —(CH2)nCOOR6;
n is from 1 to 10;
R5 represents isoprene, a methyl group, an ethyl group, a propyl, a butyl, a pentyl group, a hexyl group, an isopropyl group, an isobutyl group, a sec-butyl group, a tert-butyl group, a tert-pentyl group, a neo-pentyl group, an isopentyl group, an isohexyl group, a neohexyl group, styrene, or
wherein R11, R12, and R13 independently represent OH, a methyl group, ethyl group, a propyl group, a butyl group, an isopropyl group, a tert-butyl group, an isoprene, or a tert-pentyl group;
R6 represents an alkyl group having C10 to C30;
and
wherein the formula includes pharmaceutically acceptable salts thereof;
1-10 percent by weight skin penetration enhancer;
9-11 percent by weight paraffinic oil; and
0.5-5 percent by weight of a preservative mixture comprising propylene glycol, diazolidinyl urea, methylparaben, and propylparaben and tetrasodium ethylenediaminetetraacetic acid;
wherein once the topical composition is compounded, the topical composition is a cream emulsion.

### Claim 2

A topical composition comprising:
30-75 percent by weight water;
3-6 percent by weight surfactant;
1-50 percent by weight lipophilic carrier having a molecular weight between 150 and 600;
0.25-4 percent by weight lipophilic antioxidant having a formula:
wherein:
R3 and R4 independently represent a C1 to C6 branched alkyl;
Y2 represents a C1 to C6 linear or branched alkyl group, —R5, or —(CH2)nCOOR6;
R5 represents isoprene, a methyl group, an ethyl group, a propyl, a butyl, a pentyl group, a hexyl group, an isopropyl group, an isobutyl group, a sec-butyl group, a tert-butyl group, a tert-pentyl group, a neo-pentyl group, an isopentyl group, an isohexyl group, a neohexyl group, styrene, or
wherein R11, R12, and R13 independently represent OH, a methyl group, ethyl group, a propyl group, a butyl group, an isopropyl group, a tert-butyl group, an isoprene, or a tert-pentyl group, and
R6 represents an alkyl group having C10 to C30;
n is from 1 to 10;
and
wherein the formula includes pharmaceutically acceptable salts thereof;
1-10 percent by weight skin penetration enhancer;
9-11 percent by weight paraffinic oil; and
0.5-5 percent by weight of a preservative mixture comprising propylene glycol, diazolidinyl urea, methylparaben, and propylparaben and tetrasodium ethylenediaminetetraacetic acid;
wherein once the topical composition is compounded, the topical composition is a cream emulsion.

### Claim 3

A topical composition comprising:
30-75 percent by weight water;
3-6 percent by weight surfactant;
1-50 percent by weight lipophilic carrier having a molecular weight between 150 and 600;
0.25-4 percent by weight lipophilic antioxidant having a formula:
wherein:
R3 and R4 independently represent a C1 to C6 branched alkyl;
Y3 represents a linear or branched alkyl group having C10 to C30;
and
wherein the formula includes pharmaceutically acceptable salts thereof;
1-10 percent by weight skin penetration enhancer;
9-11 percent by weight paraffinic oil; and
0.5-5 percent by weight of a preservative mixture comprising propylene glycol, diazolidinyl urea, methylparaben, and propylparaben and tetrasodium ethylenediaminetetraacetic acid;
wherein once the topical composition is compounded, the topical composition is a cream emulsion.