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WO2025021582A1 - Composition topique à effets cutanés améliorés - Google Patents

Composition topique à effets cutanés améliorés Download PDF

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Publication number
WO2025021582A1
WO2025021582A1 PCT/EP2024/070078 EP2024070078W WO2025021582A1 WO 2025021582 A1 WO2025021582 A1 WO 2025021582A1 EP 2024070078 W EP2024070078 W EP 2024070078W WO 2025021582 A1 WO2025021582 A1 WO 2025021582A1
Authority
WO
WIPO (PCT)
Prior art keywords
composition
polyglyceryl
weight
skin
acid
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
PCT/EP2024/070078
Other languages
English (en)
Inventor
Hui-Ing Donna Hwang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beiersdorf AG
Original Assignee
Beiersdorf AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Beiersdorf AG filed Critical Beiersdorf AG
Publication of WO2025021582A1 publication Critical patent/WO2025021582A1/fr
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/06—Emulsions
    • A61K8/062—Oil-in-water emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/044—Suspensions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/11—Encapsulated compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/14—Liposomes; Vesicles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/25—Silicon; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/41—Particular ingredients further characterized by their size

Definitions

  • the present invention relates to a topical, particularly cosmetic composition which comprises a specific combination of active ingredients and lipid particles.
  • Lipid nanoparticles are a colloidal carrier system and have been investigated for providing better chemical protection of a lipophilic cosmetic active or active pharmaceutical ingredient (API), greater control over its release, and better physical stability since the early 1990s.
  • API lipophilic cosmetic active or active pharmaceutical ingredient
  • Solid lipid nanoparticles are introduced as the new generation of carriers for cosmetics, especially UV blockers for use on human skin and/or hair, and the production thereof is described.
  • EP 2099420 Al discloses cosmetic preparations for topical application containing nanocrystals of cosmetic actives, which result in an increased bioactivity of molecules in the skin, and methods of making the cosmetic preparations.
  • the nanocrystals can be added to any cosmetic topical formulation, e.g., creams, lotions and liposomal dispersions.
  • the drug nanocrystals are produced by a combination process of low energy pearl milling followed by a high energy high-pressure homogenization leading to nanocrystal suspensions (nanosuspensions) of improved physical stability.
  • lipid nanoparticle technology The known characteristics of lipid nanoparticle technology are the ability to enhance the photo stability of photolabile UV absorbers, to sustain the release of UV actives over time, and to reduce skin irritation caused by the actives.
  • the lipid nanoparticle technology is focused on entrapping the actives to have the maximum entrapment efficiency in the final products.
  • the ratio of lipids and active as well as the selected types of lipids and oils are important factors which determine the success of the encapsulation. These factors limit the amounts of UV actives used for the entrapment and thus, limit the photoprotection. Therefore, the sun protection factor (SPF) achievable by this technology is only up to about 30.
  • Lipid nanoparticles for use in this invention are preferably compatible with UV filters and capable of scattering and/or reflecting UV rays in synergism with the UV filters.
  • the lipids are preferably selected from natural and synthetic lipids such as vegetable oils, hydrogenated vegetable oils, squalene, monoglycerides, diglycerides, triglycerides, tristearin, fatty acids, fatty alcohols, ethers, esters, butters, and waxes.
  • natural and synthetic lipids such as vegetable oils, hydrogenated vegetable oils, squalene, monoglycerides, diglycerides, triglycerides, tristearin, fatty acids, fatty alcohols, ethers, esters, butters, and waxes.
  • the lipids are preferably selected from rice brain oil, glyceryl monostearate, glyceryl distearate, glyceryl behenate, lauryl laurate, polyhydroxy stearic acid, cetyl palmitate, cetearyl alcohol, hydrogenated castor oil, jojoba butter, beeswax, candelilla wax, bayberry wax, rice bran wax, carnauba wax, sunflower wax, microcrystalline wax, and combinations thereof.
  • the composition of the invention preferably comprises one or more O/W emulsifiers.
  • suitable OAV emulsifiers include hydrogenated phosphatidylcholine, polysorbate 60, polyglyceryl esters, polyglyceryl-4 laurate, poly glyceryl- 6 laurate, poly glyceryl- 6 oleate, polyglyceryl-4 stearate, polyglyceryl-10 stearate, polyglyceryl-3 methyl glucose distearate, polyglyceryl-6 stearate, poly glyceryl- 6 behenate, polyglyceryl-3 distearate, and polyglyceryl-6 distearate.
  • Preferred emulsifiers include polyglyceryl esters, in particular polyglyceryl-3 distearate and/or polyglyceryl-3 methylglucose distearate.
  • emulsifiers with good biocompatibility and biodegradability.
  • the skin adhesion enhancers are preferably selected from fumed silica, hydrophobic modified fumed silica, hydrated silicate, amorphous silica, crystalline silica, magnesium aluminum silicates, aluminosilicates, hectorite, bentonite, laponite, clays, smectite clays, kaolinite, montmorillonite, and combinations thereof.
  • composition of the invention comprises one or more active ingredients, especially cosmetic active ingredients.
  • active ingredients are preferably selected from light protection filters, moisturizers, active skin care ingredients such as, e.g., hyaluronic acid, niacinamide, ceramides, retinol, AHAs, BHAs, vitamins A, C and E, and peptides.
  • Non-limiting examples of these skin actives can be lipophilic and/or hydrophilic actives which include, e.g., Thiamidol® (A-[4-(2,4-Dihydroxyphenyl)-l,3-thiazol-2-yl]-2- methylpropanamid), coenzyme Q10, albumin, peptides, hyaluronic acid, retinol (vitamin A), niacinamide, bakuchiol, salicylic acid, and glycolic acid.
  • Thiamidol® A-[4-(2,4-Dihydroxyphenyl)-l,3-thiazol-2-yl]-2- methylpropanamid
  • coenzyme Q10 coenzyme Q10
  • albumin e.g., albumin, peptides, hyaluronic acid, retinol (vitamin A), niacinamide, bakuchiol, salicylic acid, and glycolic acid.
  • Light protection filters as actives in the composition of this invention are preferably selected from homosalate, ethylhexyl salicylate, octocrylene, avobenzone, ethylhexyl triazone, bisethylhexyloxyphenol methoxyphenyl triazine, phenylbenzimidazolesulfonic acid, diethylamino hydroxybenzoyl hexyl benzoate, benzophenone, camphor derivatives, and ethylhexyl methoxycinnamate, as well as physical sunscreens, especially zinc oxide and titanium dioxide.
  • the concentration of the one or more active ingredients is advantageously in the range from about 0.1 % to about 85 % by weight, preferably from about 2 % to about 50 % by weight, more preferably from about 5 % to about 30 % by weight, based on the total weight of the composition.
  • composition according to the invention preferably comprises one or more natural or synthetic antioxidants.
  • the natural or synthetic antioxidants can be included in this composition to maintain and/or increase the efficacy of the photoprotection.
  • Antioxidants preferably used in this invention are capable of interacting with and/or neutralizing free radicals, thus minimizing UV-induced oxidative damage and mitigating skin photoaging.
  • Natural antioxidants included in this invention can be selected from plant sources, microalgae, vegetables.
  • Non-limiting examples of skin actives for use in the composition of this invention include free-radical scavengers, antioxidants, anti-irritants and anti-inflammatory agents, including tocopherol (vitamin E), ascorbic acid (vitamin C), sodium ascorbyl phosphate, ascorbyl palmitate, beta-carotene, glycyrrhetinic acid, Glycyrrhiza Inflata root extract, liccochalcone, especially, liccochalcone A, bisabolol, allantoin, black currant seed oil, rice bran oil, rice germ oil, soybean oil, phytosterol, oryzanol, ferulic acid, ricetrienol, and diethylhexyl syringylidenemalonate.
  • the composition of the invention can be used in various application forms.
  • Examples of application forms include cream, lotion, stick, roll-on, ointment, butter, paste, pump spray, aerosol spray and, not limiting, a gel, preferably cream and lotion.
  • the preparation of the invention can be used for improving the effectiveness of active substances in cosmetic treatment processes, especially for improving the photoprotective effect in comparison to a sun protection composition that comprises the same amount of sun protective active ingredients.
  • composition of the invention may also be used for an improved release of active substances onto or into the skin.
  • an equally effective skin improvement can be achieved with the same amount of active ingredient, i.e., compared to a composition without the inventive combination, and with the same UV filter content an increased SPF is achievable.
  • This also means that the same SPF can be obtained with a lower amount of UV filter. In other words, the amount of UV filter can thus be reduced and the same light protection can still be achieved.
  • a high-pressure homogenization (HPH) of an O/W emulsion alone does not result in improved product performance.
  • HPH high-pressure homogenization
  • compositions which are obtainable by means of an HPH process are capable of providing the effects and especially the photoprotection benefits obtainable by the composition of the invention.
  • the particulate lipids play a critical role.
  • the lipid phase and the water phase of four cosmetic compositions are separately heated to 80 °C. Then the two phases are combined using a high-shear mixer to form a pre-emulsion. After cooling down to room temperature, the pre-emulsions of sample B and sample D are further processed through a high-pressure homogenizer at 500- 1,500 bar. This cycle is repeated with three to five consecutive runs until the particle size of the lipids has fallen within the range of from > 100 nm to 500 nm.
  • compositions of sample A and sample B are identical and the compositions of sample C and sample D are identical as well. All samples are processed through a high shear mixer to form a pre-emulsion. Only sample B and sample D are further processed through a high- pressure homogenizer to reduce the particle size.
  • Mastersizer 3000 Malvern static laser light diffraction was used to measure the particle size distribution. The calculation is based on the model of the Mie-theory.
  • the particle size distributions (D50) of sample B and sample D are within the range of from 110 nm to 500 nm. This confirms that a high-pressure homogenizer is capable of reducing the particle size down to the range suitable for use in the instant invention.
  • a Labsphere UV-2000 Ultraviolet Transmittance Analyzer further was used to measure the diffuse transmittance of the samples in the ultraviolet wavelength region from 250 nm to 450 nm. The measurement complied with industry standards for in-vitro sunscreen analysis.
  • sample D is not significantly different from (compositionally identical) sample C.
  • the high-pressure homogenization of sample C does not result in a significant improvement.
  • Sample B contains lipid nanoparticles and has been processed by a high-pressure homogenizer. These results set forth above show that sample B has a strong affinity to skin and is capable of sustaining UV actives on skin to enhance UV absorption, thereby providing a better photoprotection. In addition, the lipid nanoparticles in sample B were densely packed on the surface of the skin and formed an occlusive film on the skin that provides additional skin benefits such as improved moisturization.
  • Sample D did not contain lipid particles and failed to enhance the UV absorbance of the formula. During application, a layer of small oil droplets resting on the surface of the skin was observed. This indicates that sample D exhibits no skin affinity and does not enhance the UV absorbance.
  • ingredients of the composition according to the invention can be selected in the following ranges.
  • the ranges below are not limiting, and the numbers refer to proportions by weight based on the total weight of the composition.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dispersion Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Gerontology & Geriatric Medicine (AREA)
  • Cosmetics (AREA)

Abstract

L'invention concerne une composition à application topique, en particulier cosmétique, qui comprend une combinaison de principes actifs et de lipides particulaires ayant un point de fusion supérieur à 40 °C et présentant une distribution granulométrique D50 allant de > 100 nm à 1000 nm. La composition présente une efficacité améliorée des principes actifs dans des méthodes de traitement cosmétique.
PCT/EP2024/070078 2023-07-21 2024-07-16 Composition topique à effets cutanés améliorés Pending WO2025021582A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202363528150P 2023-07-21 2023-07-21
US63/528,150 2023-07-21

Publications (1)

Publication Number Publication Date
WO2025021582A1 true WO2025021582A1 (fr) 2025-01-30

Family

ID=91960565

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2024/070078 Pending WO2025021582A1 (fr) 2023-07-21 2024-07-16 Composition topique à effets cutanés améliorés

Country Status (1)

Country Link
WO (1) WO2025021582A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6814959B1 (en) * 1999-07-13 2004-11-09 Pharmasol Gmbh UV radiation reflecting or absorbing agents, protecting against harmful UV radiation and reinforcing the natural skin barrier
US7147841B2 (en) * 2002-06-17 2006-12-12 Ciba Specialty Chemicals Corporation Formulation of UV absorbers by incorporation in solid lipid nanoparticles
EP2099420A1 (fr) 2006-11-17 2009-09-16 Abbott GmbH & Co. KG Nanocristaux pour une utilisation dans des formulations cosmétiques topiques et leur procédé de fabrication
US20100272763A1 (en) * 2007-12-12 2010-10-28 Fujifilm Corporation Skin external preparation and method of producing the same

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6814959B1 (en) * 1999-07-13 2004-11-09 Pharmasol Gmbh UV radiation reflecting or absorbing agents, protecting against harmful UV radiation and reinforcing the natural skin barrier
US7147841B2 (en) * 2002-06-17 2006-12-12 Ciba Specialty Chemicals Corporation Formulation of UV absorbers by incorporation in solid lipid nanoparticles
EP2099420A1 (fr) 2006-11-17 2009-09-16 Abbott GmbH & Co. KG Nanocristaux pour une utilisation dans des formulations cosmétiques topiques et leur procédé de fabrication
US20100272763A1 (en) * 2007-12-12 2010-10-28 Fujifilm Corporation Skin external preparation and method of producing the same

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
ANGÈLE CORTIAL ET AL: "Hot homogenization process optimization for fragrance encapsulation in solid lipid nanoparticles", FLAVOUR AND FRAGRANCE JOURNAL, WILEY, NEW YORK, NY, GB, vol. 30, no. 6, 14 July 2015 (2015-07-14), pages 467 - 477, XP071708856, ISSN: 0882-5734, DOI: 10.1002/FFJ.3259 *
MUELLER ET AL., EUROPEAN JOURNAL OF PHARMACEUTIC AND BIOPHARMACEUTICS, vol. 50, 3 July 2000 (2000-07-03), pages 181 - 177
TEERANACHAIDEEKUL ET AL: "Cetyl palmitate-based NLC for topical delivery of Coenzyme Q"1"0 - Development, physicochemical characterization and in vitro release studies", EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, ELSEVIER SCIENCE PUBLISHERS B.V., AMSTERDAM, NL, vol. 67, no. 1, 30 June 2007 (2007-06-30), pages 141 - 148, XP022136348, ISSN: 0939-6411, DOI: 10.1016/J.EJPB.2007.01.015 *

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