WO2016071113A1 - Composition anti-vieillissement - Google Patents

Composition anti-vieillissement Download PDF

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Publication number
WO2016071113A1
WO2016071113A1 PCT/EP2015/074406 EP2015074406W WO2016071113A1 WO 2016071113 A1 WO2016071113 A1 WO 2016071113A1 EP 2015074406 W EP2015074406 W EP 2015074406W WO 2016071113 A1 WO2016071113 A1 WO 2016071113A1
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WO
WIPO (PCT)
Prior art keywords
oral
ageing
ageing composition
topical anti
leaf
Prior art date
Application number
PCT/EP2015/074406
Other languages
English (en)
Inventor
Vishi Bansal
John Casey
Vijay Ramchandra Gadgil
Linda Jane Wainwright
Original Assignee
Unilever Plc
Unilever N.V.
Conopco, Inc., D/B/A Unilever
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 Unilever Plc, Unilever N.V., Conopco, Inc., D/B/A Unilever filed Critical Unilever Plc
Publication of WO2016071113A1 publication Critical patent/WO2016071113A1/fr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00Preparations for affecting hair growth
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/31Hydrocarbons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00Preparations for care of the hair

Definitions

  • the invention relates to an anti-ageing composition, in particular to a composition for treating hair ageing.
  • NFE2L2 nuclear factor erythroid-2 related factor 2
  • Nrf2 nuclear factor erythroid-2 related factor 2
  • Nrf-2 is inactive and bound in the cytoplasm by cytosolic regulatory protein Kelch-like ECH-associated protein 1 (Keapl ).
  • Kelch-like ECH-associated protein 1 Kelch-like ECH-associated protein 1
  • the protein Cullin 3 degrades Nrf2 by ubiquitination.
  • Kobayashi et al Mol. Cell. Biol., 24, 16, 7130-9 (March 2004)
  • Keapl helps Cullin 3 ubiquitinate Nrf2.
  • Nrf2 is ubiquitinated, it is transported to the proteasome where it is degraded and its components recycled such that under normal conditions, Nrf2 has a half-life of only 20 minutes.
  • Yamamoto et al (Mol. Cell (Biol., 28, 8, 2758-70 (April 2008)) and Sekhar et al (Toxicol. Appl. Pharmacol., 244, 1 , 21-6 (June 2009)) disclose that oxidative stress or electrophilic stress disrupts critical cysteine residues in Keapl , disrupting the Keapl -Cullin 3 ubiquitination system.
  • Nrf2 When Nrf2 is not ubiquitinated, it builds up in the cytoplasm and translocates into the nucleus. Itoh et al (Biochem. Biophys. Res.
  • Nrf2 combines (forms a heterodimer) with a small Maf protein (a transcription factor) and binds to small regions of DNA known as Antioxidant Response Elements (ARE's) in the upstream promoter region of many anti-oxidative genes, and initiates their transcription.
  • ARE's Antioxidant Response Elements
  • the antioxidant genes include "phase II" enzymes such as NAD(P)H: quinone oxidoreductase 1 (NQO-1 ) and hemoxygenase-1 (HO-1 ).
  • the main function of the hair follicle is to produce a hair fibre.
  • the hair follicle develops from the embryonic epidermis as an epidermal finger which differentiates into the fibre, the outer root sheath (ORS) and the inner root sheath (IRS).
  • WO 2014/095289 Unilever et al.
  • Example 4 discloses in Example 4 that sulforaphane significantly up-regulates NQO-1 and HO-1 gene expression in human hair follicles and is thus an Nrf2 agonist, and in Example 3 that sulphoraphane significantly up-regulates human hair follicle growth.
  • Hair ageing is a major age-related consumer issue (hair loss, thinning hair, loss of shine, increased number of grey hairs, etc).
  • Biological routes for hair growth or preventing hair greying provide effective opportunities to target consumer hair issues.
  • Minoxidil TM and FinasterideTM are the only clinically proven, mildly effective products available for hair growth and both are classified as medicines and therefore not suitable for cosmetic use.
  • the identification of cosmetic ingredients which are able to boost hair growth, maintain anagen and/or prevent catagen may prove to be effective anti-ageing treatments to prevent or attenuate some of the symptoms associated with hair ageing.
  • HO-1 hemoxygenase-1
  • an oral or topical anti-ageing composition comprising a combination of a carotenoid and an aqueous or hydroalcoholic extract of the leaf and whole herb of Andrographis paniculata, wherein the oral or topical anti-ageing composition comprises more than 0.4 % w/w andrographolide, and wherein the oral or topical anti-ageing composition excludes 18 % dry weight Gymnema sylvastre leaf or 3 % dry weight Andropogan muricatus root or 10 % dry weight Achytantus aspera stem and leaf or 5 % dry weight Withania somnifera root.
  • the combination of carotenoid and an aqueous or hydroalcoholic extract of the leaf and whole herb of Andrographis paniculata is a synergistic combination.
  • An oral or topical anti-ageing composition according to the first aspect of the invention may be provided for use as a medicament.
  • An oral or topical anti-ageing composition according to the first aspect of the invention may be provided for use in treating hair ageing.
  • an oral or topical anti-ageing composition according to the first aspect of the invention for the manufacture of a medicament for use in treating hair ageing.
  • an oral or topical anti-ageing composition according to the first aspect of the invention for use in treating hair ageing.
  • a method for treating hair ageing to a human in need thereof comprising the step of applying to the hair a topical or imbibing an oral anti-ageing composition according to the first aspect of the invention.
  • treating hair ageing means promoting hair fibre growth or reducing hair fibre loss.
  • the carotenoid is preferably lycopene or lutein.
  • the oral anti-ageing composition of the first aspect of the invention preferably comprises a daily dosage of 1 to 100, preferably 3 to 50 mg carotenoid in the form of one or more unit doses, and/or a daily dosage of 10 to 500, preferably 50 to 250 mg aqueous or hydroalcoholic extract of the flowers of Andrographis paniculata in the form of one or more unit doses.
  • the anti-ageing composition of the first aspect of the invention preferably comprises 5 to 0.005, preferably 2 to 0.05 % w/w carotenoid, and/or 0.4 to 10, preferably 0.4 to 5, most preferably 0.4 to 2 % w/w an aqueous extract or hydroalcoholic extract of the leaf and whole herb of Andrographis paniculata.
  • the aqueous or hydroalcoholic extract of the leaf and whole herb of Andrographis paniculata preferably comprises at least 5, preferably at least 10, most preferably at least 20 % w/w andrographolide.
  • the carotenoid is not complexed with a phospholipid.
  • the oral or topical anti-ageing composition of the first aspect of the invention excludes a phospholipid and/or a hydrolysed milk protein
  • the topical anti-ageing composition of the first aspect of the invention will comprise a dermatologically acceptable vehicle which acts as a diluent, a dispersant and/or a carrier not only for the ingredients which are essential for the invention but also for any other optional but often preferred ingredients.
  • the dermatologically acceptable vehicle may be water or oil- based, anhydrous or an emulsion, with water-in-oil or oil-in-water emulsions being generally preferred. If water-based or an emulsion, the dermatologically acceptable vehicle comprises 5 to 99, most preferably 40 to 80 % w/w of the topical composition, including all ranges subsumed therein.
  • the dermatologically acceptable vehicle may also comprise organic solvents, such as alkanols and ester oils.
  • Typical examples of alkanols are ethyl alcohol and isopropyl alcohol.
  • Typical examples of ester oils are isopropyl myristate, cetyl myristate, 2-octyldodecyl myristate, avocado oil, almond oil, olive oil, and neopentylglycol dicaprate.
  • the dermatologically acceptable vehicle may also comprise 0.1 to 50 % w/w emollients such as alcohols (for example cetyl alcohol), silicone oils and esters, and esters.
  • Silicone oils include cyclic or linear polydimethylsiloxanes containing from 3 to 9, preferably from 4 to 5, silicon atoms.
  • Non-volatile silicone oils include polyalkyl siloxanes (for example polydimethylsiloxanes), polyalkylaryl siloxanes and polyether siloxane copolymers.
  • Esters include alkenyl or alkyl esters of fatty acids having 10 to 20 carbon atoms (for example isoarachidyl neopentanoate, isononyl isonanonoate, oleyl myristate, oleyl stearate and oleyl oleate.), ether-esters (for example fatty acid esters of ethoxylated fatty alcohols), polyhydric alcohol esters (for example ethylene glycol mono- and di-fatty acid esters, diethylene glycol mono- and di-fatty acid esters, polyethylene glycol (200-6000) mono- and di-fatty acid esters, propylene glycol mono- and di-fatty acid esters, polypropylene glycol 2000 monooleate, polypropylene glycol 2000 monostearate
  • the dermatologically acceptable vehicle may also comprise fatty acids having from 10 to 30 carbon atoms (for example pelargonic, lauric, myristic, palmitic, stearic, isostearic, oleic, linoleic, arachidic, behenic and erucic acids).
  • fatty acids having from 10 to 30 carbon atoms (for example pelargonic, lauric, myristic, palmitic, stearic, isostearic, oleic, linoleic, arachidic, behenic and erucic acids).
  • the dermatologically acceptable vehicle may also comprise 0.2 to 25, preferably 0.5 to 15 % w/w humectant which increase the effectiveness of the emollient, reduces scaling, stimulates removal of built-up scale and improves skin feel.
  • the humectants is a polyhydric alcohol (for example glycerol, polyalkylene glycols and more preferably alkylene polyols and their derivatives, including propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol and derivatives thereof, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1 ,3-butylene glycol, 1 ,2,6-hexanetriol, ethoxylated glycerol, propoxylated glycerol and mixtures thereof).
  • the humectant is glycerol.
  • the dermatologically acceptable vehicle may also comprise 0.0001 to 5%, preferably 0.001 to 1 %, most preferably 0.01 to 0.5 % w/w thickener (for example cross-linked acrylates such as Carbopol 982, hydrophobically-modified acrylates such as Carbopol 1382, cellulosic derivatives (such as sodium carboxymethylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, ethyl cellulose and hydroxymethyl cellulose) and natural gums (such as guar, xanthan, sclerotium, carrageenan, and pectin)).
  • cross-linked acrylates such as Carbopol 982, hydrophobically-modified acrylates such as Carbopol 1382
  • cellulosic derivatives such as sodium carboxymethylcellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, ethyl cellulose
  • the topical anti-ageing composition of the first aspect of the invention may also comprise 0.001 to 40, preferably 0.001 to 20, most preferably 0.01 to 5 % w/w surfactant selected from the group consisting of anionic, nonionic, cationic, amphoteric surfactants, and mixtures thereof.
  • Preferred nonionic surfactants include a C10-C20 fatty alcohol or acid hydrophobe condensed with from 2 to 100 moles of ethylene oxide or propylene oxide per mole of hydrophobe, mono- and di- fatty acid esters of ethylene glycol, fatty acid monoglyceride, sorbitan-, mono- and di- C8-C20 fatty acids, block copolymers (such as ethylene oxide/propylene oxide), polyoxyethylene sorbitan, and alkyl polyglycosides and saccharide fatty amides (such as methyl gluconamides).
  • Preferred anionic surfactants include soap, alkyl ether sulfate and sulfonates, alkyl sulfates and sulfonates, alkylbenzene sulfonates, alkyl and dialkyl sulfosuccinates, C8-C20 acyl isethionates, acyl glutamates, and C8-C20 alkyl ether phosphates.
  • the topical anti-ageing composition of the first aspect of the invention may also comprise other optional ingredients such as fragrances, fillers (such as talc and silica), alpha-hydroxy acids, beta-hydroxy acids (such as salicylic acid), zinc salts (such as zinc pyrithione), preservatives, sunscreens, both organic and inorganic (such as derivatives of para- aminobenzoic acid (PABA), cinnamate and salicylate (for example avobenzophenone, octyl methoxycinnamate and 2-hydroxy-4-methoxy benzophenone, zinc oxide and titanium dioxide), and anti-dandruff actives (such as ketoconazole, climbazole, and zinc pyrithione).
  • fragrances such as talc and silica
  • fillers such as talc and silica
  • alpha-hydroxy acids such as salicylic acid
  • zinc salts such as zinc pyrithione
  • preservatives such as derivatives of para- aminobenzoic acid (P
  • the topical anti-ageing composition of the first aspect of the invention may also comprise 0.01 to 10, more preferably 0.1 to 5, most preferably 0.5 to 3 % w/w conditioning silicone (such as dimethiconol, silicone gums and amino functional silicones).
  • the topical composition of the invention will normally comprise 0.01 to 5, preferably 0.05 to 1 , more preferably 0.08 to 0.5 % w/w cationic polymer for enhancing deposition of the silicone on hair fibres (such as dimethyldiallylammonium chloride homopolymer (Polyquaternium 6), copolymers of acrylamide and dimethyldiallylammonium chloride (Polyquaternium 7), mineral acid salts of amino-alkyl esters of homo-and copolymers of unsaturated carboxylic acids having from 3 to 5 carbon atoms (as described in US 4 009 256), cationic polyacrylamides (as described in WO 95/2231 1 ), and cationic polysaccharide poly
  • the topical anti-ageing composition of the first aspect of the invention can be manufactured by mixing the ingredients in no particular order and usually at 70 to 80°C and under atmospheric pressure.
  • the packaging for the topical composition of the invention can be a patch, bottle, tube, roll-ball applicator, propellant driven aerosol device, squeeze container or lidded jar.
  • the oral anti-ageing composition of the first aspect of the invention may be in the form of a solid, a slurry, a solution, a suspension, a gel or an emulsion.
  • the oral anti-ageing composition of the first aspect of the invention may be in the form of a supplement of one or more unit dosages such as capsules, cachets, lozenges, pills, tablets, caplets, each comprising a predetermined amount of the essential ingredients of the invention.
  • the oral anti-ageing composition of the first aspect of the invention may be selected from the group of foodstuffs consisting of a beverage (for example a fruit or tea (for example Camellia sinensis) based beverage, a supplement, a soup (in dry, paste or liquid form), margarine, a ready-to-eat meal, a dressing, a mayonnaise, mustard, a tomato-based condiment, a sauce, a seasoning (for example as unit doses in the form of a powder, a compressed powder in the form of, for example, a cube, a liquid or suspension, or a gel), a yoghurt and a frozen confection.
  • a beverage for example a fruit or tea (for example Camellia sinensis) based beverage
  • a supplement for example a soup (in dry, paste or liquid form)
  • margarine for example, a soup (in dry, paste or liquid form), margarine, a ready-to-eat meal, a dressing, a mayonnaise, mustard
  • frozen confection is meant a sweet-tasting fabricated foodstuff intended for consumption in the frozen state (i.e. under conditions wherein the temperature of the foodstuff is less than 0°C, and preferably under conditions wherein the foodstuff comprises significant amounts of ice).
  • Frozen confections include ice cream, sorbet, sherbet, frozen yoghurt, water ice, milk ice and the like.
  • the frozen confection has a total solids content (i.e. the sum of the weights of all the ingredients other than water, expressed as a percentage of the total weight) of at least 20 %, more preferably at least 25 %.
  • Frozen confections may be aerated or unaerated.
  • the frozen confection is aerated.
  • the frozen confection may be manufactured by any suitable process, typically by preparing a mix of ingredients; then pasteurising and optionally homogenising the mix; and then freezing and optionally aerating the mix to produce the frozen confection.
  • DMEM Dulbecco's Modified Eagle Serum
  • FBS foetal bovine serum
  • Test solutions were prepared in ethanol or DMSO and added directly to the cells and treated for 24 hours.
  • the test solutions were prepared with selected concentrations of test material as set forth in Table 2. The cells were then pelleted.
  • the lysis buffer contained 1 % NP-40, 0.1 % sodium deoxycholate, 0.1 % SDS, 6 mM sodium chloride and 0.05 M Tris at pH 7.6.
  • Protease inhibitor cocktail 1000X; Sigma P8340 was added prior to use at a level of 10 ⁇ per ml of lysis buffer.
  • the clarified cell lysate was frozen at -80 °C until needed.
  • the total protein concentration of each cell lysate was measured using the Pierce BCA protein assay kit.
  • a set of eight standard solutions ranging from 0 to 1200 ⁇ g ml protein was prepared from the supplied 2 mg/ml BSA stock solution. 10 ⁇ I of standard or cell lysate was added to duplicate wells of a flat-bottomed, 96-well microtitre plate.
  • the reagent solution was prepared according to the kit instructions from 50 parts reagent A and 1 part reagent B. 200 ⁇ of the final reagent was added to each well of the microtitre plate. The plate was mixed, covered and incubated at 37 °C for 30 minutes and absorbance read at 562 nm. A protein standard curve was constructed and used to determine the protein concentration of each cell lysate.
  • HO-1 ELISA Assay Designs
  • Protein samples were diluted in sample diluent, and 100 ⁇ transferred to the pre-coated anti- human HO-1 immunoassay plate (Assay Designs (ERK-800)).
  • a 7-point recombinant HO-1 standard curve ranging from 25 to 0.39 ng/ml, was also prepared in sample diluent.
  • the immunoassay plate was incubated at room temperature for 30 minutes, washed six times with Wash Buffer, and incubated for a further 60 minutes at room temperature with 100 ⁇ /well of anti-human HO-1 antibody solution. The plate was washed as above and incubated for 30 minutes at room temperature with 100 ⁇ /well of horseradish peroxidase conjugate solution.
  • the results are summarized in Table 1 .
  • the vehicle for lutein was dimethyl sulphoxide (DMSO)
  • the vehicle for the aqueous extract of the whole herb of Andrographis paniculata was distilled water
  • the vehicle for the combination was a 50/50 by volume mixture of distilled water and DMSO.
  • the vehicle for lycopene, and for its combination with an aqueous extract of the whole herb of Andrographis paniculata was a 50/50 by volume mixture of distilled water and tetrahydrofuran (THF).
  • THF tetrahydrofuran
  • lutein did not significantly up-regulate HO- 1 protein levels in primary human dermal fibroblast cells compared to vehicle.
  • 5 and 10 ⁇ lutein did significantly up-regulate HO-1 protein levels compared to vehicle.
  • HO-1 protein pg ⁇ g protein
  • normalized HO-1 protein pg ⁇ g protein
  • levels of primary human dermal fibroblast cells treated with lycopene, lutein, an aqueous extract of the whole herb of Andrographis paniculata, and mixtures thereof hatchched values indicate a synergy
  • Lycopene Lutein An aqueous HO-1 HO-1 Normalised Sum of ( ⁇ ) ( ⁇ ) extract of the protein protein HO-1 protein normalised whole herb of (pg/Mg (pg/Mg (pg/Mg HO-1 protein Andrographis protein) protein) protein) (pg/Mg paniculata (Mg/ml) for test for protein) sample vehicle

Abstract

La présente invention concerne une composition anti-vieillissement, en particulier une composition pour le traitement du vieillissement des cheveux. Ainsi, selon un aspect de l'invention, celle-ci concerne une composition anti-vieillissement à administrer par voie orale ou topique, ladite composition anti-vieillissement à administrer par voie orale ou topique comprenant une association d'un caroténoïde et d'un extrait aqueux ou hydroalcoolique de feuilles et de plantes entières d'Andrographis paniculata, la composition anti-vieillissement à administrer par voie orale ou topique comprenant plus de 0,4 % en poids d'andrographolide, et la composition anti-vieillissement à administrer par voie orale ou topique ne comprenant pas 18 % en poids sec de feuilles de Gymnema sylvastre ou 3 % en poids sec de racines d'Andropogan muricatus ou 10 % en poids sec de tiges et de feuilles d'Achytantus aspera ou 5 % en poids sec de racines de Withania somnifera. Le caroténoïde est de préférence du lycopène ou de la lutéine. Les caractéristiques du vieillissement des cheveux comprennent la perte des cheveux, l'amincissement des cheveux, la perte d'éclat et l'augmentation du nombre de cheveux gris.
PCT/EP2015/074406 2014-11-04 2015-10-21 Composition anti-vieillissement WO2016071113A1 (fr)

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EP14191688 2014-11-04
EP14191688.2 2014-11-04

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