Skincare composition

Abstract

To provide a personal care composition that improves the appearance of pale-looking skin by applying to the skin a composition capable of improving bilirubin decomposition, and to provide a skin care composition that can provide skin care benefits in addition to the bilirubin decomposition effect.SOLUTION: Methods and compositions for improving the appearance of skin are provided. The methods and compositions are particularly suited for improving the appearance of pale-looking skin by enhancing the decomposition of bilirubin in the skin. The methods and compositions herein utilize one or more sucrose esters that demonstrate a surprising ability to reduce bilirubin levels. The methods comprise applying a skin care composition containing an effective amount of a sucrose ester to a target area of the skin where reduced bilirubin levels are desired.SELECTED DRAWING: None

Description

[Technical Field]

[0001] This disclosure relates, in general, to skincare compositions for treating skin tone conditions. More specifically, this disclosure relates to a method for providing a bilirubin-degrading effect using an effective amount of sucrose ester. [Background technology]

[0002] Poor complexion or a yellowish appearance of skin is generally associated with poor health or aging, and various physiological and environmental factors may be at play. For example, yellowish or poorly complexion of skin is well known to be caused by the accumulation of a yellow pigment known as bilirubin. Bilirubin, for instance, is responsible for the yellowish discoloration of skin associated with bruises or jaundice. Bilirubin is produced as a result of the catabolic breakdown of heme in red blood cells when old or damaged cells are removed from the body. Typically, bilirubin is processed by the liver and then excreted from the body as waste. Therefore, it would be desirable to provide methods to improve the appearance of yellowish or poorly complexion of skin associated with bilirubin accumulation.

[0003] One known method to reduce bilirubin levels in the skin is phototherapy (also known as light therapy). Certain wavelengths of light react with bilirubin, converting it into a form that is more easily processed and eliminated by the body. Phototherapy is one of the common forms used to treat undesirable high bilirubin levels (i.e., hyperbilirubinemia) in newborns. However, phototherapy can require spending considerable time (e.g., 12–72 hours) under artificial light in an environment away from home (e.g., a hospital), which can be undesirable for many people suffering from such a condition. Therefore, it would be desirable to offer a more convenient method of breaking down bilirubin in the skin to improve the appearance of skin with a poor complexion.

[0004] Cosmetic compositions claiming to improve bilirubin breakdown are commercially available, and many, though not all, of these products are intended for use in improving the appearance of dark circles around the eyes. For example, Lipotec's Eyedeline® Marine Ingredients brand of cosmetic eye care products is said to improve the appearance of dark circles around the eyes, among other things, by improving bilirubin breakdown. Truthinaging.com discloses that cosmetic and beauty products containing N-hydroxysuccinimide, such as eye products available from AQ Skin Solution, activate the elimination of blood-derived pigments such as bilirubin that contribute to the appearance of dark circles around the eyes. In another example, a plant ingredient derived from the White Bird of Paradise flower (commercially available as Vivillume® from Lonza (New Jersey)) is said to break down bilirubin. A cosmetic product marketed by Avani (Spain) for treating dark circles around the eyes is advertised as containing Vivillume®. Eye treatment products are formulated to treat relatively small areas of skin present in the periorbital region of the face, and therefore may not be suitable for treating larger areas of skin to address cosmetic issues associated with the presence of bilirubin in the skin (e.g., pale-looking skin and / or uneven skin tone). In addition, at least some people with pale-looking skin also desire skincare products that address other cosmetic skin conditions such as fine lines, wrinkles, pigmented spots, and / or dull skin. [Overview of the Initiative] [Problems that the invention aims to solve]

[0005] Therefore, it is desirable to provide a personal care composition that improves the appearance of skin with poor blood circulation by applying a composition capable of improving bilirubin degradation to the skin. It is also desirable to provide a skincare composition that provides skincare effects in addition to bilirubin degradation effects. [Means for solving the problem]

[0006] A method for improving the appearance of the skin and / or a method for decomposing bilirubin in the skin are described herein. The method includes identifying a target portion of the skin of a person in whom a reduction in bilirubin is desired, and applying a composition comprising an effective amount of a sucrose ester selected from sucrose laurate, sucrose dilaurate, and / or sucrose trilaurate to the target portion of the skin during a treatment period, wherein the effective amount of the sucrose ester reduces bilirubin levels during the treatment period.

Brief Description of the Drawings

[0007] [Figure 1] It is a diagram showing the in vitro effect of sucrose ester on the b* value. [Figure 2] It is a diagram showing the in vitro effect of sucrose ester on bilirubin levels. [Figure 3] It is a diagram showing the in vivo effect of a sucrose ester composition on the yellowness of the skin. [Figure 4] It is a diagram showing the direct correlation between bilirubin levels and the b* value.

Modes for Carrying Out the Invention

[0008] The drawbacks associated with the presence and / or accumulation of bilirubin in the skin are well-known, but conventional treatments for reducing bilirubin levels in the skin, such as phototherapy, may not be suitable for all users. Prior to this discovery, it was not known that specific sucrose esters such as sucrose laurate, sucrose dilaurate, and sucrose trilaurate could be used to decompose bilirubin. Surprisingly, it has now been found that the appearance of skin with poor blood color and / or uneven skin tone can be improved using a skin care composition containing a sucrose ester.

[0009] References to “embodiments” in this specification mean that certain materials, features, structures, and / or properties described in relation to those embodiments are included in at least one embodiment, or optionally in a number of embodiments, but not that all embodiments incorporate the described materials, features, structures, and / or properties. Furthermore, materials, features, structures, and / or properties may be combined in any preferred manner across different embodiments, and materials, features, structures, and / or properties may be excluded from or substituted for those described. Accordingly, the embodiments and aspects described herein may include or be combined with elements or components of other embodiments and / or aspects, even if they are not explicitly illustrated in combination, unless otherwise specified or incompatible.

[0010] In all embodiments, unless otherwise stated, all percentages of ingredients are based on the weight of the cosmetic composition. Unless otherwise specified, all ratios are weight ratios. Significant figures do not represent limitations on the quantities indicated or on the precision of the measurements. Unless otherwise specified, all quantities are understood to be modified by the word “approximately”. Unless otherwise specified, all measurements are understood to have been made under ambient conditions of approximately 25°C, where “ambient conditions” means conditions of approximately 1 atmosphere and approximately 50% relative humidity. All numerical ranges are inclusive and can be combined to form narrower ranges not expressly disclosed. For example, separated upper and lower range limits are interchangeable in creating further ranges.

[0011] The compositions of the present invention include, are essentially composed of, or consist of the essential and optional components described herein. As used herein, “essentially composed of” means that a composition or component may contain only additional components that do not substantially alter the basic and novel properties of the claimed composition or method. As used herein and in the appended claims, the singular forms “a,” “an,” and “the” are intended to include the plural form unless the context clearly indicates otherwise.

[0012] definition "Approximately" modifies a specific value by referring to a range equal to plus or minus 20 percent (±20%) of the mentioned value, or a value lower than that (for example, 15%, less than 10%, or even less than 5%).

[0013] The term "agent" refers to a material and its components intended to provide a specific effect or function. For example, a emollient is a material (e.g., fatty alcohol) intended to provide a skin-softening effect, and a thickener is generally a material intended to increase the viscosity of a composition.

[0014] When used in relation to the composition, "apply" or "apply" means applying or spreading the composition of the present invention onto the surface of human skin, such as the epidermis.

[0015] "Bilirubin" has been identified with CAS number 635-65-4 and has the chemical formula C 33 H 36 This refers to N4O6 and compounds having the following structures.

[0016] [ka]

[0017] "Cosmetic composition" means a composition containing a cosmetic agent such as sucrose ester described in this specification. Examples of cosmetic compositions include color cosmetics (e.g., foundation, lipstick, concealer, and mascara), skin care compositions (e.g., moisturizers and sunscreens), personal care compositions (e.g., rinse-off and non-rinse-off body soaps and bar soaps), and hair care compositions (e.g., shampoos and conditioners).

[0018] As used herein, "derivative" means an amide, ether, ester, amino, carboxyl, acetyl, and / or alcohol derivative of a given compound.

[0019] "Effective amount" means an amount of a compound and composition sufficient to significantly induce a positive effect on keratinous tissue over the course of a treatment period. The positive effect can be an effect on health, appearance, and / or feel, including, independently or in combination, the effects disclosed herein. In certain embodiments, an effective amount of sucrose ester is an amount sufficient to reduce bilirubin levels.

[0020] "Improving appearance" means providing a significant desirable change or effect in the appearance of a person's skin, which can be quantified, for example, by a decrease in the b * value. Exemplary methods for determining appearance improvement are described in more detail below.

[0021] <​​​​​​​​​​​​​​(iii) the value of which indicates magenta, and the position of the color between yellow and blue (i.e., negative b * The value is shown in blue, and positive b * The value indicates yellow.

[0022] "A safe and effective dose" means an effective amount of an ingredient that is low enough to avoid serious side effects (within the bounds of sound medical judgment).

[0023] In this specification, "poor complexion" with respect to skin appearance means an abnormal and / or undesirable yellow or pale skin tone in relation to a particular individual, generally associated with an unhealthy condition. Skin with a poor complexion appearance is objectively (e.g., L * or b * It can be diagnosed using color values ​​such as those mentioned above, or subjectively (for example, by a skincare professional or through self-diagnosis by a consumer).

[0024] "Skincare" means the control and / or improvement of skin condition. Some non-exclusive examples include improving the appearance and / or feel of the skin by providing a smoother, more uniform appearance and / or feel; increasing the thickness of one or more layers of skin; improving the elasticity or resilience of the skin; improving skin firmness; reducing the oily, shiny and / or dull appearance of the skin; improving the moisture content or hydration of the skin; improving the appearance of fine lines and / or wrinkles; improving exfoliation or desquamation of the skin; plumping the skin; improving skin barrier properties; improving skin tone; reducing the appearance of redness or skin blemishes; and / or improving skin brightness, radiance or clarity.

[0025] "Skincare active substances" refer to compounds or combinations of compounds that, when applied to the skin, produce acute and / or chronic effects on the skin or a type of cell normally found in the skin. Skincare active substances can modulate and / or improve the skin or related cells (e.g., improve skin elasticity, skin moisture content, skin barrier function, and / or cellular metabolism).

[0026] "Skincare composition" means a composition that contains skincare active substances and modulates and / or improves the condition of the skin.

[0027] "Skin tone" refers to the overall appearance of basic skin color or uniformity of color. Skin tone is typically characterized over a larger area of ​​skin, including the entire face or other body skin surfaces (e.g., arms, legs, back, hands, neck, chest, and abdomen), and this is generally 100 mm². 2 It exceeds [value]. Skin tone can be measured by image analysis. One measure of skin tone is brightness, L * a * b * L in the color space * Skin tone can be measured using coordinates (International Commission on Illumination). Chromophore mapping, such as melanin and / or bilirubin mapping, can also be used as an indicator of skin tone. The mean values ​​of melanin and / or bilirubin can be calculated from chromophore map data. In addition, skin tone may correlate with the uniformity of melanin and / or bilirubin (e.g., standard deviation), and melanin uniformity can also be calculated from chromophore map data.

[0028] As used herein, “treatment period” means the length of time and / or frequency over which the material or composition is applied to the target skin surface.

[0029] composition The compositions herein contain an effective amount of sucrose esters mediated by a dermatologically acceptable carrier and are intended for topical application to human skin. The amount of sucrose esters should be sufficient to demonstrate a bilirubin-degrading effect in vitro and / or sufficient to improve the appearance of skin with a poor complexion after a suitable treatment process (e.g., 2, 4, or 8 weeks). The compositions herein may also treat other skin conditions and may optionally contain one or more additional skin-active substances or other components of a type commonly found in topical skincare compositions. The skincare compositions herein can be prepared using conventional methods for combining skincare composition components.

[0030] The skincare compositions described herein may be cosmetic compositions, pharmaceutical compositions, or medicated cosmetic compositions, and can be provided in a variety of product forms, including but not limited to solutions, suspensions, lotions, creams, gels, toners, sticks, sprays, aerosols, ointments, cleansing liquids and solid bars, pastes, foams, mousses, shaving creams, wipes, strips, patches, electric patches, hydrogels, film-forming products, facial and skin masks (with and without insoluble sheets); and makeup such as foundations, eyeliners and eyeshadows. In some cases, the form of the composition may depend on a specific dermatologically acceptable carrier selected. For example, the composition (and carrier) may be provided in the form of an emulsion (e.g., water-in-oil, oil-in-water, or water-in-oil-in-water) or an aqueous dispersion.

[0031] Sucrose esters The compositions herein comprise effective amounts of sucrose esters selected from sucrose laurate, sucrose dilaurate, sucrose trilaurate, their derivatives, and combinations thereof. As used herein, "sucrose laurate" refers to a compound of formula C 24 H 44 O 12This refers to compounds having CAS#25339-99-5. "Sucrose dilaurate" is a compound with formula C 36 H 66 O 13 And it means a compound having CAS#25915-57-5, and "sucrose trilaurate" is a compound with formula C 48 H 88 O 14 This refers to compounds having CAS#94031-23-9. Sucrose esters may be present in amounts of 0.0001% to 15% by weight of the total composition (e.g., 0.0002% to 10% by weight, 0.001% to 15% by weight, 0.025% to 10% by weight, 0.05% to 7% by weight, 0.05% to 5% by weight, or even 0.1% to 3% by weight). In some cases, the sucrose ester may be a single sucrose ester (e.g., 100% sucrose laurate, sucrose dilaurate, sucrose trilaurate, or derivatives thereof) or a blend of two or three sucrose esters, where two or more sucrose esters are present in a ratio of 1:10 to 1:1 (e.g., 1:7, 1:5, 1:3, or 1:2) of any one sucrose ester to another. In some cases, the sucrose ester may be a blend of sucrose laurate and sucrose dilaurate, with sucrose laurate present in 50% to 80% by weight of the sucrose ester and sucrose dilaurate present in 20% to 45% by weight of the sucrose ester. Alternatively, the sucrose ester may be a blend of sucrose laurate, sucrose dilaurate, and sucrose trilaurate, with sucrose dilaurate present in 35% or more by weight of the sucrose ester. A preferred example of a sucrose ester for use herein is BC10034 from BASF, which is a blend of sucrose laurate and sucrose dilaurate. In the BC10034 sucrose ester material, the ratio of sucrose laurate to sucrose dilaurate may be in the range of 3:1 to 3:2.

[0032] Dermatologically acceptable carriers The bilirubin-degrading compositions herein include a dermatologically acceptable carrier (which may be referred to as the "carrier"). The term "dermatologically acceptable carrier" means that the carrier is suitable for topical application to keratinous tissue, has good aesthetic properties, is compatible with the active substances in the composition, and does not raise any unreasonable concerns regarding safety or toxicity. In one embodiment, the carrier is present at levels of about 50% to about 99% by weight, about 60% to about 98% by weight, about 70% to about 98% by weight, or or about 80% to about 95% by weight.

[0033] The carrier may take on a wide variety of forms. In some cases, the form and characteristics of the carrier can be determined by the solubility or dispersibility of its components (e.g., extracts, sunscreens, additional components). Non-limiting examples include simple solutions (e.g., aqueous or anhydrous), dispersions, emulsions, and solid forms (e.g., gels, sticks, fluid solids, or amorphous materials). In some cases, the dermatologically acceptable carrier is in the form of an emulsion. The emulsion may have a continuous aqueous phase (e.g., oil-in-water or water-in-oil-in-water emulsions) or a continuous oil phase (e.g., water-in-oil or oil-in-water-in-oil emulsions). The oil phase of the present invention may include silicone oils, hydrocarbon oils, non-silicone oils such as esters and ethers, and mixtures thereof. The aqueous phase typically includes water and water-soluble components (e.g., water-soluble humectants, conditioning agents, antimicrobial agents, wetting agents, and / or other skincare active substances). However, in some cases, the aqueous phase may contain components other than water, including but not limited to water-soluble humectants, conditioning agents, antimicrobial agents, wetting agents, and / or other water-soluble skincare active substances. In some cases, the non-aqueous components of the composition include wetting agents such as glycerin and / or other polyols.

[0034] In some cases, the compositions herein are in the form of oil-in-water ("O / W") emulsions that provide a light, non-greasy feel. Preferred O / W emulsions herein may contain more than 50% by weight of a continuous aqueous phase, with the remainder being a dispersed oil phase. The aqueous phase may contain 1% to 99% water, based on the weight of the aqueous phase, along with any water-soluble and / or water-miscible components. In these cases, the dispersed oil phase is typically present in less than 30% by weight of the composition (e.g., 1% to 20%, 2% to 15%, 3% to 12%, 4% to 10%, or even 5% to 8%) to help avoid some of the undesirable tactile effects of the oily composition. The oil phase may contain one or more volatile and / or non-volatile oils (e.g., vegetable oils, silicone oils, and / or hydrocarbon oils). Some non-limiting examples of oils that may be suitable for use in this composition are disclosed in U.S. Patent No. 9,446,265 and U.S. Patent Application Publication No. 2015 / 0196464.

[0035] The carrier may contain one or more dermatologically acceptable hydrophilic diluents. As used herein, “diluents” include materials that can disperse, dissolve, or otherwise incorporate sucrose esters. Examples of hydrophilic diluents include water, lower monohydric alcohols (e.g., C1-C4), and organic hydrophilic diluents such as low molecular weight glycols and polyols, which include propylene glycol, polyethylene glycol (e.g., molecular weight 200-600 g / mol), polypropylene glycol (e.g., molecular weight 425-2025 g / mol), glycerol, butylene glycol, 1,2,4-butanetriol, sorbitol esters, 1,2,6-hexanetriol, ethanol, isopropanol, sorbitol esters, butanediol, etherpropanol, ethoxylated ethers, propoxylated ethers, and combinations thereof.

[0036] Other optional components The compositions herein may contain one or more optional components known for use in topical skincare compositions, provided that the optional components do not alter the composition to an unacceptable degree. Additional components must be suitable for use in contact with human skin tissue without causing excessive toxicity, incompatibility, instability, allergic reactions, etc. If present, optional components may be included in the composition in an amount of about 0.001% to 50% by weight (e.g., 0.01% to 40% by weight, 0.1% to 30% by weight, 0.5% to 20% by weight, or 1% to 10% by weight). Some non-limiting examples of additional ingredients include vitamins, minerals, peptides and peptide derivatives, sugar amines, sunscreens, oil control agents, microparticles, flavonoid compounds, hair growth regulators, antioxidants and / or antioxidant precursors, preservatives, protease inhibitors, tyrosinase inhibitors, anti-inflammatory agents, moisturizers, exfoliants, skin whitening agents, sunscreens, sunless tanning agents, lubricants, anti-acne agents, anti-cellulite agents, chelating agents, anti-wrinkle active substances, anti-atrophy active substances, phytosterols and / or plant hormones, N-acyl amino acid compounds, antibacterial agents, and antifungal agents. Other non-limiting examples of additional ingredients and / or skincare active substances that may be suitable for use herein include U.S. Patent Application Publications 2002 / 0022040, 2003 / 0049212, 2004 / 0175347, 2006 / 0275237, 2007 / 0196344, 2008 / 0181956, 2008 / 0206373, 2010 / 00092408, 2008 / 0206373, 2010 / 0239510, 2010 / 0189669, and 2 It is described in Patent Nos. 010 / 0272667, 2011 / 0262025, 2011 / 0097286, 2012 / 0197016, 2012 / 0128683, 2012 / 0148515, 2012 / 0156146, and 2013 / 0022557, as well as in U.S. Patent Nos. 5,939,082, 5,872,112, 6,492,326, 6,696,049, 6,524,598, 5,972,359, and 6,174,533.

[0037] Conditioning agent The compositions herein may contain 0.1% to 50% by weight of conditioning agents (e.g., 0.5% to 30%, 1% to 20%, or even 2% to 15%). The addition of conditioning agents may help provide compositions having desirable tactile properties (e.g., a silky smooth feel upon application). Some non-limiting examples of conditioning agents include hydrocarbon oils and waxes, silicones, fatty acid derivatives, cholesterol, cholesterol derivatives, diglycerides, triglycerides, vegetable oils, vegetable oil derivatives, acetoglyceride esters, alkyl esters, alkenyl esters, lanolin, wax esters, beeswax derivatives, sterols and phospholipids, salts, isomers, and derivatives thereof, as well as combinations thereof. Particularly preferred examples of conditioning agents include volatile or non-volatile silicone fluids such as dimethicone copolyol, dimethylpolysiloxane, diethylpolysiloxane, mixed C1-30 alkylpolysiloxane, phenyldimethicone, dimethiconol, dimethicone, silicone crosspolymer, and combinations thereof. Dimethicone may be particularly preferred because some consumers associate the tactile properties provided by certain dimethicone fluids with good moisturizing properties. Other examples of silicone fluids that may be suitable for use as conditioning agents are described in U.S. Patent No. 5,011,681.

[0038] Rheologically modifying agents The compositions herein may contain 0.1% to 5% of a rheology modifier (e.g., a thickener) to provide compositions having suitable rheological and skin-touch properties. Some non-limiting examples of thickeners include cross-linked polyacrylate polymers, polyacrylamide polymers, polysaccharides, gums, and mixtures thereof. In particularly preferred examples, the compositions may contain superabsorbent polymer thickeners such as sodium polyacrylate, starch-grafted sodium polyacrylate, or combinations thereof. Some non-limiting examples of superabsorbent polymer thickeners are described, for example, in U.S. Patent No. 9,795,552.

[0039] Some consumers find compositions using silicone fluids as conditioning agents to have an undesirable greasy or heavy feel. Therefore, it may be desirable to provide compositions that do not contain or are substantially free of silicone fluids. It may also be desirable to adjust superabsorbent polymer thickeners to give compositions a light and airy feel by, for example, adjusting the amount of water in the composition, the water-to-oil ratio (e.g., between 12:1 and 1:1), and / or the ratio of water to thickener or oil to thickener.

[0040] emulsifier If the composition is in the form of an emulsion, it may contain an emulsifier. The emulsifier may be nonionic, anionic, or cationic. Suitable emulsifiers are disclosed, for example, in U.S. Patent Nos. 3,755,560 and 4,421,769, U.S. Patent Application Publication No. 2006 / 0275237, and McCutcheon's Detergents and Emulsifiers, North American Edition, pages 317-324 (1986). Suitable emulsions can have a wide range of viscosities depending on the desired product form.

[0041] When a composition in this specification contains any optional component, it may be desirable to select a component that does not form a complex with other components in the composition, particularly niacinamide, salicylates, and peptides (e.g., pH-sensitive components such as palmitoyl-lysine-threonine (pal-KT) or palmitoyl-lysine-threonine-threonine-lysine-serine (pal-KTTKS), or at least does not interact with them in an undesirable way). In particular, the additional component should not undesirably affect the ability of the sucrose ester to break down bilirubin. In some cases, it may be desirable to select skincare active ingredients that function through different biological pathways so that active ingredients that could reduce the effectiveness of both agents do not interfere with each other.

[0042] How to use This method comprises identifying a target area of ​​skin of a person requiring treatment, and applying a composition comprising, during the treatment period, one or more sucrose esters described herein and optionally one or more additional skincare agents to the target area of ​​skin. The target area of ​​skin may be on the surface of the face (forehead, perimum of mouth, chin, perimum of orbit, nose, and / or cheeks) or on another part of the body (e.g., hands, arms, legs, back, chest). A person requiring treatment may be a person with undesirable levels of bilirubin in the skin and / or another person with an undesirable cosmetic skin condition. Bilirubin levels can be determined according to any suitable method known in the art. For example, bilirubin levels can be determined by blood sample analysis. In another embodiment, a certain threshold level corresponding to an undesirable high bilirubin level is exceeded. * If the target area of ​​the skin has a value, an undesirable bilirubin level may be indicated. *The values ​​can be determined according to the color imaging methods detailed below. In some cases, a person may be identified as requiring treatment if their skin has a yellowish or sallow appearance, and / or if they have an uneven skin tone. In another embodiment, a person may be identified as requiring treatment if a professional (e.g., a dermatologist or cosmetics professional) determines that an undesirable level of yellowness is present in a target area of ​​skin. A person requiring treatment may also be identified if a target area of ​​skin is present. In some cases, a target area of ​​skin may not appear to be suffering from bilirubin accumulation, but the user (e.g., a person with or prone to jaundice or bruising) may still wish to treat the target area of ​​skin as a precautionary measure (e.g., a person prone to developing conditions that cause bilirubin accumulation, such as jaundice).

[0043] The composition can be applied daily to the target area of ​​skin and, if desired, to the surrounding skin at least once, twice, or more times during the treatment period. When applied twice daily, there should be an interval of at least 1 to 12 hours between the first and second applications. The composition is typically applied in the morning and / or before going to bed at night. When used according to the method herein, the composition contains, for example, at least 5% (e.g., at least 10%, 15%, 20%, 25%, or more) of b * As demonstrated by the reduction, reducing bilirubin levels improves the appearance of the skin. In some cases, the reduction of bilirubin levels can be determined by measuring bilirubin levels according to conventional in vivo methods (e.g., blood analysis) and comparing the measured level to a predetermined threshold or a baseline level of bilirubin measured before the start of the treatment period.

[0044] The treatment period is, ideally, a period of time sufficient for the sucrose esters present in the composition to reduce bilirubin levels in the target area of ​​the skin. In some cases, the bilirubin-reducing effect provided by the sucrose esters is determined by a certain b *value (i.e., b * b compared to baseline value or threshold * This can be demonstrated by a reduction in the value. In addition, the bilirubin reduction effect is measured by b * The values ​​and / or bilirubin levels can be demonstrated by comparing them to a control value (e.g., a vehicle control) or other reference value. The treatment period may last for at least one week (e.g., about two, four, eight, or even twelve weeks). In some cases, the treatment period may extend to several months (i.e., three to twelve months). In some cases, during a treatment period of at least two, four, eight, or twelve weeks, the composition may be applied at least once a day, or even twice a day, for most of the days of the week (e.g., at least four, five, or six days a week).

[0045] The process of applying the composition can be carried out by topical application. The terms “topical,” “local,” or “spot-based” in relation to the application of the composition mean delivering the composition to a target area (e.g., a pigmented blemish or part thereof) while minimizing delivery to skin surfaces that do not wish to be treated. The composition can be applied to a skin area and gently massaged in. The form of the composition or a dermatologically acceptable carrier should be selected to facilitate topical application. While certain embodiments herein envision the topical application of the composition to a certain area, it will be understood that the compositions herein may be applied further systemically or extensively to one or more skin surfaces. In certain embodiments, the compositions herein may be used as part of a multi-step cosmetic procedure, in which the composition may be applied before and / or after one or more other compositions.

[0046] method Bilirubin degradation assay This assay provides an in vitro method for determining how a material or composition affects bilirubin degradation. Three replicas of each test sample are prepared in a 96-well plate (e.g., FALCON brand 96-well tissue culture plate or equivalent) at a total volume of 250 μL / well. A stock solution of 250 ug / mL indirect bilirubin (i.e., the unconjugated form of bilirubin most commonly found in serum) is prepared by dissolving bilirubin powder (Cayman Chemicals Company, catalog no. 17161) in DMSO (Sigma, catalog no. D8414-100 mL) to obtain a stock solution at a 10-fold working concentration. The working concentration of bilirubin is set to 25 ug / mL in all wells except the negative / vehicle control well. Each test well contains 25 ul of 250 ug / mL bilirubin stock solution, 200 ul of PBS, and 25 ul of 10-fold treated stock solution prepared with DMSO. For 0.01% (w / v) sucrose ester treatment, a 10-fold concentrated 0.1% (w / v) stock was prepared with DMSO. Naturally, the amount of DMSO can be adjusted depending on the solubility of the active substance (e.g., 80% or more DMSO for water-insoluble active substances such as the sucrose esters specified herein), and it should be understood that a stable solution for testing can be provided. In the negative / vehicle control wells, DMSO was mixed with PBS to achieve the same final DMSO concentration as the test wells (e.g., 80% (v / v) or higher). In the positive control wells, 25 µl of 250 µg / ml bilirubin stock prepared with DMSO, 200 µl of PBS (AccuGENE, catalog number 51225), and sufficient DMSO were added to achieve the same final DMSO concentration as the test wells.

[0047] The plate containing the test sample was covered with aluminum foil and placed on a microplate shaker (VWR, catalog no. 12620-938). Incubation was performed at room temperature for 20 hours with constant shaking at 150 rpm. After 20 hours of incubation, the bilirubin concentration was quantified, and the effect of bilirubin degradation was determined as a result of the active treatment compared to a positive bilirubin control. A commercially available bilirubin quantification kit (Cell Biolab, catalog no. MET-5010) was used for bilirubin quantification. The assay is based on the Jendrassik-Grof method, in which diazotized sulfanilic acid reacts with bilirubin to form azobilirubin, which can be detected at an OD of 540 nm. A standard bilirubin curve is generated using the same bilirubin used for processing and quantification. Table 1 below describes the standard curve settings.

[0048] [Table 1]

[0049] Bilirubin concentrations in all test legs are calculated using linear regression to a standard bilirubin curve. The bilirubin concentrations obtained after administration are compared to those in the bilirubin-positive control leg. Bilirubin degradation activity can be confirmed by a paired Student's t-test (P<0.05) by the decrease in bilirubin levels between the administered leg and the bilirubin-positive control leg. [Examples]

[0050] Example 1: Formulation Table 2 below provides an example of a topical skincare composition containing sucrose esters. This exemplary composition is prepared by blending the A phase components in a suitable mixer (e.g., Tekmar RW20DZM or equivalent), heating to a temperature of 70-80°C, and maintaining that temperature while stirring. Separately, the B phase components are blended in a suitable mixer and heated to 70-75°C, maintaining the temperature while mixing. Phase B is added to Phase A and mixed thoroughly at the same time to form an oil-in-water (O / W) emulsion. The emulsion is then ground for 5 minutes using a suitable mill (e.g., Tekmar T-25 or equivalent). When the emulsion is 60°C, Phase C is added while continuing to mix. At 40°C, the components of Phases D and E are added to the emulsion. The emulsion is then ground for 5 minutes to obtain a homogeneous composition.

[0051] [Table 2-1]

[0052] [Table 2-2] 1. DOWSIL, available from Dow Chemical. 2. DRYFLO TS, available from Nouryon. 3. KSP-100 is available from Shin-Etsu Chemical Co., Ltd. 4. MAKIMOUSSE-25, available from Kobo Products. 5. Simulgel inns available from Seppic. 6. BASF BC10034. 7. SYMDIOL 68, available from Symrise. 8. XIAMETER PMX-1503, available from Dow Corning.

[0053] Example 2: Sucrose ester provides a bilirubin-degrading effect. This example demonstrates the ability of sucrose esters to dose-dependently reduce the yellowness caused by insoluble bilirubin. Test and control compositions were prepared as described in the bilirubin degradation assay above. The two test compositions contained 0.01% and 0.05% sucrose ester (BASF BC10034), respectively. The plate containing the test compositions was covered with aluminum foil and placed on a microplate shaker (VWR, catalog no. 12620-938). Incubation was performed at room temperature for 20 hours with constant shaking at 150 rpm. Yellowness (b * ) was determined by measuring the absorbance of the sample at 10 nm intervals from 350 nm to 750 nm using a suitable spectrophotometer, and as follows (b * Assay). Absorbance was measured three times at T=0 (i.e., immediately after plate setup) and after a 20-hour incubation. The absorbance spectra from the yellowness measurements were then converted by computer using conversion software. * a * b * Convert to a value. A summary of the analysis results is shown in Table 3 and Figure 1. As can be seen from Table 3 and Figure 1, sucrose esters showed a statistically significant increase in yellowness (b) compared to the positive control. * The skincare compositions herein reduced the amount of (e.g., at least 15%, 20%, 25%, 30%, 35%, 40%, 50%, or more) compared to the vehicle control. * It may contain an effective amount of sucrose ester to reduce the value.

[0054] [Table 3]

[0055] Furthermore, test samples were analyzed after 20 hours of incubation, and the amount of bilirubin degraded by sucrose ester administration was measured. The amount of bilirubin was quantified according to the bilirubin degradation assay. The results of this analysis are shown in Figure 2. Figure 2 shows that sucrose ester reduced bilirubin levels compared to the positive control. In some cases, it may be desirable to formulate skincare compositions to contain an amount of sucrose ester that reduces bilirubin levels by at least 10% (e.g., at least 15%, 20%, 25%, 30%, 35%, 40%, 50%, or more) compared to the positive control.

[0056] The 0.01% (w / v) sucrose ester test leg showed better bilirubin reduction than the 0.05% (w / v) sucrose ester test leg, which was unexpected. Normally, a higher concentration of sucrose ester can be expected to result in a better dose-response response, leading to better bilirubin degradation than lower concentrations. However, although not limited by theory, the atypical dose-response observed in this example is thought to be due to the insolubility of sucrose ester in 20% DMSO solution. Indeed, at high concentrations of sucrose ester, it appears that the sucrose ester "crashes out" of the solution, thereby reducing the effectiveness of the test composition. Increasing the amount of DMSO in the test composition (e.g., to 80% (v / v) or higher) should yield the expected dose-response curve.

[0057] Example 3: Clinical Trial This example demonstrates the ability of a 1% sucrose ester composition to provide improved bilirubin degradation throughout the treatment period. An 8-week trial was conducted with 336 female subjects (25–55 years old) using a test composition containing 1% sucrose ester. The trial was conducted using a half-side, randomized, vehicle-controlled, round-robin method, with 96 observations per test leg. During the trial, some subjects applied the 1% sucrose ester test composition to one side of their face and the vehicle control to the other. The test compositions are shown in Table 4 below. The test compositions and vehicle controls were formulated using the standard method for preparing oil-in-water emulsion skincare compositions.

[0058] [Table 4] 1 BASF BC10034

[0059] Using the image analysis system REAL (Rapid Evaluation of Anti-aging Leads), digital images of each subject's face were captured and analyzed every two weeks. * The values ​​were determined. The REAL image analysis system is described in Miyamoto et al., "Development of Digital Imaging System for Objective Measurement of Hyperpigmented Spots on Face," Skin Res Technol 2002;8:227-35. A summary of the clinical trial results is shown in Table 5 and Figure 3 below. A p-value of 0.1 or less is considered statistically significant. As can be seen from Table 5 and Figure 3, the test composition significantly suppressed the increase in skin yellowness after 6 weeks of use compared to the vehicle control.

[0060] [Table 5]

[0061] This was not so noticeable in the test composition, but throughout the test, b *Note that the value appears to be increasing. Although not limited by theory, b * The increase in values ​​is thought to be due to the tests being conducted in the summer. Increased sunlight intensity and exposure, which are more common in summer, tend to increase melanin production in the skin, and the higher the melanin level, the greater the b * It is well known that the value becomes higher. Thus, due to the increase in melanin levels associated with the subjects' summer sun exposure, b over the course of the 8-week trial, * The values ​​are thought to have increased more significantly. However, subjects using the test composition showed a higher b compared to the vehicle control. * The increase was small, demonstrating the effectiveness of the test composition.

[0062] Example 4: Correlating bilirubin concentration with yellowness. While not bound by theory, it is believed that bilirubin concentration in the skin directly correlates with the appearance of yellow or sallow skin. To determine the correlation between bilirubin concentration and yellowness, a bilirubin standard curve is generated. Bilirubin powder (Cayman Chemicals Company, catalog no. 17161) is dissolved in DMSO (Sigma, catalog no. D8414-100mL) to prepare a 500 ug / mL bilirubin stock solution. This bilirubin stock solution is diluted in PBS as shown in Table 1 above to obtain bilirubin levels of 50, 25, 12.5, 5, 2.5, and 0 ug / mL. Yellowness (b * To measure the yellowness, the samples are packed in a triple 96-well plate, and the absorbance of each sample is measured in 10 nm increments from 350 nm to 750 nm using a suitable spectrophotometer. The absorbance spectra from the yellowness measurements are then converted by a computer using suitable conversion software. * a * b * Convert to a value.

[0063] As shown in Table 6 and Figure 4, b *The score shows a linear correlation with bilirubin concentrations in the range of 0 ug / mL to 50 ug / mL. Human biological bilirubin concentrations fall within this range. Therefore, the data indicates a direct correlation between bilirubin concentration in the skin and the appearance of poor complexion.

[0064] [Table 6]

[0065] The dimensions and values ​​disclosed herein should not be understood as being strictly limited to the exact numerical values ​​listed. Instead, unless otherwise indicated, each such dimension is intended to mean both the listed value and the functionally equivalent range encompassing that value. For example, a dimension disclosed as "40 mm" is intended to mean "approximately 40 mm".

[0066] All documents referenced herein, including any patents or patent applications that are cross-referenced or related, and any patent applications or patents on which this application claims priority or benefit thereof, are incorporated herein by reference in their entirety unless otherwise explicitly stated to be excluded or limited. No document reference shall be deemed prior art to any invention disclosed or claimed herein, nor shall it be deemed to teach, suggest or disclose any such invention, either alone or in combination with any other reference(s). Furthermore, if any meaning or definition of a term in this document conflicts with any meaning or definition of the same term in any document incorporated by reference, the meaning or definition given to the term in this document shall prevail.

[0067] While specific embodiments of the present invention have been illustrated and described, it will be apparent to those skilled in the art that various other changes and modifications can be made without departing from the spirit and scope of the invention. Therefore, it is intended that all such changes and modifications within the scope of the invention be covered in the appended claims.

Claims

1. a) an effective amount of sucrose ester, b) Dermatologically acceptable carriers, A skincare composition containing, A skincare composition wherein the sucrose ester is a combination of sucrose laurate and sucrose dilaurate, the weight ratio of sucrose laurate to sucrose dilaurate is 3:1 to 3:2, and the effective amount of sucrose ester reduces the yellowness according to the b* assay by at least 10% compared to a vehicle control that contains a dermatologically acceptable carrier but does not contain sucrose ester.

2. The skincare composition according to claim 1, wherein the sucrose ester is present in an amount of 0.001% to 10% by weight of the composition.

3. The skincare composition according to claim 1, wherein the composition further comprises at least one additional component selected from the group consisting of vitamins, minerals, peptides, sugar amines, sunscreens, oil control agents, flavonoid compounds, antioxidants, preservatives, protease inhibitors, tyrosinase inhibitors, anti-inflammatory agents, moisturizers, exfoliants, skin whitening agents, lubricants, anti-acne active substances, chelating agents, anti-wrinkle active substances, anti-atrophy active substances, phytosterols, N-acyl amino acid compounds, antibacterial agents, and antifungal agents, conditioning agents, emulsifiers, rheology modifying agents, and combinations thereof.

4. The skincare composition according to claim 3, wherein the additional component is selected from the group consisting of vitamin B3 compounds, vitamin E compounds, peptides, retinoids and combinations thereof.

5. The skincare composition according to claim 3, wherein the additional component comprises a rheological modifier selected from sodium polyacrylate superabsorbent polymer, starch-grafted sodium polyacrylate superabsorbent polymer, and combinations thereof.

6. The skincare composition according to claim 1, further comprising at least 10% silicone fluid.

7. The skincare composition according to claim 1, wherein the skincare composition is an oil-in-water emulsion.

8. The skincare composition according to claim 7, further comprising a nonionic emulsifier.

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