Vitamin C topical composition
Topical compositions with ascorbate and green tea polyphenols address photoaging by reducing wrinkles and improving skin texture and firmness, showing noticeable improvements over time.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2021-06-28
- Publication Date
- 2026-04-13
AI Technical Summary
Existing cosmetic compositions fail to effectively prevent and mitigate the effects of photoaging and associated skin disorders caused by free radicals and UV radiation, leading to issues like wrinkles, loss of elasticity, and hyperpigmentation.
Topical compositions comprising an emulsion of an aqueous and oily phase with an antioxidant system containing ascorbate components and green tea polyphenols are developed to protect and improve skin appearance by reducing the impact of free radicals and UV damage.
The compositions demonstrate improvements in reducing fine lines, increasing skin smoothness and radiance, and enhancing skin firmness, with significant effects observed at 4, 8, and 12 weeks post-treatment.
Smart Images

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Abstract
Description
[Technical Field]
[0001] Cross-references to related applications This application claims priority to U.S. Provisional Patent Application No. 63 / 045,409, filed on 29 June 2020, which is incorporated in its entirety by reference.
[0002] This invention relates to a cosmetic composition for skincare applications. [Background technology]
[0003] Excessive exposure to sunlight and other toxic free radical sources and irritants can induce skin damage and lead to various skin conditions that impair appearance. Among these skin conditions, wrinkles, fine lines, loss of elasticity, sagging, dryness, and age spots are caused by sun damage and aging. Skin wrinkles can be either deep grooves and folds or fine lines. Wrinkles can occur on any part of the body, but are especially common in areas with the greatest sun exposure, such as the face, neck, forearms, and hands.
[0004] Free radicals derived from ultraviolet (UV) radiation are known to increase in densely populated areas along with air pollution, thereby exacerbating the problem. Free radicals are destructive in that they hydrolyze elastin fibers in the skin and synthesize collagen in the deeper dermis layer of the skin, thereby causing wrinkles and other damaged skin conditions.
[0005] Today, people are often seeking ways to prevent and / or mitigate the effects of aging and sun exposure. Various cosmetic compositions, as well as homeopathic and prescription treatments, are available to consumers seeking to achieve a more youthful and healthy appearance. However, there remains a need for topical compositions that provide effective treatments and preventative measures against photoaging of the skin and associated skin disorders. [Overview of the project]
[0006] In certain embodiments of this disclosure, the objective is to provide topical compositions for protection against atmospheric or extrinsic aging, methods for preparing such topical compositions, and methods for using such topical compositions.
[0007] In certain embodiments of this disclosure, the object is to provide topical compositions, methods for preparing such topical compositions, and methods for using such topical compositions, for mitigating, attenuating, minimizing, and treating early signs of aging caused by reactive oxygen species (ROS) from sources such as free radicals, IRA, UVA, UVB, HEV (blue) light, IR, pollution, allergens, irritants, or specific light sources.
[0008] In certain embodiments of this disclosure, the objective is to provide topical compositions, methods for preparing such topical compositions, and methods for using such topical compositions as part of a regimen before or after a dermatological procedure (such as non-excisional dermatological procedures, chemical peels, microablation, and lasers).
[0009] In certain embodiments of this disclosure, the objective is to provide topical compositions for improving the appearance, elasticity, and firmness of the skin, or to mitigate the visible signs of photoaged skin, sunburn, wrinkles, and related skin disorders.
[0010] The above objectives and one or more others can be satisfied in certain embodiments of this disclosure relating to topical compositions comprising an emulsion of an aqueous phase and an oily phase, the topical composition comprising an antioxidant system ranging from over 0 wt.% to about 10 wt.% including an ascorbate component and green tea polyphenols.
[0011] In certain embodiments, the Disclosure relates to methods for treating skin in question for the effects of radical-induced damage, for brightening skin in question, for treating skin in question for the effects of airborne or solar aging, or to a treatment regimen using certain dermatological procedures. These methods include administering to skin in question one of the topical compositions described herein.
[0012] In certain embodiments, the disclosure relates to compositions and methods for treating skin in question for the effects of aging caused by air, the skin exhibiting improvements in the appearance of fine lines in the eye area, smoothness, and skin radiance.
[0013] In certain embodiments, the Disclosure relates to compositions and methods for treating skin in question, wherein the skin exhibits at least one of the following: reduction or attenuation of fine lines in the eye area; increase or maintenance of smooth skin; increase or maintenance of radiance; reduction or maintenance of wrinkles on the global face; reduction or maintenance of wrinkles in the eye area; reduction or maintenance of hyperpigmentation; and increase or maintenance of firmness.
[0014] In certain embodiments, the Disclosure relates to compositions and methods for treating the skin in question, wherein the skin exhibits improvement at 4 weeks, 8 weeks, and / or 12 weeks compared to at least one baseline of fine lines around the eyes; skin smoothness; radiance; overall facial wrinkles; eye area wrinkles; hyperpigmentation; and firmness, as examined using a modified Griffith 10-point scale.
[0015] In certain embodiments, the disclosure relates to compositions and methods for treating skin in question, wherein the skin exhibits improvement in fine lines around the eyes at 4 weeks, 8 weeks, and 12 weeks, respectively, compared to at least one baseline of -5% to -25%, -15% to -35%, or -25% to -45%, as measured by a modified Griffith 10-point scale.
[0016] In certain embodiments, the disclosure relates to compositions and methods for treating skin in question, wherein the skin exhibits improvement in skin smoothness at weeks 4, 8, and 12, respectively, compared to at least one baseline of -1% to -10%, -5% to -15%, or -10% to -20%, as measured by a modified Griffith 10-point scale.
[0017] In certain embodiments, the disclosure relates to compositions and methods for treating skin in question, wherein the skin exhibits improvement in radiance at weeks 4, 8, and 12, respectively, compared to at least one baseline of -1% to -10%, -3% to -13%, or -5% to -15%, as measured by a modified Griffith 10-point scale.
[0018] In certain embodiments, the disclosure relates to compositions and methods for treating skin in question, wherein the skin exhibits improvement in wrinkles across the entire face at weeks 4 and 12, respectively, compared to at least one baseline of -1% to -10% or -3% to -13%, as measured by a modified Griffith 10-point scale.
[0019] In certain embodiments, the disclosure relates to compositions and methods for treating skin in question, wherein the skin exhibits improvement in at least one baseline of -1% to -10% or -2% to -12% for eye area wrinkles at 4 weeks and 12 weeks, respectively, as examined using a modified Griffith 10-point scale.
[0020] In certain embodiments, the disclosure relates to compositions and methods for treating a target skin, wherein the skin exhibits improvement in hyperpigmentation at 4 weeks and 12 weeks, respectively, from -1% to -10% or from -5% to -15%, compared to at least one baseline.
[0021] In certain embodiments, the disclosure relates to compositions and methods for treating a target skin, wherein the skin exhibits improvement in firmness at weeks 4 and 12, respectively, compared to at least one baseline of -1% to -10% or -3% to -13%, as measured by a modified Griffith 10-point scale.
[0022] In certain embodiments, the Disclosure relates to compositions and methods for treating the skin of a subject, wherein at least 50%, at least 60%, at least 70%, at least 80%, at least 90%, or at least 95% of the subject exhibits improvement compared to baseline in at least one of the following, as examined by a modified Griffith 10-point scale: fine lines around the eyes; skin smoothness; radiance; wrinkles across the face; wrinkles in the eye area; hyperpigmentation; and firmness.
[0023] The term “administering a topical composition,” as used herein, means applying it topically to the skin of interest, such as the face, neck, hands, feet, elbows, knees, etc. The terms “apply,” “to apply,” and “to apply,” as used herein, in relation to the disclosed topical formulation or the method of using the disclosed topical formulation, mean any method of administering a topical formulation to the skin, such as the skin of a person, including the skin of a patient, in medical or cosmetic practice, delivering the formulation to the surface of the patient's skin. Rubbing, scrubbing, spreading, and spraying the disclosed topical formulation, with or without the aid of a suitable device, are all included within the scope of the term “apply,” as used herein. The terms “topical” or “topically” in relation to the administration or application of the disclosed skincare formulation mean epidermal administration or application to the skin. Application may be manual (e.g., directly by hand), administered, or administered via an applicator, cloth, device, roll-on, wipe, unit-dose sponge applicator, swab or cotton ball, liquid, impregnated gauze or other substrate, coated silicone sheet or other sheet product, coated bandage or externally secured device, small towel, individually packaged cotton thread or pad, transdermal delivery system, etc. Administration may be self-administered or administered by a healthcare professional or caregiver.
[0024] In certain embodiments, the disclosure relates to a method for preparing any of the topical compositions described herein by combining an ascorbate component and an antioxidant system comprising green tea polyphenols in an amount ranging from over 0 wt.% to about 10 wt.%. [Brief explanation of the drawing]
[0025] [Figure 1] This is a summary of the improvements across all clinical efficacy parameters in the clinical study of Example 2. [Figure 2] This is a summary of the clinical grade improvement experienced by the subjects of the clinical study in Example 2. [Figure 3]This is an overview of the ultrasound measurements in the clinical study of Example 2. [Modes for carrying out the invention]
[0026] The following definitions will be used unless otherwise specified.
[0027] As used herein, the term "alkyl" refers to both linear and branched hydrocarbon groups. For individual radicals such as propyl, only linear radicals are included; branched isomers such as isopropyl are referred to specifically.
[0028] The terms "halo" or "halogen" as used herein refer to fluoro, chloro, bromo, and iodine.
[0029] The term "carbocyclic" refers to a single saturated (i.e., cycloalkyl) or single partially unsaturated (e.g., cycloalkenyl, cycloalkadienyl, etc.) ring (i.e., a (C3-C7) carbocyclic ring) having 3 to 7 carbon atoms. The term "carbocyclic" also includes multiple fused ring systems (e.g., ring systems containing 2, 3, or 4 carbocyclic rings). Thus, carbocyclic rings include polycyclic carbocyclic rings having 7 to 12 carbon atoms as a dicyclic ring and up to approximately 20 carbon atoms as a polycyclic ring. Polycyclic carbocyclic rings can be bonded to each other via a single carbon atom to form spirobonds (e.g., spiropentane, spiro[4,5]decane, spiro[4.5]decane), or via two adjacent carbon atoms to form condensed bonds such as bicyclo[4,5], [5,5], [5,6], or [6,6] systems, or to form nine or ten ring atoms arranged as bicyclo[5,6] or [6,6] systems (e.g., decahydronaphthalene, norsabinane, norcalane), or via two non-adjacent carbon atoms to form bridging bonds (e.g., norbornane, bicyclo[2.2.2]octane). A “carbocyclic ring” or “carbocyrill” can also be optionally substituted with one or more (e.g., one, two, or three) oxo groups. Non-limiting examples of monocyclic carbocyclic compounds include cyclopropyl, cyclobutyl, cyclopentyl, 1-cyclopenta-1-enyl, 1-cyclopenta-2-enyl, 1-cyclopenta-3-enyl, cyclohexyl, 1-cyclohexa-1-enyl, 1-cyclohexa-2-enyl, 1-cyclohexa-3-enyl, and cycloheptyl.
[0030] The term "aryl," as used herein, refers to a single aromatic ring or a multi-ring fused system. For example, an aryl group may have 6 to 20 carbon atoms, 6 to 14 carbon atoms, or 6 to 12 carbon atoms. Aryls include phenyl radicals. Aryls also include multi-ring fused systems (e.g., ring systems containing 2, 3, or 4 rings) having about 9 to 20 carbon atoms, with at least one ring being aromatic. Such multi-ring fused systems may, as needed, be substituted with one or more (e.g., 1, 2, or 3) oxo groups at any carbocyclic portion of the multi-ring fused system. It should be understood that the bonding sites of the multi-ring fused systems defined above can be at any position in the ring system containing the aryl or at any carbocyclic portion of the ring. Typical aryl groups include, but are not limited to, phenyl, indenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, and anthracenyl.
[0031] Those skilled in the art will understand that the compounds of the present invention having a chiral center exist and can be isolated in optically active and racemic forms. Some compounds may exhibit pleomorphism. It should be understood that the present invention encompasses any racemic, optically active, pleomorphic, stereoisomer, or mixture thereof of the compounds of the present invention having the useful properties described herein, and how the optically active form is prepared using a chiral stationary phase (e.g., by decomposition of the racemic form, by recrystallization techniques, by synthesis from optically active starting materials, by chiral synthesis, or by chromatographic separation) is well known in the art.
[0032] As used herein, “not containing or substantially not containing” means a topical composition containing less than about 1 wt.%, less than about 0.5 wt.%, less than about 0.25 wt.%, less than about 0.1 wt.%, less than about 0.05 wt.%, less than about 0.01 wt.%, or 0 wt.% of the aforementioned component.
[0033] Topical compositions According to various embodiments, the disclosure relates to topical compositions which are emulsions of an aqueous phase and an oily phase. The topical compositions include an antioxidant system comprising an ascorbate component and green tea polyphenols. In certain embodiments, the topical composition further comprises at least one additional cosmetically acceptable excipient.
[0034] The ascorbate component of any of the topical compositions described herein may include ascorbic acid or its derivatives, such as ascorbyl palmitate, sodium ascorbate, potassium ascorbate, ammonium ascorbate, triethanolamine ascorbate, ascorbyl phosphate, or magnesium ascorbyl phosphate; ascorbic acid polypeptide; ascorbyl glucosamine; ascorbic acid polymer; ascorbic acid ester; ascorbic acid amide; L-ascorbic acid, known as vitamin C; tetrahexyldecyl ascorbate or other derivatives; or related compounds, including acerola extract, citrus extract, or botanical or herbal extracts such as strawberry, which can supply L-ascorbic acid or its derivatives. In certain embodiments, the ascorbate component of the topical composition includes ascorbic acid, tetrahexyldecyl ascorbate, or a combination thereof.
[0035] The ascorbate component of any of the topical compositions described herein may be present in concentrations ranging from about 0.1 wt.%, about 1 wt.%, about 5 wt.%, about 10 wt.%, about 12 wt.%, about 15 wt.%, about 18%, about 20 wt.%, about 23 wt.%, or about 25 wt.%, to about 28 wt.%, about 30 wt.%, about 35 wt.%, about 40 wt.%, about 45 wt.%, about 50 wt.%, about 75 wt.%, or about 95 wt.%, based on the total weight of the topical composition. In certain embodiments, the ascorbate component is present in any of the topical compositions described herein in amounts ranging from about 5 wt.% to about 40 wt.%, about 10 wt.% to about 30 wt.%, or about 15 wt.% to about 25 wt.%, based on the total weight of the topical composition.
[0036] In certain embodiments, the ascorbate component includes ascorbic acid (e.g., L-ascorbic acid) in the topical composition in amounts ranging from about 2 wt.% to about 30 wt.%, about 5 wt.% to about 25 wt.%, about 10 wt.% to about 30 wt.%, or about 10 wt.% to about 20 wt.%, based on the total weight of the topical composition.
[0037] In certain embodiments, the ascorbate component is present in the topical composition in amounts ranging from about 1 wt.% to about 20 wt.%, about 1 wt.% to about 15 wt.%, about 2 wt.% to about 20 wt.%, about 2 wt.% to about 10 wt.%, or about 3 wt.% to about 7 wt.%, based on the total weight of the topical composition, including tetrahexyldecyl ascorbate.
[0038] In certain embodiments, the ascorbate component of the topical composition includes, comprises, consists of, or essentially comprises L-ascorbic acid combined with tetrahexyldecyl ascorbate in concentrations (individually or cumulatively) ranging by weight from about 0.1 wt.%, about 1 wt.%, about 5 wt.%, about 10 wt.%, about 12 wt.%, about 15 wt.%, about 18 wt.%, about 20 wt.%, about 23 wt.%, or about 25 wt.%, to about 28 wt.%, about 30 wt.%, about 35 wt.%, about 40 wt.%, about 45 wt.%, about 50 wt.%, about 75 wt.%, or about 95 wt.%, based on the total weight of the topical composition.
[0039] In certain embodiments, the ascorbate component comprises, or essentially comprises, L-ascorbic acid combined with tetrahexyldecyl ascorbate in weight up to a weight ratio of L-ascorbic acid to tetrahexyldecyl ascorbate of about 10:1 to about 1:10, about 8:1 to about 1:8, about 5:1 to about 1:5, about 3:1 to about 1:3, about 3:1 to about 1:1, about 5:1 to about 1:1, about 8:1 to about 1:1, or about 10:1 to about 1:1.
[0040] Certain plants, such as green tea, which are composed of high-content polyphenols that are bioflavonoids and possess antioxidant properties, are included in any of the topical compositions described herein. The antioxidant system of the topical compositions described herein is, based on the total weight of the topical composition, in any of the following amounts: greater than 0%, about 0.01 wt.%, about 0.05 wt.%, about 0.1 wt.%, about 0.15 wt.%, about 0.2 wt.%, about 0.25 wt.%, about 0.3 wt.%, about 0.35 wt.%, or about 0.4 wt.%, about 0.45 wt.%, about 0.5 wt.%, about 0.55 wt.%, or about 0.6 wt.%. It may be present at concentrations up to t.%, approximately 0.65 wt.%, approximately 0.7 wt.%, approximately 0.75 wt.%, approximately 0.8 wt.%, approximately 0.85 wt.%, approximately 0.9 wt.%, approximately 0.95 wt.%, approximately 1 wt.%, approximately 1.5 wt.%, approximately 2 wt.%, approximately 3 wt.%, approximately 4 wt.%, approximately 5 wt.%, approximately 6 wt.%, approximately 7 wt.%, approximately 8 wt.%, approximately 9 wt.%, or approximately 10 wt.%.
[0041] In certain embodiments, the topical composition contains an effective amount of polyphenol isolates derived from green tea, which possess potent antioxidant properties that help minimize free radical-induced skin damage. Suitable green tea polyphenols include, but are not limited to, catechins, e.g., epigallocatechin gallate (EGCG), epigallocatechin (EGC), epicatechin gallate (ECG), and epicatechin (EC), their cis and trans isomers, their salts, their equivalent derivatives, and combinations thereof.
[0042] In certain embodiments, the topical composition comprises an antioxidant system containing any of the green tea polyphenols described herein, in combination with at least one additional antioxidant.
[0043] In one embodiment, additional antioxidants in the antioxidant system can be selected from the group consisting of cinnamic acid, ferulic acid, caffeic acid, p-coumaric acid, sinapic acid, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof. In another embodiment, additional antioxidants in the antioxidant system (and generally in topical compositions) may not include or substantially include cinnamic acid, ferulic acid, caffeic acid, p-coumaric acid, sinapic acid, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof.
[0044] In certain embodiments, additional antioxidants in the antioxidant system can be selected from the group consisting of gallic acid, delphinidin, luteolin, quercetin, cyanidin, taxifolin, kaempferol, malvidin, hesperidin, pelargonidin, apigenin, naringenin, chrysin, ergothioneine, glutathione, Emblica, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof.
[0045] In certain embodiments, additional antioxidants in the antioxidant system can be selected from the group consisting of apigenin, ergothioneine, glutathione, Emblica, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof.
[0046] Each antioxidant in the antioxidant system is, based on the total weight of the topical composition, in any of the following ranges: greater than 0 wt.%, about 0.01 wt.%, about 0.05 wt.%, about 0.1 wt.%, about 0.15 wt.%, about 0.2 wt.%, about 0.25 wt.%, about 0.3 wt.%, about 0.35 wt.%, or about 0.4 wt.%, ranging from about 0.45 wt.%, about 0.5 wt.%, about 0.55 wt.%, about 0.6 wt.%, and about They may be present individually or cumulatively at concentrations up to 0.65 wt.%, approximately 0.7 wt.%, approximately 0.75 wt.%, approximately 0.8 wt.%, approximately 0.85 wt.%, approximately 0.9 wt.%, approximately 0.95 wt.%, approximately 1 wt.%, approximately 1.5 wt.%, approximately 2 wt.%, approximately 3 wt.%, approximately 4 wt.%, approximately 5 wt.%, approximately 6 wt.%, approximately 7 wt.%, approximately 8 wt.%, approximately 9 wt.%, or approximately 10 wt.%.
[0047] In certain embodiments, the antioxidant system includes apigenin present in the topical composition in amounts ranging from more than 0 wt.% to about 0.5 wt.%, more than 0 wt.% to about 0.1 wt.%, or more than 0 wt.% to about 0.01 wt.%, based on the total weight of the topical composition.
[0048] In certain embodiments, the antioxidant system includes ergothioneine present in the topical composition in amounts ranging from more than 0 wt.% to about 0.5 wt.%, more than 0 wt.% to about 0.1 wt.%, or more than 0 wt.% to about 0.01 wt.%, based on the total weight of the topical composition.
[0049] In certain embodiments, the antioxidant system contains green tea polyphenols in amounts ranging from more than 0 wt.% to about 0.5 wt.%, more than 0 wt.% to about 0.1 wt.%, or more than 0 wt.% to about 0.01 wt.%, based on the total weight of the topical composition.
[0050] In certain embodiments, the antioxidant system is based on the total weight of the topical composition and is one of the following: greater than 0 wt.%, about 0.01 wt.%, about 0.05 wt.%, about 0.1 wt.%, about 0.15 wt.%, about 0.2 wt.%, about 0.25 wt.%, about 0.3 wt.%, about 0.35 wt.%, or about 0.4 wt.%, ranging from about 0.45 wt.%, about 0.5 wt.%, about 0.55 wt.%, about 0.6 wt.%, about 0.65 wt.%, about 0.7 wt.%, about 0.75 wt.%, about 0.8 wt.%, or about 0.85 wt.%. A combination of any of the green tea polyphenols described herein and at least one of apigenin and ergothioneine, in concentrations (individually or cumulatively) up to approximately 0.9 wt.%, approximately 0.95 wt.%, approximately 1 wt.%, approximately 1.5 wt.%, approximately 2 wt.%, approximately 3 wt.%, approximately 4 wt.%, approximately 5 wt.%, approximately 6 wt.%, approximately 7 wt.%, approximately 8 wt.%, approximately 9 wt.%, or approximately 10 wt.%, includes, contains, consists of, or essentially comprises, any combination of any of the green tea polyphenols described herein and at least one of apigenin and ergothioneine.
[0051] In certain embodiments, the weight ratio of green tea polyphenols to one or more additional antioxidants ranges (individually or cumulatively) from about 10:1 to about 1:10, from about 8:1 to about 1:8, from about 5:1 to about 1:5, from about 3:1 to about 1:3, from about 2:1 to about 1:2, or about 1:1.
[0052] In certain embodiments, the topical composition further comprises cosmetically acceptable excipients. Exemplary cosmetically acceptable excipients include, but are not limited to, epidermal penetration enhancers, solvents, mild surfactants, oils, emulsifiers, pearlescent waxes, consistency modifiers, thickeners, rheological modifiers, suspending agents, chelating agents, preservatives, superfatting agents, stabilizers, polymers, silicones or siloxane compounds, fats, waxes, lecithins, phospholipids, UV photoprotective factors, bioactive ingredients, additional antioxidants, deodorants, antiperspirants, anti-dandruff agents, film-forming agents, swelling agents, insect repellents, self-tanning agents, tyrosinase inhibitors, hydrotropes, solubilizers, fragrances, pigments, zinc oxide, fatty alcohols, fatty acid esters, adjuvants, natural or synthetic triglycerides including glyceryl esters and derivatives, hydrocarbon oils, superfatting agents, polymers, bioactive ingredients, hydrophrenic agents, antibacterial inhibitors, colorants, UV screening agents, agents that absorb UV light and provide photoprotection to the skin, or combinations thereof. In certain embodiments, the topical composition comprises a cosmetically acceptable excipient selected from the group consisting of a solvent, emulsifier, consistency modifier, thickener, suspending agent, additional antioxidant, preservative, fragrance oil, or a combination thereof. In certain embodiments, the topical composition is free of or substantially free of silicone compounds.
[0053] Suitable solvents that can be used in the topical compositions described herein include, but are not limited to, polysorbate 20, water, alkanediols (e.g., ethylene glycol, propylene glycol, butylene glycol), ethoxylated or propoxylated diglycols, ethanol, propanol, isopropanol, glycerin, methoxyisopropanol, PPG-2 methyl ether, PPG-3 methyl ether, propylene glycol butyl ether, PPG-2 butyl ether, phenoxyisopropanol, butoxyethanol, butoxydiglycol, methoxydiglycol, phenoxyethanol, PPG-3 butyl ether, PPG-2 propyl ether, propylene glycol propyl ether or dipropylene glycol dimethyl ether, or mixtures and combinations thereof, or their individual ethoxylates, propoxylates and glyceryl esters.
[0054] In certain embodiments, the solvent includes, comprises, consists of, or is essentially an alkanediol (such as ethylene glycol, propylene glycol, or butylene glycol), glycerin, water, or a mixture thereof. In one embodiment, the solvent includes, comprises, consists of, or is essentially a mixture of glycerin, propylene glycol, isopentyl diol, and water.
[0055] In some embodiments, each individual solvent or all solvents combined may be present in the topical composition at concentrations ranging from about 0.5 wt.%, about 1 wt.%, about 5 wt.%, about 10 wt.%, about 12 wt.%, about 15 wt.%, about 18 wt.%, about 20 wt.%, about 23 wt.%, or about 25 wt.%, based on the total weight of the topical composition, to about 28 wt.%, about 30 wt.%, about 35 wt.%, about 40 wt.%, about 45 wt.%, about 50 wt.%, about 55 wt.%, about 60 wt.%, about 65 wt.%, about 70 wt.%, about 75 wt.%, or about 95 wt.% based on the total weight of the topical composition. In a particular embodiment, the concentrations of all solvents in the topical composition, excluding water, range from about 0.5 wt.%, about 1 wt.%, about 5 wt.%, about 10 wt.%, about 12 wt.%, about 15 wt.%, about 18 wt.%, about 20 wt.%, about 23 wt.%, or about 25 wt.%, to about 28 wt.%, about 30 wt.%, about 35 wt.%, about 40 wt.%, about 45 wt.%, or about 50 wt.%, based on the total weight of the topical composition.
[0056] In certain embodiments, the cosmetically acceptable excipients include an alkanediol (e.g., propylene glycol, also known as propanediol) present in the topical composition in amounts of about 2 wt.% to about 25 wt.%, about 5 wt.% to about 15 wt.%, or about 8 wt.% to about 12 wt.%, based on the total weight of the topical composition.
[0057] In certain embodiments, cosmetically acceptable excipients include glycerin in the topical composition in amounts of about 2 wt.% to about 25 wt.%, about 5 wt.% to about 15 wt.%, or about 8 wt.% to about 12 wt.%, based on the total weight of the topical composition.
[0058] In certain embodiments, the cosmetically acceptable excipients include water in the topical composition in amounts of about 5 wt.% to about 95 wt.%, about 10 wt.% to about 95 wt.%, about 20 wt.% to about 80 wt.%, about 35 wt.% to about 70 wt.%, or about 50 wt.% to about 60 wt.%, based on the total weight of the topical composition.
[0059] In certain embodiments, cosmetically acceptable excipients include natural gums (e.g., natural plant gums). Suitable natural gums include, but are not limited to, guar gum, carob gum, konjac gum, xanthan gum, sclerotium gum, acacia gum, cellulose gum (modified or unmodified), or combinations thereof. In one embodiment, the natural gum in the topical composition is sclerotium gum. The natural gum contributes to the texture of the topical composition and may also act as a suspending agent for the oily phase in the aqueous phase of the emulsion.
[0060] In certain embodiments, cosmetically acceptable excipients include natural gum in the topical composition in amounts ranging from more than 0 wt.% to about 5 wt.%, from about 0.1 wt.% to about 2 wt.%, or from about 0.2 wt.% to about 0.8 wt.%, based on the total weight of the topical composition.
[0061] In certain embodiments, cosmetically acceptable excipients include emulsifiers. Suitable emulsifiers include, but are not limited to, PEG-30 dipolyhydroxystearate, PEG-4 dilaurate, PEG-8 dioleate, PEG-40 sorbitan peroleate, PEG-7 glyceryl cocoate, PEG-20 almond glyceride, PEG-25 hydrogenated castor oil, glyceryl stearate (and) PEG-100 stearate, PEG-7 olive fatty acid, PEG-8 oleate, PEG-8 laurate, PEG-60 almond glyceride, PEG-20 methyl glucose sesquistearate, PEG-40 stearate, PEG-100 stearate, and laurate. Examples include PEG-80 sorbitan phosphate, steareth-2, steareth-12, oleth-2, ceteth-2, laureth-4, oleth-10, oleth-10 / polyoxyl-10 oleyl ether, ceteth-10, isosteareth-20, ceteareth-20, oleth-20, steareth-20, steareth-21, ceteth-20, isoceteth-20, laureth-23, steareth-100, glyceryl stearate citrate, glyceryl stearate SE (self-emulsifying), stearic acid, salts of stearic acid, polyglyceryl-3-methyl glucose distearate, or combinations thereof.
[0062] Further preferred emulsifiers include phosphate esters and their salts, such as cetyl phosphate (Amphisol® A), cetyl phosphate diethanolamine (Amphisol® DEA), potassium cetyl phosphate (Amphisol® K), sodium cetearyl sulfate, sodium glyceryl oleate phosphate, hydrogenated vegetable glycerides and mixtures thereof. Further preferred emulsifiers include sorbitan oleate, sorbitan sesquioleate, sorbitan isostearate, sorbitan trioleate, cetearyl glucoside, lauryl glucoside, decyl glucoside, sodium stearoyl glutamate, sucrose polystearate, and hydrated polyisobutene. In addition, one or more synthetic polymers can be used as emulsifiers. For example, PVP eicosen copolymer, acrylate / C 10 ~30 Alkyl acrylate crosspolymer, acrylate / steareth-20 methacrylate copolymer, PEG-22 / dodecyl glycol copolymer, PEG-45 / dodecyl glycol copolymer, and mixtures thereof.
[0063] In certain embodiments, cosmetically acceptable excipients include an emulsifier in the topical composition in amounts of more than 0 wt.% to about 5 wt.%, about 0.1 wt.% to about 2 wt.%, or about 0.2 wt.% to about 0.8 wt.%, based on the total weight of the topical composition. In one embodiment, cosmetically acceptable excipients include an emulsifier, which is olive fatty acid PEG-7, in the topical composition in amounts of more than 0 wt.% to about 5 wt.%, about 0.1 wt.% to about 2 wt.%, or about 0.2 wt.% to about 0.8 wt.%, based on the total weight of the topical composition.
[0064] In certain embodiments, cosmetically acceptable excipients include chelating agents. Suitable chelating agents include, but are not limited to, disodium ethylenediaminetetraacetate (EDTA), diethylenetriaminepentaacetic acid (DTPA), N-(hydroxyethyl)-ethylenediaminetriacetic acid (HEDTA), and nitrilotriacetic acid (NTA).
[0065] In certain embodiments, the cosmetically acceptable excipients include a chelating agent in the topical composition in amounts of more than 0 wt.% to about 5 wt.%, about 0.01 wt.% to about 0.5 wt.%, or about 0.05 wt.% to about 0.3 wt.%, based on the total weight of the topical composition. In one embodiment, the cosmetically acceptable excipients include a chelating agent, which is EDTA, in the topical composition in amounts of more than 0 wt.% to about 5 wt.%, about 0.01 wt.% to about 0.5 wt.%, or about 0.05 wt.% to about 0.3 wt.%, based on the total weight of the topical composition.
[0066] In certain embodiments, cosmetically acceptable excipients include additional antioxidants, such as forms of vitamin E. Preferred forms of vitamin E that can be included in topical compositions can be selected from alpha, beta, delta, and gamma tocopherols, as well as alpha, beta, delta, and gamma tocotrienols, and combinations thereof.
[0067] In certain embodiments, any combination of any form of vitamin E may be present in the topical composition (individually or cumulatively) in amounts of about 0.1 wt.% to about 5 wt.%, about 0.3 wt.% to about 3 wt.%, or about 0.5 wt.% to about 2 wt.%, based on the total weight of the topical composition.
[0068] In certain embodiments, cosmetically acceptable excipients in topical compositions include preservatives. Suitable preservatives include, for example, solutions of phenoxyethanol, parabens, pentanediol, and sorbic acid, as well as silver complexes known under the commercially available reference Surfacine®, and other classes of substances set out in Appendix 6, Parts A and B of the Cosmetic Regulation, i.e., suitable preservatives.
[0069] In certain embodiments, the cosmetically acceptable excipients include a preservative in an amount of greater than 0 to about 5 wt.%, about 0.3 wt.% to about 3 wt.%, or about 0.5 wt.% to about 2 wt.%, based on the total weight of the topical composition. In certain embodiments, the cosmetically acceptable excipients include a preservative, phenoxyethanol, in an amount of greater than 0 to about 5 wt.%, about 0.3 wt.% to about 3 wt.%, or about 0.5 wt.% to about 2 wt.%, based on the total weight of the topical composition.
[0070] In certain embodiments, cosmetically acceptable excipients include fragrant oils. Preferred fragrant oils include mixtures of natural and synthetic fragrances. Natural fragrances are extracts from flowers (lily, lavender, rose, jasmine, neroli, ylang-ylang), stems and leaves (geranium, patchouli, petitgrain), fruits (aniseed, coriander, cumin, juniper), fruit peels (bergamot, lemon, orange), roots (mace, angelica, celery, cardamom, costus, iris, calamus), woods (pine, sandalwood, guaiac wood, cedar, rosewood), herbs and plants (tarragon, lemongrass, sage, thyme), needles and branches (spruce, fir, pine, pine), resins and balsams (galbanum, elemi, benzoin, myrrh, olibanum, opoponax). Typical synthetic aromatic compounds are ester, ether, aldehyde, ketone, alcohol, and hydrocarbon products. Examples of ester-type aromatic compounds include benzyl acetate, phenoxyethyl isobutyrate, p-tert-butylcyclohexyl acetate, linalyl acetate, dimethylbenzylcarbinyl acetate, phenylethyl acetate, linalyl benzoate, benzyl formate, ethyl-methylphenylglycinate, allyl cyclohexylpropionate, styraryl propionate, and benzyl salicylate. Examples of ethers include benzyl ethyl ether; examples of aldehydes include linear alcanals having 8 to 18 carbon atoms, citral, citronellal, citronellyloxyacetaldehyde, cyclamenaldehyde, hydroxycitronellal, lilial, and burgeonal; examples of ketones include ionone, α-isomethylionone, and methylcedyl ketone; examples of alcohols include anethole, citronellol, eugenol, isoeugenol, geraniol, linalool, phenylethyl alcohol, and terpineol; and examples of hydrocarbons include mainly terpenes and balsams.
[0071] In addition, essential oils with relatively low volatility, primarily used as aromatic components, are suitable as fragrance oils, such as sage oil, chamomile oil, clove oil, melissa oil, mint oil, cinnamon leaf oil, linden flower oil, juniper berry oil, vetiver oil, olibanum oil, galbanum oil, labdanum oil, and lavandin oil. Other suitable oils, either alone or in mixtures, include bergamot oil, dihydromyrcenol, lilial, liral, citronellol, phenylethyl alcohol, α-hexyl cinnamaldehyde, geraniol, benzylacetone, cyclamenaldehyde, linalool, boytham blenforte, ambroxan, indole, hedione, sandelice, lemon oil, mandarin oil, orange oil, allylamyl glycolate, cyclobertal, lavandin oil, clary sage oil, β-damascone, geranium oil bourbon, cyclohexyl salicylate, Vertofixeseu, iso-E-super, fixolid NP, ebernyl, iraldine gamma, phenylacetic acid, geranylacetic acid, benzyl acetate, rose oxide, romilat, ilotyl, and floramate.
[0072] In certain embodiments, cosmetically acceptable excipients include fragrance oils, which are essential oils selected from the group consisting of lavender oil, bergamot oil, eucalyptus oil, chamomile oil, melaleuca oil, or combinations thereof. In one embodiment, cosmetically acceptable excipients include lavender oil, chamomile oil, or combinations thereof.
[0073] In certain embodiments, the fragrance oils (each fragrance oil individually or cumulatively all fragrance oils in the topical composition) are present in the topical composition in amounts ranging from more than 0 wt.% to about 5 wt.%, more than 0 wt.% to about 1 wt.%, or from about 0.01 wt.% to about 0.3 wt.%, based on the total weight of the topical composition.
[0074] In certain embodiments, the pH of the topical composition ranges from about 2.0, about 2.1, about 2.2, about 2.3, about 2.4, about 2.5, about 2.6, about 2.7, about 2.8, about 2.8, or about 2.9 to about 3.0, about 3.1, about 3.2, about 3.3, about 3.4, about 3.5, about 3.6, about 3.7, about 3.8, about 3.8, about 3.9, or about 4.0. In certain embodiments, the pH of the topical composition ranges from about 2.0 to about 4.0, about 2.5 to about 3.5, or about 2.7 to about 3.3.
[0075] In certain embodiments, the topical compositions described herein are lightweight formulations comprising fast-absorbing components and / or components that diffuse into the skin over time. In certain embodiments, the formulations provide one or more of the benefits of skin moisturization, environmental protection, skin tone brightening, and anti-aging. In certain embodiments, the texture of the topical composition is one or more of smooth, silky, soft, and non-greasy.
[0076] The topical compositions described herein may be formulated as any dermatologically acceptable vehicle, such as a serum, emulsion, cream, foam, spray, ointment, gel, or lotion, or as a pad or roll-on application formulation, which may contain ingredients for physically or cosmetically improving, modifying, or stabilizing the composition.
[0077] The topical compositions relating to this disclosure may also contain one or more additional cosmetically acceptable excipients as described below.
[0078] fatty alcohol Guerbet alcohols based on fatty alcohols having 6 to 18, preferably 8 to 10, carbon atoms, including cetyl alcohol, stearyl alcohol, cetearyl alcohol, oleyl alcohol, octyldodecanol, benzoates of C12-C15 alcohols, acetylated lanolin alcohol, etc.
[0079] fatty acid esters Linear C3~C 24 Linear C6-C with alcohol 24 Fatty acid esters, linear C6-C 24 Branching off from fatty alcohols C6~C 13 Carboxylic acid esters, linear C6-C6 compounds with branched alcohols 24 Fatty acid esters, especially 2-ethylhexanol, linear or branched C6-C 22 Esters of hydroxycarboxylic acids with fatty alcohols, especially dioctyl malate, polyhydric alcohols (e.g., propylene glycol, dimeric diols or trimer triols) and / or Guerbet alcohols, such as caproic acid, caprylic acid, 2-ethylhexanoic acid, capric acid, lauric acid, isotridecanoic acid, myristic acid, palmitic acid, palmitoleic acid, stearic acid, isostearic acid, oleic acid, elaidic acid, petroseric acid, linoleic acid, linolenic acid, ellaeostearic acid, arachidic acid, gadoleic acid, behenic acid and erucic acid, and technical grade mixtures thereof (e.g., obtained by pressure removal of natural fats and oils, reduction of aldehydes from Roelen oxo synthesis, or dimerization of unsaturated fatty acids), alcohols, such as isopropyl alcohol, caproic acid alcohol, Esters of linear and / or branched fatty acids with caprylic alcohol, 2-ethylhexyl alcohol, caprin alcohol, lauryl alcohol, isotridecyl alcohol, myristyl alcohol, cetyl alcohol, palmoleil alcohol, stearyl alcohol, isostearyl alcohol, oleyl alcohol, elaidyl alcohol, petroselinyl alcohol, linoleyl alcohol, linolenyl alcohol, elaeostearyl alcohol, arachidyl alcohol, gadleyl alcohol, behenyl alcohol, erucyl alcohol and brassidyl alcohol and technical grade mixtures thereof (e.g., obtained as monomer fractions by technical grade methyl esters or aldehydes from Roelen oxo synthesis based on fats and oils, and by dimerization of unsaturated fatty alcohols).
[0080] Examples of such ester oils are isopropyl myristate, isopropyl palmitate, isopropyl stearate, isopropyl isostearate, isopropyl oleate, n-butyl stearate, n-hexyl laurate, n-decyl oleate, isooctyl stearate, isononyl isononanoate, isononyl isononanoate, 2-ethylhexyl palmitate, 2-hexyl laurate, 2-hexyl decyl stearate, 2-octyldodecyl palmitate, oleyl oleate, oleyl elicate, elsyl oleate, elsyl elicate, cetearyl octanoate, cetyl palmitate, cetyl stearate, cetyl oleate, cetyl behenate, cetyl acetate, myristyl myristate, myristyl behenate, myristyl oleate, myristyl stearate, myristyl palmitate, myristyl lactate, propylene glycol dicaprylate / caprate, stearyl heptanoate, diisostearyl malate, octyl hydroxystearate, etc.
[0081] Other adjuvants Diethylhexyl 2,6-naphthalate, di-n-butyl adipate, di(2-ethylhexyl)-adipate, di(2-ethylhexyl)-succinate and diisotridecyl acetate, and furthermore diol esters, for example, ethylene glycol dioleate, ethylene glycol diisotridecanoate, propylene glycol di(2-ethylhexanoate), propylene glycol diisostearate, propylene glycol dipelargonate, butanediol diisostearate and neopentyl glycol dicaprylate. Aromatic carboxylic acids, saturated and / or unsaturated, especially C6-C 24 Esters of fatty alcohols and / or geraniol, straight-chain or branched alcohols having from one to twenty-two carbon atoms or polyols having from two to ten carbon atoms and from two to six hydroxy groups with C2-C 12 Esters of dicarboxylic acids.
[0082] Natural or synthetic triglycerides and derivatives including glyceryl esters C6-C modified by reaction with other alcohols 18 Di or triglycerides based on fatty acids (e.g., caprylic / capric triglyceride, wheat germ glyceride). Fatty acid esters of polyglycerin (polyglyceryl-n, e.g., polyglyceryl-4 caprate, polyglyceryl-2 isostearate, etc.), or castor oil, hydrogenated vegetable oil, sweet almond oil, wheat germ oil, sesame oil, hydrogenated cottonseed oil, coconut oil, avocado oil, corn oil, hydrogenated castor oil, shea butter, cocoa butter, soybean oil, mink oil, sunflower oil, safflower oil, macadamia nut oil, olive oil, hydrogenated animal fat, apricot kernel oil, hazelnut oil, borage oil, etc.
[0083] Waxes containing esters of long-chain acids and alcohols, as well as compounds having wax-like properties, such as carnauba wax, beeswax (white or yellow), lanolin wax, candelilla wax, ozokerite, japonica wax, paraffin wax, microcrystalline wax, ceresin, cetearyl ester wax, synthetic beeswax, etc. Furthermore, hydrophilic waxes as cetearyl alcohol or partial glycerides.
[0084] Pearlescent wax: Alkylene glycol esters, particularly ethylene glycol distearate; fatty acid alkanolamides, particularly coco-fatty acid diethanolamide; partial glycerides, particularly monoglyceride stearate; esters of polyvalent, unsubstituted or hydroxysubstituted carboxylic acids with fatty alcohols having 6 to 22 carbon atoms, particularly long-chain esters of tartaric acid; fatty substances, e.g., fatty alcohols, fatty ketones, fatty aldehydes, fatty ethers and fatty carbonates having at least 24 carbon atoms in total, particularly lauryl and distearyl ethers; fatty acids, e.g., stearic acid, hydroxystearic acid or behenic acid; ring-opening products of olefin epoxides having 12 to 22 carbon atoms with fatty alcohols having 12 to 22 carbon atoms, and / or polyols having 2 to 15 carbon atoms and 2 to 10 hydroxyl groups, and mixtures thereof.
[0085] hydrocarbon oils: Mineral oils (light oil or heavy oil), petrolatum (yellow or white), microcrystalline waxes, paraffinic and isoparaffinic compounds, hydrogenated isoparaffinic molecules as polydecene and polybutene, hydrogenated polyisobutene, squalane, isohexadecane, isododecane, and others from the plant and animal kingdoms.
[0086] Silicone or siloxane (organo-substituted polysiloxane) Dimethylpolysiloxane, methylphenylpolysiloxane, cyclic silicones, and, moreover, amino, fatty acid, alcohol, polyether, epoxy, fluorine, glycoside and / or alkyl-modified silicone compounds, which may be either liquid or resinous at room temperature. Linear polysiloxanes, dimethicone (Dow Corning 200 fluid, Rhodia Mirasil DM), dimethiconol, cyclic silicone fluids, cyclopentasiloxane volatiles (Dow Corning 345 fluid), phenyl trimethicone (Dow Corning 556 fluid). More preferably, simethicone is a mixture of dimethicone and a hydrogenated silicate having an average chain length of 200 to 300 dimethylsiloxane units. A further detailed study of preferred volatile silicones by Todd et al. can be found in Cosm. Toil. 91, 27 (1976).
[0087] emulsifier Any conventionally available emulsifier can be used for the composition. The emulsifier system may include, for example,: carboxylic acids and their salts: alkaline soaps of sodium, potassium, and ammonium; metallic soaps of calcium or magnesium; organic basic soaps, e.g., lauric acid, palmitic acid, stearic acid, and oleic acid; alkyl phosphates or phosphate esters, acid phosphates, diethanolamine phosphate, potassium cetyl phosphate; ethoxylated carboxylic acids or polyethylene glycol esters, PEG-n acylates; branched 2 to 30 mol ethylene oxide and / or 0 to 5 mol propylene oxide, with linear fatty alcohols having 8 to 22 carbon atoms, fatty acids having 12 to 22 carbon atoms, and alkylphenols having 8 to 15 carbon atoms in the alkyl group; fatty alcohol polyglycol ethers, e.g., laureth-n, ceteareth-n, steareth-n, oleth-n; fatty acid polyglycol ethers, e.g., PEG-n stearate, PEG-n oleate, PEG-n coconut oil fatty acid. Monoglycerides and polyol esters. C12-C22 fatty acid mono and diesters of addition products of 1 to 30 mol of ethylene oxide with polyols. Fatty acid and polyglycerol esters, e.g., monostearate glycerol, diisostearoyl polyglyceryl-3-diisostearate, polyglyceryl-3-diisostearate, triglyceryl diisostearate, polyglyceryl-2-sesquiisostearate, or polyglyceryl dimerate. Mixtures of compounds from multiple of these material classes are also suitable. Fatty acid polyglycol esters, e.g., monostearate diethylene glycol, fatty acid and polyethylene glycol esters, fatty acid and sucrose esters, e.g., sucrose esters, glycerol and sucrose esters, e.g., sucrose glycerides. Sorbitol and sorbitan, sorbitan mono and diesters of saturated and unsaturated fatty acids having 6 to 22 carbon atoms, as well as ethylene oxide addition products.Polysorbate-n series, sorbitan esters, e.g., sesquiisostearate, sorbitan, PEG-(6)-isostearate sorbitan, PEG-(10)-laurate sorbitan, PEG-17-dioleate sorbitan. Glucose derivatives, C8-C22 alkyl-mono and oligo-glycosides and ethoxylated analogs, with glucose preferred as the sugar component. O / W emulsifiers, e.g., methyl gluceth-20 sesquistearate, sorbitan stearate / coconut fatty acid sucrose, methyl glucose sesquistearate, cetearyl alcohol / cetearyl glucoside. W / O emulsifiers, e.g., methyl glucose dioleate / methyl glucose isostearate. Sulfates and sulfonated derivatives, dialkyl sulfosuccinates, dioctyl succinate, alkyl lauryl sulfonates, linear sulfonated paraffins, tetrapropylene sulfonated sulfonates, sodium lauryl sulfate, ammonium and ethanolamine lauryl sulfates, lauryl ether sulfates, sodium laureth sulfate, sulfosuccinates, acetyl isothionate, alkanolamide sulfates, taurine, methyl taurine, imidazole sulfate. Polysiloxane / polyalkyl / polyether copolymers and derivatives, dimethicone, copolyols, silicone polyethylene oxide copolymers, silicone glycol copolymers. Propoxylated or POE-n ethers (meloxapole), poloxamers or poly(oxyethylene) m-block-poly(oxypropylene) n-block (oxyethylene). Amphoteric surfactants supporting at least one quaternary ammonium group and at least one carboxylate group and / or sulfonate group in the molecule.Particularly suitable amphoteric surfactants are betaines, such as N-alkyl-N,N-dimethylammonium glycinates, cocoalkyldimethylammonium glycinates, N-acylaminopropyl-N,N-dimethylammonium glycinates, cocoacylaminopropyldimethylammonium glycinates, and 2-alkyl-3-carboxymethyl-3-hydroxyethylimidazolines, each having 8 to 18 carbon atoms in the alkyl or acyl group, as well as cocoacylaminoethylhydroxyethylcarboxymethyl glycinates, N-alkylbetaines, N-alkylaminobetaines, alkylimidazolines, alkylopeptides, lipoamino acids, self-emulsifying bases, and compounds as described in KF DePolo, A short textbook of cosmetology, Chapter 8, Table 8-7, pp. 250-251.
[0088] Nonionic bases, for example, PEG-6 beeswax (and) PEG-6 stearate (and) polyglyceryl-2-isostearate, glyceryl stearate (and) PEG-100 stearate, PEG-5 glyceryl stearate, sorbitan oleate (and) polyglyceryl-3 ricinolate, sorbitan stearate and sucrose coconut fatty acid, glyceryl stearate and laureth-23, cetearyl alcohol and ceteth-20, cetearyl alcohol and polysorbate 60 and PEG-150 and stearate-20, cetearyl alcohol and cetearyl polyglucoside, cetearyl alcohol and ceteareth-20, cetearyl alcohol and PEG-40 castor oil, cete Allyl alcohol and PEG-40 castor oil and sodium cetearyl sulfate, stearyl alcohol and steareth-7 and steareth-10, cetearyl alcohol and steareth-7 and steareth-10, glyceryl stearate and PEG-75 stearate, propylene glycol ceteth-3 acetate, propylene glycol isoceth-3 acetate, cetearyl alcohol and ceteth-12 and oleth-12, PEG-6 stearate and PEG-32 stearate, PEG-6 stearate and ceteth-20 and steareth-20, PEG-6 stearate and ceteth-20 and glyceryl stearate and steareth-20, glyceryl stearate and ceteareth-20.
[0089] Anionic alkaline bases, e.g., PEG-2 SE stearate, glyceryl SE stearate, propylene glycol stearate. Anionic acid-bases, e.g., cetearyl alcohol and sodium cetearyl sulfate, cetearyl alcohol and sodium lauryl sulfate, tollaneth-4 phosphate and glycol stearate, and PEG-2 stearate, glyceryl stearate and sodium lauryl sulfate. Cationic acid-bases, e.g., cetearyl alcohol and cetrimonium bromide.
[0090] Adjuvants and additives Cosmetic sunscreen compositions, such as creams, gels, lotions, alcoholic and aqueous / alcoholic solutions, emulsions, wax / fat compositions, stick preparations, powders, or ointments, may also contain, in addition, mild surfactants, superfatizers, consistency modifiers, thickeners, polymers, stabilizers, bioactive ingredients, swelling agents, further UV photoprotective factors, antioxidants, hydrolytic agents, preservatives, self-tanning agents, solubilizers, fragrances, colorants, and antibacterial inhibitors as further adjuvants and additives.
[0091] Superfat agent Suitable substances for use as superfatting agents include, for example, lanolin and lecithin, as well as polyethoxylated or acetylated lanolin and lecithin derivatives, polyol fatty acid esters, monoglycerides, and fatty acid alkanolamides, the latter of which also act as foam stabilizers.
[0092] surfactant Examples of suitable mild surfactants, i.e., surfactants that exhibit particularly good tolerance to the skin, include fatty alcohol polyglycol ether sulfates, sulfate monoglycerides, mono and / or dialkyl sulfosuccinates, fatty acid isethionates, fatty acid sarcosinates, fatty acid taurids, fatty acid glutamates, alpha-olefin sulfonates, ether carboxylic acids, alkyl oligoglucosides, fatty acid glucamides, alkylamide betaines, and / or protein fatty acid condensation products, the latter preferably based on wheat protein.
[0093] Consistency modifiers / thickeners and rheological modifiers Silicon dioxide, magnesium silicate, aluminum silicate, polysaccharides or their derivatives, such as hyaluronic acid, xanthan gum, guar guar, agar, alginate, carrageenan, gellan, pectin, or modified cellulose, such as hydroxycellulose, hydroxypropyl methylcellulose. In addition, the following are polyacrylates or homopolymers of acrylic acid and polyacrylamide, carbomers (CARBOPOL types 980, 981, 1382, ETD2001, ETD2020, ULTREZ10) or the SALCARE range, for example, SALCARE SC80 (steareth-10 allyl ether / acrylate copolymer), SALCARE SC81 (acrylate copolymer), SALCARE SC91 and SALCARE AST (sodium acrylate copolymer / PPG-1 trideceth-6), SEPIGEL 305 (polyacrylamide / laureth-7), SIMULGEL NS and SIMULGEL EG (hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer), STABILEN 30 (acrylate / vinyl isodecanoate crosspolymer), PEMULEN TR-1 (acrylate / C10-30 alkyl acrylate crosspolymer), LUVIGEL Examples include EM (sodium acrylate copolymer) and ACULYN28 (acrylate / beheneth-25 methacrylate copolymer).
[0094] polymer Examples of anionic, amphoteric, amphoteric, and nonionic polymers include vinyl acetate / crotonic acid copolymer, vinylpyrrolidone / vinyl acrylate copolymer, vinyl acetate / butyl maleate / isobornyl acrylate copolymer, methyl vinyl ether / maleic anhydride copolymer and its esters, uncrosslinked polyacrylic acid and polyacrylic acid crosslinked with polyols, acrylamidopropyl-trimethylammonium chloride / acrylate copolymer, octylacrylamide / methyl methacrylate-tert-butylaminoethyl methacrylate / 2-hydroxypropyl methacrylate copolymer, polyvinylpyrrolidone, vinylpyrrolidone / vinyl acetate copolymer, vinylpyrrolidone / dimethylaminoethyl methacrylate / vinyl caprolactam terpolymer, and, if necessary, derivatized cellulose ethers and silicones. Furthermore, polymers as described in European Patent No. 1093796 (pages 3-8, paragraphs 17-68) may be used.
[0095] Bioactive ingredients Bioactive ingredients should be understood to mean, for example, tocopherol, tocopherol acetate, tocopherol palmitate, deoxyribonucleic acid, retinol, bisabolol, allantoin, phytantriol, panthenol, AHA acids, amino acids, ceramides, pseudoceramides, essential oils, plant extracts, and complex vitamins.
[0096] Antioxidants In addition to primary photoprotective agents, secondary photoprotective agents of the antioxidant type can also be used to interrupt the photochemical reaction chains triggered when UV radiation penetrates the skin or hair. Typical examples of such antioxidants include amino acids (e.g., glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (e.g., urocanic acid) and their derivatives, peptides, e.g., D,L-carnosine, D-carnosine, L-carnosine and its derivatives (e.g., anserine), carotenoids, carotene, lycopene and its derivatives, chlorogenic acid and its derivatives, lipoic acid and its derivatives (e.g., dihydrolipoic acid), aurothioglucose, propylthiouracil and other thiols (e.g., thioredoxin, glutathione, cysteine, cystine, cystamine, and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl, lauryl, palmitoyl, oleyl, Linoleyl, cholesteryl and glyceryl esters) and their salts, dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acid and its derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and salts), and sulfoximine compounds (e.g., butionine sulfoximine, homocysteine sulfoximine, butionine sulfone, penta-, hexa-, hepta-thionine sulfoximine), and (metal) chelating agents (e.g., hydroxylipids) Fatty acids, phytic palmitate, lactoferrin), hydroxy acids (e.g., citric acid, lactic acid, malic acid), humic acid, bile acids, bile extracts, bilirubin, biliverdin, EDTA, EDDS, EGTA and its derivatives, unsaturated fatty acids and their derivatives (e.g., linolenic acid, linoleic acid, oleic acid), folic acid and its derivatives, ubiquinone and ubiquinol and their derivatives, vitamin C and its derivatives (e.g., ascorbyl palmitate, magnesium ascorbyl phosphate, ascorbyl acetate), tocopheryl Roll and derivatives (e.g., vitamin E acetate), vitamin A and derivatives (e.g., vitamin A palmitate), and thereafter benzoin resin coniferyl benzoate, rutin and its derivatives, glycosylrutin, ferulic acid, furfrillidendenglucitol, carnosine, butylhydroxytoluene, butylhydroxyanisole, nordihydroguayaletic acid, trihydroxybutyrophenone, uric acid and its derivatives, mannose and its derivatives, superoxide dismutase, N-[3-(3,[5-di-tert-butyl-4-hydroxyphenyl)propionyl]sulfanilic acid (and its salts, e.g., disodium salt), selenium and its derivatives (e.g., seleniummethionine), stilbene and its derivatives (e.g., stilbene oxide, trans-stilbene oxide), and preferred derivatives of the described active ingredients according to the present invention (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides, and lipids). HALS (= "hindered amine light stabilizers") compounds may also be described.
[0097] Hydrolytic agent To improve flow behavior, refractory agents may also be used, such as ethoxylated or non-ethoxylated mono-alcohols, diols, or polyols with a small number of carbon atoms, or their ethers (e.g., ethanol, isopropanol, 1,2-dipropanediol, propylene glycol, glycerin, ethylene glycol, ethylene glycol monoethyl ether, ethylene glycol monobutyl ether, propylene glycol monomethyl ether, propylene glycol monoethyl ether, propylene glycol monobutyl ether, diethylene glycol monomethyl ether; diethylene glycol monoethyl ether, diethylene glycol monobutyl ether, and similar products). Polyols considered for this purpose preferably have 2 to 15 carbon atoms and at least 2 hydroxyl groups. Polyols may also contain further functional groups, particularly amino groups, and / or be modified with nitrogen. Typical examples include: glycerol, alkylene glycols, e.g., ethylene glycol, diethylene glycol, propylene glycol, butylene glycol, hexylene glycol, and polyethylene glycol having an average molecular weight of 100 to 1000 daltons; technical oligoglycerol mixtures having an intrinsic degree of condensation of 1.5 to 10, e.g., technical diglycerol mixtures having a diglycerol content of 40% to 50% by weight; methylol compounds, e.g., trimethylolethane in particular, trimethylolethane. Rollpropane, trimethylolbutane, pentaerythritol and dipentaerythritol; lower alkyl glucosides, especially those having 1 to 8 carbon atoms in the alkyl radical, e.g., methyl and butyl glucosides; sugar alcohols having 5 to 12 carbon atoms, e.g., sorbitol or mannitol; sugars having 5 to 12 carbon atoms, e.g., glucose or sucrose; amino sugars, e.g., glucamine; dialcoholamines, e.g., diethanolamine or 2-amino-1,3-propanediol.
[0098] Preservatives and bacterial inhibitors Suitable preservatives include, for example, methyl-, ethyl-, propyl-, and butyl-parabens, benzalkonium chloride, 2-bromo-2-nitro-propane-1,3-diol, dehydroacetic acid, diazolidinyl urea, 2-dichlorobenzyl alcohol, DMDM hydantoin, formaldehyde solution, methyldibromoglutaronitrile, phenoxyethanol, sodium hydroxymethylglycinate, imidazolidinyl urea, triclosan, and further classes of substances listed in the following reference: KF DePolo - A short textbook of cosmetology, Chapter 7, Tables 7-2, 7-3, 7-4 and 7-5, pp. 210-219.
[0099] Bacterial inhibitors Typical examples of bacterial inhibitors are preservatives that have a specific effect against Gram-positive bacteria, such as 2,4,4'-trichloro-2'-hydroxydiphenyl ether, chlorhexidine (1,6-di(4-chlorophenyl-biguanide)hexane), or TCC (3,4,4'-trichlorocarbanilide). Numerous aromatic substances and etheric oils also possess antimicrobial properties. Typical examples are the active ingredients eugenol, menthol, and thymol in clove oil, mint oil, and thyme oil. A natural deodorant of interest is the terpene alcohol farnesol (3,7,11-trimethyl-2,6,10-dodecatriene-1-ol), found in lime blossom oil. Glycerol monolaurate has also been proven to be a bacteriostatic agent.
[0100] coloring agent As colorants, for example, substances that are suitable for cosmetic purposes and are permitted may be used, as edited in the publication “Kosmetische Farbemittel” of the Farbstoffkommission der Deutschen Forschungsgemeinschaft, Verlag Chemie, Weinheim, 1984, pages 81 to 106.
[0101] UV screening agent Suitable sunscreens include 1(+ / -)-1,7,7-trimethyl-3-[(4-methylphenyl)methylene]bicyclo-[2.2.1]heptan-2-one; p-methylbenzylidene camphor, 1,7,7-trimethyl-3-(phenylmethylene)bicyclo[2.2.1]heptan-2-one; benzylidene camphor, (2-hydroxy-4-methoxyphenyl)(4-methylphenyl)methanone, 2,4-dihydroxybenzophenone, 2,2',4,4'-tetrahydroxybenzophenone, 2-hydroxy-4-methoxybenzophenone Phenolic acid, 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid, 2,2'-dihydroxy-4,4'-dimethoxybenzophenone, 2,2'-dihydroxy-4-methoxybenzophenone, alpha-(2-oxoborn-3-ylidene)toluene-4-sulfonic acid and its salts, 1-[4-(1,1-dimethylethyl)phenyl]-3-(4-methoxyphenyl)propane-1,3-dione, methyl N,N,N-trimethyl-4-[(4,7,7-trimethyl-3-oxobicyclo[2,2,1]-hepta-2-ylidene)methyl [L]anilinium sulfate, 3,3,5-trimethylcyclohexyl-2-hydroxybenzoate, isopentyl p-methoxycinnamate, menthyl-o-aminobenzoate, 2-ethylhexyl 2-cyano, 3,3-diphenyl acrylate, 2-ethylhexyl 4-(dimethylamino)benzoate, 2-ethylhexyl 4-methoxycinnamate, 2-ethylhexyl salicylate, benzoic acid, 4,4',4"-(1,3,5-triazine-2,4,6-triyltriimino)tris-, tris(2-ethylhexyl)est L, 4-aminobenzoic acid, benzoic acid, 4-amino-, ethyl ester, polymer with oxirane, 2-phenyl-1H-benzimidazole-5-sulfonic acid, 2-propenamide, N-[[4-[(4,7,7-trimethyl-3-oxobicyclo[2.2.1]hepta-2-ylidene)methyl]phenyl]methyl]-, homopolymer, triethanolamine salicylate, 3,3'-(1,4-phenylenedimethylene)bis[7,7-dimethyl-2-oxobicyclo[2.2.1]heptane-1methanesulfonic acid], titanium dioxide, 2,2'-Methylene-bis-[6-(2H-benzotriazol-2-yl)-4-(1,1,3,3-tetramethylbutyl)-phenol], bis-ethylhexyloxyphenol methoxyphenyl triazine, 1H-benzimidazole-4,6-disulfonic acid, 2,2'-(1,4-phenylene)bis-, disodium salt, benzoic acid, 4,4'-[[6-[[4-[[(1,1-dimethylethyl)amino]carbonyl]-phenyl]amino]1,3,5-triazine-2,4-diyl]diimino]bis-, phenol, 2-(2H-benzotriazol-2 -yl)-4-methyl-6-[2-methyl-3-[1,3,3,3-tetramethyl-1-[(trimethylsilyl)oxy]disiloxanyl]propyl]-, dimethicone diethyl benzalmalonate, benzenesulfonic acid, 3-(2H-benzotriazol-2-yl)-4-hydroxy-5-(1-methylpropyl)-, monosodium salt, benzoic acid, 2-[4-(diethylamino)-2-hydroxybenzoyl]-, hexyl ester, 1-dodecaneaminonium, N-[3-[[4-(dimethylamino)benzoyl]amino]-propyl]N,N-dimethyl-, Salt with 4-methylbenzenesulfonic acid (1:1), 1-propaneaminium, N,N,N-trimethyl-3-[(1-oxo-3-phenyl-2-propenyl)amino]-, chloride, 1H-benzimidazole-4,6-disulfonic acid, 2,2'-(1,4-phenylene)bis-, 1,3,5-triazine, 2,4,6-tris(4-methoxyphenyl)-,1,3,5-triazine, 2,4,6-tris[4-[(2-ethylhexyl)oxy]phenyl]-, 1-propaneaminium, 3-[[3-[3-(2H-benzotriazol-2-yl)-5 -(1,1-dimethylethyl)-4-hydroxyphenyl]-1-oxopropyl]amino]-N,N-diethyl-N-methyl-, methyl sulfate (salt), 2-propenoic acid, 3-(1H-imidazole-4-yl)-, benzoic acid, 2-hydroxy-, [4-(1-methylethyl)phenyl]methyl ester, 1,2,3-propanetriol, 1-(4-aminobenzoate), benzeneacetic acid, 3,4-dimethoxy-α-oxo-, 2-propenoic acid, 2-cyano-3,3-diphenyl-, ethyl ester, anthranilic acid, p-mentha-3-yl ester, 2,This includes a range of organic UV screening agents selected from the group consisting of 2'-bis(1,4-phenylene)-1H-benzimidazole-4,6-disulfonic acid monosodium salt or phenyldibenzimimidazole tetrasulfonic acid disodium, 1,3,5-triazine-2,4,6-triamine, and N,N'-bis[4-[5-(1,1-dimethylpropyl)-2-benzoxazolyl]phenyl]-N”-(2-ethylhexyl).
[0102] A drug that absorbs ultraviolet rays and provides photoprotection to the skin. A suitable agent that absorbs ultraviolet light, provides photoprotection to the skin, and provides sunless tanning as needed is Formula I:
[0103] [ka] It may contain compounds of or salts thereof. (In the formula, Each R 1 These are independently H, (C1-C6) alkyl, (C3-C7) carbon ring, or R a C(=O)- and two R 4 The groups combine to form a -(C3~C8)alkyl group, a -(C2~C6)alkyl-Y-(C2~C6)alkyl group, or a -(C1~C6)alkyl-Y'-(C1~C6)alkyl group; or Each R 4 These are independently H, (C1-C6) alkyl, (C3-C7) carbon ring, or R a C(=O)- and two R 1 The groups combine to form a -(C3~C8)alkyl group, a -(C2~C6)alkyl-Y-(C2~C6)alkyl group, or a -(C1~C6)alkyl-Y'-(C1~C6)alkyl group; or Two R's 4 The groups combine to form a -(C3~C8) alkyl group, a -(C2~C6) alkyl-Y-(C2~C6) alkyl group, or a -(C1~C6) alkyl-Y'-(C1~C6) alkyl group, with two R groups. 1The groups combine to form a -(C3~C8)alkyl group, a -(C2~C6)alkyl-Y-(C2~C6)alkyl group, or a -(C1~C6)alkyl-Y'-(C1~C6)alkyl group; There are no dashed bonds labeled "a", and all dashed bonds labeled "b" are double bonds; or, all dashed bonds are single bonds; R 2 is H, (C1-C6) alkyl or aryl, where aryl is one or more Z 1 Substituted as needed in the base; R 3 is H, (C1-C6) alkyl or aryl, where aryl is one or more Z 1 Substituted as needed in the base; Y is O, S, NH, NR c , P, P(=O) or POH; Y' is Si(R b )2 or -Si(R b )2-O-Si(R b )2-; Each R a These are independently (C1-C6) alkyl, (C3-C7) carbocyclic, or aryl, where aryl is one or more Z 1 Substituted as needed in the base; Each R b These are independently (C1-C6) alkyl, (C3-C7) carbocyclic, or aryl, where the aryl is one or more Z 1 Substituted as needed in the base; Each R c R is independent g It is either oxo (=O), hydroxy, mercapto, (C1~C6) alkoxy, (C1~C6) alkoxycarbonyl, (C1~C6) alkanoyloxy, NR d R e C1-C11 are optionally substituted with one or more groups independently selected from carboxylate and aryl groups. 18 A saturated or unsaturated carbon chain, where R c Any aryl of is one or more Rf It is replaced as needed; Each R d and R e These are H, (C1-C6) alkyl, (C1-C6) alkanoyl, phenyl, benzyl, and R g Selected independently of; Each R f is independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkoxycarbonyl, (C1-C6)alkanoyloxy, -C(=O)-phenyl, and -C(=O)CH2C(=O)-phenyl, where any phenyl is optionally substituted with one or more groups independently selected from (C1-C6)alkyl, -SO3H, and (C1-C6)alkoxy; Each R g teeth,
[0104] [ka] And, each Z 1 These are (C1~C6) alkyl, halogen, -CN, -OR n1 , -NR q1 R r1 , -NR n1 COR p1 , -NR n1 CO2R p1 NO2, -C(O)R n1 , -C(O)OR n1 and -C(O)NR q1 R r1 , independently selected from, Z 1 Any (C1-C6) alkyl group is optionally substituted with one or more (e.g., 1, 2, 3, 4, 5, or 6) halogens; Each R n1 R is independently selected from H and (C1~C6) alkyl groups. n1 Any (C1-C6) alkyl group is optionally substituted with one or more (e.g., 1, 2, 3, 4, 5, or 6) halogens; Each R p1These are independently (C1-C6) alkyl groups; R q1 and R r1 The elements are independently selected from H and (C1-C6) alkyl groups, or R q1 and R r1 (These, together with the nitrogen they are bound to, form piperidine, pyrrolidine, morpholine, azetidine, thiomorpholine, piperazine, or 4-methylpiperazine.)
[0105] Specific groups of compounds of formula I and specific compounds of formula I that can be incorporated into the topical compositions described herein, as well as methods for preparing such compounds, are described in U.S. Patent No. 9,403,778 and U.S. Patent No. 9,987,211, which are incorporated herein by reference in their entirety.
[0106] A suitable agent that absorbs ultraviolet light and / or provides photoprotection to the skin and / or provides sunless tanning as needed is Formula II:
[0107] [ka] It may contain compounds of or salts thereof. (In the formula, R 1 is H, (C1-C6) alkyl, (C3-C7) carbon ring or R a C(=O)- and; R 2 Z is H, (C1-C6) alkyl or aryl, where aryl is one or more (e.g., 1, 2, 3, 4 or 5) 1 Substituted as needed in the base; R 4 is H, (C1~C 10 ) alkyl, (C3~C7) carbon ring or R a C(=O)- and; R ais (C1-C6) alkyl, (C3-C7) carbocyclic or aryl, where aryl is optionally substituted with one or more (e.g., 1, 2, 3, 4 or 5) Z 1 groups; each Z 1 is independently selected from (C1-C6) alkyl, halogen, -CN, -OR n1 , -NR q1 R r1 , -NR n1 COR p1 , -NR n1 CO2R p1 , NO2, -C(O)R n1 , -C(O)OR n1 and -C(O)NR q1 R r1 and any (C1-C6) alkyl of Z is optionally substituted with one or more (e.g., 1, 2, 3, 4, 5 or 6) halogen; 1 each R is independently selected from H and (C1-C6) alkyl, and any (C1-C6) alkyl of R is optionally substituted with one or more (e.g., 1, 2, 3, 4, 5 or 6) halogen; n1 each R n1 is independently (C1-C6) alkyl; R p1 and R R q1 and R r1 are each independently selected from H and (C1-C6) alkyl or R q1 and R r1 together with the nitrogen to which they are attached form piperidine, pyrrolidine, morpholine, azetidine, thiomorpholine, piperazine or 4-methylpiperazine)
[0108] Certain groups of the compounds of Formula II, certain compounds of Formula II, and methods for preparing such compounds that can be incorporated into the topical compositions described herein are described in U.S. Patent No. 9,987,211, which is incorporated herein by reference in its entirety.
[0109] Suitable agents that absorb ultraviolet light and provide photoprotection to the skin include compounds of formula III:
[0110]
Chemical formula
[0111] [ka] And, each Z 1 These are (C1~C6) alkyl, halogen, -CN, -OR n1 , -NR q1 R r1 , -NR n1 COR p1 , -NR n1 CO2R p1 NO2, -C(O)R n1 , -C(O)OR n1 and -C(O)NR q1 R r1 , independently selected from, Z 1 Any (C1-C6) alkyl group is optionally substituted with one or more (e.g., 1, 2, 3, 4, 5, or 6) halogens; Each R n1 R is independently selected from H and (C1~C6) alkyl groups. n1 Any (C1-C6) alkyl group is optionally substituted with one or more (e.g., 1, 2, 3, 4, 5, or 6) halogens; Each R p1 These are independently (C1-C6) alkyl groups; R q1 and R r1 The elements are independently selected from H and (C1-C6) alkyl groups, or R q1 and R r1 (These, together with the nitrogen they are bound to, form piperidine, pyrrolidine, morpholine, azetidine, thiomorpholine, piperazine, or 4-methylpiperazine.)
[0112] Specific groups of compounds of formula III and specific compounds of formula III that can be incorporated into the topical compositions described herein, as well as methods for preparing such compounds, are described in U.S. Patent No. 9,364,406 and U.S. Patent No. 9,987,211, which are incorporated herein by reference in their entirety.
[0113] sunscreen Topical compositions disclosed herein include sunscreens such as avobenzone, ecamsul, methyl anthranilate, oxybenzone, dioxybenzone, sulisobenzone, octinoxate, homosalate, octocrylene, and octisaleate. Such compositions may include organic UV filters effective in the UVA region and / or UVB region and / or IR and / or VIS region (absorbers), so-called hydrophilic or lipophilic sunscreen filters. These substances can be selected from, in particular, cinnamic acid derivatives, salicylic acid derivatives, camphor derivatives, triazine derivatives, β,β-diphenyl acrylate derivatives, p-aminobenzoic acid derivatives, as well as polymer filters and silicone filters, which are described in International Publication No. 93 / 04665. Further examples of organic filters are shown in European Patent Application Publication No. 0487404. Particularly preferred for combination are para-aminobenzoic acid and its derivatives: PABA, ethyl PABA, ethyl dihydroxypropyl PABA, ethylhexyldimethyl PABA, e.g., commercially available from ISP under the name "Escalol 507", glyceryl PABA, PEG-25 PABA, e.g., commercially available from BASF under the name "Uvinul P25".
[0114] Other UV filter components that can be incorporated into the topical compositions of this disclosure include:
[0115] Salicylate: Homosalate, marketed by Merck under the name "Eusolex HMS"; ethylhexyl salicylate, e.g., marketed by Symrise under the name "Neo Heliopan OS"; dipropylene glycol salicylate, e.g., marketed by Scher under the name "Dipsal"; TEA salicylate, e.g., marketed by Symrise under the name "Neo Heliopan TS".
[0116] β,β-diphenyl acrylate derivatives: Octocrylene, for example, the one marketed by Merck under the name "Eusolex(registered trademark) OCR", or "Uvinul N539" manufactured by BASF, or Octocrylene, for example, the one marketed by BASF under the name "Uvinul N35".
[0117] Benzophenone derivatives: Benzophenone-1, e.g., marketed under the name "Uvinul 400"; Benzophenone-2, e.g., marketed under the name "Uvinul D50"; Benzophenone-3 or oxybenzone, e.g., marketed under the name "Uvinul M40"; Benzophenone-4, e.g., marketed under the name "Uvinul MS40"; Benzophenone-9, e.g., marketed by BASF under the name "Uvinul DS-49"; Benzophenone-5; Benzophenone-6, e.g., marketed by Norquay under the name "Helisorb 11"; Benzophenone-8, e.g., marketed by American Cyanamid under the name "Spectra-Sorb UV-24"; Benzophenone-12 2-(4-diethylamino-2-hydroxybenzoyl) n-hexyl benzoate, or 2-hydroxy-4-methoxybenzophenone, which is marketed by Merck and Darmstadt under the name Eusolex® 4360.
[0118] Benzylidene camphor derivatives: 3-Benzylidene camphor, for example, marketed by Chimex under the name "Mexoryl SD"; 4-Methylbenzylidene camphor, for example, marketed by Merck under the name "Eusolex 6300"; Benzylidene camphor sulfonic acid, for example, marketed by Chimex under the name "Mexoryl SL"; Camphor benzalkonium methosulfate, for example, marketed by Chimex under the name "Mexoryl SO"; Terephthalylidene disodium camphor sulfonic acid, for example, marketed by Chimex under the name "Mexoryl SX"; Polyacrylamide methylbenzylidene camphor, for example, marketed by Chimex under the name "Mexoryl SW".
[0119] Phenylbenzimidazole derivatives: Phenylbenzimidazole sulfonic acid, for example, marketed by Merck under the name "Eusolex 232"; disodium phenyldibenzimidazole tetrasulfonate, for example, marketed by Symrise under the name "Neo Heliopan AP".
[0120] Phenylbenzotriazole derivatives: Drometrizole trisiloxane, for example, marketed by Rhodia Chimie under the name "Silatrizole".
[0121] Methylenebis(benzotriazolyl)tetramethylbutylphenol in solid form, for example, commercially available from Fairmount Chemical under the name "MIXXIM BB / 100," or in finely powdered aqueous dispersion form, for example, commercially available from BASF under the name "Tinosorb M."
[0122] Triazine derivatives: Ethylhexyl triazone, for example, marketed by BASF under the name "Uvinul T150"; diethylhexyl butamide triazone, for example, marketed by Sigma 3V under the name "Uvasorb HEB"; 2,4,6-tris(diisobutyl 4'-aminobenzalmalonate)-s-triazine or 2,4,6-tris(biphenyl)-1,3,5-triazine. The product marketed by BASF as Tinosorb A2B is 2,2'-[6-(4-methoxyphenyl)-1,3,5-triazine-2,4-diyl]bis[5-(2-ethylhexyl)oxy]phenol; the product marketed by BASF as Tinosorb S is N2,N4-bis[4-[5-(1,1-dimethylpropyl)-2-benzoxazolyl]phenyl]-N-6-(2-ethylhexyl)-1,3,5-triazine-2,4,6-triamine; and the product marketed by Sigma 3V as Uvasorb K 2A.
[0123] Anthraniline derivatives: Menthyl anthranilate, for example, the one marketed by Symrise under the name "Neo Heliopan MA".
[0124] Imidazole derivative: Ethylhexyl dimethoxybenzylidene dioxoimidazoline propionate.
[0125] Benzalmalonate derivatives: Polyorganosiloxanes containing functional benzalmalonate groups, such as polysilicone-15, for example, those marketed by Hoffmann LaRoche under the name "Parsol SLX".
[0126] 4,4-Diarylbutadiene derivative: 1,1-Dicarboxy(2,2'-dimethylpropyl)-4,4-Diphenylbutadiene.
[0127] Benzoxazole derivatives: 2,4-bis[5-(1-dimethylpropyl)benzoxazole-2-yl(4-phenyl)imino]-6-(2-ethylhexyl)imino-1,3,5-triazine, for example, those commercially available by Sigma 3V under the name Uvasorb K2A, and mixtures containing the same.
[0128] Suitable organic UV protective substances can preferably be selected from ethylhexyl salicylate, phenylbenzimidazole sulfonic acid, benzophenone-3, benzophenone-4, benzophenone-5, n-hexyl 2-(4-diethylamino-2-hydroxybenzoyl)benzoate, 4-methylbenzylidene camphor, terephthalylidene camphor sulfonic acid, disodium phenyldibenzimidazole tetrasulfonate, methylenebis(benzotriazol)tetramethylbutylphenol, ethylhexyl triazone, diethylhexyl butamide triazone, drometrizole trisiloxane, polysilicone-15, 1,1-dicarboxy(2,2'-dimethylpropyl)-4,4-diphenylbutadiene, 2,4-bis[5-1(dimethylpropyl)benzoxazole-2-yl(4-phenyl)imino]-6-(2-ethylhexyl)imino-1,3,5-triazine and mixtures thereof.
[0129] The composition of the present invention may further include inorganic UV filters, so-called particulate UV filters. These combinations with particulate UV filters can be in powder, dispersion, or paste form. In some embodiments, the inorganic UV filter is titanium dioxide, for example, coated titanium dioxide (e.g., Eusolex® T-2000, Eusolex® T-AQUA, Eusolex® T-AVO, Eusolex® T-OLEO), zinc oxide (e.g., Sachtotec), iron oxide, or cerium oxide and / or zirconium oxide. Furthermore, combinations with pigment-grade titanium dioxide or zinc oxide are also possible, with particle sizes of 200 nm or more, for example, Hombitan® FG or Hombitan® FFPharma.
[0130] The compositions of the present invention may include inorganic UV filters post-treated by conventional methods, as described, for example, in Cosmetics & Toiletries, 1990, 105, 53-64. One or more of the following post-treatment components may be amino acids, beeswax, fatty acids, fatty acid alcohols, anionic surfactants, lecithin, phospholipids, sodium, potassium, zinc, iron or aluminum salts of fatty acids, polyethylene, silicone, proteins (especially collagen or elastin), alkanolamines, silicon dioxide, aluminum oxide, further metal oxides, phosphates such as sodium hexametaphosphate, or glycerin.
[0131] In one embodiment, the particulate UV filter used in the composition of the present invention is: • Untreated titanium dioxide, for example, Tayca's Microtitanium Dioxide MT 500 B; Degussa's Titanium Dioxide P25. • Micronized titanium dioxide post-treated with aluminum oxide and silicon dioxide, for example, Tayca's product "Microtitanium Dioxide MT 100 SA" or Uniqema's product "Tioveil Fin", • Micronized titanium dioxide post-treated with aluminum oxide and / or aluminum stearate / laurate, e.g., Microtitanium Dioxide MT 100 T from Tayca, Eusolex T-2000 from Merck, • Micronized titanium dioxide post-treated with iron oxide and / or iron stearate, for example, Tayca's product "Microtitanium Dioxide MT 100 F", • Micronized titanium dioxide post-treated with silicon dioxide, aluminum oxide, and silicone, for example, Tayca's product "Microtitanium Dioxide MT 100 SAS", This refers to micronized titanium dioxide post-treated with sodium hexametaphosphate, such as Tayca's product "Microtitanium Dioxide MT 150 W".
[0132] The processed, finely powdered titanium dioxide used in the combination also includes the following: Octyltrimethoxysilane; for example, product Tego Sun T 805 manufactured by Evonik Goldschmidt GmbH. • Silicon dioxide; for example, products manufactured by DSM such as Parsol TX, • Aluminum oxide and stearic acid; for example, Sachtleben's UV-Titan M160 product. • Aluminum and glycerin; for example, UV-Titan products manufactured by Sachtleben. • Aluminum and silicone oils; for example, Sachtleben's UV-Titan M262 product. • Sodium hexametaphosphate and polyvinylpyrrolidone, • Polydimethylsiloxane, for example, Cardre's product 70250 Cardre UF TiO2SI3, The product may be post-treated with polydimethylhydrogenosiloxane, for example, "Microtitanium Dioxide USP Grade Hydrophobic" manufactured by Color Techniques.
[0133] In certain embodiments, the composition of the present invention may include untreated zinc oxide, for example, BASF (Sunsmart) product Z-Cote, Elementis product Nanox. In other specific embodiments, the composition of the present invention may include post-treated zinc oxide, for example, the following products: • Toshibi's "Zinc Oxide CS-5" (ZnO post-treated with polymethylhydrogenosiloxane); ·Nanogard Zinc Oxide FN manufactured by Nanophase Technologies; • "SPD-Z1" manufactured by Shin-Etsu Chemical Co., Ltd. (ZnO post-treated with silicone graft acrylic polymer dispersed in cyclodimethylsiloxane; • ISP's "Escalol Z100" (aluminum oxide post-treated ZnO dispersed in an ethylhexyl methoxycinnamate / PVP-hexadecene / methicone copolymer mixture); and It may also contain "Fuji ZNO-SMS-10" (ZnO post-treated with silicon dioxide and polymethylsilsesquioxane) manufactured by Fuji Pigment Co., Ltd.
[0134] In another specific embodiment, the composition of the present invention may include an untreated cerium oxide fine pigment, for example, one manufactured by Rhone Poulenc and designated as "Colloidal Cerium Oxide." In yet another specific embodiment, the composition of the present invention may include an untreated and / or post-treated iron oxide, designated as Nanogar, manufactured by Arnaud.
[0135] For example, mixtures of various metal oxides such as titanium dioxide and cerium oxide, with or without post-treatment, such as Sunveil A manufactured by Ikeda Bussan Co., Ltd., can also be used. In addition, mixtures of aluminum oxide, silicon dioxide, and silicone-post-treated titanium dioxide and zinc oxide, such as UV-Titan M261 manufactured by Sachtleben, can also be used in combination with the UV protective agent according to the present invention.
[0136] How to use In some embodiments, this disclosure relates to methods for treating skin in question for the effects of radical-induced damage. Radical-induced damage may include damage caused by free radicals from sunlight (UVB, UVA, visible light), HEV (blue) light, infrared (IR), pollution, irritants, allergens, and various environmental toxins that are destructive to the skin, for example, by hydrolyzing elastin fibers in the skin and breaking down collagen in the lower dermis layer of the skin. Exemplary radical-induced damages that can be treated, prevented, minimized, mitigated, or attenuated after administering an effective amount of any of the topical compositions described herein to skin in question include, but are not limited to, wrinkles, fine lines, rough skin, sagging skin, loss of skin firmness, loss of skin elasticity, senile lentigines, hyperpigmentation, scars, uneven skin surface, rosacea, acne, psoriasis, impaired skin regeneration and renewal processes, sunburned appearance, yellowing, redness, dryness, ichthyosis, and other damaged skin conditions.
[0137] In certain embodiments, the present disclosure relates to a method for brightening a target skin by administering an effective amount of any of the topical compositions described herein to the target skin, wherein the skin becomes brighter after the administration of the topical composition.
[0138] In certain embodiments, the Disclosure relates to a method for treating a target skin for the effects of airborne or exogenous aging by administering an effective amount of any of the topical compositions described herein to the target skin, wherein the skin exhibits a reduction or attenuation of the effects of airborne or exogenous aging after administration.
[0139] In certain embodiments, this disclosure relates to a treatment regimen method comprising administering an effective amount of one of the topical compositions described herein to the skin of a subject that has undergone a dermatological treatment. Dermatological treatments that may be benefits following (i.e., post-treatment) the administration of the topical compositions described herein include, but are not limited to, non-excisional dermatological treatments, chemical peels, microablation, lasers, and the like. In certain embodiments, the method described herein further comprises performing the dermatological treatment after and / or before the administration of the topical composition, depending on the treatment regimen. In certain embodiments, the topical compositions described herein may help improve the outcome of a dermatological treatment, for example, by promoting healing, alleviating discomfort, suppressing reactive oxygen species (ROS), inducing collagen formation, or any combination thereof.
[0140] As used herein, the terms “treatment” or “to treat” in relation to a skin condition generally mean “having a positive effect on the skin condition” and include reduction, improvement, and / or alleviation of at least one symptom of the skin condition, reduction, improvement, and / or alleviation of the severity of the skin condition, or delay, prevention, or inhibition of the progression of the skin condition, or the perception thereof. Treatment, as used herein, does not require complete healing of the condition. Formulations of the Disclosure useful for treating a skin condition, or methods for treating a skin condition, only require reducing the severity of the skin condition, reducing the severity of its associated symptoms, providing an improvement in the patient’s quality of life, or delaying, preventing, or inhibiting the onset of one or more symptoms of the skin condition. As used herein, these terms also include aesthetic improvement to the skin when applying a disclosed formulation having, for example, a combination of ascorbate and green tea polyphenols.
[0141] As used herein, the phrase “effective amount” means an amount of the topical composition or components of the present disclosure that is effective in treating any of the skin conditions noted above, including, but not limited to, an improvement in one or more aesthetic criteria, including, but not limited to, a perceived improvement in the appearance of skin wrinkles, fine lines, rough skin, sagging skin, skin firmness, skin elasticity, senile lentigines, hyperpigmentation, scars, uneven skin surface, rosacea, acne, psoriasis, skin regeneration and renewal processes, sunburned appearance, yellowing, redness, dryness, ichthyosis, and other damaging skin conditions, ranging from a detectable local improvement in the area of topical application to substantial relief of symptoms.
[0142] The effective dose varies depending on the specific condition or condition being treated, the severity of the condition, the duration of treatment, the specific components of the composition being used, and other factors. In certain embodiments, the topical compositions described herein are suitable for administration by frequent, periodic application, for example, by application once, twice, three times, or four or more times per day for a duration such as at least one day, at least three days, at least five days, at least seven days, at least ten days, at least fourteen days, at least twenty-one days, or at least thirty days. Thus, in certain embodiments, the methods described herein further include periodically repeating the administration of the topical composition.
[0143] In certain embodiments, the topical compositions described herein are suitable for administration before or after dermatological procedures.
[0144] In certain embodiments, since the topical composition described herein is an emulsion of an aqueous phase and an oily phase, the two phases may separate during storage. Therefore, in certain embodiments, the method described herein further includes shaking the topical composition to uniformly disperse the oily phase in the aqueous phase before administration.
[0145] Preparation method This disclosure also relates to a method for preparing any of the topical compositions described herein. The method involves producing any of the topical compositions described herein by combining an ascorbate component, an antioxidant system comprising more than 0 wt.% to about 1 wt.% including green tea polyphenols, and optionally at least one cosmetically acceptable excipient.
[0146] Topical compositions can be formulated into serums, gels, lotions, creams, pads, and other application formulations. [Examples]
[0147] Exemplary Examples The following examples are provided to aid in understanding the present invention and, of course, should not be construed as specifically limiting the present invention as described herein and claimed. Such modifications of the present invention that are within the scope of those skilled in the art, including the substitution of all equivalents known at present or to be developed later, and minor changes in formulation or experimental design are considered to be within the scope of the present invention as incorporated herein.
[0148] [Example 1] The topical compositions according to the embodiments described herein were formulated into serum having the compositions shown in Table 1 below. The serum was an emulsion of an aqueous phase and an oily phase, with a pH ranging from about 2.5 to about 3.5.
[0149] [Table 1]
[0150] [Example 2] Clinical trials were conducted to evaluate the safety and efficacy of topical compositions containing vitamins C and E, as well as green tea polyphenols (CE-GTP), on photoaged facial skin.
[0151] The study was conducted over 12 weeks to evaluate the safety and efficacy of CE-GTP serum on photoaged facial skin in 31 women aged 21 to 65 years who had not undergone any facial treatment in the previous 6 months. Detailed inclusion and exclusion criteria are shown in Table 2, and a summary of demographic information is shown in Table 3.
[0152] [Table 2-1]
[0153] [Table 2-2]
[0154] [Table 3]
[0155] Participants were instructed to avoid applying any topical moisturizing products to their face for at least two days prior to their first visit. During the 12-week study period, participants were instructed to wash their face twice daily (morning and evening) with the provided supplemental cleanser, apply the provided sunscreen in the morning, reapply as needed, and apply the test substance (CE-GTP serum) twice daily (morning and evening). Participants were also instructed to avoid prolonged sun exposure, as well as the use of tanning beds and sunless tanning products, mechanical / chemical cleansers and devices on the face during the study period, anti-aging products, and any new facial products other than the assigned CE-GTP serum during the study period. Participants were permitted to continue using all of their regularly used brands of color cosmetics, makeup removers, and sunscreens.
[0156] Outcome measurement Clinical grading of efficacy parameters was performed at visits 1 (baseline), 2 (week 4), 3 (week 8), and 4 (week 12). Safety assessments and VISIA-CR imaging were performed between each post-baseline visit, i.e., visits 2, 3, and 4. For efficacy parameters, each subject was clinically graded using the modified Griffith 10-point scale for fine wrinkles in the eye area, wrinkles throughout the face and in the eye area, skin smoothness, hyperpigmentation, radiance, firmness, and overall photodamage to the face. Skin smoothness and firmness were assessed as visual examinations. The clinical grading of efficacy parameters using the modified Griffith 10-point scale is shown in Table 4.
[0157] Safety was assessed by clinical evaluation of signs of erythema, edema, dryness, and desquamation. Participants also assessed the safety of the CE-GTP composition by self-reporting the overall degree of burning, stinging, and itching. Safety evaluations are shown in Table 5.
[0158] [Table 4]
[0159] [Table 5]
[0160] Digital images were acquired for each subject's face (left, center, and right images) using a VISA-CR photostation (Canfield Imaging Systems, Fairfield, NJ) with a Canon Mark II digital SLR camera (Canon Incorporated, Tokyo, Japan) under the following cross-polarized and parallel-polarized lighting conditions: Standard 1 (visible [bright]), Standard 2 (visible), and Standard 3 (rake light on the crow's footprint area). Ultrasound measurements were also performed at the baseline visit and the 12-week visit, i.e., visits 1 and 4. Single measurements were performed on the left crow's footprint area using a 50 MHz ultrasound transducer connected to a DUB 6100 OEM system (Taberna Pro Medicum, Luneburg, Germany) to measure skin density. Subject-reported outcomes were measured via self-assessment questionnaires at weeks 4, 8, and 12 to evaluate the treatment outcomes and product performance received by the subjects.
[0161] Compliance Participants completed daily diaries recording the application of the test substance during the study, adverse events, and comments. The diaries were reviewed for compliance at each post-baseline visit. The volume of the provided CE-GTP composition was visually inspected at each post-baseline study visit to assess treatment compliance. In addition, units of the test substance were weighed before distribution and at weeks 4, 8, and 12 to quantify the participants' use of CE-GTP serum.
[0162] statistical analysis Descriptive statistical summaries for all efficacy grading parameters, safety assessment parameters, and ultrasound measurements included the N, mean, median, SD, MIN, and MAX of the score / value at all applicable time points. The mean change from baseline (defined as post-baseline value - baseline value) was estimated at the post-baseline time point. The null hypothesis that the mean change from baseline was zero was tested for efficacy and safety outcomes using the Wilcoxon signed-rank test. Paired t-tests were used to compare ultrasound measurements.
[0163] The questionnaire was presented in a table, and the frequency and percentage of all response options were reported for each question and time point. A binomial (signed) test was performed to determine whether the proportion of the combined specified preferred responses was equal to the proportion of the combined specified undesirable responses for each applicable question.
[0164] All statistical tests were two-tailed with a significance level of alpha = 0.05 unless otherwise specified. Multiple test correction was not considered in the study. Statistical analysis was performed using SAS software version 9.4 (SAS Statistical Institute).
[0165] A total of 31 participants were included in the intention-to-treat (ITT) population, and 30 participants completed the study. Data from participant 003 (from baseline to week 8), who did not continue, were included in the statistical analysis as part of the ITT population. This study was conducted in accordance with federal regulations and guidelines for conducting clinical trials of pharmaceuticals.
[0166] Clinical grading of efficacy parameters When the clinical grading of the efficacy parameters was analyzed and compared to baseline scores for fine wrinkles in the eye region, skin smoothness, and radiance, statistically significant improvements (decreases) were observed in the scores at weeks 4, 8, and 12. For scores related to fine wrinkles in the eye region, the mean changes were -0.55±0.42, -0.77±0.59, and -1.20±0.77 at weeks 4, 8, and 12, respectively, with mean percentage changes of -16.6%, -23.4%, and -36.2% (p=<0.001, <0.001, <0.001, respectively). For skin smoothness scores, the mean changes at weeks 4, 8, and 12 were -0.29±0.25, -0.52±0.30, and -0.65±0.27, respectively, with mean percentage changes of -6.2%, -11.1%, and -13.9% (p=<0.001, <0.001, <0.001, respectively). For radiance scores, the mean changes at weeks 4, 8, and 12 were -0.24±0.25, -0.39±0.25, and -0.58±0.27, respectively, with mean percentage changes of -4.9%, -7.9%, and -11.9% (p=<0.001, <0.001, <0.001, respectively). At weeks 8 and 12, statistically significant improvements were observed in scores for wrinkles, hyperpigmentation, and firmness in the entire face and the eye area. The mean change in score for wrinkles in the entire face was -0.11±0.21 and -0.32±0.31 at weeks 8 and 12, respectively, representing mean percentage changes of -2.4% and -6.6% (p=0.016 and <0.001, respectively). The mean change in score for wrinkles in the eye area was -0.19±0.31 and -0.30±0.34 at weeks 8 and 12, respectively, representing mean percentage changes of -4.1% and -6.4% (p=0.002 and <0.001, respectively). Regarding the hyperpigmentation score, the mean change was -0.29±0.25 and -0.43±0.17 at weeks 8 and 12, respectively, with mean percentage changes of -6.0% and -8.9% (p=<0.001 and <0.001).Regarding the needle score, the mean change was -0.24±0.25 and -0.38±0.22 at weeks 8 and 12, respectively, with mean percentage changes of -5.0% and -7.9% (p=<0.001 and <0.001, respectively). At week 12, there was a statistically significant improvement in the overall photodamage score. The mean change was -0.43±0.17, with a mean percentage change of -8.9% (p=<0.001). The results for the clinically graded efficacy parameters are shown in Figure 1.
[0167] For all efficacy parameters, more than 50% of subjects showed improvement at week 12. Notably, at week 12, 96.7% of subjects showed improvement in their scores for fine lines in the eye area, 96.7% in their smoothness scores, and 93.3% in their radiance scores. Figure 2 illustrates the percentage of subjects showing improvement at weeks 4, 8, and 12 for each efficacy parameter. No subjects showed a deterioration in scores for any of the efficacy parameters at week 12.
[0168] Safety evaluation Analysis of safety data showed a statistically significant improvement (decrease) in the score for overall facial erythema at week 12 compared to baseline scores (mean change %=-84.6, p=0.004). Compared to baseline scores, there were no statistically significant changes (increases or decreases) in the scores for dryness, desquamation, burning, or stinging at any post-baseline time point. Edema and itchiness were scored as 0 (none) at each time point.
[0169] No serious adverse events were reported. Of the 31 participants in the study, only one experienced non-severe adverse events, including itching and dry skin in the eye area, as well as peeling skin on the forehead and mouth. These symptoms were temporary and resolved completely.
[0170] Ultrasonic measurement Ultrasound measurements were analyzed and compared to baseline values, showing a statistically significant increase in skin density at week 12 (mean change %=44.5, p=<0.001), indicating thickening of the epidermal and dermal tissues. The results are illustrated in Figure 3.
[0171] This study demonstrated that CE-GTP serum is safe and effective in improving photoaged facial skin. CE-GTP serum can correct hyperpigmentation and increase firmness, along with a wide range of aesthetic problems associated with short-term use. Notably, the majority of subjects showed statistically significant improvement across all clinical parameters within 12 weeks. It is also noteworthy that subjects showed sustained improvement across all clinical parameters throughout the study period, indicating that continued use leads to sustained aesthetic improvement.
[0172] The CE-GTP composition rapidly targeted the periorbital region, as evidenced by the fact that the majority of subjects showed statistically significant improvement in fine wrinkles in the eye region within four weeks. Furthermore, ultrasound measurements revealed significant thickening of the epidermal and dermal tissue in crow's feet at 12 weeks, resulting in younger, healthier skin.
[0173] The CE-GTP composition meets the demand for effective, natural personal skincare products. Studies have reported that CE-GTP serum is highly tolerable, non-irritating, and easy to use and apply; therefore, this vitamin and plant-based product can be safely and easily incorporated into at-home skincare routines.
[0174] For the sake of simplicity, embodiments of the methods of this disclosure are illustrated and described as a series of actions. However, the actions of this disclosure may occur in various orders and / or simultaneously, as well as in conjunction with other actions not presented and described herein. Furthermore, not all illustrated actions are required to carry out the methods of the disclosed subject matter. In addition, those skilled in the art will understand and recognize that the methods may be alternatively represented as a series of interrelated states via a state diagram or events.
[0175] The preceding description includes numerous specific details, such as specific materials, dimensions, and process parameters, in order to provide a complete understanding of the present invention. Specific properties, structures, materials, or features can be combined in any preferred manner in one or more embodiments. The terms “example” or “exemplary” are used herein to mean that they serve as examples, cases, or illustrations. Any embodiment or design described herein as “example” or “exemplary” should not necessarily be construed as being preferable or advantageous to other embodiments or designs. Rather, the use of the terms “example” or “exemplary” is intended to present a concept in a specific way. Where used herein, the term “or” is intended to mean an inclusive “or” rather than an exclusive “or.” That is, unless otherwise specified or evident from the context, “X includes A or B” is intended to mean any of the obvious inclusive order. That is, if X includes A; X includes B; or X includes both A and B, then “X includes A or B” satisfies any of the examples above. In addition, the articles “a” and “an” used in this application and the attached claims should generally be understood to mean “one or more” unless otherwise specified or the context makes it clear that a singular form is intended. Throughout this specification, any reference to “a certain embodiment,” “a particular embodiment,” or “one embodiment” means that a particular characteristic, structure, or feature described in relation to an embodiment is included in at least one embodiment. Therefore, the occurrence of the phrases “a certain embodiment,” “a particular embodiment,” or “one embodiment” in various parts of this specification does not necessarily all refer to the same embodiment.
[0176] References to numerical ranges throughout this specification should not be interpreted as limitations, but rather as encompassing not only each number within the enumerated range and / or narrower ranges, but also the limits outside the range.
[0177] The term "approximately" should be understood to include a measurement error of up to 10% when referring to a physical quantity. For example, "approximately 100°C" should be understood to mean "100 ± 10°C".
[0178] The present invention has been described with reference to certain exemplary embodiments thereof. Therefore, this specification and the drawings should be considered illustrative rather than restrictive. In addition to those shown and described herein, various modifications of the invention will be apparent to those skilled in the art and are intended to fall within the scope of the appended claims. The present invention also includes the following embodiments. <1> A topical composition comprising an emulsion of an aqueous phase and an oily phase, wherein the emulsion comprises Ascorbate component; and Antioxidant compounds containing green tea polyphenols, ranging from over 0 wt.% to a maximum of approximately 1 wt.% A topical composition containing the above. <2> The topical composition according to claim 1, wherein the ascorbate component is present in the topical composition in an amount ranging from about 5 wt.% to about 40 wt.%, about 10 wt.% to about 30 wt.%, or about 15 wt.% to about 25 wt.%, based on the total weight of the topical composition. <3> The topical composition according to any one of 1 to 2 above, wherein the ascorbate component comprises ascorbic acid, tetrahexyldecyl ascorbate, or a combination thereof. <4> The topical composition according to claim 3, wherein the ascorbate component contains ascorbic acid present in the topical composition in an amount ranging from about 2 wt.% to about 30 wt.%, about 5 wt.% to about 25 wt.%, or about 10 wt.% to about 20 wt.%, based on the total weight of the topical composition. <5> The topical composition according to any one of 3 to 4, wherein the ascorbate component contains tetrahexyldecyl ascorbate present in the topical composition in an amount ranging from about 1 wt.% to about 15 wt.%, about 2 wt.% to about 10 wt.%, or about 3 wt.% to about 7 wt.%, based on the total weight of the topical composition. <6> The topical composition according to any one of 3 to 5 above, wherein the ascorbate component comprises a wt:wt ratio of ascorbic acid to tetrahexyldecyl ascorbate of about 10:1 to about 1:10, about 8:1 to about 1:8, about 5:1 to about 1:5, about 3:1 to about 1:3, about 3:1 to about 1:1, about 5:1 to about 1:1, about 8:1 to about 1:1, or about 10:1 to about 1:1. <7> The topical composition according to any one of 1 to 6 above, wherein the green tea polyphenol comprises epigallocatechin gallate, epigallocatechin, epicatechin gallate, catechin, epicatechin, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof. <8> The topical composition according to any one of 1 to 7 above, wherein the antioxidant system comprises an additional antioxidant selected from the group consisting of cinnamic acid, ferulic acid, caffeic acid, p-coumaric acid, sinapic acid, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof. <9> The topical composition according to any one of 1 to 7 above, wherein the antioxidant system does not contain or substantially contains antioxidants selected from the group consisting of cinnamic acid, ferulic acid, caffeic acid, p-coumaric acid, m-coumaric acid, sinapic acid, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof. <10> A topical composition according to any one of 1 to 9 above, wherein the antioxidant system comprises an additional antioxidant selected from the group consisting of gallic acid, delphinidin, luteolin, quercetin, cyanidin, taxifolin, kaempferol, malvidin, hesperidin, pelargonidine, apigenin, naringenin, chrysin, ergothioneine, glutathione, Emblica, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof. <11> The topical composition according to any one of 1 to 10 above, wherein the antioxidant system comprises apigenin, ergothioneine, its cis and trans isomers, its salts, its equivalent derivatives, and combinations thereof. <12> The topical composition according to 11, wherein the antioxidant system contains apigenin present in the topical composition in an amount ranging from more than 0 wt.% to about 0.5 wt.%, more than 0 wt.% to about 0.1 wt.%, or more than 0 wt.% to about 0.01 wt.%, based on the total weight of the topical composition. <13> The topical composition according to any one of 11 to 12, wherein the antioxidant system contains ergothioneine present in the topical composition in an amount ranging from more than 0 wt.% to about 0.5 wt.%, more than 0 wt.% to about 0.1 wt.%, or more than 0 wt.% to about 0.01 wt.%, based on the total weight of the topical composition. <14> The topical composition according to any one of 1 to 13, wherein the antioxidant system contains green tea polyphenols present in the topical composition in an amount ranging from more than 0 wt.% to about 0.5 wt.%, more than 0 wt.% to about 0.1 wt.%, or more than 0 wt.% to about 0.01 wt.%, based on the total weight of the topical composition. <15> The topical composition according to any one of 8 to 14, wherein the wt:wt ratio of the green tea polyphenol to the additional antioxidant is in the range of about 10:1 to about 1:10, about 8:1 to about 1:8, about 5:1 to about 1:5, about 3:1 to about 1:3, about 2:1 to about 1:2, or about 1:1. <16> A topical composition according to any one of items 1 to 15, further comprising a cosmetically acceptable excipient. <17> The topical composition according to 16, wherein the cosmetically acceptable excipient is selected from the group consisting of epidermal penetration enhancers, solvents, mild surfactants, oils, emulsifiers, pearlescent waxes, consistency modifiers, thickeners, suspending agents, chelating agents, preservatives, fat-suppressing agents, stabilizers, polymers, silicone compounds, fats, waxes, lecithin, phospholipids, UV photoprotective factors, bioactive ingredients, additional antioxidants, deodorants, antiperspirants, film-forming agents, swelling agents, insect repellents, self-tanning agents, tyrosinase inhibitors, hydrotropes, solubilizers, fragrance oils, pigments, or combinations thereof. <18> The topical composition according to 17, wherein the cosmetically acceptable excipient is selected from the group consisting of solvents, emulsifiers, consistency modifiers, thickeners, suspending agents, preservatives, additional antioxidants, fragrance oils, or combinations thereof. <19> A topical composition according to any one of items 17 to 18 above, which does not contain or substantially contains a silicone compound. <20> The topical composition according to any one of 17 to 19, wherein the cosmetically acceptable excipient comprises a solvent. <21> The topical composition according to 20, wherein the solvent comprises an alkanediol, glycerin, water, or a combination thereof. <22> The topical composition according to 21, wherein the alkanediol is present in the topical composition in an amount of about 2 wt.% to about 25 wt.%, about 5 wt.% to about 15 wt.%, or about 8 wt.% to about 12 wt.%, based on the total weight of the topical composition. <23> The topical composition according to any one of 21 to 22, wherein the alkanediol comprises a propanediol. <24> The topical composition according to any one of 21 to 23, wherein the glycerin is present in the topical composition in an amount of about 2 wt.% to about 25 wt.%, about 5 wt.% to about 15 wt.%, or about 8 wt.% to about 12 wt.%, based on the total weight of the topical composition. <25> The topical composition according to any one of 21 to 24, wherein the water is present in the topical composition in an amount of about 20 wt.% to about 80 wt.%, about 35 wt.% to about 70 wt.%, or about 50 wt.% to about 60 wt.%, based on the total weight of the topical composition. <26> A topical composition according to any one of 16 to 25, wherein the cosmetically acceptable excipient includes natural gum. <27> The topical composition according to 26, wherein the natural gum comprises sclerotium gum. <28> The topical composition according to any one of 26 to 27, wherein the natural gum is present in the topical composition in an amount of more than 0 wt.% to about 5 wt.%, about 0.1 wt.% to about 2 wt.%, or about 0.2 wt.% to about 0.8 wt.%, based on the total weight of the topical composition. <29> The topical composition according to any one of 16 to 28, further comprising the cosmetically acceptable excipient PEG-7 olive fatty acid. <30> The topical composition according to 29, wherein the olive fatty acid PEG-7 is present in the topical composition in an amount of more than 0 wt.% to about 5 wt.%, about 0.1 wt.% to about 2 wt.%, or about 0.2 wt.% to about 0.8 wt.%, based on the total weight of the topical composition. <31> The topical composition according to any one of the above 1 to 30, wherein the pH of the topical composition is about 2.0 to about 4.0, about 2.5 to about 3.5, or about 2.7 to about 3.3. <32> The topical composition according to any one of 16 to 31, wherein the cosmetically acceptable excipient includes a chelating agent. <33> The topical composition according to 32, wherein the chelating agent comprises disodium EDTA. <34> The topical composition according to any one of 32 to 33, wherein the chelating agent is present in the topical composition in an amount of more than 0 wt.% to about 5 wt.%, about 0.01 wt.% to about 0.5 wt.%, or about 0.05 wt.% to about 0.3 wt.%, based on the total weight of the topical composition. <35> The topical composition according to any one of 16 to 34, wherein the cosmetically acceptable excipient comprises a form of vitamin E selected from alpha, beta, delta, and gamma tocopherols, and alpha, beta, delta, and gamma tocotrienols, and combinations thereof. <36> The topical composition according to 35, wherein the form of vitamin E is present in the topical composition in an amount of about 0.1 wt.% to about 5 wt.%, about 0.3 wt.% to about 3 wt.%, or about 0.5 wt.% to about 2 wt.%, based on the total weight of the topical composition. <37> A topical composition according to any one of 16 to 36, wherein the cosmetically acceptable excipient includes a preservative. <38> The topical composition according to 37 above, wherein the preservative comprises phenoxyethanol. <39> The topical composition according to any one of 37 to 38, wherein the preservative is present in the topical composition in an amount of more than 0 to about 5 wt.%, about 0.3 wt.% to about 3 wt.%, or about 0.5 wt.% to about 2 wt.%, based on the total weight of the topical composition. <40> The topical composition according to any one of 16 to 39, wherein the cosmetically acceptable excipient is a fragrance oil selected from the group consisting of lavender oil, bergamot oil, eucalyptus oil, chamomile oil, melaleuca oil, or a combination thereof. <41> The topical composition according to 40, wherein the essential oil comprises lavender oil, chamomile oil, or a combination thereof. <42> The topical composition according to any one of 40 to 41, wherein the fragrance oil is present in the topical composition in an amount of more than 0 wt.% to about 5 wt.%, more than 0 wt.% to about 1 wt.%, or about 0.01 wt.% to about 0.3 wt.%, based on the total weight of the topical composition. <43> A method for treating the skin in question for the effects of radical-induced injury, Administering the topical composition described in any of items 1 to 42 above to the skin. Includes, The skin exhibits radical-induced damage or a reduction or attenuation of its effects after administration. method. <44> A method for brightening the target skin, Administering the topical composition described in any of items 1 to 42 above to the skin. A method comprising the above, wherein the skin becomes lighter after administration. <45> A method for treating the skin in question in relation to the effects of aging caused by the atmosphere, Administering the topical composition described in any of items 1 to 42 above to the skin. A method comprising the following, wherein the skin exhibits reduced or attenuated effects of aging after administration. <46> Administering any of the topical compositions described in 1 to 42 above to skin undergoing dermatological treatment. A method comprising the dermatological treatment being selected from the group consisting of chemical peeling, microablation, and laser treatment. <47> A method for treating skin in question for the effects of aging caused by air, comprising administering a topical composition described in any of items 1 to 42 above to the skin, wherein the skin exhibits improvement in the appearance of fine wrinkles in the eye area, smoothness, and skin radiance. <48> A method for treating target skin, comprising administering a topical composition described in any of items 1 to 42 above to the skin, wherein the skin exhibits at least one of: reduction or attenuation of fine wrinkles in the eye area; increase or maintenance of smooth skin; increase or maintenance of radiance; reduction or maintenance of wrinkles over the entire face; reduction or maintenance of wrinkles in the eye area; reduction or maintenance of hyperpigmentation; and increase or maintenance of firmness. <49> A method for treating a target skin, comprising administering a topical composition described in any of 1 to 42 above to the skin, wherein the skin exhibits improvement at 4 weeks, 8 weeks, and / or 12 weeks compared to at least one baseline of fine lines around the eyes; skin smoothness; radiance; wrinkles across the face; wrinkles in the eye area; hyperpigmentation; and firmness, as examined using a modified Griffith 10-point scale. <50> A method for treating a target skin, comprising administering a topical composition described in any of 1 to 42 above to the skin, wherein the skin exhibits improvement in fine wrinkles around the eyes at weeks 4, 8, and 12, respectively, compared to at least one baseline of -5% to -25%, -15% to -35%, or -25% to -45%, as measured by the modified Griffith 10-point scale. <51> A method for treating a target skin, comprising administering a topical composition described in any of 1 to 42 above to the skin, wherein the skin exhibits an improvement in skin smoothness at weeks 4, 8, and 12, respectively, of -1% to -10%, -5% to -15%, or -10% to -20%, as measured by the Modified Griffith 10-point scale. <52> A method for treating a target skin, comprising administering a topical composition described in any of 1 to 42 above to the skin, wherein the skin exhibits an improvement in radiance at weeks 4, 8, and 12, respectively, of -1% to -10%, -3% to -13%, or -5% to -15%, compared to at least one baseline, as measured by a modified Griffith 10-point scale. <53> A method for treating target skin, comprising administering a topical composition described in any of 1 to 42 above to the skin, wherein the skin exhibits improvement in wrinkles across the entire face at weeks 4 and 12, respectively, compared to at least one baseline of -1% to -10% or -3% to -13%, as measured by the modified Griffith 10-point scale. <54> A method for treating a target skin, comprising administering a topical composition described in any of items 1 to 42 above to the skin, wherein the skin exhibits improvement in wrinkles in the eye area at weeks 4 and 12, respectively, compared to at least one baseline of -1% to -10% or -2% to -12%, as measured by the modified Griffith 10-point scale. <55> A method for treating target skin, comprising administering a topical composition described in any of items 1 to 42 above to the skin, wherein the skin exhibits improvement in hyperpigmentation at weeks 4 and 12, respectively, compared to at least one baseline of -1% to -10% or -5% to -15% as measured by the modified Griffith 10-point scale. <56> A method for treating target skin, comprising administering a topical composition described in any of items 1 to 42 above to the skin, wherein the skin exhibits improvement in firmness at weeks 4 and 12, respectively, compared to at least one baseline of -1% to -10% or -3% to -13%, as measured by the modified Griffith 10-point scale. <57> A method for treating target skin, comprising administering to the skin a topical composition described in any of items 1 to 42 above, wherein at least 50%, at least 60%, at least 70%, at least 80%, at least 90%, or at least 95% of the target exhibits improvement compared to baseline in at least one of the following, as examined by the Modified Griffith 10-point Scale: fine lines around the eyes; skin smoothness; radiance; wrinkles throughout the face; wrinkles in the eye area; hyperpigmentation; and firmness.
Claims
1. A topical composition comprising an emulsion of an aqueous phase and an oily phase, wherein the emulsion comprises Ascorbic acid and ascorbate components including tetrahexyldecyl ascorbate; and Antioxidant formulations containing green tea polyphenols and at least one of apigenin and ergothioneine, ranging from over 0 wt.% to a maximum of 1 wt.%. Includes, The ascorbic acid is present in an amount ranging from 10 wt.% to 30 wt.% based on the total weight of the topical composition. The tetrahexyldecyl ascorbate is present in an amount ranging from 2 wt.% to 15 wt.% based on the total weight of the topical composition. A topical composition wherein the topical composition contains water in an amount of 50 wt.% to 60 wt.% based on the total weight of the topical composition.
2. The topical composition according to claim 1, wherein the ascorbate component is present in the topical composition in an amount ranging from 12 wt.% to 40 wt.% based on the total weight of the topical composition.
3. The topical composition according to claim 1 or 2, wherein the tetrahexyldecyl ascorbate is present in the topical composition in an amount ranging from 2 wt.% to 10 wt.% based on the total weight of the topical composition.
4. The topical composition according to any one of claims 1 to 3, wherein the wt:wt ratio of ascorbic acid to tetrahexyldecyl ascorbate is 10:1 to 1:
3.
5. The topical composition according to any one of claims 1 to 4, wherein the green tea polyphenol comprises epigallocatechin gallate, epigallocatechin, epicatechin gallate, catechin, epicatechin, its cis and trans isomers, its salts, and combinations thereof.
6. The topical composition according to any one of claims 1 to 5, further comprising an additional antioxidant selected from the group consisting of cinnamic acid, ferulic acid, caffeic acid, p-coumaric acid, sinapic acid, its cis and trans isomers, its salts, and combinations thereof.
7. The topical composition according to any one of claims 1 to 5, wherein the topical composition does not contain an antioxidant selected from the group consisting of cinnamic acid, ferulic acid, caffeic acid, p-coumaric acid, m-coumaric acid, sinapic acid, its cis and trans isomers, its salts, and combinations thereof.
8. A topical composition according to any one of claims 1 to 7, further comprising an additional antioxidant selected from the group consisting of gallic acid, delphinidin, luteolin, quercetin, cyanidin, taxifolin, kaempferol, malvidin, hesperidin, pelargonidine, naringenin, chrysin, glutathione, Emblica, its cis and trans isomers, its salts, and combinations thereof.
9. The topical composition according to claim 1, wherein the apigenin is present in the topical composition in an amount ranging from more than 0 wt.% to 0.5 wt.% based on the total weight of the topical composition.
10. The topical composition according to claim 1, wherein the ergothioneine is present in the topical composition in an amount ranging from more than 0 wt.% to 0.5 wt.% based on the total weight of the topical composition.
11. The topical composition according to claim 1, wherein the green tea polyphenol is present in the topical composition in an amount ranging from more than 0 wt.% to 0.5 wt.% based on the total weight of the topical composition.
12. The topical composition according to claim 6, wherein the wt:wt ratio of the green tea polyphenol to the additional antioxidant is in the range of 10:1 to 1:
10.
13. A topical composition according to any one of claims 1 to 12, further comprising a cosmetically acceptable excipient.
14. The topical composition according to claim 13, wherein the cosmetically acceptable excipient is selected from the group consisting of epidermal penetration enhancers, solvents, mild surfactants, oils, emulsifiers, pearlescent waxes, consistency modifiers, thickeners, suspending agents, chelating agents, preservatives, fat-suppressing agents, stabilizers, polymers, silicone compounds, fats, waxes, lecithin, phospholipids, UV photoprotective factors, bioactive ingredients, additional antioxidants, deodorants, antiperspirants, film-forming agents, swelling agents, insect repellents, self-tanning agents, tyrosinase inhibitors, hydrotropes, solubilizers, fragrance oils, pigments, or combinations thereof.
15. The topical composition according to claim 14, wherein the cosmetically acceptable excipient is selected from the group consisting of solvents, emulsifiers, consistency modifiers, thickeners, suspending agents, preservatives, additional antioxidants, fragrance oils, or combinations thereof.
16. A topical composition according to claim 14 or 15, which does not contain a silicone compound.
17. The topical composition according to any one of claims 14 to 16, wherein the cosmetically acceptable excipient comprises a solvent.
18. The topical composition according to claim 17, wherein the solvent comprises an alkanediol, glycerin, water, or a combination thereof.
19. The topical composition according to claim 18, wherein the alkanediol is present in the topical composition in an amount of 2 wt.% to 25 wt.%, 5 wt.% to 15 wt.%, or 8 wt.% to 12 wt.%, based on the total weight of the topical composition.
20. The topical composition according to claim 18 or 19, wherein the alkanediol comprises a propanediol.
21. The topical composition according to any one of claims 18 to 20, wherein the glycerin is present in the topical composition in an amount of 2 wt.% to 25 wt.%, 5 wt.% to 15 wt.%, or 8 wt.% to 12 wt.%, based on the total weight of the topical composition.
22. The topical composition according to any one of claims 13 to 21, wherein the cosmetically acceptable excipient includes natural gum.
23. The topical composition according to claim 22, wherein the natural gum comprises sclerotium gum.
24. The topical composition according to claim 22 or 23, wherein the natural gum is present in the topical composition in an amount of more than 0 wt.% to 5 wt.%, 0.1 wt.% to 2 wt.%, or 0.2 wt.% to 0.8 wt.%, based on the total weight of the topical composition.
25. The topical composition according to any one of claims 13 to 24, further comprising the cosmetically acceptable excipient PEG-7 olive fatty acid.
26. The topical composition according to claim 25, wherein the olive fatty acid PEG-7 is present in the topical composition in an amount of more than 0 wt.% to 5 wt.%, 0.1 wt.% to 2 wt.%, or 0.2 wt.% to 0.8 wt.%, based on the total weight of the topical composition.
27. The topical composition according to any one of claims 1 to 26, wherein the pH of the topical composition is 2.0 to 4.0, 2.5 to 3.5, or 2.7 to 3.
3.
28. The topical composition according to any one of claims 13 to 27, wherein the cosmetically acceptable excipient comprises a chelating agent.
29. The topical composition according to claim 28, wherein the chelating agent comprises EDTA disodium.
30. The topical composition according to claim 28 or 29, wherein the chelating agent is present in the topical composition in an amount of more than 0 wt.% to 5 wt.%, 0.01 wt.% to 0.5 wt.%, or 0.05 wt.% to 0.3 wt.%, based on the total weight of the topical composition.
31. The topical composition according to any one of claims 13 to 30, wherein the cosmetically acceptable excipient comprises forms of vitamin E selected from alpha, beta, delta, and gamma tocopherols, and alpha, beta, delta, and gamma tocotrienols, and combinations thereof.
32. The topical composition according to claim 31, wherein the form of vitamin E is present in the topical composition in an amount of 0.1 wt.% to 5 wt.%, 0.3 wt.% to 3 wt.%, or 0.5 wt.% to 2 wt.%, based on the total weight of the topical composition.
33. The topical composition according to any one of claims 13 to 32, wherein the cosmetically acceptable excipient includes a preservative.
34. The topical composition according to claim 33, wherein the preservative comprises phenoxyethanol.
35. The topical composition according to claim 33 or 34, wherein the preservative is present in the topical composition in an amount of more than 0 to 5 wt.%, 0.3 wt.% to 3 wt.%, or 0.5 wt.% to 2 wt.%, based on the total weight of the topical composition.
36. The topical composition according to any one of claims 13 to 35, wherein the cosmetically acceptable excipient comprises a fragrance oil which is an essential oil selected from the group consisting of lavender oil, bergamot oil, eucalyptus oil, chamomile oil, melaleuca oil, or a combination thereof.
37. The topical composition according to claim 36, wherein the essential oil comprises lavender oil, chamomile oil, or a combination thereof.
38. The topical composition according to claim 36 or 37, wherein the fragrance oil is present in the topical composition in an amount of more than 0 wt.% to 5 wt.%, more than 0 wt.% to 1 wt.%, or 0.01 wt.% to 0.3 wt.%, based on the total weight of the topical composition.
39. A topical composition according to any one of claims 1 to 38 for treating the target skin.
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