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WO2018134714A1 - Composition de soin de la peau blanchissante à base de dihydromyricétine, de niacinamide et d'un modificateur de ph - Google Patents

Composition de soin de la peau blanchissante à base de dihydromyricétine, de niacinamide et d'un modificateur de ph Download PDF

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Publication number
WO2018134714A1
WO2018134714A1 PCT/IB2018/050223 IB2018050223W WO2018134714A1 WO 2018134714 A1 WO2018134714 A1 WO 2018134714A1 IB 2018050223 W IB2018050223 W IB 2018050223W WO 2018134714 A1 WO2018134714 A1 WO 2018134714A1
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Prior art keywords
composition
modifier
niacinamide
dihydromyricetin
resorcinol
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PCT/IB2018/050223
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English (en)
Inventor
Rajan Raghavachari
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R&r Salons Pvt Ltd
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R&r Salons Pvt Ltd
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Publication of WO2018134714A1 publication Critical patent/WO2018134714A1/fr
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    • 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
    • A61K8/34—Alcohols
    • A61K8/347—Phenols
    • 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
    • A61K8/36—Carboxylic acids; Salts or anhydrides thereof
    • A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides 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
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
    • A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
    • 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
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin

Definitions

  • the subject matter relates to cosmetic compositions in general.
  • the subject matter relates to skin care compositions. Even more specifically the subject matter relates to compositions for skin lightening.
  • the skin colour is primarily determined by the amount of melanin present in the skin.
  • Melanin is a brown-black pigment present in the skin which is produced within the cells known as melanocytes which reside below or between the basal cells of the epidermis, the outermost skin layer.
  • Solutions aiming at skin lighting generally include ingredients that may inhibit the melanin in skin by inhibiting either it's generation or it's distribution on the skin.
  • Some of the commercially available ingredients have a number of problems. For example, some ingredients deteriorate and tend to lose it physical characteristics in a short span of time. In one possibility some ingredients may discolor and lose aesthetic charm for a user. In some other examples, the ingredients do not make a homogeneous solution and they tend to separate thus resulting in effective failure of the compositions. Some compositions fail merely because its ingredients have relatively opposing requirements, that is to say, satisfying one ingredient's requirements may lead to adversely affecting another ingredient.
  • One of the desirable ingredients in a cosmetic composition may be an antioxidant.
  • Dihydromyricetin (generally traded as telocapilTM and used interchangeably throughout this specification) is one such antioxidant.
  • Another desirable ingredient in the cosmetic composition can be an ingredient that influences the process of melanogenesis.
  • One such ingredient is niacinamide. While, both the ingredients are desirable, use of these two ingredients together in a single cosmetic composition is challenging because of their opposing requirements.
  • Another ingredient that is desirable for enhancing the cosmetic effect of the cosmetic composition is derivative of resorcinol. However derivative of resorcinol, for example -butyl resorcinol, poses difficulties in solubilizing. Therefore, the ingredients such as discussed above, are though desirable, present challenges for their use in a single composition.
  • the present subject matter provides a solution that addresses above and other problems and enables employing of the ingredients that have contrary or competing requirements.
  • the present subject matter provides a cosmetic composition comprising dihydromyricetin and niacinamide in a cosmetically acceptable vehicle.
  • the composition is provided with a pH modifier.
  • the pH modifier is configured to adjust pH of the cosmetic composition at a level to control discoloration of the dihydromyricetin while protecting niacinamide from significantly getting converted into nicotinic acid.
  • the cosmetic composition further comprises derivative of resorcinol and polyol that is an effective solubilizer.
  • Providing polyol not only addresses solubility challenges of derivative of resorcinol but also enhances effectiveness of the cosmetic composition as an anti-irritant ingredient.
  • providing pH modifier not only protects niacinamide from getting converted to nicotinic acid and discoloration of dihydromyricetin, but also enhances effectiveness of the cosmetic composition as a tyrosinase suppressor.
  • the present subject matter provides a cosmetic skin care composition comprising: dihydromyricetin, niacinamide, and a pH modifier on a cosmetically acceptable vehicle, wherein the pH modifier is configured to adjust pH of the cosmetic composition at a level to control discoloration of the dihydromyricetin and chemical degradation of the niacinamide.
  • the cosmetic composition is provided with the pH modifier in a concentration low enough to prevent discoloration of the dihydromyricetin and high enough to prevent chemical degradation of the niacinamide.
  • the pH modifier is present in the composition in any one of range of: o.i- 20 wt%, 0.2- 12.0 wt% and 0.5 - 8 wt%.
  • the pH modifier is an alpha hydroxy acid.
  • Some examples of the alpha hydroxy acid are glycolic, malic, tartaric, lactic, citric, acetic acids etc.
  • the pH modifier is glycolic acid.
  • the composition has a pH in any one of the range of: 3.0-6.0, 4.0-5.5 and 4.0- 5.0.
  • the dihydromyricetin is present in the composition in any one of range: 0.01-20 wt%, 0.1-5.0 wt% and 0.2-3.0 wt%.
  • the niacinamide is present in the composition in any one of range: 0.1-10 wt%, 0.2-5 wt% and 0.5-3 wt%.
  • the cosmetic composition further comprises resorcinol.
  • the resorcinol is 4-butyl resorcinol.
  • the resorcinol is present in the composition in any one of amount range of: 0.1- 10 wt%, 0.1- 5 wt% and 0.2-0.5 wt%.
  • the composition also comprises a polyol selected from 1,3-propane diol, propylene glycol, glycerol, sorbitol, and polyethylene glycol.
  • the polyol is present in the composition in any one of range of: 0.1- 30 wt%, 0.2- 20 wt% and 0.5- 16 wt%.
  • the composition further comprises an agent selected from a chelating agent and an antioxidant or a combination thereof.
  • the chelating agent is selected from disodium ethylenediaminetetraacetate (EDTA), diethylenetriaminepentaacetic acid (DTPA), trisodium ethylenediaminedisuccinate (EDDS) or a combination thereof.
  • the antioxidant is selected from sodium-bisulphite, butylated hydroxytoluene (BHT), ascorbic acid and its derivatives, tocopherol and its derivatives or a combination thereof.
  • FIG. l shows comparative graphical representation of melanin reduction resulting from a number of compositions, including the compositions of the present of the present subject matter.
  • FIG. 2 and FIG. 3 show results of discoloration and stability study of a number of compositions, including the compositions of the present of the present subject matter.
  • Melanin also referred as “melanin pigment” or merely “pigment” protects the body from the damaging effects of ultraviolet radiation. The exposure to sunlight or other UV radiation can stimulate the melanocytes to produce melanin. The skin colour is due to melanin pigment that skin cells generate.
  • Melanin is dark in color. Due to dark colour of the melanin, lower amounts and concentrated distribution of melanin result in lighter skin colour while higher amounts and uniform broad dispersion of melanin result in darker skin colour. Melanin is formed through a process termed as 'melanogenesis'. There are a number of biological pathways involved in the generation of melanin and its transfer all the way to the top layer of the skin. In this process, Tyrosinase, a copper containing enzyme present in the body tissues, serves as a catalyst to oxidize amino acid tyrosine to dihydroxyphenylalanine in melanocytes.
  • melanin is bound to a protein matrix to form melanosomes where tyrosinase converts tyrosine to eumelanin (black pigment) or phenomelanin (yellowish and reddish pigment).
  • Melanin bio-synthesis involves chain of oxidative reactions catalysed by a series of enzymes.
  • DOPAchrometautomerase (TRP-2) and DHICA oxidase (TRP-i) proteins are responsible for converting DOPAchrome to 5,6-dihydroxy indole -2-carboxy acid which leads to the formation of eumelanin.
  • compositions have been developed to reduce the amount of melanin in the skin and therefore whiten/lighten the skin by reducing or inhibiting melanogenesis or reducing hyperactive melanocytes.
  • the development efforts have been focused on actives that inhibit the function or activity of tyrosinase or block the chain reaction at various points in the melanogenesis process.
  • the compositions accordingly may achieve skin whitening/lightening by blocking tyrosinase activity, reducing tyrosinase synthesis, inhibiting TRP-i and/or TRP-2, blocking melanin transfer from melanocytes to keratinocytes.
  • Keratinocyte is predominant cell type in the epidermis -the outermost layer of the skin- constituting 90% of the cells.
  • the skin lightening or cosmetic compositions not only have an ingredient that influences or affects only one pathway of melanogenesis but carry a combination of ingredients those influence or affect multiple different pathways in a synchronous manner, so that the cosmetic composition provides enhanced skin lightening benefit.
  • a composition for achieving desired skin color through depigmentation of skin has been one of the desirable cosmetic benefits.
  • Some of the ingredients are used individually for slowing down the proliferation of melanocytes and keratinocytes, suppression of tyrosinase, inhibition of melanogenesis, exfoliation of dead skin cells, and also for soothing skin from stresses due to oxidation and inflammation.
  • Niacinamide is one of the often used skin lightening ingredients, which can inhibit not only tyrosinase activity that is involved in melanin synthesis but also suppresses the transfer of melanosomes-containing-melanin from melanocyte to keratinocyte. Niacinamide is also a TRP-i inhibitor. Dihydromyricetin (telocapilTM) is another ingredient that helps in achieving lighter skin colour through its antioxidant action. There are other ingredients like resorcinol and its derivations such as 4-butyl resorcinol that enhances the skin lightening benefit by inhibiting the activity of tyrosinase and tyrosinase- related-protein TRPi.
  • niacinamide and dihydromyricetin have contradictory or opposing chemical requirements to remain effective.
  • Dihydromyricetin requires highly acidic environment, in the absence of which it gets easily oxidized and causes discolouration of the composition.
  • niacinamide requires a slightly lower acidic environment (i.e. higher acidic pH) to maintain its chemical form and hence its activity. Highly acidic environment leads to conversion of nicotinamide to nicotinic acid that makes the composition less effective.
  • resorcinol in another challenge faced is solubility of ingredients such as resorcinol and its derivative in an aqueous composition.
  • ingredients such as resorcinol and its derivative in an aqueous composition.
  • resorcinol such as 4-butyl resorcinol tends to separate out from the aqueous composition (e.g. aqueous mist, gel) and thus leaving the composition not fit for use.
  • compositions may be available having any of the above ingredients individually. However a composition having a combination of any of these ingredients is a challenge to a chemist. Therefore, there is a need to provide a composition that enables use of desirable ingredients in combination.
  • the present subject matter provides a composition which offers a suitable environment that effectively exploits benefits of the ingredient, enhances cosmetic benefit of the composition and does not have challenges discussed above and other challenges.
  • the present subject matter provides a cosmetic composition comprising dihydromyricetin as telocapilTM and niacinamide in a cosmetically acceptable vehicle. I n the following discussions units are in wt/wt.
  • the composition comprises telocapil in an amount of o.oi- 20 wt%.
  • the telocapil is present between 0.1- 5.0 wt%.
  • the telocapil is present between 0.2-3 wt%.
  • the composition comprises niacinamide in an amount of o.i-io wt%.
  • the niacinamide is present between 0.2-5 wt%.
  • the niacinamide is present between 0.5- 3 wt%.
  • Dihydromyricetin requires highly acidic environment, in the absence of which it easily oxidizes and causes discolouration of the composition.
  • the discoloration of the cosmetic composition is not desirable because, it not only reduces aesthetic appeal of the cosmetic composition, but also, reduces the commercial value and may indicate deterioration of the composition.
  • H igh acidic environment is not desirable for niacinamide.
  • Highly acidic environment leads to conversion of niacinamide to nicotinic acid that makes the composition less suitable for use a skin care composition.
  • the cosmetic composition provides a pH modifier.
  • the pH modifier is configured to adjust pH of the cosmetic composition at a level to control discoloration of the dihydromyricetin and conversion of niacinamide into nicotinic acid.
  • the "acidic pH" of the composition is low enough to prevent discoloration of the dihydromyricetin and high enough to prevent significant conversion of niacinamide into nicotinic acid.
  • the pH modifier is an alpha hydroxyl acid. It shall become clear to a person in the art, that the pH modifier is a hydrogen ion donor.
  • the acidifying agent may be from a class of hydroxy or carboxylic acids.
  • the alpha hydroxyl acid is selected from but not limited to glycolic acid, lactic acid, tartaric acid, citric acid, malic acid and mandelic etc.
  • the pH modifier is glycolic acid.
  • pH of the composition is maintained between 3.8-5.5.
  • pH of the composition is maintained between 4 - 5.5.
  • pH of the composition is maintained between 4- 5-
  • the pH modifier may be present in an amount between o.oi- 25 wt%.
  • the pH modifier is present in an amount between o.i-io.o wt%.
  • the pH modifier is present in an amount between 0.2- 8 wt%.
  • the discoloration of the dihydromyricetin is controlled by using a chelating agent and an antioxidant or a combination thereof.
  • the composition comprises the chelating agent.
  • the chelating agent may include disodium ethylenediaminetetraacetate (EDTA), diethylenetriaminepentaacetic acid (DTPA), trisodium ethylenediaminedisuccinate (EDDS), gluconolactone and a combination thereof.
  • the chelating agents may be present in the composition in the range o.oi- 2 wt% and in some embodiments, 0.1- 1 wt%.
  • the composition comprises the antioxidant.
  • antioxidant undergoes oxidation instead of the inhibitor (e.g. dihyromyricetin) in the composition.
  • the antioxidants used in the present subject matter are selected from but not limited to sodium-bisulphite, butylated hydroxytoluene (BHT), ascorbic acid and its derivatives, tocopherol and its derivatives and a combination thereof.
  • BHT butylated hydroxytoluene
  • the antioxidants may be present in the composition in the range 0.01-2 wt% and in some embodiments in the range of o.1-1 wt%.
  • the composition comprises resorcinol and/or derivative of resorcinol.
  • resorcinol and/or derivative of resorcinol is present in an amount of 0.1-10 wt%.
  • the resorcinol and/or derivative of resorcinol is present in an amount between 0.1-5 wt%.
  • the resorcinol and/or derivative of resorcinol is present in an amount between 0.2-0.5 wt%.
  • the derivative of resorcinol is -butyl resorcinol also known as a variant of kopsinol.
  • the kopsinol alone turns out to be cytotoxic.
  • the kopsinol used in the combination according to the present subject matter in that kopsinol in combination with niacinamide and dihydromyricetin, the cytotoxicity of the combination dramatically reduces.
  • the resorcinol is dissolved in a solvent.
  • the solvent is a polyol.
  • the polyol is selected from but not limited to 1,3-propane diol, propylene glycol, PEG, glycerol, sorbitol, etc.
  • the solvent used is 1,3-propane diol.
  • the polyol is present in an amount of 0.1-30 wt%. In another embodiment, the polyol is present in an amount between 0.2-20 wt%. In yet another embodiment, the polyol is present in an amount between 0.5- 16 wt%.
  • composition provided by the present subject matter also offer body and facial hair growth retardation effect.
  • the composition comprises a cosmetically acceptable vehicle suitable for topical application to skin.
  • Cosmetically acceptable vehicles are well known in the art and are selected based on the end use of the application.
  • the cosmetically acceptable vehicle of the present subject matter includes, but not limited to, those suitable for application to the skin.
  • Such vehicles are well known to those of ordinary skill in the art, and can include one or more compatible liquid or solid filler diluents or vehicles which are suitable for application to the skin.
  • the exact amount of a cosmetically acceptable vehicle will depend upon the level of any other optional ingredients that one of ordinary skill in the art would classify as distinct from the cosmetically acceptable vehicle (e.g., other active components).
  • the compositions of the present subject matter preferably comprise from about 40-99 wt%, more preferably from about 70- 98 wt%, and most preferably from about 80-98 wt%, of a cosmetically acceptable vehicle.
  • the cosmetically acceptable vehicle and the compositions herein can be formulated in a number of ways, including but not limited to emulsions.
  • suitable emulsions include: oil-in-water, water-in-oil, water-in-oil-in-water, oil-in- water-in-oil, oil-in-water-in-silicone emulsions or other simple aqueous formulations.
  • Desirable compositions comprise an oil-in-water emulsion and simple aqueous formulations.
  • compositions of the present invention can be formulated into a wide variety of product types, including: creams, waxes, pastes, lotions, milks, mousses, gels, oils, tonics, roll-ons, serum, concentrate, and aqueous or non-aqueous sprays. Desired compositions are formulated into lotions, serum, concentrate, roll-on, creams, gels, and aqueous sprays. These product forms may be used for a number of applications, including but not limited to, hand and body lotions, cold creams, facial moisturizers, anti-acne preparations, topical analgesics, underarm roll-on, facial serum, ingrown hair concentrate, body mist/spray and the like. Any additional components required to formulate such products vary with product type and can be routinely chosen by one skilled in the art, after reading this specification.
  • the formulation also can comprise other components that may be chosen depending on the vehicle and/or the intended use of the formulation. Additional components include, but are not limited to, water soluble sunscreens (such as Eusolex 232); oil soluble sunscreens (such as octyl methoxycinnamate); and organic sunscreens (such as camphor derivatives, cinnamates, salicylates, benzophenones, triazines, PABA derivatives, diphenylacrylate derivatives, and dibenzoylmethane derivatives.); antioxidants (such as BHT); chelating agents (such as disodium EDTA); emulsion stabilizers/thickener (such as carbomer); preservatives (such as phenoxyethanol); fragrances (such as pinene); humectants/polyols (such as glycerin, sorbitol, PEG, propanediol ); polymers (such as PVP/Eicosene copolymer); water soluble sunscreens
  • compositions can also encompass one or more active components, and as such can be either cosmetic or pharmaceutical compositions.
  • useful actives include, but are not limited to, those that improve or eradicate age spots, keratoses and wrinkles, analgesics, anesthetics, anti-acne agents, antibacterials, antiyeast agents, antifungal agents, antiviral agents, antidermatitis agents, antipruritic agents, antiemetics, antihyperkeratolytic agents, anti-dry skin agents, antiperspirants, antipsoriatic agents, antiseborrheic agents, antiaging agents, antiwrinkle agents, sunscreen agents, antihistamine agents, depigmenting agents, wound-healing agents, vitamins, corticosteroids, tanning agents or hormones.
  • useful active agents include retinoids such as retinol, and esters, acids, and aldehydes thereof; ascorbic acid, and esters and metal salts thereof, tocopherol and esters and amide derivatives thereof; milk proteins; alpha- or beta-hydroxy acids; DHEA and derivatives thereof; clotrimazole, ketoconazole, miconozole, griseofulvin, hydroxyzine, diphenhydramine, pramoxine, lidocaine, procaine, mepivacaine, monobenzone, erythromycin, tetracycline, clindamycin, meclocyline, hydroquinone, minocycline, naproxen, ibuprofen, theophylline, cromolyn, albuterol, hydrocortisone, hydrocortisone 21-acetate, hydrocortisone 17- valerate, hydrocortisone 17-butyrate, betamethasone valerate, betamethasone diproprionate
  • the above subject matter is practiced in a body lotion composition as illustrated below in Tablei.
  • Polyols could be one or more combination of glycerine, propylene glycol, 1,3, Propane diol.
  • the chelating agent, antioxidant and preservative indicated below are just one of the examples in their respective category of ingredients.
  • the example ⁇ shows the synergy between niacinamide and dihydromyricetin whereas the example ⁇ shows the avoidance of discolouration of dihydromyricetin (traded as telocapilTM) by lowering the pH with the help of glycolic acid in the composition and at the same time avoiding significant conversion of niacinamide into nicotinic acid.
  • the example IC demonstrates the enhancement of skin lightening solution with the addition of 4-butyl resorcinol and example ID demonstrates the power of 1,3-propane diol in solubilizing 4- butyl resorcinol .
  • telocapil dihydromyricetin
  • 4-butyl resorcinol traded as Kopsinol
  • this premix is added to the main mixer.
  • the contents are mixed well and then recirculated for 5 minutes to ensure homogeneity of the bulk before discharging the batch for packing.
  • the total duration of the batch time is approximately 1 hour. The colour, odour, appearance, pH and density of the finished good are checked.
  • the subject matter is practiced in a facial serum composition as illustrated below in Table 2.
  • Niacinamide and glycolic acid are premixed with DM water and this is then added to the mixer. Having ensured the pH of the bulk contents is in the range of 4 to 5, then dihydromyricetin (telocapil) is added. Kopsinol is dissolved in required quantities of 1,3- propane diol and after ensuring complete dissolution of Kopsinol, this premix is added to the main mixer. The contents are mixed well and then recirculated for 5 minutes to ensure homogeneity of the bulk before discharging the batch for packing. The total duration of the batch time is approximately 80 minutes. The colour, odour, appearance, pH and density of the finished good are checked.
  • Polyols could be one or more combination of glycerine, sorbitol, propylene glycol, 1,3, Propane diol etc.
  • the antioxidant and preservative indicated are just one of the examples in their respective category of ingredients and a chelating agent can also be beneficial in such a composition e.g. disodium EDTA, DTPA, TrisodiumEthylenediamineDisuccinate, gluconolactone etc.
  • a suspension of sumica pearl in demineralized water is added and continuously stirred to achieve uniform dispersion.
  • niacinamide dissolved in demineralized water is added.
  • a low pH solution of glycolic acid is added to lower the pH of the composition.
  • dihydromyricetin telocapil
  • Sensive SC 50 is then added.
  • 4-butyl resorcinol (Kopsinol) is dissolved in required quantities of 1,3- propane diol and after ensuring complete dissolution of kopsinol, this premix is added to the main mixer.
  • the contents are mixed well and then recirculated for 5 minutes to ensure homogeneity of the bulk before discharging the batch for packing.
  • the total duration of the batch time is 105 minutes.
  • the colour, odour, appearance, pH and density of the finished good are checked.
  • CarbopolUltrez 30 (Cross-linked - 0.8-1.5
  • carbopolUltraz 30 with or without xanthan gum are slowly added to the main mixer after adding all the ingredients as described above to make a viscous aqueous gel. Care is taken to avoid lumps whenever powder material is added by stirring well.
  • the thickener indicated in this example is one of its types and it is not limited to CarbopolUltraz 30 or natural gums like xanthan gum or guar gum.
  • the thickeners include acacia gum, carrageenan, mineral thickeners (aluminium magnesium silicate, silica), cellulosic thickeners (hydroxyl ethyl cellulose), polyvinyl pyrolidone (PVP), guar hydroxypropyltrimonium chloride etc.
  • TelocapilTM, Niacinamide, and KopsinolTM are assessed for their melanin inhibition capability. It shall become clear to a person in the art that effect of the composition on the melanin pigmentation must study in an environment such that the cells understudy survives during the experiment. If the cells fail to survive during the experiment, to draw a conclusion regarding effect of the composition on the melanin inhibition is not possible. Therefore the cells under experiment must be protected as best possible from the cytotoxic effects of the composition. To ensure the same, the experiments are conducted in concentrations that are suitable for observing the effect of the composition on the cells.
  • Melanocytes (B16F10) are seeded in 6-well cell culture plates in appropriate medium at a density of 50,000 cells/well. A day later, the cells are treated with appropriate actives and combinations. Second, the medium is removed from plate after 8hrs incubation and each well is washed twice with Phosphate-buffered saline (PBS). Third, about 0.5 ml of 2% TritonX-ioo is added to the well and cells are scrapped from the wells. TritonX-ioo causes lysis of the cells. The resulted cell lysates are transferred to 2ml tube and incubated for 1 hour on ice. Pellet is collected by centrifuging the tubes at 10,000 rpm/ °C for lomins.
  • PBS Phosphate-buffered saline
  • Telocapil and Niacinamide in combination resulted in less melanin synthesis when compared to treatment with Telocapil alone. A further decrease in melanin synthesis was observed when cells were treated with a combination of Telocapil, Niacinamide and Kopsinol.
  • Table 5 Legends of the Table 5 are as follows, T: Telocapil, N: Niacinamide, K: Kopcinol, UT: Untreated.
  • the melanin reduction may result from a number of reasons.
  • One of the reasons for melanin reduction is inhibition of tyrosinase activity. Tyrosinase inhibition has been observed in experimental results of the present subject matter. Below discussion dwells into details of the experiment and results obtained thereof. It shall become clear to a person, after reading this specification, that experiments assessing other causes of melanin reduction may be performed, however for the sake of brevity only inhibition of tyrosinase activity is being discussed herein.
  • Tyrosinase is a multicopper monoxygenase enzyme and is known as the polyphenoloxydase (PPO). It is involved in biosynthesis of melanin through oxidation of DOPA (dihydroxyphenylalanine) to dopaquinone (o-quinone), the latter then transforms into the melanin pigments through a series of enzymatic and non-enzymatic reactions in the skin. Inhibiting the activity of tyrosinase would result in reduction of melanin.
  • DOPA dihydroxyphenylalanine
  • o-quinone dopaquinone
  • the in vitro tyrosinase inhibitory activity is determined by the dopachrome method.
  • the actives are added individually and in combination at a concentration of 50 ⁇ g/ml to L-DOPA solution (10 mlW, dissolved in a 5 mM acetate buffer, pH 5).
  • tyrosinase enzyme is added to each solution in different test tubes to a final concentration of 4 U/ml.
  • the amount of dopachrome in the reaction mixture is measured after incubation at 38°C for 60 min at 475 nm by UV-Vis spectrophotometer.
  • Kojic acid at the concentration of 50 ⁇ g/ml is used as reference and a blank reaction is conducted without a sample. All measurements are performed in triplicate sample.
  • the inhibition activity of each active is expressed using the formula:
  • IA% [(OD blank - ODwith active)/ OD blank] x ioo(OD means Optical Density)
  • Example 7 Discoloration of the composition:
  • the discoloration of the composition according to the present subject matter, having a pH modifier and without the pH modifier is studied.
  • the compositions are observed for 12 weeks at temperature zero degree Celsius and forty five degree Celsius. At both the temperatures the composition without the pH modifier shows discoloration, whereas the composition of the present subject matter does not show any discoloration.
  • FIG. 2 shows discoloration of the composition without pH modifier.
  • FIG. 3 shows no discoloration of the composition according to the present subject matter. Therefore the present subject matter provides a composition which more stable and has longer shelf life.

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  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention concerne une composition cosmétique de soin de la peau. La composition comprend de la dihydromyricétine, du niacinamide et un modificateur de pH sur un véhicule cosmétiquement acceptable. Le modificateur de pH est configuré pour ajuster le pH de la composition cosmétique à un niveau permettant de réguler la décoloration de la dihydromyricétine et la dégradation chimique du niacinamide.
PCT/IB2018/050223 2017-01-21 2018-01-13 Composition de soin de la peau blanchissante à base de dihydromyricétine, de niacinamide et d'un modificateur de ph Ceased WO2018134714A1 (fr)

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CN110638809A (zh) * 2019-11-13 2020-01-03 浙江万里学院 一种具有美白作用的组合物
CN111803416A (zh) * 2020-07-17 2020-10-23 堇色生物科技(中山)有限责任公司 一种含有显齿蛇葡萄的抗衰老面霜及其制备方法
US10959933B1 (en) 2020-06-01 2021-03-30 The Procter & Gamble Company Low pH skin care composition and methods of using the same
CN112570726A (zh) * 2020-11-24 2021-03-30 山东省分析测试中心 二氢杨梅素功能化银纳米粒子及其绿色合成方法与应用
US11110049B2 (en) 2017-06-23 2021-09-07 The Procter & Gamble Company Composition and method for improving the appearance of skin
US11583488B2 (en) 2020-06-01 2023-02-21 The Procter & Gamble Company Method of improving penetration of a vitamin B3 compound into skin
US11622963B2 (en) 2018-07-03 2023-04-11 The Procter & Gamble Company Method of treating a skin condition
WO2023119230A1 (fr) 2021-12-22 2023-06-29 L'oreal Compositions de modulation de la voie de coagulation et de la voie de nicotinamide-adénine dinucléotide et leurs procédés d'utilisation

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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11110049B2 (en) 2017-06-23 2021-09-07 The Procter & Gamble Company Composition and method for improving the appearance of skin
US11622963B2 (en) 2018-07-03 2023-04-11 The Procter & Gamble Company Method of treating a skin condition
CN110638809A (zh) * 2019-11-13 2020-01-03 浙江万里学院 一种具有美白作用的组合物
CN110638809B (zh) * 2019-11-13 2022-11-29 浙江万里学院 一种具有美白作用的组合物
US10959933B1 (en) 2020-06-01 2021-03-30 The Procter & Gamble Company Low pH skin care composition and methods of using the same
US11583488B2 (en) 2020-06-01 2023-02-21 The Procter & Gamble Company Method of improving penetration of a vitamin B3 compound into skin
US11911498B2 (en) 2020-06-01 2024-02-27 The Procter & Gamble Company Low pH skin care composition and methods of using the same
CN111803416A (zh) * 2020-07-17 2020-10-23 堇色生物科技(中山)有限责任公司 一种含有显齿蛇葡萄的抗衰老面霜及其制备方法
CN112570726A (zh) * 2020-11-24 2021-03-30 山东省分析测试中心 二氢杨梅素功能化银纳米粒子及其绿色合成方法与应用
WO2023119230A1 (fr) 2021-12-22 2023-06-29 L'oreal Compositions de modulation de la voie de coagulation et de la voie de nicotinamide-adénine dinucléotide et leurs procédés d'utilisation

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