Stable skin care emulsions and methods of using the same

Abstract

It is well known that sucrose esters such as sucrose laurate and sucrose dilaurate are difficult to emulsify in oil-in-water emulsions and tend to destabilize these types of emulsions. It has now been found that the combination of sucrose esters with certain hydrophobically modified aqueous rheology modifiers and nonionic stearic acid derivative emulsifiers can greatly improve emulsion stability.

Description

Technical Field

[0001] This disclosure generally relates to improving the stability of emulsions containing unstable ingredients. More specifically, this disclosure relates to improving the stability of skin care composition emulsions containing emulsions that destabilize sucrose esters. Background Technology

[0002] The skin is the first line of defense against environmental damage, which would otherwise harm sensitive underlying tissues and organs. For example, the skin maintains a relatively water-impermeable barrier between the organism and its environment to prevent dehydration. Furthermore, the skin plays a crucial role in a person's appearance. Generally speaking, most people desire younger-looking, healthier skin. And for some of these people, signs of skin aging, such as thinning skin, wrinkles, and age spots, are undesirable indications of fading youth. Therefore, in today's youth-conscious society, addressing signs of skin aging has become a rapidly growing industry. Treatments range from beauty creams and moisturizers to various forms of cosmetic surgery.

[0003] Many natural and synthetic skincare agents are known to be used in skincare compositions commercially available to treat various skin conditions, particularly those associated with aging. For example, U.S. Patent 9,949,917 and U.S. Publication 2005 / 0220726 disclose cosmetic compositions containing sucrose fatty acid esters (such as sucrose laurate, sucrose dilaurate, and sucrose trilaurate) as skin brightening agents. However, when skincare compositions are provided in the form of emulsions, these sucrose fatty acid esters can destabilize the emulsion due to their emulsifying properties (i.e., due to the hydrophilic and lipophilic portions of these compounds). Emulsion instability can manifest in various ways (e.g., flocculation, paste formation, precipitation, or aggregation), all of which are generally undesirable in skincare compositions.

[0004] Therefore, it is desirable to provide a skin care composition in the form of an emulsion, which contains sucrose fatty acid esters as skin care agents and has desired stability. Summary of the Invention

[0005] This document discloses a skincare composition with improved emulsion stability, comprising: from about 0.0001% to about 10% by weight of a sucrose ester selected from sucrose laurate, sucrose dilaurate, sucrose trilaurate, and combinations thereof; from about 0.01% to about 5% by weight of a hydrophobically modified aqueous rheology modifier; from about 0.005% to about 5% by weight of a nonionic stearic acid derivative emulsifier; and a dermatologically acceptable carrier in the form of an oil-in-water emulsion. Methods for preparing and using the novel compositions of this document are also disclosed. Attached Figure Description

[0006] Figure 1 An example of an unstable O / W emulsion exhibiting precipitation is shown.

[0007] Figure 2 An example of a stable O / W emulsion is shown.

[0008] Figure 3 The instability index values ​​for various emulsions are shown. Detailed Implementation

[0009] The use of sucrose fatty acid esters in skincare compositions is known. However, at least some sucrose fatty acid esters, such as sucrose laurate and sucrose dilaurate, can destabilize the oil phase of emulsions, especially oil-in-water emulsions. It has now been surprisingly found that selecting specific emulsifiers and rheology modifiers can significantly improve the stability of emulsions containing sucrose fatty acid esters. Specifically, when sucrose esters are present, selecting hydrophobically modified hydrophilic rheology modifiers and suitable nonionic medium- to long-chain fatty acid derivative emulsifiers (e.g., stearic acid-derived emulsifiers) can significantly improve emulsion stability.

[0010] References to "implementation" or similar methods herein refer to specific materials, features, structures, and / or characteristics described in connection with that implementation being included in at least one implementation, or optionally multiple implementations, but do not imply that all implementations include the described materials, features, structures, and / or characteristics. Furthermore, materials, features, structures, and / or characteristics may be combined in any suitable manner in different implementations, and materials, features, structures, and / or characteristics may be omitted or replaced as described. Therefore, unless otherwise stated or declared as incompatible, although not expressly illustrated in the combination, the implementations and aspects described herein may include elements or components of other implementations and / or aspects, or may be combined with elements or components of other implementations and / or aspects.

[0011] In all embodiments, unless otherwise specified, all ingredient percentages are based on the weight of the cosmetic composition. Unless otherwise specified, all ratios are by weight. Significant figures do not express any limitation on the quantities shown or on the accuracy of the measurement. All values ​​should be understood to be modified by the word “about” unless otherwise specified. Unless otherwise specified, all measurements are understood to have been performed at approximately 25°C and ambient conditions, where “ambient conditions” means conditions at approximately 1 atmosphere and approximately 50% relative humidity. All numerical ranges are inclusive and can be combined to form narrower ranges not explicitly disclosed. For example, the upper and lower limits of the depicted ranges are interchangeable to form additional ranges.

[0012] The compositions of the present invention may comprise, consist of, or be composed of the basic components described herein, as well as optional ingredients. As used herein, “consistently consisting of” means that a composition or component may contain only additional ingredients that do not substantially alter the essential and novel features of the composition or method protected by the claims. As used in the specification and appended claims, unless the context clearly indicates otherwise, the singular forms “a,” “an,” and “the” are intended to include the plural forms as well.

[0013] definition

[0014] The word “about” modifies a specific value by referring to a range equal to or less than 20 percent (+ / - 20%) of the specified value (e.g., less than 15%, 10%, or even less than 5%).

[0015] "Reagent" refers to a material and any of its components that are intended to provide a particular beneficial effect or function. For example, an emollient is a material (e.g., fatty alcohol) intended to provide a moisturizing effect to the skin, and a thickener is a material that is generally intended to increase the viscosity of a composition.

[0016] As used with respect to the composition, “apply” or “spread” means to apply or spread the composition described herein onto a body surface such as skin or hair.

[0017] "Cosmetic composition" means a composition containing a relevant solvent and intended for non-therapeutic (i.e., non-medical) use. Examples of cosmetic compositions include tinted cosmetics (such as foundation, lipstick, concealer, and mascara), skin care compositions (such as moisturizers and sunscreens), personal care compositions (such as rinse-off and leave-on bath products and soaps), and hair care compositions (such as shampoos and conditioners).

[0018] In this article, “derivative” means an amide, ether, ester, amino, carboxyl, acetyl, and / or alcohol derivative of a given compound.

[0019] "Effective amount" means an amount of compound or composition sufficient to significantly induce a positive beneficial effect on keratinocytes during the treatment period. Positive beneficial effects can be health, appearance, and / or sensory benefits, including individual or combined beneficial effects disclosed herein.

[0020] "Emulsion stability" and its variations refer to the ability of an emulsion to resist changes in its properties over time. These changes can be physical or chemical, and can be visible or invisible. For example, a lack of emulsion stability can manifest as visible phase separation (i.e., paste formation or precipitation). In another example, emulsion instability can manifest as invisible (to the human eye) aggregation of droplets in the dispersed phase, leading to changes in viscosity or flow properties. Emulsion stability is characterized herein as an instability index, which can be determined by optical centrifugation testing, described in more detail below.

[0021] "Skincare" refers to conditioning and / or improving skin condition (e.g., skin health, appearance, or texture / feel). Some non-limiting examples of improving skin condition include improving skin appearance and / or feel by providing a smoother, more even appearance and / or feel; increasing the thickness of one or more layers of skin; improving skin elasticity or resilience; improving skin firmness; and reducing the oily, shiny, and / or dull appearance of skin; improving skin hydration or moisturization; improving the appearance of fine lines and / or wrinkles; improving skin peeling or flaking; plumping the skin; improving skin barrier properties; improving skin tone; reducing the appearance of redness or rashes; and / or improving skin radiance, luminosity, or translucency.

[0022] "Skincare active ingredients" refer to compounds or combinations of compounds that, when applied to the skin, provide immediate and / or long-lasting beneficial effects to the skin or the cell types typically present therein. Skincare active ingredients can modulate and / or improve the skin or its related cells (e.g., improve skin elasticity, hydration, skin barrier function, and / or improve cell metabolism).

[0023] "Skincare composition" refers to a composition that includes skincare active ingredients and regulates and / or improves skin condition.

[0024] As used herein, “treatment period” refers to the length of time and / or frequency of application of a material or composition to the target skin surface.

[0025] Composition

[0026] The compositions described herein are in the form of emulsions (e.g., oil-in-water emulsions) containing sucrose esters, hydrophobically modified aqueous rheology modifiers, nonionic mediators to long-chain fatty acid derivative emulsifiers, and dermatologically acceptable carriers in the form of oil-in-water emulsions. Combinations of rheology modifiers and sucrose esters are selected to provide emulsions with improved stability. The stable emulsions described herein have an instability index of less than 5% (e.g., less than 4%, 3%, 2%, 1%, or even less than 0.5%). When normalized relative to a negative control, the stable emulsions described herein have a relative instability of less than 25% (e.g., less than 20%, 15%, or even less than 10%). Stable emulsions may include very stable emulsions and partially stable emulsions, both of which are consumer acceptable. Suitable methods for determining the instability index are described in more detail below.

[0027] The compositions described herein may optionally contain one or more additional skin-active substances or other types of ingredients commonly included in topical skincare compositions. For example, the compositions described herein may contain fatty alcohols (e.g., hexyldecyl alcohol) to act as skin softeners or emollients. When a composition contains fatty alcohols, a combination of sucrose esters and fatty alcohols may be chosen to provide a synergistic improvement in cellular ATP production, for example, as described in co-pending U.S. Provisional Serial No. 63 / 125,011 entitled “Method of Treating Oxidative Stress in Skin and ComDositions Therefor” filed by Hakozaki et al. on December 14, 2020.

[0028] The skincare compositions described herein can be prepared using conventional methods. However, in some cases, it may be difficult to solubilize sucrose esters in the composition using conventional methods. In these cases, it may be desirable to solubilize the sucrose esters in a two-step dilution process using a glycol premix or other suitable solubilizer before adding it to the composition. An example of this method is described in co-pending U.S. Provisional Serial No. 63 / 124,870, filed December 14, 2020 by Tanaka et al. entitled “Cosmetic Compositions Comprising Sucrose Esters and Solvents”.

[0029] Compared to similar types of skin compositions known to have surfactant systems with HLB values ​​of 12 or greater (e.g., greater than 13, 14, or 15), the compositions described herein may have surfactant systems with HLB values ​​less than 10. In the comparative compositions, when the HLB value of the surfactant system is below 10, the composition (i.e., the emulsion) may become unstable. However, as shown in the examples below, simply adjusting the HLB value may not overcome the instability observed when sucrose esters are present in the composition. Therefore, specifically selecting a suitable combination of ingredients may be important to ensure emulsion stability.

[0030] The compositions described herein may be cosmetic, pharmaceutical, or medicated cosmetic compositions applicable to keratinized tissues (e.g., skin, hair, and nails), and may be provided in a variety of product forms, including but not limited to solutions, suspensions, emulsions, creams, gels, toners, sticks, sprays, aerosols, ointments, cleansing liquids and solid sticks, pastes, foams, mousses, shaving creams, wipes, strips, patches, motorized patches, hydrogels, film-forming products, facial and skin masks (with and without insoluble sheets), cosmetics such as foundation, eyeliner, and eyeshadow. In some cases, the composition form may conform to a selected, dermatologically acceptable carrier (i.e., an oil-in-water (O / W) emulsion). It is particularly desirable to provide the compositions of the present invention as skin creams, lotions, serums, or essences.

[0031] sucrose esters

[0032] The compositions herein comprise effective amounts of sucrose and fatty acid esters, wherein the fatty acids are selected from those having 12 to 24 carbon atoms (e.g., 12 to 22 carbon atoms or 12 to 18 carbon atoms). Particularly suitable fatty acids may be selected from those having saturated alkyl groups. In some cases, sucrose esters are selected from the group consisting of sucrose laurates, sucrose dilaurates, sucrose trilaurates, derivatives thereof, and combinations thereof. As used herein, “sucrose laurate” refers to an ester having the formula C 24 H 44 O 12 And the compound with CAS number 25339-99-5; "sucrose dilaurate" refers to the compound with the formula C 36 H 66 O 13 And the compound with CAS number 25915-57-5; and "sucrose trilaurate" refers to the compound having the formula C 48 H 88 O 14And the compound with CAS number 94031-23-9. Sucrose esters may be present in 0.0001% to 15% (e.g., 0.0002% to 10%, 0.001% to 15%, 0.025% to 10%, 0.05% to 7%, 0.05% to 5%, or even 0.1% to 3%) by weight of the composition.

[0033] In some cases, sucrose esters may be blends of two or more sucrose esters, wherein the two or more sucrose esters are present in any ratio of one sucrose ester to another of 1:10 to 1:1 (e.g., 1:7, 1:5, 1:3, or 1:2). In some cases, sucrose esters may be blends of sucrose laurate and sucrose dilaurate, wherein sucrose laurate is present at 50% to 80% by weight of the sucrose ester, and sucrose dilaurate is present at 20% to 45% by weight of the sucrose ester. Alternatively, sucrose esters may be blends of sucrose laurate, sucrose dilaurate, and sucrose trilaurate, wherein sucrose dilaurate is present at 35% or more by weight of the sucrose ester. Particularly suitable examples of sucrose esters used herein are derived from BC10034 is a blend of sucrose laurate and sucrose dilaurate. BC10034 sucrose ester material may have a sucrose laurate to sucrose dilaurate ratio in the range of 3:1 to 3:2.

[0034] Dermatologically acceptable carriers

[0035] The compositions disclosed herein include dermatologically acceptable carriers (which may be referred to as "carriers"). The phrase "dermatologically acceptable carrier" means that the carrier is suitable for topical application to keratinocytes, has good aesthetic properties, is compatible with the active substance in the composition, and does not cause any unreasonable safety or toxicity problems. In one embodiment, the carrier is present in an amount of about 50% to about 99% by weight, about 60% to about 98% by weight, about 70% to about 98% by weight, or alternatively about 80% to about 95% by weight.

[0036] The carrier described herein is in the form of an oil-in-water emulsion. That is, the emulsion has a continuous aqueous phase and a dispersed oil phase. The oil phase may contain silicone oils, non-silicone oils such as hydrocarbon oils, esters, ethers, etc., and mixtures thereof. The aqueous phase may contain water and / or water-soluble or water-miscible ingredients (e.g., ethanol, polyols such as glycerin, moisturizers, conditioning agents, antimicrobial agents, humectants, and / or other skin-care active substances). O / W emulsions provide a light and non-greasy sensory experience. Suitable O / W emulsions described 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 by weight based on the aqueous phase, and any water-soluble and / or water-miscible ingredients. In these cases, the dispersed oil phase will typically be present at 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 undesirable sensory effects of oily compositions. The oil phase may include 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 suitable for use in the compositions of the present invention are disclosed in U.S. Patent No. 9,446,265 and U.S. Publication No. 2015 / 0196464.

[0037] The carrier may contain one or more dermatologically acceptable hydrophilic diluents. As used herein, "diluent" includes materials such as sucrose esters that can be dispersed, dissolved, or otherwise incorporated therein. Hydrophilic diluents include water, organic hydrophilic diluents such as lower monovalent alcohols (e.g., C1-C4) and low molecular weight diols and polyols, including propylene glycol, polyethylene glycol (e.g., molecular weight 200 g / mol to 600 g / mol), polypropylene glycol (e.g., molecular weight 425 g / mol to 2025 g / mol), glycerol, butylene glycol, 1,2,4-butanetriol, sorbitan esters, 1,2,6-hexanetriol, ethanol, isopropanol, sorbitan esters, butylene glycol, ether propanol, ethoxylated ethers, propoxylated ethers, and combinations thereof.

[0038] rheology modifiers

[0039] The compositions described herein contain 0.05% to 5% of a hydrophobically modified aqueous rheology modifier (e.g., a thickener) to provide suitable rheological, stability, and skin-feel properties to the compositions. Some non-limiting examples of rheology modifiers suitable for use herein include crosslinked polyacrylate polymers such as PEMULEN EZ-4U, PEMULEN TR-1, PEMULENTR-2, and certain ULTREZ brand acrylate / C10-30 alkyl acrylate crosslinked polymers, all purchased from [unspecified source]. Other examples include vinyl isodecanoate crosspolymers, such as those made from 3V STABYLEN 30, a polyacrylate crosspolymer-6, sold for sale, such as those made from... SEPIMAX ZEN is sold as well as sodium polyacrylamide dimethyl taurate, such as ARISTOFLEX SILK sold by Clariant. In some cases, it may be desirable to exclude polyacrylamide-based thickeners, such as SEPIGEL 305 polyacrylamide thickener, because these types of thickeners may destabilize the emulsion.

[0040] The rheology modifiers of the compositions described herein may include medium- to long-chain fatty acid derivative emulsifiers (e.g., about 12-20 carbon chains, alternatively 16-20 carbon chains). In some examples, the emulsifier may include nonionic medium- to long-chain fatty acid derivative emulsifiers, such as stearyl polyoxyethylene ether-2, stearyl polyoxyethylene ether-21, PEG-100 stearate, glyceryl polyether-25 pyrrolidone carboxylic acid isostearate, and combinations thereof. "Stearic acid-derived emulsifiers" refers to emulsifiers in which at least one of the lipophilic domains of the surfactant is composed of a saturated 18-carbon chain (similar to stearic acid). These emulsifiers typically contain stearate, stearyl polyoxyethylene ether, or isostearate in their chemical names and are often derived from stearic acid in combination with other chemical moieties. Particularly suitable emulsifiers include stearic acid-derived emulsifiers with a hydrophilic-lipophilic balance (HLB) value of 14 or higher. Emulsifiers may be present in the composition at 0.05% to 5% (e.g., 0.1% to 4%, 0.5% to 3%, or even 1% to 2%). In some cases, it may be desirable to exclude certain polyether-modified siloxane emulsifiers, such as PEG-11 methyl ether polydimethylsiloxane, PEG-12 polydimethylsiloxane, PEG / PPG 19 / 19 polydimethylsiloxane, or other polyethylene glycol-modified polydimethylsiloxanes, which may destabilize the oil-in-water emulsion.

[0041] Optional ingredients

[0042] The compositions described herein may contain one or more optional ingredients known for use in topical skincare compositions, provided that the optional components do not unacceptably alter the desired beneficial effects of the compositions of the invention. Specifically, optional ingredients should not introduce undesirable instabilities into the emulsion. For example, it may be desirable to select optional ingredients that do not form complexes with other ingredients in the composition, especially pH-sensitive ingredients such as vitamin B3 compounds, salicylates, and peptides. When optional skincare active substances are included in the compositions of the invention, it may be desirable to select skincare active substances that act via biological pathways different from other skin active substances present in the composition, so that the active substances do not interfere with each other.

[0043] When included, optional ingredients should be suitable for contact with human skin tissue without undue toxicity, incompatibility, instability, allergic response, etc. When present, additional ingredients may be included in an amount of about 0.001% to 50% (e.g., 0.01% to 40%, 0.1% to 30%, 0.5% to 20%, or even 1% to 10%) by weight of the composition. Some non-limiting examples of additional ingredients include vitamins, minerals, peptides and peptide derivatives, glycosamines, sunscreens, oil-controlling agents, particles, flavonoids, hair growth regulators, antioxidants and / or antioxidant precursors, preservatives, protease inhibitors, tyrosinase inhibitors, anti-inflammatory agents, moisturizers, exfoliating agents, skin brighteners, sunscreens, sun-free tanning agents, lubricants, anti-acne agents, degreasing agents, chelating agents, anti-wrinkle active substances, anti-atrophy active substances, phytosterols and / or phytohormones, N-acyl amino acid compounds, antimicrobial agents, and antifungal agents. Some particularly suitable examples of additives include one or more skincare active substances selected from the group consisting of: vitamin B3 compounds (e.g., niacinamide), n-acyl amino acids (e.g., undecenoyl phenylalanine), vitamin E compounds (e.g., tocopheryl acetate), palmitoylated dipeptides (e.g., palmitoyl-lysine-threonine), palmitoylated pentapeptides (e.g., palmitoyl-lysine-threonine-threonine-lysine-serine), vitamin A compounds (e.g., retinol and retinyl propionate), and combinations thereof. Other non-limiting examples of optional ingredients and / or skincare active substances that may be used herein are described in U.S. Patent Publications 2002 / 0022040, 2003 / 0049212, 2004 / 0175347, 2006 / 0275237, 2007 / 0196344, 2008 / 0181956, 2008 / 0206373, 2010 / 0092408, 2008 / 0206373, 2010 / 0239510, 2010 / 0189669, and 20 US Patent Nos. 10 / 0272667, 2011 / 0262025, 2011 / 0097286, 2012 / 0197016, 2012 / 0128683, 2012 / 0148515, 2012 / 0156146 and 2013 / 0022557, and US Patent Nos. 5,939,082, 5,872,112, 6,492,326, 6,696,049, 6,524,598, 5,972,359 and 6,174,533.

[0044] In some cases, it may be desirable to include fatty alcohols in skincare compositions. At least some fatty alcohols act as emollients, which helps to moisturize the skin. Additionally or alternatively, some fatty alcohols, such as hexyldecyl alcohol, can improve the penetration of certain skin-active substances (e.g., vitamin B3 compounds) into the skin and / or independently provide beneficial effects on skin health or appearance. Fatty alcohols are high molecular weight, straight-chain primary alcohols having the following general formula:

[0045]

[0046] Where n = 8 to 32.

[0047] Fatty alcohols can be natural or synthetic, saturated or unsaturated, branched or linear. Some non-limiting examples of fatty alcohols commonly used in skincare compositions include octanol, decanol, lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, and behenyl alcohol. Fatty alcohols as used herein are generally indicated by the number of carbon atoms in the molecule. For example, "C12 alcohol" refers to an alcohol having 12 carbon atoms in its chain (i.e., dodecyl alcohol). Some particularly suitable fatty alcohols for use herein include ricinoleate, 12-hydroxystearate, and hexyldecyl alcohol. Fatty alcohols may be included in the compositions herein in amounts from 0.0001% to 15% by weight (e.g., 0.0002% to 10%, 0.001% to 15%, 0.025% to 10%, 0.05% to 7%, 0.05% to 5%, or even 0.1% to 3%).

[0048] Conditioner

[0049] The compositions described herein may contain 0.1% to 50% by weight of a conditioning agent (e.g., 0.5% to 30%, 1% to 20%, or even 2% to 15%). Adding a conditioning agent can help provide the composition with desired sensory properties (e.g., a silky, lubricating feel upon application). Some non-limiting examples of conditioning agents include hydrocarbon oils and waxes, siloxanes, fatty acid derivatives, cholesterol, cholesterol derivatives, diglycerides, triglycerides, vegetable oils, vegetable oil derivatives, acetylglucosides, alkyl esters, alkenyl esters, lanolin, wax esters, beeswax derivatives, sterols and phospholipids, their salts, isomers and derivatives, and combinations thereof. Particularly suitable examples of conditioning agents include volatile or non-volatile silicone fluids, such as polydimethylsiloxane copolyols, dimethylpolysiloxanes, diethylpolysiloxanes, mixed C1-30 alkylpolysiloxanes, phenyl polydimethylsiloxanes, polydimethylsiloxane alcohols, polydimethylsiloxanes, polydimethylsiloxanes, siloxane crosspolymers, and combinations thereof. Polydimethylsiloxanes may be particularly suitable because some consumers associate the sensory properties provided by certain polydimethylsiloxane fluids with good moisturizing properties. Other examples of silicone fluids suitable as conditioning agents are described in U.S. Patent 5,011,681.

[0050] How to use

[0051] This method involves identifying a target portion of the human keratinized tissue (e.g., skin or hair) to be treated and applying an effective amount of the composition to it during the treatment process. The target keratinized tissue portion may be the facial skin surface (such as the forehead, perioral region, chin, periorbital region, nose, and / or cheeks) or another part of the body (e.g., hands, arms, legs, back, chest). The target skin portion to be treated may be a portion exhibiting signs of oxidative stress or aging (such as fine lines, wrinkles, hyperpigmentation, uneven skin tone, and / or other visible skin features commonly associated with aging). In some cases, the target skin portion may not exhibit visible signs of skin aging, but if the area is one that typically develops such problems as a person ages, the user (e.g., a relatively young user) may still wish to target that skin area. In this way, this method can be used as a preventative measure to delay the onset of visible signs of skin aging.

[0052] The skincare composition described herein can be applied to the target skin area and, if necessary, to the surrounding skin at least once daily, twice daily, or more frequently daily during the treatment period. When applied twice daily, the first and second applications should be spaced at least 1 to 12 hours apart. Typically, the composition can be applied in the morning and / or at bedtime. When used according to the methods described herein, the compositions of the invention can, for example, improve the appearance of skin affected by oxidative stress by increasing ATP production in skin cells.

[0053] The treatment period described herein ideally provides sufficient time for the combination of sucrose esters and fatty alcohols present in the composition to increase ATP production in skin cells undergoing oxidative stress, thereby improving the appearance of visible signs of skin aging. The beneficial ATP production effect provided by this method can be demonstrated by a synergistic increase in ATP production relative to the use of sucrose esters and fatty alcohols alone. In some cases, this method can provide a synergistic increase in ATP production of at least 5% (e.g., 10%, 15%, 20%, 25% or more) relative to the expected increase in ATP production. The treatment period can last for at least one week (e.g., about two, four, eight, or even twelve weeks). In some cases, the treatment period will be extended to several months (i.e., three to twelve months). In some cases, the composition can be applied for most of the week (e.g., at least four, five, or six days a week), at least once daily or even twice daily during a treatment period of at least two, four, eight, or twelve weeks.

[0054] The application of the composition can be achieved through topical application. Regarding the application of the composition, the terms "topical," "local," and "partially" refer to delivering the composition to a target area (e.g., wrinkles or fine lines) while minimizing delivery to skin surfaces that are not intended for treatment. The composition can be applied to and gently massaged into the skin area. The form of the composition or a dermatologically acceptable carrier should be chosen to facilitate topical application. While some embodiments herein envision topical application of the composition to a specific area, it should be understood that the compositions herein can be widely applied to one or more skin surfaces. In some embodiments, the compositions herein can be used as part of a multi-step cosmetic regimen, wherein the compositions of the present invention can be applied before and / or after one or more other compositions.

[0055] Optical centrifugation test

[0056] This testing method provides the use of a dispersion analyzer (e.g., the LUMiSizer from LUM GMBH). TMA dispersion analyzer is used to evaluate the emulsion stability of samples at baseline and the manner in which they age at elevated temperatures over time. Samples are placed in a suitable container for testing (e.g., LUM 2mm, polycarbonate rectangular synthetic cell cuvettes (LUM GMBH: 110-131xx)) and run at 40°C and 4000 rpm for 1 hour. Accelerated stability testing using optical centrifugation techniques is well documented in the literature (e.g., Reference: Badolato, GG et al., “Evaluation of long-term stability of model emulsions by multi-sample analytical centrifugation,” Surface and interfacial forces—from basic principles to applications. Springer, Berlin, Heidelberg, 2008, 66-73). This method involves centrifuging the sample by illuminating the entire sample cell with parallel near-infrared or blue light. Transmitted light is detected by a CCD sensor and converted into an extinction profile. Changes in transmittance during centrifugation indicate various instability mechanisms, such as precipitation, paste formation, flocculation, and / or emulsion aggregation. For emulsions, based on the relative density of phase separation, precipitation and paste formation can be observed by increasing the transmittance of the top (precipitation) or bottom (paste formation) of the sample. For example, Figure 1 The O / W emulsion exhibiting precipitation was shown, which was observed as a lower-density oil separating from the rest of the emulsion upon centrifugation at the top of the sample. In contrast, Figure 2 An example of a stable O / W emulsion is shown.

[0057] The instability of emulsions measured by optical centrifugation can be quantified using the instability index (Detloff, T., T. Sobisch, and D. Lerche, “Instability index”, Dispersion Letters Technical 4 (2013): 1–4). The instability index is based on the increase in transmittance, also known as clarity, due to precipitation or gelation. The index is a dimensionless number between 0 and 1, where “0” indicates complete stability without change during centrifugation, and “1” indicates complete instability, as indicated by the change in transmittance over the region of interest. The dimensionless index can be multiplied by 100% to express the instability index as a percentage. This index provides a relative ranking of the stability of the different samples tested. The measured instability index can be normalized relative to a negative control to provide a more informative indication of emulsion stability.

[0058] Instability indices can be obtained using appropriate software tools (e.g., The software or equivalent is calculated according to the following formula. Formula 1 is used to calculate clarity ( The difference between the first transmittance and the subsequent transmittanceFormula 2 is used to calculate the clarity change of curve i up to a certain time, which is calculated as the sum of incremental clarity within the region of interest. Formula 3 is used to calculate the maximum possible clarity. Formula 4 calculates the instability index as the change in transmittance divided by the maximum possible change within the region of interest.

[0059] Formula 1:

[0060] T i diff =T i -T1 where i≥2

[0061] Where: T is transmittance, and i is the number of curves.

[0062] Formula 2:

[0063]

[0064] Where: r are the maximum and minimum values ​​of the region of interest, and j is the position increment (in LUMiSizer) TM (The value is 14 micrometers).

[0065] Formula 3:

[0066]

[0067] in It is the average transmittance of cells containing only water, and It is the first transmittance curve, and j is the position increment at the minimum and maximum r positions.

[0068] Formula 4:

[0069]

[0070] As can be seen from the formula, the instability index is based on the relative ranking of regional interest with respect to the maximum possible clarity within that region. For the instability index measurement reported in this paper, the region of interest is taken across the entire sample of cells because the absolute value of the instability index is influenced by the selected region of interest. Therefore, relative comparisons for a given region of interest may be more interesting than the reported absolute values. Relative comparisons can be provided by normalizing the observed instability index relative to a control.

[0071] In addition to the instability index, the rate of change of the instability index also indicates the separation kinetics. This can be evaluated by plotting the instability index against time. This rate of change is related to the rate of precipitation or paste formation, and it can also be quantified based on Stokes' law. As noted, the precipitation rate is defined by Stokes' law as shown in Equation 5, where v is the velocity, ρ is the density, r is the particle size, η is the dynamic viscosity of the continuous phase, g is gravity, α is the particle concentration, and RCA is the relative centrifugal acceleration.

[0072] Formula 5:

[0073]

[0074] Unrestricted by theory, it is believed that the main driver of emulsion instability is the change in droplet radius r from sucrose ester-driven aggregation, which is associated with higher sedimentation rates.

[0075] Examples and combinations

[0076] Example 1: Formulation

[0077] Table 1 below provides examples of stable emulsion skincare compositions containing sucrose esters. Exemplary compositions can be prepared as follows: A sucrose ester premix is ​​prepared by combining sucrose esters, pentylene glycol, and water and mixing until the sucrose esters are completely dissolved. Heating may be used, where appropriate, to aid in the dissolution of the sucrose esters. An aqueous phase is prepared separately by dispersing one or more thickeners and one or more polymeric emulsifiers in the aqueous phase. After the one or more thickeners are dispersed and homogenized, any one or more additional emulsifiers (e.g., high HLB emulsifiers) are added to the aqueous phase. The remaining aqueous phase components are added and the pH is adjusted as needed (e.g., pH 5-7). In a separate container, the oil phase components are combined and mixed until homogenized, and heated as needed (e.g., to melt any solid materials). The oil phase is then emulsified into the aqueous phase by slowly adding the oil phase while mixing, continuing mixing until the emulsion is completely homogenized. After the emulsion is completely homogenized, any remaining components are added while mixing until homogenized. The sucrose ester premix phase may be added to the batch before or after the emulsification step and then mixed until the batch is homogenized.

[0078] Table 1 - Exemplary Formulations

[0079]

[0080]

[0081] Table 1 - Continued

[0082]

[0083]

[0084] 1. ELDEWPS-203, purchased from

[0085] 2. KSG-16, purchased from

[0086] 3. KF-6011, purchased from

[0087] 4. BC10034, from

[0088] 5. CARBOPOL ULTREZ 20, purchased from

[0089] 6. PEMULEN TR-1, purchased from

[0090] 7. PEMULEN EZ-4U, purchased from

[0091] 8. STABLYEN 30, purchased from 3V

[0092] 9. SEPIGEL 305, purchased from

[0093] 10. SEPIWHITE, purchased from

[0094] 11. Dryflots, purchased from

[0095] 12. SEPIMAX ZEN, purchased from

[0096] 13. ARISTOFLEX SILK, purchased from Clariant

[0097] +Equilibrate to near neutral pH 5-7

[0098] Example 2 - Instability Index Variables

[0099] This example demonstrates the influence of various emulsifiers and rheology modifiers on the instability index. In this example, stability test samples were prepared as described in Example 1, and tests were performed according to the aforementioned optical centrifugation method. Whole-cell analysis was performed using Lum GMBH by selecting relevant regions of interest at the gas / liquid interface and the bottom of the sample. Software was used to quantify the instability index. The instability index values ​​for each test composition and control were determined after aging at 50°C for 2 weeks. As previously stated, stable emulsions have an instability index of less than 5% (e.g., less than 4%, 3%, 2%, 1%, or even less than 0.5%). Partially stable emulsions, where minimal oil separation and / or paste formation is observed in the sample after photocentrifugation, are typically observed in the range of 2.5%–5% instability index. Very stable emulsions are noted when no oil separation is observed in the sample after photocentrifugation, typically observed in the range of less than 2.5%, alternatively less than 2%. Partially stable emulsions may be consumer-acceptable, although they may be slightly less preferred compared to very stable emulsions. The compositions tested are shown in Table 2 below. Composition A, which does not contain a nonionic stearic acid-derived emulsifier, was used as a negative control. The instability index results were normalized relative to the negative control.

[0100] Table 2 - Test Formulations

[0101]

[0102] + Balance to a pH of 5.5-6.5.

[0103] 1. ELDEW PS-203, purchased from

[0104] 2. KSG-16, purchased from

[0105] 3. KF-6011, purchased from

[0106] 4. BC10034, purchased from

[0107] 5. CARBOPOL ULTREZ 20, purchased from

[0108] 6. PEMULEN TR-1, purchased from

[0109] 7. SEPIGEL 305, purchased from

[0110] 8. SEPIWHITE, purchased from

[0111] The test results are summarized in Table 3 below and shown in the table below. Figure 3 From Table 3 and Figure 3 As can be seen from the above, the composition H of the present invention (which includes sucrose esters, hydrophobically modified polymer thickeners (e.g., Pemulin))TM The appropriate combination of nonionic stearic acid-derived emulsifiers is the most stable composition relative to the comparative example. When normalized relative to the negative control, it exhibits an instability index of less than 1% and a relative instability index of less than 5%.

[0112] Example C is also stable and has a lower content of hexyldecyl alcohol in combination with sucrose dilaurate compared to A and B.

[0113] By reducing the amount of hydrophobic modified polymer thickener Carbopol Ultrez 20 TM (It is not as good as the hydrophobically modified polymer Pemulen TR-1) TM Partially stable formulations were observed using nonionic stearic acid-derived emulsifiers in the presence of an effective agent.

[0114] Table 3 - Instability Index

[0115]

[0116] Example 3 - Sucrose esters destabilize O / W emulsions

[0117] This example demonstrates the instability of sucrose dilaurate in O / W emulsion skincare compositions by comparing a test composition containing sucrose dilaurate with a control composition not containing sucrose dilaurate. Both the test and control compositions are O / W emulsions and are identical in all respects, except that the test composition contains 1% sucrose dilaurate (BC10034, from...). The composition was prepared according to the method described in Example 1 and tested according to the above-described optical centrifugation test. Samples were prepared in LUM 2mm polycarbonate rectangular synthetic cells and run at a constant temperature of 40°C and 4000 RPM for 1 hour on a LUMISIZER dispersion analyzer, with measurements taken every 10 seconds. Lum GmbH was used. The software was used to analyze and quantify the instability index by selecting relevant regions of interest from the total sample cells. Similar to the previous examples, the instability index value of each composition was determined after aging at a high temperature of 50°C for 2 weeks. The results of this test are summarized in Table 4 below. As can be seen from Table 4, the addition of sucrose esters to the O / W emulsion compositions introduced significant instability compared to the control.

[0118] Table 4

[0119]

[0120]

[0121] + Balance to a pH of 5.5-6.5.

[0122] 1. ELDEW PS-203, purchased from

[0123] 2. KSG-16, purchased from

[0124] 3. KF-6011. Purchased from [unclear - possibly a retailer's name or address].

[0125] 4. BC10034, purchased from

[0126] 5. CARBOPOL ULTREZ 20, purchased from

[0127] 6. SEPIGEL 305, purchased from

[0128] 7. SEPIWHITE, purchased from

[0129] Example 4 - The Key to Selecting Rheology Modifiers and Emulsifiers

[0130] This example demonstrates the importance of selecting appropriate rheology modifiers and emulsifiers to overcome emulsion instability caused by sucrose esters. A dose-response model of polysorbate-20 (a well-known ethoxylated sorbitan ester emulsifier) ​​was performed to rebalance the HLB with the present sucrose dilaurate. It was found that simply rebalancing the HLB with the emulsifier using polysorbate-20 was insufficient to stabilize the oil-in-water emulsion, even at a polysorbate-20 content of 10%, as shown in Tables 5 and 6. It was also found that using hydrophobically modified rheology modifiers such as Pemulen TR-1 alone was also insufficient. TM This is also insufficient to completely stabilize the emulsion. Surprisingly, hydrophobic rheology modifiers (e.g., Pemulen) were found to be effective. TM Stabylen 30 TM SepimaxZen TM Aristoflex Silk TM The combination of hydrophobic rheology modifiers and stearic acid derivative emulsifiers (e.g., PEG-100 stearate, stearyl polyoxyethylene ether-2 / stearyl polyoxyethylene ether-21 blends and / or glyceryl polyether-25PCA isostearate) can adequately stabilize the emulsion, and increased stability and improved dose response are observed when hydrophobic rheology modifiers are combined with stearic acid derivative emulsifiers in certain combinations as shown in Table 7.

[0131] The HLB experimental compositions are shown in Table 5. The base formulation was modified by varying the content of polysorbate-20. Test samples of each composition were prepared according to the method described in Example 1 and tested according to the above-described optical centrifugation method. The base compositions did not contain sucrose esters, while the test compositions contained 1% sucrose esters and varying amounts of polysorbate-20. The results of these tests are summarized in Table 6.

[0132] Table 5

[0133]

[0134] + Balance to a pH of 5.5-6.5.

[0135] *Sucrose ester (SE) premixes are for testing purposes only.

[0136] 1. ELDEW PS-203, purchased from

[0137] 2. KSG-16, purchased from

[0138] 3. KF-6011, purchased from

[0139] 4. BC10034, purchased from

[0140] 5. CARBOPOL ULTREZ 20, purchased from

[0141] 6. SEPIGEL 305, purchased from

[0142] 7. SEPIWHITE, purchased from

[0143] Table 6

[0144] Instability Index Observation results Basic formula (0% SE) 0.3％ Stablize Basic formula + 1% SE + 0.5% polysorbate 20.1％ Oil phase separation Basic formula + 1% SE + 2% polysorbate 23％ Oil phase separation Basic formula + 1% SE + 10% polysorbate 52.97％ Oil phase separation

[0145] Tables 7A, 7B, and 7C provide additional inventive and comparative compositions that demonstrate the importance of selecting an appropriate combination of sucrose esters, hydrophobically modified aqueous rheology modifiers, and nonionic stearic acid-derived emulsifiers. Composition A was used as a positive control, and composition B was used as a negative control. The example compositions in Tables 7A-7C were prepared using the methods described herein.

[0146] Table 7A

[0147]

[0148]

[0149] Table 7B

[0150]

[0151]

[0152] Table 7C

[0153]

[0154]

[0155] Balance to a pH of 5.5-6.5.

[0156] 1. BC10034, from

[0157] 2. PEMULEN TR-1, from

[0158] 3. CARBOPOL ULTREZ 20, from

[0159] 4. SEPIGEL 305, from

[0160] 5. KSG-16, purchased from

[0161] 6. KF-6011, purchased from

[0162] 7. STABLYEN 30, purchased from 3V

[0163] 8. SEPIMAX ZEN, from

[0164] 9. ARISTOFLEX SILK, from Clariant

[0165] In addition to determining the instability index (AT) of the compositions, visual observations were performed to describe the stability or instability of the emulsion. Table 7D below provides a summary of the visual observations performed on each composition.

[0166] Table 7D

[0167] Composition Observation results A Stablize B Unstable - Complete oil phase separation C Partially stabilized - paste D Partially stable - paste with slight oil separation E Unstable - Complete oil phase separation F Stablize G Stablize H Stablize I Stablize J Stablize K Stablize L Stablize M Stablize N Stablize O Stablize P Stablize Q Stablize R Partially stabilized - paste S Stablize T Stablize

[0168] The dimensions and values ​​disclosed herein should not be construed as strictly limited to the precise numerical values ​​cited. Rather, unless otherwise specified, each such dimension is intended to represent the stated value and a range around which it is functionally equivalent. For example, a dimension disclosed as “40 mm” is intended to represent “approximately 40 mm”.

[0169] Unless expressly excluded or otherwise limited, every reference cited herein, including any cross-references or related patents or patent applications, and any patent application or patent claiming priority to or benefiting from it, is incorporated herein by reference in its entirety. Reference to any reference is not an endorsement of it as prior art to any disclosed or protected art herein, nor is it an endorsement of any such invention, either on its own or in combination with any one or more references. Furthermore, where any meaning or definition of a term in this invention conflicts with any meaning or definition of the same term in referenced documents, the meaning or definition given to that term in this invention shall prevail.

[0170] While specific embodiments of the invention have been shown 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 falling within the scope of the invention be covered by the appended claims.

Claims

1. A skincare composition with improved emulsion stability, comprising: a) 0.0001% to 10% by weight of sucrose esters, said sucrose esters being selected from sucrose laurate, sucrose dilaurate, sucrose trilaurate, and combinations thereof; b) 0.01% to 5% by weight of acrylate-based rheology modifier; c) 0.005% to 5% by weight of nonionic medium-chain to long-chain fatty acid derivative emulsifiers; and d) Dermatologically acceptable carriers in the form of oil-in-water emulsions; The sucrose ester comprises 50% to 80% sucrose laurate by weight of the sucrose ester, and 20% to 45% sucrose dilaurate by weight of the sucrose ester. The nonionic medium-chain to long-chain fatty acid derivative emulsifier is selected from the group consisting of: stearyl polyoxyethylene ether-2, stearyl polyoxyethylene ether-21, PEG-100 stearate, and glyceryl polyether-25 pyrrolidone carboxylic acid isostearate. The acrylate-based rheology modifier is selected from the group consisting of: sodium polyacrylamide dimethyl taurate, acrylate / acrylate C10-30 alkyl ester crosspolymers, acrylate vinyl isodecanoate crosspolymers, and combinations thereof.

2. The skincare composition according to claim 1, wherein, according to a photocentrifugation test, the skincare composition exhibits an instability index value of less than 10%.

3. The skincare composition according to claim 1, wherein, according to photocentrifugation testing, the skincare composition exhibits an instability index value of less than 5%.

4. The skincare composition according to claim 1, wherein, according to photocentrifugation testing, the skincare composition exhibits an instability index value of less than 2%.

5. The skincare composition according to any one of claims 1 to 4, wherein the skincare composition exhibits a normalized instability index value of less than 20% relative to the negative control.

6. The skincare composition according to any one of claims 1 to 4, wherein the skincare composition exhibits a normalized instability index value of less than 15% relative to the negative control.

7. The skincare composition according to any one of claims 1 to 4, wherein the skincare composition exhibits a normalized instability index value of less than 10% relative to the negative control.

8. The skin care composition according to any one of claims 1 to 4, wherein the skin care composition exhibits a normalized instability index value of less than 5% relative to the negative control.

9. The skincare composition according to claim 1, wherein the composition is free of polyether-modified siloxane emulsifiers.

10. The skin care composition according to claim 1 further comprises 0.0001% to 10% by weight of fatty alcohol.

11. The skin care composition according to claim 10, wherein the fatty alcohol is hexyldecyl alcohol.

12. The skincare composition of claim 1, further comprising additional ingredients selected from the group consisting of: vitamins, minerals, peptides, glycosamines, sunscreens, oil-controlling agents, flavonoids, antioxidants, preservatives, protease inhibitors, tyrosinase inhibitors, anti-inflammatory agents, moisturizers, exfoliating agents, skin brightening agents, lubricants, anti-acne active substances, chelating agents, anti-wrinkle active substances, anti-atrophy active substances, phytosterols, N-acyl amino acid compounds, antimicrobial and antifungal agents, conditioning agents, emulsifiers, rheology modifiers, and combinations thereof.

13. The skincare composition of claim 12, wherein the additional ingredient is a skincare active substance selected from the group consisting of: vitamin B3 compounds, undecylenoyl phenylalanine, vitamin E compounds, palmitoylated dipeptides, palmitoylated pentapeptides, vitamin A compounds, and combinations thereof.

14. A non-therapeutic method of treating skin with cosmetics, comprising: a) Identify the target skin region to be treated; as well as b) Apply the skincare composition according to any of the preceding claims to the target skin portion during the treatment period.

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