Whitening ingredients

Abstract

The present invention relates to personal care compositions that provide an even and bright skin tone by including in the topical composition a resorcinol derivative in combination with oil derived from Moringa seeds in a cosmetically acceptable carrier.

Description

[Technical Field]

[0001] The present invention relates to personal care compositions that provide a bright and even skin tone. [Background technology]

[0002] Many people consider the appearance of their skin, especially their face, to be an important indicator of their beauty and health. Therefore, a bright, blemish-free, and even skin tone is a desire for many. The degree and uniformity of skin pigmentation is affected by factors such as age, hormonal changes, acne breakouts, and exposure to sunlight and air pollution. These factors can lead to dark spots, freckles, hyperpigmentation in specific areas of the skin, and dark circles under the eyes. Many believe that certain lifestyle factors, such as hydration (amount of water consumed), type of diet, and quantity and quality of sleep, also affect skin appearance, including dark circles under the eyes. Recognizing that changes such as living a healthier lifestyle can take a long time to even out skin appearance, people turn to cosmetics that provide a temporary solution to dark spots. People also seek products that reduce darkening caused by sun exposure. To address this need, numerous attempts have been made to develop products that reduce pigment production in melanocytes.

[0003] The present inventors have been working in this field for many years, filing several patent applications and bringing various cosmetic products to market, and have specifically sought a highly effective solution to this problem that could also be used as a general cosmetic product to achieve a uniform and bright complexion, especially on exposed skin surfaces. Summary of the Invention [Problem to be solved by the invention]

[0004] Through extensive research to understand the factors and active ingredients that influence pigmentation, and through exploration into two seemingly unrelated areas, the human skin microbiome, the inventors surprisingly discovered that combining a known skin-lightening active ingredient, a resorcinol derivative, with moringa seed oil, which is fermented by resident skin bacteria and found to be a suitable prebiotic for the skin microbiome, interacts synergistically to produce a more even and brighter skin tone. Moringa oil has been used safely on the skin for many years, providing a natural alternative to chemical active ingredients that some people may find harsh. To the inventors' knowledge, no combination of active ingredients has previously been known to produce such an effect.

[0005] It is therefore an object of the present invention to provide a solution to the problem of uneven skin appearance by providing a topical composition that imparts a uniform and bright skin appearance.

[0006] Another object of the present invention is to provide a solution containing active ingredients that are known to be gentle and safe on the skin. [Means for solving the problem]

[0007] A first aspect of the present invention is (a) Moringa seed oil; (b) substituted resorcinols; and (c) Cosmetically acceptable carriers 1. A personal care composition comprising: The present invention relates to a personal care composition in which the moringa seed oil is fermented by normal skin bacteria.

[0008] Another aspect of the present invention relates to a method of lightening the skin comprising applying to the skin the composition of the first aspect. DETAILED DESCRIPTION OF THE INVENTION

[0009] These and other aspects, features, and advantages will become apparent to those skilled in the art upon reading the following detailed description and the appended claims. For the avoidance of doubt, any feature of one aspect of the present invention can be utilized in any other aspect of the present invention. The term "comprising" is intended to mean "including," but not necessarily "consisting of" or "composed of." In other words, the steps or options described need not be all-inclusive. It should be noted that the examples described below are intended to clarify the invention but are not intended to limit the invention to the examples themselves. Similarly, unless otherwise indicated, all percentages are weight / weight percent and can be abbreviated as "wt%." Except in the examples and comparative examples, or unless explicitly stated, all numbers in this "Detailed Description" and "Claims" describing amounts of materials or reaction conditions, physical properties of materials, and / or uses should be understood to be modified by the word "about." Numerical ranges expressed in the format "from x to y" are understood to include both x and y. When multiple preferred ranges for a particular feature are stated in the format "from x to y," it is understood that all ranges combining the different endpoints are also contemplated.

[0010] The compositions of the present invention are intended for use in personal care or cosmetic applications and may also be referred to as personal care compositions or cosmetic compositions. As used herein, "personal care composition" is meant to include compositions for topical application, i.e., application to the external surface of human skin. Such compositions can be classified as leave-on or rinse-off and include products applied to the human body for appearance improvement, cleansing, odor control, or general beauty. The compositions are preferably leave-on. The compositions of the present invention can be in the form of a liquid, lotion, cream, foam, stick, serum, essence, or gel. Preferred compositions include leave-on gels, lotions, serums, or creams, preferably in the form of a cream. As used herein, "skin" includes the skin of the face and body (e.g., neck, chest, back, arms, underarms, hands, feet, and scalp), particularly exposed areas thereof.

[0011] The present invention provides a personal care composition comprising moringa seed oil; a substituted resorcinol; and a cosmetically acceptable carrier, wherein the moringa seed oil is fermented by normal skin bacteria (the composition).

[0012] The genus Moringa includes approximately 14 species (among which Moringa peregrina, M. aptera, M. concanensis, M. drouhardii, M. hildebrandtii, and M. longituba), of which Moringa pterygosperma is the most well-known. Moringa seeds are characterized by the presence of oil, the content of which may vary from 20 to 80% depending on the seed type and maturity. For the species Moringa oleifera, the oil content reported in the literature ranges from 21 to 34%.

[0013] A comparison of the seed oils of Moringa oleifera, M. peregrina, M. concanensis, and M. drouhardii shows that the fatty acid content is very similar, and all of these oils contain primarily oleic acid with some saturated fatty acids. Preferably, the oil is extracted from the seeds of at least one of Moringa oleifera, Moringa pterygosperma, Moringa peregrina, Moringa concanensis, or Moringa drouhardii. It is particularly preferred that the oil be extracted from Moringa oleifera or Moringa pterygosperma. Preferably, the amount of oil in the composition of the present invention is 0.015-0.4% by weight. The oil is rich in oleic acid fatty acids. It is particularly preferred that the moringa seed oil used in the present invention contains 60-80% oleic acid and 2-10% palmitic acid.

[0014] In Int. J. Mol. Sci. 2016, 17, 2141;doi:10.3390 / ijms17122141, Leone et. al. disclose a literature review on the composition of moringa oil.

[0015] Preferably, the oil is extracted almost completely by solvent extraction, particularly with n-hexane, more preferably at an extraction ratio of 3:1 to 8:1 (by weight). Alternatively, the oil is extracted by cold pressing. Cold pressing has been reported to extract about 69% (on average) of the total oil contained in the seeds.

[0016] The composition comprises moringa seed oil fermented by normal skin flora, preferably Staphylococcus epidermidis, Staphylococcus hominis, Cutibacterium acnes, Micrococcus luteus, Corynebacterium species (e.g., Corynebacterium xerosis, Corynebacterium pseudogenitalium, and Corynebacterium tuberculostearicum). Examples of moringa seed oil include one or more species of Moringa tuberculostearicum. Moringa seed oil is preferably contained in an amount of 0.01 to 1 wt %, preferably 0.05 to 1 wt %, preferably 0.1 to 1 wt %, preferably 0.5 to 1 wt % of the composition. The effects of the present invention are expected to be obtained when (unfermented) Moringa seed oil in the composition of the present invention is applied to the skin. When applied in this manner, Moringa seed oil is expected to interact with the aforementioned resident bacteria, such as S. epidermidis, which is normally present on the skin, and ferment the Moringa seed oil in situ on the skin, thereby exerting the same effects as when Moringa seed oil is fermented ex situ. Therefore, the Moringa seed oil used in the present composition can be fermented either ex situ or in situ by resident skin bacteria.

[0017] "Resorcinol" is a dihydroxyphenolic compound (i.e., 1,3-dihydroxybenzene) characterized by alcohol groups (—OH) at the 1- and 3-positions. The chemical structure of resorcinol may be modified to result in substituted resorcinols characterized by at least one substituent at the 2-, 4-, 5-, or 6-position. Preferably, the resorcinol contains at least one substituent containing 2 to 11 carbon atoms, preferably 2 to 8 carbon atoms, and most preferably 2 to 6 carbon atoms. It is particularly preferred that at least one substituent contains an alkyl group. The resorcinol compound contained in the cosmetic composition of the present invention is an oil-soluble substituted resorcinol.

[0018] Preferably, the resorcinol in the cosmetic composition is substituted only at the 4-position, preferably with an alkyl group. Illustrative, non-limiting examples of substituted resorcinols include 4-ethylresorcinol, 4-hexylresorcinol, 4-phenylethylresorcinol, 4-cyclopentylresorcinol, 4-cyclohexylresorcinol, 4-octylresorcinol, and mixtures thereof. Preferred substituted resorcinols for use in the present invention are one or both of 4-ethylresorcinol and 4-hexylresorcinol; most preferred is 4-hexylresorcinol. The composition preferably comprises 0.00001 to 1%, preferably 0.0001 to 1%, preferably 0.001 to 1%, preferably 0.01 to 1%, and preferably 0.1 to 0.5%, e.g., 0.25%, by weight of the cosmetic composition of the substituted resorcinol, including all ranges encompassed therein.

[0019] An advantage of the present invention is that by including fermented moringa seed oil, a natural source, it has been found that it is preferable to include much less of a synthetic active, such as a substituted resorcinol, to achieve the same efficacy.

[0020] Without wishing to be bound by theory, the inventors believe that the combination of active ingredients acts to provide the benefits of the present invention by inhibiting the activity and levels of the enzyme tyrosinase in melanocytes.

[0021] The composition preferably has a Hansen total solubility parameter (δ) in the range of 16.5 to 22. t The composition preferably comprises an oil having a saturation value of 0.05 to 0.15. The preferred oil may be selected from one or more of isopropyl myristate, isopropyl palmitate, caprylic / capric triglyceride, and benzyl alcohol. These oils are preferably present in an amount of 8 to 25% by weight of the composition.

[0022] The composition of the present invention preferably contains an emulsifying polymer, which is preferably a swellable polymer powder made of pure acrylic acid monomers or a mixture of acrylic acid monomers and methacrylic acid monomers, and preferably an acrylate / C 10-30 The polymer may be a polymer having the chemical name alkyl acrylate crosspolymer, carbomer, or a mixture thereof. In one embodiment, the polymer is a crosslinked homopolymer or a non-crosslinked homopolymer. In another embodiment, the polymer is a crosslinked copolymer or a non-crosslinked copolymer. The emulsifying polymer is multifunctional and can emulsify the composition, stabilize the composition, and / or build the viscosity of the composition. It is within the scope of the present invention to use the polymeric emulsifier alone or in combination with other additional polymeric emulsifiers. Exemplary non-limiting acrylate / C for use in the cosmetic composition of the present invention include: 10-30Alkyl acrylate crosspolymers are commercially available from The Lubrizol Corporation under trade names such as PEMULEN® TR-1, PEMULEN® TR-2, PEMULEN® EZ-4U, CARBOPOL® Ultrez 20, CARBOPOL® Ultrez 21, CARBOPOL® 1382, and CARBOPOL® ETD 2020. Preferred carbomers for use in the compositions of the present invention include CARBOPOL® Ultrez 10 and CARBOPOL® 980, both of which are commercially available from The Lubrizol Corporation. The emulsifying polymer is present in the cosmetic composition in an amount of 0.01 to 5% by weight of the composition, preferably 0.02 to 4% by weight, and more preferably 0.03 to 3% by weight. More preferably, the polymer is present in the cosmetic composition at 0.04 to 2% by weight of the cosmetic composition, and most preferably at 0.05 to 1% by weight, including all ranges therein.

[0023] The compositions of the present invention may further comprise one or more of a sunscreen, a light stabilizer, a whitening agent, a wrinkle reducing agent, and a colorant.

[0024] The composition may further comprise an organic sunscreen selected from one or both of UVA sunscreens and UVB sunscreens. Sunscreens include materials commonly used to block ultraviolet rays. Exemplary compounds are PABA, cinnamate, and salicylate derivatives. For example, avobenzophenone (Parsol 1789®), octyl methoxycinnamate, and 2-hydroxy-4-methoxybenzophenone (also known as oxybenzone) can be used. Octyl methoxycinnamate and 2-hydroxy-4-methoxybenzophenone are commercially available under the trade names Parsol MCX and Benzophenone-3, respectively. The exact amount of sunscreen used in the composition can vary depending on the desired degree of protection from the sun's ultraviolet rays. Additives that reflect or scatter sunlight can also be used. These additives include oxides such as zinc oxide and titanium dioxide.

[0025] The compositions of the present invention may further comprise a cosmetically acceptable carrier, which may act as a diluent, dispersant, and / or carrier for the active agents used in the composition to facilitate their distribution when the composition is applied to the skin. Cosmetically acceptable vehicles suitable for use in the present invention may be aqueous, anhydrous, or emulsion-based; preferably, they are aqueous or emulsion-based, with the emulsion being a water-in-oil emulsion or an oil-in-water emulsion, the latter being most preferred. Water, when present, typically constitutes the balance of the composition. Preferably, water is present in a concentration of 5 to 99% by weight of the composition, more preferably 20 to 80% by weight, and even more preferably 40 to 80% by weight.

[0026] The composition of the present invention can be delivered in the form of a serum, cream, lotion, or gel, preferably in the form of a cream. A preferred solid form of the composition is a cream, more preferably a cream having a vanishing cream base. The vanishing cream base contains 3 to 25% by weight of a fatty acid. Optionally, the composition may contain 0.1 to 10% by weight of soap. If present, the fatty acid is preferably a C10 to C22 fatty acid, more preferably a C16 to C18 fatty acid. Most preferably, the fatty acid is stearic acid or palmitic acid or a mixture thereof, and the soap is preferably a potassium salt of the fatty acid mixture. The fatty acid is often hystric acid, which is essentially (generally about 90 to 95%) a mixture of 45% stearic acid and 55% palmitic acid. The most preferred cream is a cream having 3 to 25% by weight of a fatty acid and 0.1 to 10% by weight of soap.

[0027] Preferably, the composition comprises an emollient. Examples of emollients that may be used in the leave-on composition include stearyl alcohol, glyceryl monoricinoleate, mink oil, isopropyl isostearate, isobutyl palmitate, isocetyl stearate, oleyl alcohol, isopropyl laurate, hexyl laurate, decyl oleate, octadecane-2-ol, isocetyl alcohol, eicosanyl alcohol, behenyl alcohol, cetyl palmitate, silicone oils such as dimethylpolysiloxane, dibutyl sebacate, isopropyl myristate, palmitate, sorbitan isostearate ... Isopropyl myristate, isopropyl stearate, butyl stearate, polyethylene glycol, triethylene glycol, lanolin, cocoa butter, corn oil, cottonseed oil, olive oil, palm kernel oil, rapeseed oil, safflower seed oil, evening primrose oil, soybean oil, sunflower seed oil, avocado oil, sesame seed oil, coconut oil, peanut oil, castor oil, acetylated lanolin alcohol, petrolatum, mineral oil, butyl myristate, isopropyl linoleate, lauryl lactate, myristyl lactate, decyl oleate, myristyl myristate, and mixtures thereof.

[0028] Preferably, the composition contains a solvent. Examples of solvents that can be used in the composition include ethyl alcohol, isopropanol, acetone, ethylene glycol monoethyl ether, diethylene glycol monobutyl ether, diethylene glycol monoethyl ether, and mixtures thereof. The composition can contain a polyhydric alcohol that can be selected from one or more of glycerin, 1,3-butylene glycol, propylene glycol, 1,3-propanediol, pentylene glycol, hexylene glycol, and sorbitol.

[0029] Preferably, the composition comprises a powder, examples of which include chalk, talc, Fuller's earth, kaolin, starch, gum, colloidal silica, sodium polyacrylate, tetraalkyl and / or trialkylarylammonium smectite, chemically modified magnesium aluminum silicate, organically modified montmorillonite clay, hydrated aluminum silicate, fumed silica, carboxyvinyl polymer, sodium carboxymethylcellulose, ethylene glycol monostearate, and mixtures thereof.

[0030] Preferably, the composition contains a preservative to protect against the growth of potentially harmful microorganisms. Examples of ingredients that can be used as preservatives in the composition include alkyl esters of parahydroxybenzoic acid, hydantoin derivatives, propionate salts, and various quaternary ammonium compounds. More preferably, ingredients that can be used as preservatives in the composition are sodium benzoate, iodopropynyl butylcarbamate, methylisothiazolinone, iodopropynyl butylcarbamate, phenoxyethanol, methylparaben, propylparaben, imidazolidinyl urea, sodium dehydroacetate, ethylhexylglycerin, benzyl alcohol, alkanediols, and mixtures thereof. When present in the composition, the preservative is preferably added in an amount of 0.001 to 5% by weight, more preferably 0.01 to 3% by weight, most preferably 0.02 to 2% by weight, and even more preferably 0.25 to 1.5% by weight.

[0031] Preferably, the composition contains a range of other optional ingredients including antioxidants, binders, buffers, colorants, astringents, fragrances, opacifiers, conditioners, exfoliants, pH adjusters, skin sensates, skin soothing and skin healing agents, and the like.

[0032] It is within the scope of the present invention that the compositions claimed herein are environmentally friendly and, therefore, free of certain ingredients that are increasingly associated with long-term harm to the environment. Accordingly, one embodiment of the present invention relates to compositions that preferably do not contain sulfate surfactants. Another embodiment relates to compositions herein that preferably do not contain preservatives. Yet another embodiment relates to compositions that preferably do not contain acrylate polymers. Also within the scope of the present invention are compositions that preferably do not contain titanium dioxide. Green (i.e., biodegradable) chelating agents are preferred for use in such compositions, i.e., the compositions preferably do not contain traditional chelating agents such as EDTA. According to the present invention, "free" of a particular ingredient means that the composition contains less than 0.1% by weight of the composition, preferably less than 0.05% by weight, and more preferably less than 0.01% by weight of the ingredient. Optimally, they are not present in the composition.

[0033] The packaging for the compositions of the present invention may be a patch, bottle, tube, roll-ball applicator, propellant-driven aerosol device, squeeze container, or lidded jar.

[0034] In an alternative aspect, the present invention relates to the use of a composition according to the invention for skin lightening, preferably the use being non-therapeutic or cosmetic in nature.

[0035] In yet another aspect, the present invention relates to a method of providing lightness or even tone to human skin, said method comprising applying to said skin a composition according to the present invention. Preferably, the use is non-therapeutic or cosmetic in nature.

[0036] In yet another aspect of the present invention, there is provided a method of providing microbiome benefits to skin, said method comprising applying to said skin a composition according to the present invention. Preferably, the use is non-therapeutic or cosmetic in nature.

[0037] The invention will now be illustrated by the following non-limiting examples. [Example]

[0038] Examples A to K, 1 to 4: Percentage of melanin reduction achieved with the active agent combination according to the invention and the control Various samples containing the actives were prepared and the % reduction in melanin was measured. The protocol for measuring melanin reduction is outlined below.

[0039] Co-cultures of HaCat keratinocytes and primary human melanocytes were mixed in a 1:1 ratio of 40,000 cells per well in 1 mL of a 1:1 mixture of the respective culture media and seeded into each well of a 12-well plate. After 24 hours, the cultures were treated with various concentrations of the test substances listed in Table 1 and then incubated for an additional 72 hours. A comparative vehicle control was also prepared. To estimate melanin content after 72 hours of incubation, cell viability was first measured using the calcein AM method. Briefly, the spent medium was removed, and the cells were washed once with 0.4 mL / well of 1x PBS. Fresh PBS buffer containing 1 μM calcein AM was added to each well, including the cell-free control well. The plate was covered with aluminum foil and incubated at 37°C in a CO2 incubator for 30 minutes. Calcein fluorescence was measured using a TECAN M1000 plate reader (excitation wavelength 490 nm, emission wavelength 520 nm). The solution was removed from the culture wells, dissolved in 1N NaOH containing 10% DMSO, and placed in a shaker incubator at 60°C for 1 hour. 100 μL of the supernatant was transferred to a 384-well plate, and melanin was measured using a TECAN plate reader (405 nm filter). Melanin content (MC) was expressed after correcting for cell number (MC / calcein) and expressed as % melanin.

[0040] The following samples shown in Table 1 were prepared and the measured melanin reduction rate (%) for each sample is also shown in the table.

[0041] Table 1 [Table 1]

[0042] In the above table, Moringa seed oil was obtained from Naturex SA, France.

[0043] Moringa oil was fermented as follows.

[0044] Tryptic soy agar (TSA) was prepared and autoclaved. After pouring the medium onto TSA plates and allowing it to solidify, S. epidermidis (ATCC 12228) was streaked onto the plates from a glycerol stock and incubated for 24 hours. Moringa oil was dissolved in DMSO and added to autoclaved tryptic soy agar (TSB) at the required concentrations of 0.05% and 0.01%. A 0.3 OD pure bacterial culture was prepared and inoculated into autoclaved TSB containing moringa oil and incubated in a shaker incubator at 120 rpm for 24 hours at 37°C (in a sample cup). After 24 hours of incubation, the OD was measured to confirm that the bioactive substances were not interfering with bacterial growth. The culture was transferred to a centrifuge tube and centrifuged at 6500 rpm for 10 minutes. The supernatant was sterilized by filtration using a membrane filter, aliquoted into 1 mL aliquots, stored at -80°C, and subjected to testing in skin cell cultures.

[0045] S. epidermidis-fermented moringa oil samples were diluted 1:40 in keratinocyte + melanocyte media mix and then introduced into the co-culture for melanin content assay.

[0046] The data in Table 1 above demonstrate that a composition according to the present invention (Example 1) significantly reduces melanin content compared to the use of 0.0002% 4-HR (Example B). It has been observed that the use of 4-HR at concentrations greater than 0.0002% (at the cellular level in in vitro experiments) can cause problems with cell viability. Furthermore, Example 3 demonstrates a synergistic interaction between 4-HR and Moringa seed oil.

[0047] It should be understood that the experiments described above were performed in in vitro assays. It is expected that the concentrations actually used to prepare compositions for topical use will vary significantly. These concentrations may be orders of magnitude higher due to the following factors, which affect the difference in bulk concentration compared to cellular concentration: The compositions may be formulated as emulsions or gels containing numerous additional ingredients. The concentrations of the desired active substance in the oil and aqueous phases may be significantly different. They may also have significantly different physical and hydrodynamic properties, such as partition coefficients, diffusion rates, convective transport rates, and rheological properties. Therefore, it is expected that the concentrations used when formulating compositions may differ significantly from those assessed at the cellular level. The concentrations used in formulated compositions are typically significantly higher than those used in in vitro experiments at the cellular level, typically by two to three orders of magnitude.

Claims

1. (a) Moringa seed oil; (b) substituted resorcinols; and (c) A cosmetically acceptable carrier 1. A personal care composition comprising: A personal care composition in which the moringa seed oil is fermented by normal skin bacteria.

2. 2. The composition of claim 1, wherein the substituted resorcinol comprises one or more of 4-hexylresorcinol, 4-ethylresorcinol, 4-phenylethylresorcinol, 4-cyclopentylresorcinol, 4-cyclohexylresorcinol, and 4-octylresorcinol.

3. 3. The composition of claim 2, wherein the substituted resorcinol comprises one or both of 4-hexylresorcinol and 4-ethylresorcinol, preferably 4-hexylresorcinol.

4. The composition of any one of claims 1 to 3, comprising 0.00001 to 1% by weight of the substituted resorcinol.

5. 4. The composition of claim 1, wherein the moringa seed oil comprises 60-80% oleic acid and 2-10% palmitic acid.

6. The composition according to any one of claims 1 to 3, wherein the normal skin flora is one or more of Staphylococcus epidermidis, Staphylococcus hominis, Cutibacterium acnes, Micrococcus luteus, and Corynebacterium sp.

7. 4. The composition of claim 1, comprising 0.01 to 1% by weight of moringa seed oil.

8. 4. The composition according to any one of claims 1 to 3, wherein the cosmetically acceptable carrier comprises an oil, preferably selected from one or more of isopropyl myristate, isopropyl palmitate, caprylic / capric triglyceride and benzyl alcohol.

9. The cosmetically acceptable carrier is preferably an acrylate / C copolymer, which is present in an amount of 0.01 to 5% by weight of the composition. １０－３０ The composition of any one of claims 1 to 3, comprising an emulsifying polymer selected from one or more of alkyl acrylate crosspolymers and carbomers.

10. A composition according to any one of claims 1 to 3 in the form of a serum, cream, lotion or gel, preferably in the form of a serum or cream.

11. A method for providing an even skin tone, comprising applying to the skin a composition according to any one of claims 1 to 3.

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