Cosmetic compositions and methods of use thereof
By incorporating black willow bark extract and niacinamide into a D5-free topical composition, the unpleasant feel, low durability, and irritation issues of existing UV protection compositions are addressed, achieving the effects of soothing the skin, reducing heat irritation, and maintaining UV protection.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- MARY KAY INC
- Filing Date
- 2024-12-23
- Publication Date
- 2026-07-21
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Abstract
Description
Cross-reference to related applications
[0001] This application claims priority to U.S. Provisional Patent Application No. 63 / 613,509, filed December 21, 2023, which is incorporated herein by reference in its entirety. Background of the Invention
[0002] A. Field of Invention
[0003] The present invention generally relates to cosmetic compositions that can be used to protect the skin, including protecting the skin from ultraviolet (UV) radiation (e.g., sunlight) and / or soothing the skin by reducing the immune response in the skin triggered by heat exposure.
[0004] B. Relevant Technical Description
[0005] Several UV protection compositions are currently available. These compositions have various drawbacks, ranging from unpleasant tactile properties (e.g., a heavy, oily, or sticky feel), low persistence (e.g., a tendency to migrate and accumulate at the application site or a tendency to be easily removed from the skin after only one wash), insufficient moisturizing and / or UV protection capabilities, and low directness. Furthermore, UV protection compositions may contain ingredients that irritate sensitive skin. There is a need in the art for direct sunscreen compositions that can be tolerated by sensitive skin.
[0006] Additionally, UV protection compositions that do not contain decamethylcyclopentasiloxane (D5) (also known as cyclopentasiloxane) use polydimethylsiloxane to maintain colorant dispersion. However, polydimethylsiloxane, due to its volatility, may excessively enhance the penetration of sunscreen actives (e.g., UV absorbers) into the epidermis. The presence of high levels of sunscreen actives can, in turn, irritate the skin and impair the soothing properties of the UV protection composition. Furthermore, sunscreen actives perform their UV protection function by absorbing UV energy and converting it into heat. The presence of sunscreen actives deeper within the epidermis can generate excessive heat, which can overheat the skin and cause irritation and redness. Skin with a thin epidermis is particularly susceptible to such irritation and redness caused by overheating from UV protection compositions containing polydimethylsiloxane. Invention Overview
[0007] The present invention overcomes the deficiencies in the art by providing topical compositions that do not contain decamethylcyclopentasiloxane (D5) (e.g., topical skin compositions that do not contain D5), which protect the skin from ultraviolet (UV) radiation (e.g., sunlight) and soothe the skin by reducing the immune response in the skin triggered by heat exposure.
[0008] In one example, the present invention overcomes the limitations of topical compositions containing polydimethylsiloxanes by including Salix nigra (willow) bark extract in a D5-free topical composition. As mentioned above, excessive heat caused by UV absorption can lead to skin redness, especially in thin epidermis. Adding Salix nigra bark extract to a D5-free topical composition counteracts the immune response that causes skin redness, thereby soothing the skin and reducing redness. In another example, the present invention overcomes the limitations of polydimethylsiloxanes by including niacinamide in a D5-free topical composition. Niacinamide is an antioxidant and promotes the absorption of more UV radiation by sunscreen active ingredients; therefore, a D5-free topical composition containing niacinamide can use lower levels of sunscreen active ingredients without sacrificing its UV protection effectiveness. Using lower levels of sunscreen active ingredients in such a D5-free topical composition containing niacinamide results in less heat generated in the skin due to less UV absorption, thereby reducing skin irritation and redness.
[0009] In one example, a D5-free topical composition is disclosed. In one example, the D5-free topical composition comprises any one, any combination of, or all of Salix nigra bark extract, nicotinamide, and octocrylene. The amounts of the components in the composition can vary (e.g., from as low as 0.000001% to as high as 80% w / w or any range thereof). In one example, the composition comprises: 0.0001% to 3% by weight Salix nigra bark extract, 0.01% to 5% by weight nicotinamide, and 1% to 20% by weight octocrylene. In one example, the composition also comprises polydimethylsiloxane. In one example, the composition also comprises 2% to 20% by weight polydimethylsiloxane. The composition may also contain one or more of the components described herein. For example, the composition may contain one or more additional ingredients selected from one or more conditioning agents, humectants, pH adjusters, structuring agents, inorganic salts and / or preservatives.
[0010] In one example, the D5-free topical composition comprises any, any combination of, or all of magnesium sulfate, glycerin, xanthan gum, butylene glycol, ascorbate glucoside, octyl polymethylsiloxane, butyl octyl salicylate, octisalate ethylhexyl salicylate, and / or silica. The amounts of the components in the composition can vary (e.g., from as low as 0.000001% to as high as 80% w / w or any range thereof). In one example, the composition comprises: 0.01% to 3% magnesium sulfate by weight, 1% to 10% glycerin by weight, 0.01% to 3% xanthan gum by weight, 1% to 20% butylene glycol by weight, 0.01% to 3% ascorbate glucoside by weight, 1% to 10% octyl polymethylsiloxane by weight, 1% to 15% butyl octyl salicylate by weight, 1% to 15% ethylhexyl salicylate by weight, and / or 0.01% to 3% silica by weight. The composition may also contain one or more of the ingredients described herein. For example, the composition may contain one or more additional ingredients selected from one or more conditioning agents, humectants, pH adjusters, structuring agents, inorganic salts, and / or preservatives.
[0011] The formulations disclosed herein contain active ingredients that provide protection against sun damage (e.g., ultraviolet radiation) and soothe the skin. Non-limiting examples of such active ingredients include Salix nigra bark extract, niacinamide, and octocrylene. In some embodiments, these ingredients are contained in a single topical dermal formulation, together with moisturizers, pigments, and various excipients, to produce a multipurpose cosmetic product for improving skin appearance and protecting against sun damage. In one aspect, the D5-free topical composition may have a sun protection factor (SPF) of 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, or higher, containing sufficient amounts of Salix nigra bark extract, niacinamide, octocrylene, and optionally additional sunscreen active ingredients. In one respect, compared to the second composition, the D5-free topical composition uses less octocrylene and / or additional sunscreen active ingredients to provide the same SPF, and the second composition is identical to the D5-free topical composition except that it contains D5 and / or does not contain Salix nigra bark extract, niacinamide, and / or octocrylene. In some cases, the composition contains less than 20%, 19%, 18%, 17%, 16%, 15%, 14%, 13%, 12%, 11%, 10%, 9%, 8%, 7%, 6%, 5%, 4%, 3%, 2%, or 1% of additional sunscreen active ingredients by weight. In some cases, the composition contains less than 15%, 14%, 13%, 12%, 11%, 10%, 9%, 8%, 7%, 6%, or 5% octocrylene by weight. In some cases, the composition comprises less than 40%, 39%, 38%, 37%, 36%, 35%, 34%, 33%, 32%, 31%, 30%, 29%, 28%, 27%, 26%, 25%, 24%, 23%, 22%, 21%, 20%, 19%, 18%, 17%, 16%, 15%, 14%, 13%, 12%, 11%, 10%, 9%, 8%, 7%, or 6% by weight of octocrylene and additional sunscreen active ingredients.
[0012] Methods of using the compositions disclosed herein are also disclosed. In one aspect, the disclosed D5-free topical compositions comprise Salix nigra bark extract, niacinamide, and octocrylene. In some cases, the method includes applying any of the compositions disclosed herein topically to the desired skin and / or facial and / or eye areas. In one aspect, any of the compositions disclosed herein are applied topically, and the composition is left on the application area, removed from the application area after a period of time, and / or removed directly after application. In some cases, the method includes applying any of the D5-free topical compositions disclosed herein topically to the skin, wherein any of the D5-free topical compositions disclosed herein provide UV protection to the skin while using fewer sunscreen active ingredients to provide the same level of UV protection as a second composition, which is identical to the D5-free topical composition except that it contains D5 and / or does not contain Salix nigra bark extract, niacinamide, and octocrylene.
[0013] In one example, compared to the second composition, any of the D5-free topical compositions disclosed herein reduces the penetration of sunscreen active ingredients into the skin, except that the second composition contains D5 and / or does not contain Salix nigra bark extract, niacinamide, and octocrylene, and is otherwise identical to the D5-free topical composition. In one example, compared to the second composition, any of the D5-free topical compositions disclosed herein reduces the immune response in the skin triggered by heat exposure, except that the second composition contains D5 and / or does not contain Salix nigra bark extract, niacinamide, and octocrylene, and is otherwise identical to the D5-free topical composition. In one example, any of the D5-free topical compositions disclosed herein protects the skin from irritation.
[0014] In certain aspects, the compositions of the present invention are formulated as topical skin compositions. The compositions may have dermatologically acceptable carriers or precipitants for use with the compounds, compositions, and extracts. The compositions may also contain moisturizing agents or humectants, surfactants, silicone-containing compounds, ultraviolet agents, oils, and / or other ingredients specified herein or known in the art. The compositions may be lotions, creams, body creams, masks, scrubs, lotions, gels, serums, emulsions (e.g., oil-in-water, water-in-oil, silicone-in-water, water-in-silicone, oil-in-oil, water-in-water, oil-in-water, water-in-silicone, etc.), solutions (e.g., aqueous or water-alcohol solutions), anhydrous bases (e.g., lipsticks or powders), ointments, lotions, pastes, aerosols, solid forms, ophthalmic gels, etc. The compositions may be in powder form (e.g., dried, lyophilized, granular, etc.). The composition can be formulated for topical skin application at least 1, 2, 3, 4, 5, 6, 7 or more times daily during use. In some aspects of the invention, the composition can be storage-stable or color-stable, or both. It is also anticipated that the viscosity of the composition can be selected to achieve the desired results, for example, depending on the desired type of composition, such compositions may have a viscosity from about 1 cps to well above 1 million cps or any range or integer derived therefrom (e.g., 2 cps, 3 cps, 4 cps, 5 cps, 6 cps, 7 cps, 8 cps, 9 cps, 10 cps, 20 cps, 30 cps, 40 cps, 50 cps, 60 cps, 70 cps, 80 cps, 90 cps, 100 cps, 200 cps, 300 cps, 400 cps, 500 cps, 600 cps, 700 cps, 800 cps, 900 cps, 1000 cps, 2000 cps, 3000 cps, 4000 cps, 5000 cps, 6000 cps, 7000 cps, etc.). 8000cps, 9000cps, 10000cps, 20000cps, 30000cps, 40000cps, 50000cps, 60000cps, 700 00cps, 80000cps, 90000cps, 100000cps, 200000cps, 300000cps, 400000cps, 500000cps 600,000 cps, 700,000 cps, 800,000 cps, 900,000 cps, 1,000,000 cps, 2,000,000 cps, 3,000,000 cps, 4,000,000 cps, 5,000,000 cps, 10,000,000 cps, etc., measured using a TC spindle at 25°C and 2.5 rpm on a Brookfield viscometer.
[0015] The compositions of the present invention can also be modified to have a desired oxygen radical scavenging capacity (ORAC) value. In some non-limiting aspects, the compositions of the present invention or their components or extracts specified herein may be modified to have a value of at least about 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 35, 40, 45, 50, 55, 60, or 70 mg per milligram. ORAC values of 80, 90, 95, 100, 200, 300, 400, 500, 600, 700, 800, 900, 1000, 2000, 3000, 4000, 5000, 6000, 7000, 8000, 9000, 10000, 15000, 20000, 30000, 50000, 100000 or higher, or any range derived therefrom.
[0016] In a non-limiting aspect, the pH of the composition can be from about 6 to about 9. In some aspects, the pH can be 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, or 14. The composition may contain triglycerides. Non-limiting examples include small, medium, and large chain triglycerides. In some aspects, the triglyceride is a medium chain triglyceride (e.g., caprylic / capric triglyceride). The composition may also contain preservatives. Non-limiting examples of preservatives include phenoxyethanol, methylparaben, propylparaben, or any mixture thereof. In some embodiments, the composition is free of parabens.
[0017] The compositions of the present invention may have UVA and UVB absorption properties. The compositions may have a sun protection factor (SPF) of 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 20, 25, 30, 35, 40, 45, 50, 55, 60 or higher, or any integer or derivative thereof. The compositions may be sunscreen lotions, sunscreen sprays, or sunscreen creams.
[0018] The compositions of the present invention may also contain any one, any combination, or all of the following additional ingredients: water, conditioning agents, chelating agents, humectants, pH adjusters, inorganic salts, preservatives, thickeners, silicone compounds, essential oils, structuring agents, vitamins, pharmaceutical ingredients, or antioxidants, or any combination or mixture of such ingredients. In some aspects, the composition may contain at least two, three, four, five, six, seven, eight, nine, ten, or more additional ingredients, or all of the additional ingredients specified in the preceding sentence. Non-limiting examples of such additional ingredients are pointed out in this specification and incorporated herein by reference. The amount of such ingredients may range from 0.0001% to 99.9% by weight or volume of the composition, or any integer or range therebetween as disclosed in other sections of this specification, which are incorporated herein by reference.
[0019] Kits comprising the compositions of the present invention are also contemplated. In some embodiments, the composition is contained in a container. The container may be a bottle, dispenser, or package. The container dispenses a predetermined amount of the composition. In some aspects, the composition is dispensed as a spray, mist, clump, or liquid. The container may have markings on its surface. The markings may be words, abbreviations, pictures, or symbols.
[0020] The compositions disclosed in this specification are also intended to be used as leave-on or rinse-off compositions. For example, a leave-on composition may be a composition applied topically to the skin and left on the skin for a period of time, such as at least 5, 6, 7, 8, 9, 10, 20, or 30 minutes, or at least 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, or 24 hours, or overnight or throughout the day. A rinse-off composition may be a product intended to be applied to the skin and then removed or rinsed off (e.g., with water) for a period of time, such as less than 5, 4, 3, 2, or 1 minute. Examples of rinse-off compositions may be skin cleansers, shampoos, conditioners, or soaps. Examples of leave-on compositions may be skin moisturizers, sunscreens, face masks, overnight creams, or day creams.
[0021] It is anticipated that any embodiments discussed in this specification can be implemented in conjunction with any method or composition of the invention, and vice versa. Furthermore, the compositions of the invention can be used to implement the methods of the invention.
[0022] In the context of this invention, at least 20 aspects are described: Aspect 1 includes a method of protecting skin by topical application of a composition that does not contain D5, the composition comprising Salix nigra bark extract, nicotinamide, and octocrylene, wherein the skin is protected without the use of D5. Aspect 2 depends on aspect 1, wherein the composition further comprises 0.0001% to 3% by weight of Salix nigra bark extract, 0.01% to 5% by weight of nicotinamide, and 1% to 20% by weight of octocrylene. Aspect 3 depends on aspect 1, wherein the composition further comprises polydimethylsiloxane. Aspect 4 depends on aspect 3, wherein the composition comprises 2% to 20% by weight of polydimethylsiloxane. Aspect 5 depends on aspect 1, wherein the composition further comprises magnesium sulfate, glycerin, xanthan gum, butylene glycol, ascorbate glucoside, octyl polymethylsiloxane, butyl octyl salicylate, ethylhexyl salicylate, and silica. Aspect 6 depends on aspect 5, wherein the composition comprises 0.01% to 3% magnesium sulfate, 1% to 10% glycerol, 0.01% to 3% xanthan gum, 1% to 20% butylene glycol, 0.01% to 3% ascorbate glucoside, 1% to 10% octyl polymethylsiloxane, 1% to 15% butyl octyl salicylate, 1% to 15% ethylhexyl salicylate, and 0.01% to 3% silica. Aspect 7 depends on aspect 1, wherein the composition further comprises milk thistle (Silybum marianum) fruit extract. Aspect 8 depends on aspect 1, wherein the composition further comprises one or more additional ingredients selected from colorants, chelating agents, surfactants, viscosity control agents, film-forming agents, humectants, foaming agents, pH adjusters, moisturizers, antioxidants, fragrances, skin conditioning agents, structuring agents, exfoliating agents, preservatives, and solvents. Aspect 9 depends on aspect 1, wherein the composition is formulated as an emulsion, cream, lotion, oil, gel, water-in-oil emulsion, or ointment. Aspect 10 depends on aspect 1, wherein the composition is formulated to be sweat-resistant and / or moisture-resistant. Aspect 11 depends on aspect 1, wherein the composition protects the skin from ultraviolet (UV) radiation. Aspect 12 depends on aspect 1, wherein the composition reduces the immune response in the skin triggered by heat exposure compared to a second composition containing D5 and / or not containing the key ingredient. Aspect 13 includes a D5-free topical skin care composition comprising Salix nigra bark extract, niacinamide, and octocrylene, wherein the composition does not contain D5. Aspect 14 depends on aspect 13, wherein the composition further comprises 0.0001% to 3% by weight of Salix nigra bark extract, 0.01% to 5% by weight of niacinamide, and 1% to 20% by weight of octocrylene.Aspect 15 depends on aspect 13, wherein the composition further comprises polydimethylsiloxane. Aspect 16 depends on aspect 15, wherein the composition comprises 2% to 20% polydimethylsiloxane by weight. Aspect 17 depends on aspect 14, wherein the composition further comprises magnesium sulfate, glycerin, xanthan gum, butylene glycol, ascorbate glucoside, octyl polymethylsiloxane, butyl octyl salicylate, ethylhexyl salicylate, and silica. Aspect 18 depends on aspect 13, wherein the composition is formulated as an emulsion, cream, lotion, oil, gel, or ointment, and further comprises a variety of additional functional ingredients. Aspect 19 depends on aspect 13, wherein the composition is used in formulations such as emulsions, creams, lotions, oils, gels, and ointments to provide skin benefits without D5. Aspect 20 depends on aspect 13, wherein the composition further comprises milk thistle (Silybum marianum) fruit extract. These aspects comprehensively cover D5-free topical skin compositions and their various formulations and enhancements.
[0023] In some embodiments, the compositions of the present invention may be pharmaceutically elegant or cosmetically elegant, or may have pleasant tactile properties. "Pharmaceutically elegant," "cosmetically elegant," and / or "pleasant tactile properties" describe compositions having specific tactile properties that feel pleasant on the skin (e.g., compositions that are not too thin or oily, compositions with a silky texture, non-sticky or non-greasy compositions, etc.). Pharmaceutically or cosmetically elegant may also refer to creamy or lubricating properties of the composition, or to moisturizing properties of the composition.
[0024] A product comprising the composition of the present invention is also contemplated. In a non-limiting aspect, the product may be a cosmetic product. The cosmetic product may be those described in other sections of this specification or those known to those skilled in the art. Non-limiting examples of the product include moisturizers, creams, lotions, skin softeners, serums, gels, lotions, body creams, scrubs, foundations, night creams, lipsticks, cleansers, toners, sunscreens, face masks, anti-aging products, deodorants, antiperspirants, perfumes, colognes, etc.
[0025] "Topical application" means applying or spreading the composition onto the surface of the lips or stratum corneum. "Topical skin compositions" include compositions suitable for topical application to the skin, lips, and / or stratum corneum. Such compositions are generally dermatologically acceptable because they do not exhibit undue toxicity, incompatibility, instability, allergic reactions, etc., when applied to the lips, skin, and / or stratum corneum. The topical skin care compositions of the present invention may have a selected viscosity to avoid significant dripping or aggregation after application to the lips, skin, and / or stratum corneum.
[0026] "Keratinous tissue" includes the keratin-containing layer that serves as the outermost protective covering of mammals, and includes, but is not limited to, the lips, skin, hair, and nails.
[0027] The term “about” or “approximately” is defined as close to, as understood by one of ordinary skill in the art. In one non-limiting embodiment, the term is defined as a deviation of less than 10%, preferably less than 5%, more preferably less than 1%, and most preferably less than 0.5%.
[0028] The term “substantially” and its variations are defined as being specified in a manner that is largely but not necessarily entirely as understood by one of ordinary skill in the art, and in a non-limiting embodiment, substantially refers to a range of deviations within 10%, within 5%, within 1%, or within 0.5%.
[0029] The terms “inhibition” or “reduction” or any variations thereof include any measurable reduction or complete inhibition in order to achieve the desired result. The terms “promotion” or “increase” or any variations thereof include any measurable increase in order to achieve the desired result, such as a measurable increase in a protein or molecule (e.g., matrix proteins such as fibronectin, laminin, collagen, elastin, or molecules such as hyaluronic acid).
[0030] The term "effective," as used in this specification and / or claims, means sufficient to achieve the desired, anticipated, or intended result.
[0031] When used in conjunction with the terms “comprising,” “including,” “having,” or “containing,” or any variations thereof, in the claims and / or specification, no quantifier precedes the element to mean “one / type,” but is consistent with the meaning of “one / type or more / types,” “at least one / type,” and “one / type or more than one / type.”
[0032] As used in this specification and claims, “comprising,” “having,” “including,” or “containing” is inclusive or open-ended and does not exclude additional, unlisted elements or method steps.
[0033] The composition and its method of use may “comprising,” “consistently composed of,” or “composed of” any of the ingredients or steps disclosed in this specification. Regarding the phrase “consistently composed of,” a fundamental and novel characteristic of the compositions and methods of the present invention is the ability to protect the skin from ultraviolet (UV) radiation (e.g., sunlight) and to soothe the skin by reducing the immune response in the skin triggered by heat exposure.
[0034] Other objects, features, and advantages of the invention will become apparent from the following detailed description. However, it should be understood that the detailed description and embodiments, while pointing to specific embodiments of the invention, are given by way of illustration only. Furthermore, changes and modifications contemplated within the spirit and scope of the invention will become apparent to those skilled in the art from this detailed description. Detailed Implementation
[0035] As described above, several unique aspects of the present invention involve combining Salix nigra bark extract, nicotinamide, and octocrylene in a topical composition that does not contain D5. This allows for the benefit of protecting the skin from ultraviolet (UV) radiation (e.g., sunlight) while using fewer sunscreen actives, reducing the penetration of sunscreen actives into the skin (e.g., the epidermis), protecting the skin from irritation, and soothing the skin by reducing the immune response in the skin triggered by heat exposure.
[0036] The following subsections describe the non-limiting aspects of the invention in more detail.
[0037] Some of the compositions disclosed herein are designed as topical compositions. These compositions rely on a unique combination of any one, any combination, or all of Salixnigra bark extract, nicotinamide, and octocrylene. Non-limiting examples of such compositions are provided in Example 1, Table 1.
[0038] Some of the compositions disclosed herein can be applied to the skin or hair and remain on the skin or hair for a period of time (e.g., at least 1, 2, 3, 4, 5, 10, 20, 30, or 60 minutes or longer). Thereafter, if desired, the composition can be rinsed off or peeled off the skin. Some of the compositions disclosed herein can be applied to the skin and rinsed off immediately. Some of the compositions disclosed herein can be applied to the skin and are at least partially absorbed by the skin.
[0039] These and other non-limiting aspects of the invention are described in the following sections.
[0040] A. Active ingredients
[0041] This invention is based on the determination that a combination of one or more active ingredients—Salix nigra bark extract, niacinamide, and octocrylene—can protect the skin from ultraviolet (UV) radiation (e.g., sunlight) and soothe the skin by reducing the immune response in the skin triggered by heat exposure.
[0042] Black willow (Salix nigra) bark extract, also known as willow bark extract, is an anti-irritant ingredient. It may be rich in tannins and is a natural source of salicylic acid. In some cases, this ingredient is commercially available, for example, from Active Concepts (North Carolina, USA), which offers an aqueous extract under the trade name ABS Willow Bark Extract. It has been determined that this ingredient can be used to inhibit bacterial growth and promote exfoliation without any of the typically associated irritation.
[0043] Milk thistle (Silybum marianum) fruit extract, commonly known as milk thistle extract, is recognized for its antioxidant and anti-inflammatory properties. It is rich in silymarin, a flavonoid lignan complex believed to protect against oxidative stress and support liver health. Studies have shown that this extract helps protect skin cells from UV-induced oxidative stress and may also promote skin hydration and elasticity, providing benefits without causing the irritation typically associated with chemical-based skin treatments.
[0044] Niacinamide, also known as nicotinamide, 3-pyridinecarboxamide, or vitamin B3, is an organic compound and antioxidant. Niacinamide is commercially available from a wide range of sources. It has been established that this ingredient can provide skin-conditioning benefits when used in cosmetic compositions.
[0045] Octocrylene is an organic compound and an ester formed by the condensation of diphenylcyanoacrylate and 2-ethylhexanol. It is a viscous, oily liquid that is clear and colorless. The extended conjugation of the acrylate moiety absorbs ultraviolet B (UVB) and short-wave ultraviolet A (UVA) rays with wavelengths from 280 nm to 320 nm, protecting the skin from direct DNA damage. The ethylhexanol moiety is a fatty alcohol that adds emollient and oil-like (water-resistant) properties. Octocrylene is commercially available from a wide range of sources.
[0046] This combination of ingredients can be used in different product forms to treat a variety of skin conditions. By way of non-limiting examples, this combination of ingredients can be formulated in emulsions (e.g., oil-in-water, water-in-oil), gels, serums, gel emulsions, gel serums, lotions, masks, scrubs, lotions, creams, or body moisturizers.
[0047] The extracts described herein can be extracts prepared by extraction methods and combinations thereof known in the art. Non-limiting examples of extraction methods include extraction using liquid-liquid extraction, solid-phase extraction, aqueous extraction, ethyl acetate, alcohol, acetone, oil, supercritical carbon dioxide, heat, pressure, pressure drop extraction, ultrasonic extraction, etc. The extracts can be liquids, solids, dried liquids, resuspended solids, etc.
[0048] B. Amount of components
[0049] The compositions of the present invention are intended to contain any amount of the ingredients discussed in this specification. The composition may also contain any combination of any amount of additional ingredients described in this specification (e.g., pigments, or additional cosmetic or pharmaceutical ingredients). The concentration of any ingredient within the composition may vary. In a non-limiting embodiment, for example, the composition in its final form may contain, substantially consist of, or consist of at least one ingredient mentioned in this specification and claims in the following percentages, substantially of, or constitute of the following percentages, for example, at least about 0.0001%, 0.0002%, 0.0003%, 0.0004%, 0.0005%, 0.0006%, 0.0007%, 0.0008%, 0.0009%, 0.0010%, 0.0011%, 0.0012%, 0.0013%, 0.0014%, 0.0015%, 0.0016%, 0.0017%, 0.0018%, ...15%, 0.0016%, 0.0017%, 0.0018%, 0.0012%, 0.0013%, 0.0014%, 0.0015%, 0.0016%, 0.0017%, 0.0018%, 0.0012%, 0 .0019%, 0.0020%, 0.0021%, 0.0022%, 0.0023%, 0.0024%, 0.0025%, 0.0026%, 0.0027%, 0.0028%, 0.0029%, 0.0030%, 0.0031%, 0.0032%, 0.0033%, 0.0034%, 0.0035%, 0.0036%, 0.0037%, 0.0038%, 0.0039%, 0.0040%, 0.0041%, 0.0042%, 0.0043%, 0.0044%, 0.0045%, 0.0046%, 0.00 47%, 0.0048%, 0.0049%, 0.0050%, 0.0051%, 0.0052%, 0.0053%, 0.0054%, 0.0055%, 0.0056%, 0.0057%, 0.0058%, 0.0059%, 0.0060%, 0.0061%, 0.0062%, 0.0063%, 0.0064%, 0.0065%, 0.0066%, 0.0067%, 0.0068%, 0.0069%, 0.0070%, 0.0071%, 0.0072%, 0.0073%, 0.0074%, 0.0075% 0.0076%, 0.0077%, 0.0078%, 0.0079%, 0.0080%, 0.0081%, 0.0082%, 0.0083%, 0.0084%, 0.0085%, 0.0086%, 0.0087%, 0.0088%, 0.0089%, 0.0090%, 0.0091%, 0.0092%, 0.0093%, 0.0094%, 0.0095%, 0.0096%, 0.0097%, 0.0098%, 0.0099%, 0.0100%, 0.0200%, 0.0250%, 0.0275%, 0.0300%、0.0325%、0.0350%、0.0375%、0.0400%、0.0425%、0.0450%、0.0475%、0.0500%、0.0525%、0.0550%、0.0575%、0.0600%、0.0625%、0.0650%、0.0675%、0.0700%、0.0725%、0.0750%、0.0775%、0.0800%、0.0825%、0.0850%、0.0875%、0.0900%、0.0925%、0.0950%、0.0975%、0.1000%、0.1250%、0.1500%、0.1750%、0.2000%、0.2250%、0.2500%、0.2750%、0.3000%、0.3250%、0.3500%、0.3750%、0.4000%、0.4250%、0.4500%、0.4750%、0.5000%、0.5250%、0.0550%、0.5750%、0.6000%、0.6250%、0.6500%、0.6750%、0.7000%、0.7250%、0.7500%、0.7750%、0.8000%、0.8250%、0.8500%、0.8750%、0.9000%、0.9250%、0.9500%、0.9750%、1.0%、1.1%、1.2%、1.3%、1.4%、1.5%、1.6%、1.7%、1.8%、1.9%、2.0%、2.1%、2.2%、2.3%、2.4%、2.5%、2.6%、2.7%、2.8%、2.9%、3.0%、3.1%、3.2%、3.3%、3.4%、3.5%、3.6%、3.7%、3.8%、3.9%、4.0%、4.1%、4.2%、4.3%、4.4%、4.5%、4.6%、4.7%、4.8%、4.9%、5.0%、5.1%、5.2%、5.3%、5.4%、5.5%、5.6%、5.7%、5.8%、5.9%、6.0%、6.1%、6.2%、6.3%、6.4%、6.5%、6.6%、6.7%、6.8%、6.9%、7.0%、7.1%、7.2%、7.3%、7.4%、7.5%、7.6%、7.7%、7.8%、7.9%、8.0%、8.1%、8.2%、8.3%、8.4%、8.5%、8.6%、8.7%、8.8%、8.9%、9.0%、9.1%、9.2%、9.3%、9.4%、9.5%、9.6%、9.7%、9.8%、9.9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20%, 21%, 22%, 23%, 24%, 25%, 26%, 27%, 28%, 29%, 30%, 35%, 40%, 45%, 50%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, or 99%, or any range derived therefrom. In a non-limiting respect, percentages may be calculated by weight or volume of the total composition. Those skilled in the art will understand that concentrations can vary depending on the addition, substitution, and / or reduction of ingredients in a given composition.
[0050] C. Carrier
[0051] The compositions of the present invention may comprise or incorporate all types of carriers and supports. The carrier or support may be pharmaceutically or dermatologically acceptable. Non-limiting examples of carriers or supports include water, glycerol, alcohols, oils, silicone-containing compounds, silicone compounds, and waxes. Variations and other suitable carriers will be apparent to those skilled in the art and are suitable for use in the present invention. In some aspects, the concentrations and combinations of compounds, ingredients, and reagents may be selected in such a way that the combination is chemically compatible and does not form complexes that precipitate from the final product.
[0052] D. Structure
[0053] The compositions of the present invention can be structured or formulated into a variety of different forms. Non-limiting examples include emulsions (e.g., water-in-oil, water-in-oil, water-in-oil, silicone-in-water, water-in-silicone, oil-in-water-in-oil, oil-in-water-in-silicone emulsions), creams, lotions, solutions (both aqueous and water-alcohol), anhydrous bases (such as lipsticks and powders), gels, masks, scrubs, body creams, peels, and ointments. Variations and other structures will be apparent to those skilled in the art and are suitable for use in the present invention.
[0054] E. Additional ingredients
[0055] In addition to the ingredient combinations disclosed by the inventors, the composition may also contain additional ingredients such as cosmetic ingredients and pharmaceutical active ingredients. Non-limiting examples of such additional ingredients are described in the following subsections.
[0056] 1. Cosmetic ingredients
[0057] The CTFA International Dictionary and Handbook of Cosmetic Ingredients (2004 and 2008) describes a wide range of non-limiting cosmetic ingredients that can be used in the context of this invention. Examples of these ingredient categories include: fragrance agents (artificial and natural; e.g., gluconic acid, phenoxyethanol, and triethanolamine), dyes and coloring agents (e.g., Blue 1, Blue 1 Lake, Red 40, titanium dioxide, D&C blue no. 4, D&C green no. 5, D&C orange no. 4, D&C red no. 17, D&C red no. 33, D&C violet no. 2, D&C yellow no. 10, and D&C yellow no. 11), flavorings / fragrances (e.g., stevia). Rebaudiana extract and menthol, adsorbents, lubricants, solvents, humectants (including, for example, emollients, humectants, film-forming agents, occlusive agents, and agents that affect the skin's natural moisturizing mechanisms), waterproofing agents, UV absorbers (physical and chemical absorbers such as para-aminobenzoic acid (“PABA”) and corresponding PABA derivatives, titanium dioxide, zinc oxide, etc.), essential oils, vitamins (e.g., A, B, C, D, E, and K), trace metals (e.g., zinc, calcium, and selenium), anti-irritants (e.g., steroids and nonsteroidal anti-inflammatory drugs), plant extracts (e.g., Aloe vera, chamomile, cucumber extract, ginkgo biloba extract), and other plant extracts. Biloba, ginseng, and rosemary; antimicrobial agents; antioxidants (e.g., BHT and tocopherol); chelating agents (e.g., disodium EDTA and tetrasodium EDTA); preservatives (e.g., methylparaben and propylparaben); pH adjusters (e.g., sodium hydroxide and citric acid); absorbents (e.g., aluminum octenyl succinate, kaolin, corn starch, oat starch, cyclodextrin, talc, and zeolite); skin bleaching and brightening agents (e.g., hydroquinone and nicotinamide lactate). ), humectants (e.g., sorbitol, urea, methyl gluceth-20, saccharide isomers, and mannitol), exfoliants, waterproofing agents (e.g., magnesium stearate / aluminum hydroxide), skin conditioning agents (e.g., aloe vera extract, allantoin, bisabolol, ceramides, dimethicone, hyaluronic acid, biosaccharide gum-1, ethylhexylglycerin, pentyl glycol, hydrogenated polydecene, octyl dodecyl oleate, and dipotassium glycyrrhizate), and additional ingredients (iron oxides, aluminum hydroxide, and disodium stearoyl glutamate). Non-limiting examples of some of these ingredients are provided in the following subsections.
[0058] a. Ultraviolet absorbers and / or reflectors
[0059] Ultraviolet absorbing and / or reflecting agents that can be used in combination with the compositions of the present invention include chemical and physical sunscreens. Non-limiting examples of usable chemical sunscreens include para-aminobenzoic acid (PABA), PABA esters (glyceryl PABA, pentyl dimethyl PABA, and octyl dimethyl PABA), butyl PABA, ethyl PABA, ethyl dihydroxypropyl PABA, benzophenones (hydroxybenzophenone, sulfonisobenzophenone, benzophenone, and benzophenone-1 to 12), cinnamates (octinoxate, isoamyl p-methoxycinnamate, octyl methoxycinnamate, sinoxamate, diisopropyl methyl cinnamate, DEA-methoxycinnamate, diisopropyl ethyl cinnamate, glyceryl octate dimethoxycinnamate, and ethyl methoxycinnamate), cinnamates, and salicylates (homomethyl salicylate, benzyl salicylate, ethylene glycol salicylate, isopropyl salicylate). (e.g., benzoylbenzyl esters, anthranilates, ethyl urethane, homolyl esters, octyl salicylate, dibenzoylmethane derivatives (e.g., avobenzone), octocrylene, octyl triazine, digallate trioleate, glyceryl aminobenzoate, 2-hydroxy-1,4-naphthoquinone and dihydroxyacetone, ethylhexyl triazine, dioctylbutamidotriazine, benzyl malonic acid polysiloxane, terephthalimide dicamphor sulfonic acid, disodium phenyl dibenzimidazole tetrasulfonate, diethylaminohydroxybenzoyl benzoate, bis(diethylaminohydroxybenzoyl)benzoate, bis(benzoxazolyl)phenylethylhexyliminotriazine, cresoltrazol trisiloxane, methylene bis(benzotriazolyl)tetramethylbutylphenol and bis(ethylhexyloxyphenol)methoxyphenyltriazine, 4-methylbenzylidene camphor and 4-methoxycinnamate isoamyl ester. Non-limiting examples of physical sunscreens include kaolin, talc, petrolatum, and metal oxides (e.g., titanium dioxide and zinc oxide).
[0060] b. Moisturizer
[0061] Non-limiting examples of moisturizers that can be used with the compositions of the present invention include amino acids, chondroitin sulfate, diglycerides, erythritol, fructose, glucose, glycerin, glycerol polymers, ethylene glycol, 1,2,6-hexanetriol, honey, hyaluronic acid, hydrogenated honey, hydrogenated starch hydrolysate, inositol, lactitol, maltitol, maltose, mannitol, natural moisturizing factors, PEG-15 butylene glycol, polyglyceryl sorbitol, pyrrolidone carboxylate, potassium PCA, propylene glycol, saccharide isomers, sodium glucuronate, sodium PCA, sorbitol, sucrose, trehalose, urea, and xylitol.
[0062] Other examples include acetylated lanolin, acetylated lanolin alcohol, alanine, algae extract, Aloe barbadensis, Aloe barbadensis extract, Aloe barbadensis gel, Althea officinalis extract, Prunus armeniaca kernel oil, arginine, arginine aspartate, Arnica montana extract, aspartic acid, Persea gratissima oil, barrier sphingolipids, butanol, beeswax, behenol, β-sitosterol, Betula alba bark extract, Borago officinalis extract, Ruscus aculeatus extract, butylene glycol, Calendula officinalis extract, calendula oil, and Euphorbia milii. Cerifera wax, canola oil, caprylic / capric triglycerides, cardamom (Elettaria cardamomum) oil, cocoa cerifera wax, carrot (Daucus carota sativa) oil, castor (Ricinus communis) oil, ceramides, pure ceramides, cetearyl alcohol polyether-5, cetearyl alcohol polyether-12, cetearyl alcohol polyether-20, caprylic cetearyl alcohol ester, cetearyl alcohol polyether-20, cetearyl alcohol polyether-24, cetyl acetate, caprylic cetyl ester, cetyl palmitate, chamomile (Anthemis nobilis) oil, cholesterol, cholesterol esters, cholesterol hydroxystearate, citric acid, salvia sclarea oil, cocoa (Theobroma cacao) butter, cocoa-caprylate / capric ester, coconut (Cocos nucifera) oil, collagen, collagen amino acids, corn (Zea Mays oil, fatty acids, decyl oleate, polydimethylsiloxane copolyol, polydimethylsiloxane alcohol, dioctyl adipate, dioctyl succinate, dipentaerythritol hexacaprylate / hexacaprylate, DNA, erythritol, ethoxydiethylene glycol, ethyl linoleate, Eucalyptus globulus oil, Oenothera biennis oil, fatty acids, Geranium maculatum oil, glucosamine, glucosamine glutamate / salt, glutamic acid, glyceryl polyether-26, glycerol, glyceryl, glyceryl distearate, glyceryl hydroxystearate, glyceryl laurate, glyceryl linoleate, glyceryl myristate, glyceryl oleate, glyceryl stearate, glyceryl stearate SE, glycine, ethylene glycol stearate SE, glycosaminoglycans, grape seed oil, hazelnut (Corylus)Americana oil, hazelnut (Corylus avellana) oil, hexanediol, hyaluronic acid, hybrid safflower (Carthamus tinctorius) oil, hydrogenated castor oil, hydrogenated coconut oil, hydrogenated lanolin, hydrogenated lecithin, hydrogenated palm oil, hydrogenated palm kernel oil, hydrogenated soybean oil, hydrogenated tallow oil, hydrogenated vegetable oil, hydrolyzed collagen, hydrolyzed elastin, hydrolyzed glycosaminoglycans, hydrolyzed keratin, hydrolyzed soybean protein, hydroxylated lanolin, hydroxyproline, isocetyl stearate, isocetyl stearyl stearate, isodecanyl oleate, isopropyl isostearate, isopropyl lanolinate, isopropyl myristate, isopropyl palmitate, isopropyl stearate, isostearamide DEA, isostearic acid, isostearyl lactate, isostearyl neopentanoate, jasmine (Jasminum) Officinale oil, jojoba (Buxus chinensis) oil, kelp, kukui (Aleurites moluccana) nut oil, lactamide MEA, lanolin alcohol polyether-16, lanolin alcohol polyether-10 acetate, lanolin, lanolin acid, lanolin alcohol, lanolin oil, lanolin wax, lavender (Lavandula angustifolia) oil, lecithin, lemon (Citrus medica limonum) oil, linoleic acid, linolenic acid, macadamia ternifolia oil, maltitol, chamomile (Chamomilla) Recutita oil, methyl glucosesquistearate, methylsilanol PCA, mineral oil, mink oil, *Morchella esculenta* oil, myristyl lactate, myristyl myristate, myristyl propionate, neopentyl glycol dicaprylate / dicaprylate, octyl dodecyl alcohol, octyl dodecyl myristate, octyl stearate, octyl hydroxystearate, octyl palmitate, octyl salicylate, octyl stearate, oleic acid, olive oil, sweet orange oil, palm oil, palmitic acid, panthenyl thioethylamine, panthenol, panthenol ethyl ether, paraffin wax, PCA, peach kernel oil, peanut oil, PEG-8C12-18 ester, PEG-15 cocoamine, PEG-150 distearate, PEG-60 glyceryl isostearate, PEG-5 glyceryl stearate, PEG-30 glyceryl stearate, PEG-7 hydrogenated castor oil, PEG-40 hydrogenated castor oil, PEG-60 hydrogenated castor oil, PEG-20 methylglucose sesquistearate, PEG-40 sorbitan peroleate, PEG-5 soybean sterol, PEG-10 soybean sterol, PEG-2 stearate, PEG-8 stearate, PEG-20 stearate, PEG-32 stearate, PEG-40 stearate, PEG-50 stearate, PEG-100 stearate, PEG-150 stearate, pentadecyl lactone, Menthol (Mentha) Piperrita oil, petrolatum, phospholipids, plankton extract, polyaminosaccharide condensate, polyglycerol-3 diisostearate, polyquaternium-24, polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80, polysorbate 85, potassium myristate, potassium palmitate, propylene glycol, propylene glycol dicaprylate / dicaprylate, propylene glycol dicaprylate, propylene glycol dinonanoate, propylene glycol laurate, propylene glycol stearate, propylene glycol stearate SE, PVP, pyridoxine dipalmitate, retinol, retinol palmitate, rice bran oil, RNA, rosemary oil, rose oil, safflower oil, sage oil, sandalwood oil, serine, serum albumin, sesame oil. Indicum oil, Shea butter (Butyrospermum parkii), silk powder, chondroitin sulfate sodium, sodium hyaluronate, sodium lactate, sodium palmitate, sodium PCA, sodium polyglutamate, soluble collagen, sorbitan laurate, sorbitan oleate, sorbitan palmitate, sorbitan sesquioleate, sorbitan stearate, sorbitol, soybean (Glycinesoja) oil, sphingolipids, squalane, squalene, stearamide MEA-stearate, stearic acid, stearoxydimethylsiloxane, stearoxytrimethylsilane, stearyl alcohol, glycyrrhetinic acid stearyl alcohol ester, heptanoate stearyl alcohol ester, sunflower (Helianthus annuus) seed oil, sweet almond (Prunus amygdalus) Dulcis oil, synthetic beeswax, tocopherol, tocopheryl acetate, tocopheryl linoleate, trisine, tridecyl pentoate, tridecyl stearate, triethanolamine, tristearin, urea, vegetable oil, water, wax, wheat (Triticum vulgare) germ oil and ylang-ylang (Canangaodorata) oil.
[0063] c. Antioxidants
[0064] Non-limiting examples of antioxidants that can be used with the compositions of the present invention include acetylcysteine, ascorbic acid polypeptide, ascorbate dipalmitate, ascorbate methylsilanol pectate, ascorbate palmitate, ascorbate stearate, BHA, BHT, tert-butylhydroquinone, cysteine, cysteine HCl, dipentylhydroquinone, ditert-butylhydroquinone, diceryl thiodipropionate, dioleotocopherol methylsilanol, disodium ascorbate sulfate, distearate thiodipropionate, ditridecyl thiodipropionate, dodecyl gallate, isoascorbic acid, ascorbate ester, ethyl ferulic acid, ferulic acid, gallate ester, hydroquinone, isooctyl thioglycolate, kojic acid, magnesium ascorbate, magnesium ascorbate phosphate, methylsilanol ascorbate, and more. However, plant antioxidants such as green tea or grape seed extract, nordihydroguaiac acid, octyl gallate, phenylthioglycolic acid, potassium ascorbate tocopheryl phosphate, potassium sulfite, propyl gallate, quinones, rosmarinic acid, sodium ascorbate, sodium bisulfite, sodium isoascorbate, sodium metabisulfite, sodium sulfite, superoxide dismutase, sodium thioglycolate, sorbitan furfural, thiodiethylene glycol, thiodiethylene glycolamide, thiodiethylene glycol acid, thioglycolic acid, thiolactic acid, thiosalicylic acid, tocopherol polyether-5, tocopherol polyether-10, tocopherol polyether-12, tocopherol polyether-18, tocopherol polyether-50, tocopherol, tococelen, tocopherol acetate, tocopherol linoleate, tocopherol nicotinate, tocopherol succinate, and tris(nonylphenyl) phosphite.
[0065] d. Structuring agents
[0066] In other non-limiting aspects, the compositions of the present invention may contain a structuring agent. In some aspects, the structuring agent helps to provide rheological properties to the composition to contribute to its stability. In other aspects, the structuring agent may also act as an emulsifier or a surfactant. Non-limiting examples of structuring agents include stearic acid, palmitic acid, stearyl alcohol, cetyl alcohol, behenyl alcohol, stearic acid, palmitic acid, stearyl alcohol polyethylene glycol ether having an average of about 1 to about 21 ethylene oxide units, cetyl alcohol polyethylene glycol ether having an average of about 1 to about 5 ethylene oxide units, and mixtures thereof.
[0067] e. Emulsifiers
[0068] In some aspects of the invention, the composition does not contain an emulsifier. However, in other aspects, the composition may contain one or more emulsifiers. Emulsifiers can reduce interfacial tension between phases and improve the formulation and stability of the emulsion. Emulsifiers may be nonionic, cationic, anionic, and zwitterionic emulsifiers (see U.S. Patent Nos. 5,011,681; 4,421,769; 3,755,560). Non-limiting examples include glycerides, propylene glycol esters, polyethylene glycol esters of fatty acids, sorbitan esters, dehydrated sorbitan anhydride esters, carboxylic acid copolymers, esters and ethers of glucose, ethoxylated ethers, ethoxylated alcohols, alkyl phosphates, polyoxyethylene fatty ether phosphates, fatty acid amides, acyl lactates, soaps, TEA stearate, DEA oleyl alcohol polyether-3 phosphate, polyethylene glycol 20 dehydrated sorbitan monolaurate (polysorbate 20), polyethylene glycol 5 soybean sterol, stearyl alcohol polyether-2, stearyl alcohol polyether-20, stearyl alcohol polyether-21, cetearyl alcohol polyether-20, cetearyl alcohol glucoside, cetearyl alcohol, C12-13 alkanol polyether-3, PPG-2 methyl glucoside, and more. Sugar ether distearate, PPG-5-cetyl polyether-20, bis-PEG / PPG-20 / 20 polydimethylsiloxane, cetyl polyether-10, polysorbate 80, cetyl phosphate, cetyl phosphate potassium, diethanolamine cetyl phosphate, polysorbate 60, glyceryl stearate, PEG-100 stearate, arachidonic acid, arachidonic acid glucoside, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, pentaerythritol tetra(bis-tert-butylhydroxyhydrocinnamic acid) ester, polyglycerol-4, diisostearate, polyhydroxystearate, sebacic acid ester, polydimethylsiloxane / PEG-10 / 15 crosspolymer, dipropylene glycol, sodium citrate, tocopherol, and mixtures thereof.
[0069] f. Silicone-containing compounds
[0070] In a non-limiting sense, silicone compounds include any member of the polymer product family whose molecular backbone consists of alternating silicon and oxygen atoms, with side groups attached to silicon atoms. Silicones can be synthesized into a variety of materials by varying the -Si-O- chain length, side groups, and crosslinking. These materials can vary in consistency from liquid to gel to solid.
[0071] Silicone-containing compounds that may be used in the context of this invention include those described herein or those known to those skilled in the art. Non-limiting examples include silicone oils (e.g., volatile and non-volatile oils), gels, and solids. In some aspects, silicone-containing compounds include silicone oils such as polyorganosiloxanes. Non-limiting examples of polyorganosiloxanes include polydimethylsiloxane, cyclodimethylsiloxane, polysiloxane-11, phenyltrimethylsiloxane, trimethylsiloxyamino-terminated polydimethylsiloxane, stearoxytrimethylsilane, or mixtures of these and other organosiloxane materials in any given proportion to achieve desired consistency and application characteristics according to the intended application (e.g., application to a specific area such as skin, hair, or eyes). "Volatile silicone oils" include silicone oils with low heat of vaporization, typically less than about 50 cal per gram of silicone oil. Non-limiting examples of volatile silicone oils include: cyclic polydimethylsiloxanes such as Dow Corning 344 Fluid, Dow Corning 345 Fluid, Dow Corning 244 Fluid, and Dow Corning 245 Fluid, Volatile Silicon 7207 (Union Carbide Corp., Danbury, Conn.); and low-viscosity polydimethylsiloxanes, i.e., polydimethylsiloxanes with a viscosity of about 50 cst or less (e.g., polydimethylsiloxanes such as Dow Corning 200-0.5 cst Fluid). Dow Corning Fluids are available from Dow Corning Corporation, Midland, Michigan. Cyclic polydimethylsiloxanes and polydimethylsiloxanes are described in the CTFA Dictionary of Cosmetic Ingredients, Third Edition (incorporated by reference), as mixtures of cyclic dimethyl polysiloxane compounds and fully methylated linear siloxane polymers terminated with trimethylsiloxane units, respectively. Other non-limiting volatile silicone oils that may be used in the context of this invention include those available from General Electric Co., Silicone Products Div., Waterford, NY, and SWS Silicones Div. of Stauffer Chemical Co., Adrian, Michigan.
[0072] g. Exfoliating agents
[0073] Exfoliating agents comprise components that remove dead skin cells from the outer surface of the skin. These agents can act mechanically, chemically, and / or otherwise. Non-limiting examples of mechanical exfoliating agents include abrasives such as pumice, silica, cloth, paper, shells, beads, solid crystals, solid polymers, etc. Non-limiting examples of chemical exfoliating agents include acidic and enzymatic exfoliating agents. Acids that can be used as exfoliating agents include, but are not limited to, glycolic acid, lactic acid, citric acid, α-hydroxy acids, β-hydroxy acids, etc. Other exfoliating agents known to those skilled in the art are also contemplated as useful in the context of this invention.
[0074] h. Essential oils
[0075] Essential oils comprise oils derived from herbs, flowers, trees, and other plants. These oils typically exist as tiny droplets between plant cells and can be extracted using several methods known to those skilled in the art (e.g., steam distillation, enfleurage, extraction by fat extraction, maceration, solvent extraction, or mechanical pressing). When these types of oils are exposed to air, they tend to evaporate (i.e., they are volatile oils). As a result, many essential oils are colorless, but they oxidize and darken over time. Essential oils are insoluble in water but soluble in alcohols, ethers, fixed oils (vegetarian), and other organic solvents. Typical physical properties found in essential oils include boiling points ranging from about 160°C to 240°C and densities ranging from about 0.759 to about 1.096.
[0076] Essential oils are usually named after the plant from which they are found. For example, rose oil or peppermint oil comes from the rose or peppermint plant, respectively. Non-limiting examples of essential oils that may be used in the context of this invention include sesame oil, macadamia oil, tea tree oil, evening primrose oil, Spanish sage oil, Spanish rosemary oil, coriander oil, thyme oil, pepper oil, rose oil, fennel oil, balsam oil, bergamot oil, rosewood oil, cedarwood oil, chamomile oil, sage oil, basil oil, clove leaf oil, cypress oil, eucalyptus oil, fennel oil, sea fennel oil, frankincense oil, geranium oil, ginger oil, grapefruit oil, jasmine oil, juniper oil, lavender oil, lemon oil, lemongrass oil, lime oil, orange oil, marjoram oil, myrrh oil, neroli oil, sweet orange oil, patchouli oil, pepper oil, black pepper oil, petitgrain oil, pine oil, Otto rose oil, rosemary oil, sandalwood oil, spearmint oil, spikenard oil, vetiver oil, wintergreen oil, or ylang-ylang oil. Other essential oils known to those skilled in the art are also contemplated as useful in the context of this invention.
[0077] i. Thickener
[0078] Thickeners, including thickeners or gelling agents, include substances that can increase the viscosity of a composition. Thickeners include those substances that can increase the viscosity of a composition without substantially altering the efficacy of the active ingredient within the composition. Thickeners can also increase the stability of the compositions of the present invention. In some aspects of the invention, thickeners include hydrogenated polyisobutylene, trihydroxystearin, ammonium acryloyldimethyl taurate / VP copolymer, or mixtures thereof.
[0079] Non-limiting examples of additional thickeners that may be used in the context of this invention include carboxylic acid polymers, crosslinked polyacrylate polymers, polyacrylamide polymers, polysaccharides, and gums. Examples of carboxylic acid polymers include crosslinked compounds comprising one or more monomers derived from acrylic acid, substituted acrylic acid, and salts and esters of such acrylic acid and substituted acrylic acid, wherein the crosslinking agent comprises two or more carbon-carbon double bonds and is derived from a polyol (see U.S. Patent Nos. 5,087,445; 4,509,949; 2,798,053; CTFA International Dictionary of Cosmetic Ingredients, 4th Edition, 1991, pp. 12 and 80). Examples of commercially available carboxylic acid polymers include carbomer, which is an acrylic homopolymer crosslinked with sucrose or pentaerythritol allyl ether (e.g., CARBOPOL from BF GOODRICH). TM 900 series).
[0080] Non-limiting examples of crosslinked polyacrylate polymers include cationic and nonionic polymers. Examples are described in U.S. Patent Nos. 5,100,660; 4,849,484; 4,835,206; 4,628,078; and 4,599,379.
[0081] Non-limiting examples of polyacrylamide polymers (including nonionic polyacrylamide polymers, including substituted branched or unbranched polymers) include polyacrylamide, isoparaffins and lauryl ether-7, acrylamide and substituted acrylamides with acrylic acid and substituted acrylic acid in multiblock copolymers.
[0082] Non-limiting examples of polysaccharides include cellulose, carboxymethyl hydroxyethyl cellulose, cellulose acetate propionate, hydroxyethyl cellulose, hydroxyethyl ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, methyl hydroxyethyl cellulose, microcrystalline cellulose, sodium cellulose sulfate, and mixtures thereof. Another example is alkyl-substituted cellulose, wherein the hydroxyl groups of the cellulose polymer are hydroxyalkylated (preferably hydroxyethylated or hydroxypropylated) to form hydroxyalkylated cellulose, and then further modified with C10-C30 straight-chain or branched alkyl groups via ether bonds. Typically, these polymers are ethers of C10-C30 straight-chain or branched alcohols with hydroxyalkyl cellulose. Other useful polysaccharides include linear sclerotiorum glucans containing (1-3) linked glucose units, with one (1-6) linked glucose unit for every three units.
[0083] Non-limiting examples of gums that can be used with the present invention include gum arabic, agar, alginic acid, alginate, ammonium alginate, amylopectin, calcium alginate, carrageenan calcium, carnitine, carrageenan, dextrin, gelatin, gellan gum, guar gum, guar hydroxypropyltrimethylammonium chloride, lithium montmorillonite, hyaluronic acid, hydrated silica, hydroxypropyl chitosan, hydroxypropyl guar gum, ark tarragon gum, kelp, locust bean gum, natto gum, potassium alginate, potassium carrageenan, propylene glycol alginate, sclerotinia gum, sodium carboxymethyl dextran, sodium carrageenan, tragacanth gum, xanthan gum, and mixtures thereof.
[0084] j. Preservatives
[0085] Non-limiting examples of preservatives that may be used in the context of this invention include quaternary ammonium preservatives such as polyquaternium-1 and benzalkonium chloride (e.g., benzalkonium chloride "BAC" and benzalkonium bromide), parabens (e.g., methylparaben and propylparaben), phenoxyethanol, octyl glycol, chlorophenoxyether, benzyl alcohol, chlorobutanol, phenol, sorbic acid, thimerosal, or combinations thereof.
[0086] k. Moisturizer
[0087] Useful emollients include the following: (a) silicone oils and their modifications, such as linear and cyclic polydimethylsiloxanes; amino, alkyl, alkylaryl and aryl silicone oils; (b) fats and oils, including natural fats and oils such as jojoba oil, soybean oil, sunflower oil, rice bran oil, avocado oil, almond oil, olive oil, sesame oil, peach kernel oil, castor oil, coconut oil, mink oil; cocoa butter; tallow, lard; hardened oils obtained by hydrogenation of the above oils; and synthetic mono-, di- and triglycerides such as glyceryl myristate and glyceryl 2-ethylhexanoate; (c) waxes such as carnauba wax, cetearyl wax, beeswax, lanolin and their derivatives; (d) hydrophobic plant extracts; e) Hydrocarbons such as liquid paraffin, petrolatum, microcrystalline wax, pure ceresin, squalene, pterostilbene, and mineral oil; (f) Higher fatty acids such as lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, linoleic acid, linolenic acid, lanolinic acid, isostearic acid, arachidonic acid, and polyunsaturated fatty acids (PUFAs); (g) Higher alcohols such as lauryl alcohol, cetyl alcohol, stearyl alcohol, oleyl alcohol, behenyl alcohol, cholesterol, and 2-hexyldecyl alcohol; (h) Esters such as cetyl caprylate, myristyl lactate, cetyl lactate, isopropyl myristate, myristyl myristate, isopropyl palmitate, isopropyl adipate, butyl stearate, decyl oleate, and cholic acid isostearate. Sterol esters, glyceryl monostearate, glyceryl distearate, glyceryl tristearate, alkyl lactate, alkyl citrate, and alkyl tartrate; (i) essential oils and their extracts such as peppermint, jasmine, camphor, white cedar, bitter orange peel, borneol, turpentine, cinnamon, bergamot, Satsuma mandarin, calamus, pine, lavender, bay leaf, clove, cypress, eucalyptus, lemon, starflower, thyme, peppermint, rose, sage, sesame, ginger, basil, juniper, lemongrass, rosemary, rosewood, avocado, grape, grape seed, myrrh, cucumber, watercress, calendula, elderberry flower, geranium, linden flower, amaranth, seaweed, ginkgo, ginseng, carrot, Guarana, tea tree, jojoba, comfrey, oat, cocoa, orange blossom, vanilla, green tea, peppermint oil, aloe vera, menthol, eucalyptol, eugenol, citral, citronellol, borneol, linalool, geraniol, evening primrose, camphor, thymol, spirulinol, pinene, limonene, and terpene oils; (j) lipids such as cholesterol, ceramides, sucrose esters, and pseudoceramides as described in European Patent Specification No. 556,957; (k) vitamins, minerals, and skin nutrients such as vitamins A, E, and K; vitamin alkyl esters, including vitamin C alkyl esters; magnesium, calcium, and emulsions; (l) sunscreens such as octyl methoxycinnamate (Parsol) (MCX) and butyl methoxydibenzoylmethane (Parsol 1789); (l) phospholipids; (m) polyols such as glycerol and propylene glycol; and polyols such as polyethylene glycol; (n) anti-aging compounds such as α-hydroxy acids and β-hydroxy acids; and (o) mixtures of any of the foregoing components, etc.
[0088] l. Tackifier
[0089] Examples of suitable tackifiers include, but are not limited to, aliphatic hydrocarbon resins, aromatic modified aliphatic hydrocarbon resins, hydrogenated polycyclopentadiene resins, polycyclopentadiene resins, rosin gum, rosin esters, wood rosin, wood rosin esters, tall oil rosin, tall oil rosin esters, polyterpenes, aromatic modified polyterpenes, terpene phenolic resins, aromatic modified hydrogenated polycyclopentadiene resins, hydrogenated aliphatic resins, hydrogenated aliphatic aromatic resins, hydrogenated terpenes and modified terpenes, hydrogenated rosin acid, hydrogenated rosin esters, polyisoprene, partially or fully hydrogenated polyisoprene, polybutadiene, partially or fully hydrogenated polybutadiene, etc. As demonstrated by some cited examples, tackifiers can be fully or partially hydrogenated. Tackifiers can also be nonpolar. (Non-polar means that the tackifier is substantially free of monomers having polar groups. Preferably, polar groups are absent; however, if they are present, preferably up to about 5% by weight, more preferably up to about 2% by weight, and even more preferably up to about 0.5% by weight.)
[0090] m. Coloring agent
[0091] The compositions of the present invention also comprise at least one cosmetically acceptable colorant, such as a pigment or dye. Examples of suitable pigments include, but are not limited to, inorganic pigments, organic pigments, lakes, pearlescent pigments, iridescent or optically variable pigments, and mixtures thereof. Pigment should be understood to mean inorganic or organic, white or colored particles. The pigment may optionally be surface treated within the scope of the present invention, but is not limited to treatments with silicones, perfluorinated compounds, lecithin, and amino acids.
[0092] n. surfactant
[0093] Surfactants that can be used as surfactant components in the compositions of the present invention include nonionic, anionic, cationic, and amphoteric (amphoionic) surfactants, and can be used in combination with each other.
[0094] o. pH adjuster
[0095] pH adjusters include inorganic and organic acids and bases, particularly ammonia, citric acid, phosphoric acid, acetic acid, sodium hydroxide, lactic acid, levulinic acid, glycolic acid, tartaric acid, malic acid, pyrrolidone carboxylic acid (PCA), succinic acid, citric acid, glutamic acid, 2-amino-2-methyl-1-propanol (AMP), and triethanolamine (TEA).
[0096] p. reducing agent
[0097] Suitable reducing agents include, but are not limited to, salts of thiourea, thiosulfates, sulfites, bisulfites, metabisulfites, borohydrides, and hypophosphites (such as sodium salts), ascorbic acid and its salts, esters, and derivatives (e.g., ascorbyl palmitate and ascorbyl polypeptide), and tocopherol and its salts, esters, and derivatives (e.g., tocopherol acetate). Other reducing agents are listed on pages 1655–56 of the INCI manual.
[0098] q. Spices
[0099] The compositions disclosed herein may optionally contain fragrances. Examples of possible fragrances include natural oils or naturally derived materials, as well as synthetic fragrances such as hydrocarbons, alcohols, aldehydes, ketones, esters, lactones, ethers, nitriles, and polyfunctional compounds. Non-limiting examples of natural oils include the following: basil (Ocimum basilicum) oil, laurel (Pimento acris) oil, lemon balm (Monardadidyma) oil, bergamot (Citrus aurantium bergamia) oil, cardamom (Elettaria cardamomum) oil, cedarwood (Cedrus atlantica) oil, chamomile (Anthemis nobilis) oil, cinnamon (Cinnamomum cassia) oil, lemongrass (Cymbopogon nardus) oil, sage (Salvia sclarea) oil, clove (Eugenia caryophyllus) oil, clove leaf (Eufenia caryophyllus) oil, sedge (Cyperus esculentus) oil, cypress (Cupressus sempervirens) oil, lemon eucalyptus (Eucalyptus citriodora) oil, and spotted geranium (Geranium) oil. maculatum oil, ginger oil, grapefruit oil, hazelnut oil, jasmine oil, juniper oil, juniper tar, pencil cypress oil, kiwifruit water, lavender oil, lavender angustifolia oil, lemon oil, lemongrass oil, lime oil, linden oil, linden water, orange oil. Nobilis oil, Myristica fragrans oil, Citrus aurantium dulcis flower oil, Citrus aurantium dulcis oil, Citrus aurantiumThe following are examples of synthetic fragrances: * **dulcis** water, *Pogostemon cablin* oil, *Menthepiperita* oil, *Menthe peperita* water, *Rosmarinus officinalis* oil, rose oil, *Rosa damascena* extract, *Rosa multiflora* extract, *Anibarosaeodora* extract, *Salvia officinalis* oil, sandalwood oil, *Santalum album* oil, *Menthe viridis* oil, tea tree (*Melaleuca alternifolia*) oil, and *Cananga odorata* oil. Some non-limiting examples of synthetic hydrocarbon fragrances include caryophyllene, β-farnesene, limonene, α-pinene, and β-pinene. Some non-limiting examples of synthetic alcohol fragrances include santalol, citronellol, linalool, phenethyl alcohol, and α-terpineol (R=H). Some non-limiting examples of synthetic aldehyde fragrances include 2-methylundecaldehyde, citral, hexylcinnamaldehyde, ifocitral, lily aldehyde, and 10-undecenal. Some non-limiting examples of synthetic ketone fragrances include cashmereone, α-ionone, ifocitral E, muscone, muscone, and tuna musk. Some non-limiting examples of synthetic ester fragrances include benzyl acetate, 4-tert-butylcyclohexyl acetate (cis and trans), cypress acetate, cyclognum acetate, isoborneol acetate, and α-terpinel acetate (R=acetyl). Some non-limiting examples of synthetic lactone fragrances include coumarin, jasmine lactone, muscone lactone, and peach aldehyde. Some non-limiting examples of synthetic ether fragrances include ambroxol, ansel, and galena musk. Some non-limiting examples of synthetic nitrile fragrances include cinnamonitrile and geraniol. Finally, some non-limiting examples of synthetic multifunctional fragrances include amyl salicylate, isoeugenol, methyl dihydrojasmonic acid, jasmine aldehyde, neolizard aldehyde, and vanillin.
[0100] r. foaming agent
[0101] Foaming agents include, for example, sodium lauryl sulfate, sodium lauroyl sarcosinate, sodium alkyl sulfosuccinate, sodium coconut oil fatty acid monoglyceride sulfonate, sodium α-olefin sulfonate, N-acyl amino acid salts such as N-acyl glutamate, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazoline betaine, maltitol fatty acid esters, sucrose fatty acid esters, polyglycerol fatty acid esters, fatty acid diethanolamide, polyoxyethylene sorbitan monostearate, polyoxyethylene hydrogenated castor oil, and polyoxyethylene fatty acid esters. These foaming agents can be used alone or in combination of two or more of them.
[0102] s. Tanning agent
[0103] Suitable tanning agents include, but are not limited to, α-hydroxy aldehydes and ketones, glyceraldehyde and related alcohols and aldehydes, various indoles, imidazoles and their derivatives, and various approved pigmenting agents. Other suitable tanning agents include, but are not limited to, methylglyoxal, glyceraldehyde, erythritol, allourea, 2,3-dihydroxysuccinaldehyde, 2,3-dimethoxysuccinaldehyde, 2-amino-3-hydroxysuccinaldehyde, and 2-benzylamino-3-hydroxysuccinaldehyde.
[0104] t. Astringent
[0105] Suitable astringents include, but are not limited to, aluminum citrate, aluminum lactate, birch extract, coffee extract, evening primrose extract, grape extract, frangipani extract, ivy extract, lemon extract, witch hazel extract, ammonium and potassium alum, aluminum triphosphate, aluminum glycinate and aluminum phenolsulfonate, allantoin chlorohydroxyaluminate, allantoin dihydroxyaluminate, aluminum stearate, aluminum sulfate and aluminum citrate, sodium aluminum phosphate, sodium alum, sodium chlorohydroxyaluminate aluminum, calcium lactate, calcium chloride, calcium sulfate hydrate, sodium aluminum lactate, zinc acetate, zinc chloride, zinc sulfate, zinc lactate, zinc zeolite, zinc phenolsulfonate, and combinations thereof. "Extract" means whole fruit, bean, and / or plant or selected components of such fruit, bean, and / or plant.
[0106] u. Preservatives
[0107] Suitable preservatives include, but are not limited to, methyl, ethyl, propyl, or butyl benzoic acid, phenoxyethanol, o-phenylphenol, dehydroacetic acid or its salts, p-cresol, m-cresol, o-chloro-m-xylenol, peppermint oil, echinacea, sansevieria, capsicum, tea tree oil, wild bergamot, clematis, nettle, laurel, myrrh, latani root, prickly ash, calendula, chamomile, mupirocin, neomycin sulfate, bacitracin, polymyxin B, l-ofloxacin, tetracyclines (chlortetracycline hydrochloride, oxytetracycline hydrochloride, and tetracycline hydrochloride), clindamycin phosphate, gentamicin sulfate, benzalkonium chloride, benzyl chloride, hexylresorcinol, methylbenzyl chloride, phenol, quaternary ammonium compounds, triclocarban, triclosan, and tea tree oil.
[0108] v. Deodorants and antiperspirants
[0109] Suitable antiperspirants and deodorants include, but are not limited to, zinc salts such as zinc sulfate and zinc chloride, glycine salts such as aluminum zirconium glycinate, hydrated aluminum chloride, tetrachlorohydroxyaluminum zirconium, zinc carbonate, o-phenylphenol, and quaternary ammonium compounds such as dimethylbenzylammonium chloride and hexamethylammonium chloride.
[0110] w. whitening agent
[0111] Examples of skin whitening agents include, but are not limited to, hydroquinone, kojic acid, licorice and / or its derivatives, ascorbic acid and / or its derivatives, arbutin, bearberry extract, licorice root extract and its derivatives, Chlorella vulgaris extract, perilla extract, coconut fruit extract and / or other depigmenting agents.
[0112] x. Antimicrobial agents
[0113] Examples of antimicrobial agents include, but are not limited to, triclosan, 3,4,4′-trichlorocarbazide (triclocarban); 3,4,4′-trifluoromethyl-4,4′-dichlorocarbazide (chlorofluorocarban); 5-chloro-2-methyl-4-isothiazolin-3-one; iodopropynyl butylcarbamate; 8-hydroxyquinoline; 8-hydroxyquinoline citrate; 8-hydroxyquinoline sulfate; 4-chloro-3,5-xylenol (chloroxylenol); 2-bromo-2-nitropropane-1,3-diol; diazolidinyl imidazourea; butoconazole; nystatin; teconazole; nitrofurantoin; phenacetin; acyclovir; clotrimazole; Chloroxylenol; chlorhexidine; miconazole; terconazole; butylparaben; ethylparaben; methylparaben; methylchloroisothiazolinone; methylisothiazolinone; a mixture of 1,3-bis(hydroxymethyl)-5,5-dimethylhydantoin and 3-iodo-2-propynylbutylcarbamate; hydroxyquinoline; EDTA; tetrasodium EDTA; p-hydroxybenzoate; alkylpyridinium compounds; cocophosphatidyl PG-dimethylammonium chloride; chlorhexidine gluconate; chlorhexidine disgluconate; chlorhexidine acetate; chlorhexidine hydroxyethyl sulfonate; chlorhexidine hydrochloride; benzalkonium chloride; benzyl chloride; polyhexamethylene biguanide; and mixtures thereof.
[0114] 2. Drug components
[0115] Pharmaceutical active agents are also intended for use with the compositions of the present invention. Non-limiting examples of pharmaceutical active agents include anti-acne agents, agents for treating rosacea, analgesics, anesthetics, anorectal agents, antihistamines, anti-inflammatory agents (including nonsteroidal anti-inflammatory drugs), antibiotics, antifungal agents, antiviral agents, antimicrobial agents, anticancer active agents, scabies mites, lice mites, antitumor agents, antiperspirants, antipruritics, antipsoriatic agents, antiseborrheic agents, bioactive proteins and peptides, burn treatment agents, cauterizing agents, bleaching agents, depilatory agents, diaper rash treatment agents, enzymes, hair growth stimulants, hair growth depressants (including DFMOs and their salts and analogues), hemostatic agents, keratolytic agents, oral ulcer treatment agents, cold sore treatment agents, dental and periodontal treatment agents, photosensitizing agents, skin protectants / barrier agents, steroids (including hormones and corticosteroids), sunburn treatment agents, sunscreens, transdermal active agents, nasal active agents, vaginal active agents, wart treatment agents, wound treatment agents, wound healing agents, etc.
[0116] F. Reagent kit
[0117] In certain aspects of this invention, kits are also contemplated for use. For example, the compositions of this invention may be included in a kit. The kit may comprise a container. Containers may include bottles, metal tubes, laminated tubes, plastic tubes, dispensers, pressurized containers, barrier containers, packaging, compartments, lipstick containers, powder compact containers, cosmetic trays for containing cosmetic compositions, or other types of containers such as injection-molded or blow-molded plastic containers, wherein a dispersion or composition or desired bottle, dispenser, or packaging is retained. The kit and / or container may include markings on its surface. For example, markings may be words, phrases, abbreviations, pictures, or symbols.
[0118] The container dispenses a predetermined amount of the composition. In other embodiments, the container may be squeezed (e.g., a metal, laminated, or plastic tube) to dispense the desired amount of the composition. The composition may be dispensed as a spray, aerosol, liquid, fluid, or semi-solid form. The container may have a spray, pump, or squeezing mechanism. The kit may also include instructions for using the kit components and any other compositions contained in the container. The instructions may include explanations of how to apply, use, and maintain the composition. Example
[0119] The following embodiments are included to illustrate preferred embodiments of the invention. Those skilled in the art will understand that the techniques disclosed in the following embodiments represent techniques that the inventors have found to work well in the practice of the invention and can therefore be considered to constitute preferred modes of practice. However, those skilled in the art, in view of this disclosure, will understand that many changes can be made to the specific embodiments disclosed, and similar or analogous results can still be obtained without departing from the spirit and scope of the invention.
[0120] All compositions and / or methods disclosed and claimed herein can be prepared and carried out without excessive experimentation, in view of this disclosure. While the compositions and methods of the invention have been described by way of preferred embodiments, it will be apparent to those skilled in the art that variations can be made to the compositions and / or methods, and the steps or sequence of steps of the methods described herein, without departing from the concept, spirit, and scope of the invention. More specifically, it will be apparent that certain chemically and physiologically relevant agents can be substituted for the agents described herein while achieving the same or similar results. All such similar substitutions and modifications that are apparent to those skilled in the art are considered to be within the spirit, scope, and concept of the invention as defined by the appended claims.
[0121] Example 1
[0122] (Exemplary formulation)
[0123] Formulations having the components from Example 1 were prepared as topical skin compositions. The formulations in Table 1 are examples of topical skin compositions prepared as water-in-oil emulsions.
[0124] Table 1*
[0125]
[0126] *The formulation can be prepared by mixing the components in a beaker at 70°C-75°C until homogeneous. The formulation can then be cooled to room temperature (20°C-25°C). Furthermore, additional components may be added if desired, for example, to modify the rheological properties of the composition.
[0127] **Excipients may be added, for example, to modify the rheological properties of the composition. Alternatively, the amount of water may vary, as long as the amount of water in the composition is at least 10% w / w, and preferably between 40% and 60% w / w.
[0128] Table 2*
[0129]
[0130] *The formulation can be prepared by mixing the components in a beaker at 70°C-75°C until homogeneous. The formulation can then be cooled to room temperature (20°C-25°C). Furthermore, additional components may be added if desired, for example, to modify the rheological properties of the composition.
[0131] **Excipients may be added, for example, to modify the rheological properties of the composition. Alternatively, the amount of water may vary, as long as the amount of water in the composition is at least 10% w / w, and preferably between 40% and 60% w / w.
[0132] Example 2
[0133] (Additional measurements)
[0134] The efficacy determination of any single ingredient or combination of ingredients disclosed in this specification and claims, or a composition having said ingredient combinations, can be determined by methods known to those skilled in the art. The following are non-limiting determinations that may be used in the context of this invention. It should be recognized that other testing procedures may be used, including, for example, objective and subjective procedures.
[0135] Sweat / Moisture Tolerance Assessment: Makeup integrity and appearance under sweat and moisture conditions are assessed using a defined procedure with the VISIA® CR device and expert ratings. First, a group of participants remain in a controlled environment (20°C ± 2°C, 50% ± 5% RH) for at least 30 minutes prior to assessment. Facial images, termed V1-baseline, are captured using the VISIA® CR device. This step focuses primarily on assessing sweat tolerance. Following the initial assessment, the formulation is uniformly applied to each participant's face by a technician, as detailed in the section. After allowing 15 minutes for product settling (V1-Timm), another round of clinical efficacy assessment and facial imaging is performed. Subsequently, participants are exposed to a warm chamber with controlled conditions (40°C ± 1°C, 35% ± 5% RH) for 25 ± 5 minutes, then returned to comfortable climatic conditions (20°C ± 2°C, 50% ± 5% RH) for 15 ± 5 minutes. Following exposure, further clinical efficacy assessments were performed and additional images were captured (V1–T1). During the second visit, the same participants underwent similar testing for moisture resistance; they were kept under controlled conditions prior to assessment, followed by administration of the formulation and exposure to a moisture chamber (24°C ± 2°C, 80% ± 5% RH) for 25 ± 5 minutes. Post-exposure assessment and imaging (V2-Timm, V2–T1) followed the same protocol as the first visit. Throughout both visits, trained technicians monitored for adverse events, drug use, and compliance with study restrictions. Clinical efficacy was assessed by expert ratings using a 5-point ordinal scale, focusing on attributes such as texture, fading, and color change under both sweat and moisture conditions. Each attribute was rated on the scale, with lower scores indicating better product performance relative to baseline after application, and higher scores indicating perceptible degradation or change. Color analysis using FrameScan® software compared formulation coverage before and after exposure to challenging conditions, while orthogonal polarization imaging accurately assessed formulation durability in less disturbed facial areas, such as the cheekbone region. All procedures ensured reproducibility of localization and image capture, supported by tools such as Mirror software with VISIA® CR. Statistical analyses, including the Wilcoxon Signed Rank test, were performed to assess differences across time points, ensuring rigorous evaluation of formulation performance under various environmental stresses.
[0136] B16 Pigmentation Assay: Melanogenesis is the process by which melanocytes produce melanin, a naturally occurring pigment that gives skin, hair, and eyes their color. Inhibiting melanin production is beneficial in preventing skin darkening and fading age-related dark spots. This bioassay utilizes B16-F1 melanocytes (ATCC), an immortalized mouse melanoma cell line, to analyze the effects of compounds on melanogenesis. The endpoint of this assay is a spectrophotometric measurement of melanin production and cell viability. B16-F1 melanocytes were cultured in standard DMEM growth medium containing 10% fetal bovine serum (MEDIATECH) at 37°C in 10% CO2, and then treated for 6 days with any of the active ingredients, combinations of ingredients, or compositions having said combinations disclosed in this specification. After incubation, melanin secretion was measured by absorbance at 405 nm, and cell viability was quantified.
[0137] Collagen Stimulation Assay: Collagen is an extracellular matrix protein essential for skin structure. Increased collagen synthesis contributes to improved skin firmness and elasticity. This bioassay can be used to examine the effect of any active ingredient, combination of ingredients, or composition having said combination disclosed in this specification on the production of procollagen peptides (precursors to collagen) by human epidermal fibroblasts. The endpoint of this assay is a spectrophotometric measurement reflecting the presence of procollagen peptides and cell viability. The assay employs a quantitative sandwich enzyme immunoassay technique, in which monoclonal antibodies specific to procollagen peptides are pre-coated onto microplates. Standards and samples can be transferred into the wells, and any present procollagen peptides are bound by the immobilized antibody. After washing away any unbound material, an enzyme-linked polyclonal antibody specific to procollagen peptides can be added to the wells. After washing to remove any unbound antibody-enzyme reagent, a substrate solution can be added to the wells, and color development is proportional to the amount of procollagen peptides bound in the initial step, detected using a microplate reader at 450 nm. It can stop color development and measure color intensity.
[0138] For the generation of samples and controls, sub-confluent normal adult epidermal fibroblasts (Cascade Biologics) cultured in standard DMEM growth medium containing 10% fetal bovine serum (MEDIATECH) at 37°C in 10% CO2 were treated for 3 days with each combination of components disclosed in this specification or a composition having said combinations. After incubation, the cell culture medium was collected, and the amount of pre-collagen peptide secretion was quantified using a sandwich enzyme-linked immunosorbent assay (ELISA) from TAKARA (#MK101).
[0139] Elastin stimulation assay: Elastin is a connective tissue protein that helps the skin regain its shape after stretching or contraction. Elastin is also an important load-bearing protein, used where mechanical energy needs to be stored. Elastin is produced by linking numerous soluble pro-elastin molecules in a reaction catalyzed by lysyl oxidase. Elastin secretion and elastin fibers can be monitored in cultured human fibroblasts by staining them with an immunofluorescent antibody targeting elastin.
[0140] Laminin and Fibronectin Stimulation Assay: Laminin and fibronectin are major proteins in the dermal-epidermal junction (DEJ), also known as the basement membrane. The DEJ lies between the dermis and epidermis, interlocking to form finger-like projections called reticular ridges. Epidermal cells receive their nutrients from blood vessels in the dermis. The reticular ridges increase the surface area of the epidermis exposed to these vessels and the necessary nutrients. The DEJ provides adhesion between the two tissue compartments and controls the structural integrity of the skin. Laminin and fibronectin are two structural glycoproteins located in the DEJ. Considered the glue that holds cells together, laminin and fibronectin are secreted by dermal fibroblasts to help promote intracellular and intercellular adhesion of epidermal cells to the DEJ. Laminin and fibronectin secretion can be monitored by quantitatively analyzing the levels of laminin and fibronectin in the cell supernatant of cultured human fibroblasts treated for 3 days with or without a medium containing 1.0% of the test component at a final concentration. Following incubation, the levels of laminin and fibronectin can be measured using an enzyme-linked immunosorbent assay (ELISA) with immunofluorescent antibodies against laminin and antibodies against fibronectin. Measurements are standardized to cellular metabolic activity, as determined by biotransformation with 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazonium (MTS).
[0141] Tumor Necrosis Factor α (TNF-α) Assay: TNF-α, the prototype ligand of the TNF superfamily, is a pleiotropic cytokine that plays a central role in inflammation. Increased expression of TNF-α is associated with upregulation of pro-inflammatory activity. This bioassay can be used to analyze the effect of any active ingredient, combination of ingredients, or composition having said combination disclosed in this specification on TNF-α production by human epidermal keratinocytes. The endpoint of this assay can be a spectrophotometric measurement reflecting the presence of TNF-α and cell viability. The assay employs a quantitative sandwich enzyme immunoassay technique, wherein a TNF-α-specific monoclonal antibody is pre-coated onto a microplate. Standards and samples are transferred into the wells, and any TNF-α present is bound by the immobilized antibody. After washing away any unbound material, an enzyme-linked polyclonal antibody specific to TNF-α is added to the wells. After washing to remove any unbound antibody-enzyme reagent, a substrate solution is added to the wells, and color development is proportional to the amount of TNF-α bound in the initial step, detected using a microplate reader at 450 nm. It can stop color development and measure color intensity. (In EPILIFE) TM Submerged normal adult keratinocytes cultured in standard growth medium (Cascade Biologics) at 37°C in 5% CO2 were treated for 6 hours with phorbol 12-myristate 13-acetate (PMA, 10 ng / ml, SIGMACHEMICAL, #P1585-1MG) and any active ingredient, combination of ingredients, or composition having said combination disclosed in this specification. PMA has been shown to induce a sharp increase in TNF-α secretion, which peaks at 6 hours post-treatment. After incubation, the cell culture medium was collected, and TNF-α secretion was quantified using a sandwich enzyme-linked immunosorbent assay (ELISA) from R&D Systems (#DTA00C).
[0142] Antioxidant (AO) Assay: An in vitro bioassay that measures the total antioxidant capacity of any one of the ingredients, combinations of ingredients, or compositions having said combinations disclosed in this specification. This assay relies on the ability of antioxidants in the sample to inhibit metmyoglobin from oxidizing ABTS® (2,2'-azono-di-[3-ethylbenzothiazoline sulfonate]) to ABTS®·+. The antioxidant system of organisms includes enzymes such as superoxide dismutase, catalase, and glutathione peroxidase; macromolecules such as albumin, ceruloplasmin, and ferritin; and a range of small molecules including ascorbic acid, α-tocopherol, β-carotene, reduced glutathione, uric acid, and bilirubin. The sum of endogenous and food-derived antioxidants represents the total antioxidant activity of the extracellular fluid. The synergistic effect of all the different antioxidants provides greater protection against attack by reactive oxygen or nitrogen free radicals than any single compound acting alone. Therefore, total antioxidant capacity may provide more relevant biological information than that obtained by measuring individual components, as it takes into account the cumulative effect of all antioxidants present in plasma and body fluids. The ability of antioxidants in a sample to prevent ABTS® oxidation is compared to Trolox (a water-soluble tocopherol analog) and quantified as molar Trolox equivalents. The Antioxidant Capacity Kit #709001 from CAYMAN CHEMICAL (Annaburg, Michigan, USA) is available as an in vitro bioassay to measure the total antioxidant capacity of each active ingredient, combination of ingredients, or composition having said combinations disclosed in this specification. The protocol should be followed as recommended by the manufacturer.
[0143] ORAC Assay: The oxygen radical absorption (or absorbance) capacity (ORAC) of any active ingredient, combination of ingredients, or composition having said combination disclosed in this specification can also be determined by measuring the antioxidant activity of such ingredients or compositions. Antioxidant activity indicates the ability to reduce oxidants. This assay quantifies the time and extent required to inhibit the action of oxidants, such as oxygen free radicals known to cause damage to cells, such as skin cells. The ORAC value of any active ingredient, combination of ingredients, or composition having said combination disclosed in this specification can be determined by methods known to those skilled in the art (see U.S. Publications 2004 / 0109905 and 2005 / 0163880; and commercially available kits such as the Zen-Bio ORAC Antioxidant Assay Kit (#AOX-2)). The Zen-Bio ORAC Antioxidant Assay Kit measures the loss of luciferin fluorescence over time due to the formation of peroxy radicals from the decomposition of AAPH (2,2'-azobis-2-methylpropanediamine dihydrochloride). Trolox, a water-soluble vitamin E analog, was used as a dose-dependent positive control to inhibit fluorescein decay.
[0144] Mushroom Tyrosinase Activity Assay: In mammalian cells, tyrosinase catalyzes two steps in the multi-step biosynthesis of melanin from tyrosine (and from dopa pigment polymerization). Tyrosinase is located in melanocytes and produces melanin (an aromatic quinone compound) that imparts color to skin, hair, and eyes. Purified mushroom tyrosinase (from SIGMA) can be incubated with its substrate L-DOPA (from FISHER) in the presence or absence of each active ingredient, any combination of ingredients, or a composition having said combinations disclosed in this specification. Pigment formation can be assessed by colorimetric plate readings at 490 nm. The percentage inhibition of mushroom tyrosinase activity can be calculated compared to an untreated control to determine the ability of the test ingredient or combination thereof to inhibit the activity of the purified enzyme. The inhibition of the test extract is compared with the inhibition of kojic acid (SIGMA).
[0145] Matrix metalloproteinase 3 and 9 enzyme activity (MMP3; MMP9) assay: An in vitro assay for matrix metalloproteinase (MMP) inhibition. MMPs are extracellular proteases that function in many normal and disease states due to their broad substrate specificity. MMP3 substrates include collagen, fibronectin, and laminin; while MMP9 substrates include collagen VII, fibronectin, and laminin. Using a colorimetric drug discovery kit for MMP3 (AK-400) and MMP-9 (AK-410) from BioMol International, this assay aims to measure the protease activity of MMPs using a thiopeptide as the chromogenic substrate (Ac-PLG-[2-mercapto-4-methyl-valeryl]-LG-OC2H5)5,6. The peptide bond at the MMP cleavage site is replaced by a thioester bond in the thiopeptide. MMP hydrolyzes this bond to produce a thiol group, which reacts with DTNB [5,5'-dithiobis(2-nitrobenzoic acid), Ellman's reagent] to form 2-nitro-5-thiobenzoic acid, which can be detected by absorbance at 412 nm (ε=13600 M). -1 cm -1 (At pH 6.0 and above 7). The active ingredients disclosed in this specification, any combination of ingredients, or compositions having said combinations can be determined.
[0146] Matrix Metalloproteinase 1 (MMP1) Activity Assay: An in vitro assay for MMP inhibition. MMPs are extracellular proteases that function in many normal and disease states due to their broad substrate specificity. MMP1 substrates include collagen IV. The MOLECULAR PROBES ENZ / CHEK Gelatinase / Collagenase Assay Kit (#E12055) utilizes a fluorescent gelatin substrate to detect MMP1 protease activity. A bright green fluorescence is observed during proteolytic cleavage, and enzyme activity can be measured using a fluorescent microplate reader.
[0147] The ENZ / CHEK Gelatinase / Collagenase Assay Kit (#E12055) from Invitrogen is designed as an in vitro assay to measure MMP1 enzyme activity. It can determine the active ingredients disclosed in this specification, any combination of ingredients, or compositions having said combinations. The assay relies on the ability of purified MMP1 enzyme to degrade fluorescent gelatin substrates. Once the substrate is specifically cleaved by MMP1, it exhibits bright green fluorescence, which can be monitored using a fluorescence microplate reader. Test materials are incubated in the presence or absence of purified enzyme and substrate to determine their protease inhibitory activity.
[0148] Cyclooxygenase (COX) Assay: An in vitro assay for the inhibition of cyclooxygenase-1 and cyclooxygenase-2 (COX-1, -2). COX is a bifunctional enzyme exhibiting both cyclooxygenase and peroxidase activities. Cyclooxygenase activity converts arachidonic acid to hydroperoxymonoperoxide (prostaglandin G2; PGG2), while the peroxidase component reduces the peroxidase (prostaglandin H2; PGH2) to the corresponding alcohols, namely precursors of prostaglandins, thromboxanes, and prostacyclin. This COX inhibitor screening assay measures the peroxidase component of cyclooxygenase. Peroxidase activity is colorimetrically determined by monitoring the presence of oxidized N,N,N',N'-tetramethyl-p-phenylenediamine (TMPD). This inhibitor screening assay includes both COX-1 and COX-2 enzymes to screen for isoenzyme-specific inhibitors. The colorimetric COX (sheep) inhibitor screening assay (#760111, CAYMANCHEMICAL) can be used to analyze the effect of each active ingredient, any combination of ingredients, or a combination of said ingredients disclosed in this specification on the activity of purified cyclooxygenase (COX-1 or COX-2). Following the manufacturer's instructions, the purified enzyme, heme, and test extract are mixed in the assay buffer and incubated with shaking at room temperature for 15 minutes. After incubation, arachidonic acid and the colorimetric substrate are added to initiate the reaction. Color progression can be assessed by reading the colorimetric plate at 590 nm. The percentage of inhibition of COX-1 or COX-2 activity can be calculated compared to an untreated control to determine the ability of the test extract to inhibit the activity of the purified enzyme.
[0149] Lipoxygenase (LO) Assay: An in vitro assay for lipoxygenase (LO) inhibition. LO is a non-heme iron-containing dioxygenase that catalyzes the addition of molecular oxygen to fatty acids. Linoleic acid and arachidonic acid are the main substrates of LO in plants and animals. Arachidonic acid can then be converted to hydroxyeicosatetrienoic acid (HETE) derivatives, which are subsequently converted to leukotrienes, potent inflammatory mediators. This assay provides an accurate and convenient method for screening lipoxygenase inhibitors by measuring the hydroperoxides produced when lipoxygenase (5-LO, 12-LO, or 15-LO) is incubated with arachidonic acid. The Colorimetric LO Inhibitor Screening Kit (#760700, CAYMAN CHEMICAL) can be used to determine the ability of each active ingredient, any combination of ingredients, or a combination of said combinations to inhibit enzyme activity as disclosed in this specification. The purified 15-lipoxygenase and the test ingredient can be mixed in assay buffer and incubated with shaking at room temperature for 10 minutes. After incubation, arachidonic acid can be added to initiate the reaction, and the mixture should be incubated at room temperature for another 10 minutes. A colorimetric substrate can be added to terminate the catalysis; color progress can be assessed by fluorescence plate readings at 490 nm. The percentage inhibition of lipoxygenase activity can be calculated compared to an untreated control to determine the ability of each active ingredient, any combination of ingredients, or composition having said combinations to inhibit the activity of the purified enzyme.
[0150] Elastase Assay: The ENZCHEK® Elastase Assay (Kit # E-12056) from MOLECULAR PROBES (Eugene, Oregon, USA) is available as an in vitro enzyme inhibition assay to measure the inhibition of elastase activity by each active ingredient, any combination of ingredients, or a combination of said ingredients disclosed in this specification. The ENZCHEK kit contains soluble bovine neck ligament elastin, which can be dye-labeled to quench the fluorescence of the conjugate. Non-fluorescent substrates can be digested with elastase or other proteases to produce highly fluorescent fragments. The resulting increase in fluorescence can be monitored using a fluorescence microplate reader. The digestion product from the elastin substrate exhibits maximum absorption at approximately 505 nm and maximum fluorescence emission at approximately 515 nm. When screening for elastase inhibitors using the ENZCHEK Elastase Assay Kit, the peptide N-methoxysuccinyl-Ala-Ala-Pro-Val-chloromethyl ketone can be used as a selective, bulk inhibitor of elastase.
[0151] Ceramide production: Ceramide in cell or tissue samples can be labeled with mouse monoclonal antibody anti-ceramide (ENZO LIFE SCIENCE, ref ALX-804-196 clone MID15B4) at a 1 / 50 dilution for 2 hours at room temperature using a biotin / streptoacidin amplifier system. Video microscopy can be performed to observe the ceramide (pink staining).
[0152] Oil control assay: The assay for measuring reduced sebum secretion and / or reduced sebum production by sebaceous glands can be performed using standard techniques known to those skilled in the art. In one example, the forehead can be used. Each active ingredient, any combination of ingredients, or composition having said combination disclosed in this specification may be applied once or twice daily to a portion of the forehead for a set number of days (e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, or more), while another portion of the forehead remains untreated with the composition. After the set number of days has elapsed, sebum secretion can then be measured by applying fine blotting paper to the treated and untreated forehead skin. This is done by first removing any sebum from the treated and untreated areas with a damp and then dry cloth. Blotting paper can then be applied to the treated and untreated areas of the forehead, and an elastic band can be placed around the forehead to gently press the blotting paper onto the skin. After 2 hours, the blotting paper can be removed, allowed to dry, and then transilluminated. Darker blotting paper is associated with more sebum production (or lighter blotting paper is associated with less sebum production).
[0153] Erythema Assay: Assays for measuring reduction in skin redness can be assessed using a MINOLTA colorimeter. Skin erythema can be induced by applying a 0.2% sodium lauryl sulfate solution to the subject's forearm. The area is protected with an occlusive patch for 24 hours. After 24 hours, the patch is removed, and the stimulation-induced redness can be assessed using the a* value of the MINOLTA colorimeter. The a* value measures the change in skin color within the red area. Immediately after reading, the area is treated with the active ingredient disclosed in this specification, any combination of ingredients, or a composition having said combination. Repeat measurements may be performed periodically to determine the formulation's ability to reduce redness and irritation.
[0154] Skin Moisture / Hydration Assay: The benefits of skin moisture / hydration can be measured using impedance measurements with a Nova Dermal Phase Meter. The impedance meter measures changes in skin moisture content. The outer layer of skin has unique electrical properties. When skin is dry, its conductivity is very poor. As it becomes more hydrated, its conductivity increases. Therefore, changes in skin impedance (related to conductivity) can be used to assess changes in skin hydration. The device can be calibrated according to the instrument instructions for each test day. Notes on temperature and relative humidity can also be recorded. Subjects can be assessed as follows: prior to measurement, they can equilibrate in a room with defined humidity (e.g., 30%–50%) and temperature (e.g., 68°C–72°C). Three individual impedance readings can be taken on each side of the face, recorded, and averaged. A T5 setting can be used on the impedance meter, averaging the impedance applied to the face every five seconds. Changes can be reported using statistical variance and significance. Each active ingredient disclosed in this specification, any combination of ingredients, or a composition having said combinations can be determined according to this procedure.
[0155] Skin clarity and reduction of freckles and age spots: Skin clarity and reduction of freckles and age spots can be assessed using a Minolta colorimeter. Skin color changes can be assessed to determine the likelihood of irritation due to product treatment using the a* value of the Minolta Chroma Meter. The a* value measures changes in skin color in the red area. This is used to determine whether each active ingredient, any combination of ingredients, or composition having said combinations disclosed in this specification is inducing irritation. Measurements can be performed on each side of the face and averaged as the left-right face value. Skin clarity can also be measured using the Minolta Meter. This measurement is a combination of the a*, b, and L values of the Minolta Meter, which are related to skin brightness and are correlated with skin smoothness and hydration. Skin readings are obtained as described above. In a non-limiting aspect, skin clarity can be described as L / C, where C is chromaticity and is defined as (a 2 +b 2 ) 1 / 2 .
[0156] Determination of skin dryness, fine lines, skin smoothness, and skin color: Skin dryness, fine lines, skin smoothness, and skin color can be assessed using clinical grading techniques. For example, the clinical grading of skin dryness can be determined using the five-point Kligman scale: (0) soft and moist skin; (1) normal appearance with no visible dryness; (2) slightly dry to the touch with no visible scaling; (3) dry, firm skin with a whitish appearance and some scaling; and (4) very dry, rough skin with a whitish appearance and scaling. Assessments can be performed independently by two clinicians and the average value taken.
[0157] Clinical grading of skin color: Clinical grading of skin color can be performed using a ten-point analogy scale: (10) Skin color is uniform, a uniform pinkish-brown. No dark spots, erythema, or scaly patches are visible when examined with a handheld magnifying glass. Skin texture is very uniform to the touch; (7) Uniform skin color is visible without magnification. No scaly areas, but slight discoloration due to pigmentation or erythema. No discoloration larger than 1 cm in diameter; (4) Skin discoloration and uneven texture are easily noticeable. Slight scaling. Some areas feel rough to the touch; and (1) Skin color and texture are uneven. Numerous scaling and discolored areas, whether hypopigmentation, erythema, or melanosis. Large areas of uneven color with a diameter greater than 1 cm. Assessments are performed independently by two clinicians and the average value is taken.
[0158] Clinical grading of skin smoothness: Clinical grading of skin smoothness can be analyzed using a ten-point analogy scale: (10) smooth, moist and shiny, with no resistance when a finger is rubbed across the surface; (7) slightly smooth, with slight resistance; (4) rough, with visible changes, and friction when rubbed; and (1) rough, flaky, and uneven surface. The assessment was performed independently by two clinicians and the average value was taken.
[0159] Assay for skin smoothness and wrinkle reduction using the method disclosed by Packman et al. (1978): Skin smoothness and wrinkle reduction can also be visually assessed using the method disclosed by Packman et al. (1978). For example, at each subject visit, the depth, shallowness, and total number of superficial facial lines (SFLs) for each subject can be carefully scored and recorded. Numerical scores are obtained by multiplying the quantity factor by the depth / width / length factor. Scores are obtained for the eye region and the mouth region (left and right sides) and summed together as the total wrinkle score.
[0160] Skin firmness measurement using a Hargens elastometer: Skin firmness can be measured using a Hargens elastometer, a device that assesses skin elasticity and firmness by dropping a small object onto the skin and recording its first two rebound peaks. The elastometer is a small, lightweight probe with a relatively blunt tip (4 square millimeters of contact area). The probe penetrates only slightly into the skin, causing the measurement results to depend on the properties of the outer layers of the skin, including the stratum corneum and epidermis, as well as some of the dermis.
[0161] Skin softness / flexibility determination using a gas bearing electric force gauge: Skin softness / flexibility can be assessed using a gas bearing electric force gauge, which measures the stress / strain properties of the skin. Skin viscoelasticity is related to skin hydration. Measurements are obtained by attaching the probe to the skin surface with double-sided tape at a predetermined location on the cheek area. A force of approximately 3.5 gm parallel to the skin surface can be applied, and skin displacement can be accurately measured. Skin flexibility can then be calculated and expressed as DSR (Dynamic Elasticity Coefficient, in gm / mm).
[0162] Appearance determination of fine lines and wrinkles using replicas: The appearance of fine lines and wrinkles on the skin can be assessed using replicas, which are impressions of the skin surface. Silicone rubber-like materials can be used. Replicas can be analyzed through image analysis. Changes in the visibility of fine lines and wrinkles can be objectively quantified by obtaining silicone replicas from the subject's face and analyzing the replica images using a computer image analysis system. Replicas can be obtained from the eye and neck areas and photographed using a digital camera with low-angle incident light. The digital images can be analyzed using image processing programs to determine the area of the replica covered by wrinkles or fine lines.
[0163] Skin surface profile determination using profilometer / stylus method: The surface profile of the skin can be measured using a profilometer / stylus method. This involves illuminating the surface of a replica with light or dragging a stylus across the surface of the replica. The vertical displacement of the stylus is fed into a computer via a distance sensor, and after scanning a replica of a fixed length, a cross-sectional analysis of the skin profile can be generated as a two-dimensional curve. This scan can be repeated any number of times along a fixed axis to generate a simulated 3-D image of the skin. Ten random cross-sections of the replica are obtained using the stylus technique and combined to generate an average value. Values of interest include Ra, which is the arithmetic mean of all roughness (height) values calculated by integrating the profile height relative to the average profile height. Rt is the maximum vertical distance between the highest and lowest peaks, and Rz is the average peak amplitude minus the average peak height. Values are given in mm as calibration values. The equipment should be standardized by scanning metal standards with known values before each use. The Ra value can be calculated using the following equation: R a = Standardized roughness; l m = Move (scan) length; and y = the absolute value of the position of the profile relative to the average profile height (x-axis).
[0164] MELANODERM TM Assay: In other non-limiting respects, the efficacy of each active ingredient, any combination of ingredients, or composition having said combinations disclosed in this specification may be assessed by using a dermal analogue, such as MELANODERM. TM Melanocytes are a type of cell found in skin analogues that stain positively when exposed to L-dihydroxyphenylalanine (L-DOPA), a precursor to melanin. Skin analogue MELANODERM TM Multiple matrices containing each of the active ingredients disclosed in this specification, any combination of ingredients, or a composition having said combinations may be used for treatment, or a single matrice may be used as a control. Alternatively, an untreated sample of a skin analog may be used as a control.
[0165] Polyfilament production: Changes in polyfilament production in keratinocytes can be measured due to each active ingredient disclosed in this specification, any combination of ingredients, or a composition having said combinations. Polyfilament is a precursor to natural moisturizing factor (NMF) in the skin. Increased NMF increases the skin's moisture content. Polyfilament production in treated and untreated keratinocytes can be determined using a bioassay analyzing polyfilament concentration in keratinocyte lysates. A non-limiting example of a bioassay that can be used to quantify polyfilament production is PROTEINSIMPLE® SIMON. TM Western blot protocol. For each sample, normal human epidermal keratinocytes (NHEK) were grown in calcium-containing EPI-200-MATTEK EPILIFE® growth medium from Life Technologies (M-EP-500-CA). NHEK was incubated overnight in growth medium at 37°C with 5% CO2 prior to treatment. NHEK was then incubated for 24 to 36 hours in growth medium containing 1% test compound / extract or without the compound / extract (negative control). NHEK was then washed, collected, and stored on ice or colder until lysis using lysis buffer and sonication on ice. Protein concentration in the sample can be determined and used for sample standardization. Lysates can be stored at -80°C until used for quantification.
[0166] PROTEINSIMPLE® SIMON TM Western blot bioassay employs quantitative Western blot immunoassay, using an antibody specific to fimbriae to quantitatively detect fimbriae in the test sample. Cell samples are lysed and protein concentrations are normalized. The normalized sample and molecular weight standards are then loaded, and capillary electrophoresis is performed on a denaturing protein separation gel. The proteins in the gel are immobilized and immunodetected using a fimbriae-specific primary antibody. Immobilized proteins can then be immunodetected using an enzyme-linked immunosorbent assay (ELISA) antibody bound to the primary antibody. A chemiluminescent substrate solution can then be added to the immobilized proteins to allow chemiluminescence development to be proportional to the amount of fimbriae bound in the immobilization. Chemiluminescence development is stopped at specific time points, and the intensity of the chemiluminescent signal can be measured and compared with positive and negative controls.
[0167] Closure protein production: Changes in closure protein production in keratinocytes can be measured due to each active ingredient disclosed in this specification, any combination of ingredients, or a composition having said combinations. Closure proteins are proteins essential for tight junction formation and the skin's moisture barrier function. A non-limiting example of how to determine closure protein production in treated and untreated keratinocytes is the use of a bioassay analyzing the concentration of closure proteins in keratinocyte lysates. This bioassay can be performed using PROTEINSIMPLE® SIMON. TM Western blotting was performed. For the sample, adult epidermal keratinocytes (HEKa) from Life Technologies (C-005-5C) were prepared using calcium-containing EPILIFE from Life Technologies (M-EP-500-CA). TM The growth medium was supplemented with keratinocyte growth supplement (HKGS) from Life Technologies (S-101-5), and the cells were grown at 37°C and 5% CO2 for 24 hours. HEKa was then incubated for 24 to 48 hours in growth medium containing the test compound / extract, without the compound / extract as a negative control, or containing 1 mM CaCl2 as a positive control. The HEKa was then washed, collected, and stored on ice or colder until lysis was performed on ice using lysis buffer and sonication. Protein concentration of the sample can be determined and used for sample standardization. Lysates were stored at -80°C until used for bioassays.
[0168] PROTEINSIMPLE® SIMON TM Western blot bioassay employs quantitative Western blot immunoassay, using antibodies specific to closure proteins to quantitatively detect closure proteins in test samples. Cell samples are lysed and protein concentrations are normalized. The normalized sample and molecular weight standards are then loaded, and capillary electrophoresis is performed on a denaturing protein separation gel. The proteins in the gel are then immobilized and immunodetected using a primary antibody specific to the closure protein. Immunodetection is performed on the immobilized proteins using an enzyme-linked immunosorbent assay (ELISA) antibody bound to the primary antibody. A chemiluminescent substrate solution is then added to the immobilized proteins to allow chemiluminescence development to be proportional to the amount of closure protein bound in the immobilization. Chemiluminescence development can be stopped at specific times, and the intensity of the chemiluminescent signal can be measured and compared with positive and negative controls.
[0169] Keratinocyte monolayer permeability: Changes in keratinocyte monolayer permeability caused by each active ingredient, any combination of ingredients, or a composition having said combinations disclosed in this specification can be measured. Keratinocyte monolayer permeability is a measure of skin barrier integrity. Keratinocyte monolayer permeability in treated and untreated keratinocytes can be determined using, as a non-limiting example, MILLIPORE's in vitro vascular permeability assay (ECM642). This assay analyzes endothelial cell adsorption, transport, and permeability. Briefly, adult epidermal keratinocytes from Life Technologies (C-005-5C) can be seeded onto a porous collagen-coated membrane within collection wells. The keratinocytes are then treated with calcium-containing EPILIFE from LIFE TECHNOLOGIES (M-EP-500-CA). TM The growth medium was supplemented with keratinocyte growth supplement (HKGS) from LIFE TECHNOLOGIES (S-101-5) and incubated at 37°C and 5% CO2 for 24 hours. This incubation time allowed cells to form a monolayer and close the membrane pores. The medium was then replaced with fresh medium containing (test sample) or not containing (untreated control) the test compound / extract, and the keratinocytes were incubated at 37°C and 5% CO2 for another 48 hours. To determine the permeability of the keratinocyte monolayer after incubation with / without the test compound / extract, the medium was replaced with fresh medium containing high molecular weight fluorescein isothiocyanate (FITC)-glucan, and the keratinocytes were incubated at 37°C and 5% CO2 for 4 hours. During the 4-hour incubation, FITC could cross the keratinocyte monolayer and porous membrane into the collection wells at a rate proportional to the monolayer permeability. After the 4-hour incubation, cell viability and the FITC content in the collection wells were determined. For FITC content, the culture medium in the collection wells was collected, and its fluorescence was determined at 480 nm (Em) when excited at 520 nm. The percentage of permeability and percentage of change compared to the untreated control can be determined by the following equations: Permeability percentage = [(mean Ex / Em of the test sample) / mean Ex / Em of the untreated control] * 100; Permeability percentage = Permeability percentage of the test sample – Permeability percentage of the untreated control.
[0170] Hyaluronic acid production: Changes in hyaluronic acid production in normal human dermal fibroblasts can be measured due to each active ingredient disclosed in this specification, any combination of ingredients, or a composition having said combinations. HA is a polysaccharide involved in matrix structural stability and providing turgor pressure to tissues and cells.
[0171] As a non-limiting example, HA production in treated and untreated adult dermal fibroblast (HDFa) cells can be determined using the Hyaluronic Acid DuoSet ELISA Kit from R&D Systems (DY3614). In this assay, for sample production, subconfluent HDFa cells from Cascade Biologics (C-13-5C) were incubated for 72 hours at 37°C and 10% CO2 in starvation medium (0.15% fetal bovine serum and 1% penicillin-streptomycin solution in Dulbecco's Modified Eagle Medium). Cells were then incubated for 24 hours with either the test compound, a positive control (phorbol 12-myristate 13-acetate from SIGMA-ALDRICH (P1585) and platelet-derived growth factor from SIGMA-ALDRICH (P3201)) or additive-free fresh starvation medium. The medium was then collected and frozen at -80°C until used for the ELISA assay.
[0172] In short, the ELISA assay employs a quantitative sandwich enzyme immunoassay technique, in which HA-specific capture antibodies are pre-coated onto a microplate. Standards and culture medium from treated and untreated cells are transferred into the wells of the microplate to allow any HA present to be bound by the immobilized antibody. After washing away any unbound material, HA-specific enzyme-linked detection antibodies are added to the wells. After washing to remove any unbound antibody-enzyme reagent, substrate solution is added to the wells to allow color development proportional to the amount of HA bound in the initial step. Color development is stopped at a specific time, and the color intensity at 450 nm can be measured using a microplate reader.
[0173] As another non-limiting example, human skin explants can be cultured at 37°C in viable explant medium under a humid atmosphere supplemented with 5% CO2. Treatment of the explants can be performed by topical application of the sample product (n = 3) on days D0, D2, D3, D6, D8, and D9. Control explants (n = 3) receive no treatment except for renewal of viable explant medium. Half the volume of viable medium can be renewed on days D3, D6, and D8. On D9, three explants from each condition can be taken and cut in half. One half of the explants is fixed in buffered formalin, and the other half is frozen at -80°C.
[0174] After fixing in plain Bouin for 48 hours and in formalin for 24 hours, the samples were dried and then immersed in paraffin using an automated tissue processor, Leica TP 1020. 5-micron sections were then cut using a microtome (Leica RM2125 Minotaur) and mounted on a SUPERFROST. TMOn histological slides. Microscopic observation can be performed using an optical microscope, such as a LEICA ORTHOPLAN or LEICA DM LB microscope. Images can be taken using an OLYMPUS DP72 camera and CELL^D software. General morphology can be examined on paraffin sections stained with Masson's trichrome Goldner variant. Hyaluronic acid staining can be performed with 1 / 100 dilution of anti-hyaluronic acid biotinylated protein (HABP) (SEIKAGAKU ref 400763-1A) at room temperature for 1 hour using a biotin / streptavidin amplifier system (VECTOR, VECTASTAIN PK-7200).
[0175] Inhibition of hyaluronidase activity: Changes in hyaluronidase activity caused by each active ingredient, any combination of ingredients, or a composition having said combinations disclosed in this specification can be measured. Hyaluronidase is an enzyme that degrades HA. HA is a polysaccharide involved in matrix structural stability and providing turgor pressure to tissues and cells. As a non-limiting example, hyaluronidase activity can be determined using an in vitro protocol modified from SIGMA-ALDRICH protocol # EC 3.2.1.35. Briefly, hyaluronidase type 1-S from SIGMA-ALDRICH (H3506) is added to microplate reaction wells containing the test compound or control. Tannins can be used as a positive control inhibitor, the control enzyme is not added to the test compound, and wells containing the test compound or positive control but not hyaluronidase can be used as background negative controls. The wells are incubated at 37°C for 10 minutes, and then the substrate (HA) is added. The substrate is added, and the reaction is incubated at 37°C for 45 minutes. A portion of each reaction solution was then transferred and gently mixed into a solution of sodium acetate and acetic acid at pH 3.75 to terminate that portion of the reaction (terminator well). After adding a portion of the reaction solution to the terminator well, the terminator well and the reaction well should contain the same volume of solution. Both the reaction well and the terminator well were incubated at room temperature for 10 minutes. The absorbance of both the reaction well and the terminator well at 600 nm was then measured. Inhibition can be calculated using the following formulas: Inhibitor (or control) activity = (Absorbance of inhibitor terminator well at 600 nm – Absorbance of inhibitor reaction well at 600 nm); Initial activity = Absorbance of control enzyme at 600 nm; Inhibition percentage = [(Initial activity / Inhibitor activity) * 100] - 100.
[0176] Peroxisome proliferator-activated receptor γ (PPAR-γ) activity: Changes in PPAR-γ activity caused by each active ingredient, any combination of ingredients, or a composition having said combinations disclosed in this specification can be measured. PPAR-γ is a receptor essential for sebum production. As a non-limiting example, PPAR-γ activity can be determined using a bioassay that analyzes the ability of a test compound or composition to inhibit ligand binding. In short, fluorescent small molecule pan-PPAR ligand, FLUORMONE. TM Pan-PPAR Green, available from Life Technologies (PV4894), is used to determine whether a test compound or composition can inhibit the binding of a ligand to PPAR-γ. Sample wells include PPAR-γ and the fluorescent ligand, and: the test compound or composition (test); the reference inhibitor rosiglitazone (positive control); or no test compound (negative control). The wells are incubated for a predetermined time to allow the ligand to bind to PPAR-γ. The fluorescence polarization of each sample well is then measured and compared to the negative control wells to determine the percentage of inhibition by the test compound or composition.
[0177] Cytokine array: Human epidermal keratinocytes were cultured to 70%-80% confluence. The culture medium was aspirated from the plate, and 0.025% trypsin / EDTA was added. When the cells became rounded, the culture dish was gently tapped to release the cells. The cells containing trypsin / EDTA were removed from the culture dish and neutralized. The cells were centrifuged at 180 xg for 5 minutes to form a cell pellet. The supernatant was aspirated. The resulting pellet was resuspended in EPILIFE. TM In Cascade Biologics culture medium, seed cells at approximately 10-20% confluence in 6-well plates. Once cells reach approximately 80% confluence, aspirate the culture medium and add 1.0 ml of EPILIFE to each of the two replicate wells. TM Together with phorbol 13-myristate 12-acetate (“PMA”) (a known inflammatory inducer) and test composition diluents (i.e., 1.0% (100 μl of 100X stock solution) and 0.1% (10 μl of 100X stock solution), the test composition was diluted to a final volume of 1 ml of EPILIFE. TM (In growth medium). Gently swirl the medium to ensure thorough mixing. Additionally, add 1.0 ml of EPILIFE to the control wells. TM The culture medium was prepared with and without additional PMA. The plates were then incubated at 37±1°C and 5.0±1% CO2 for approximately 5 hours after administration. After this 5-hour incubation, all culture media were collected in conical tubes and frozen at -70°C.
[0178] For analysis, 16-pad hybridization chambers were attached to three copies of a 16-pad FAST slide (WHATMAN BIOSCIENCES) containing three arrays of 16 anti-cytokine antibodies plus experimental controls, and the slides were placed in a FASTFrame (4 slides per frame). The arrays were blocked for 15 minutes at room temperature with 70 ml of S&S protein array blocking buffer (WHATMAN SCHLEICHER ANDSCHEULL). The blocking buffer was removed, and 70 ml of each supernatant sample was added to each array. The arrays were incubated with gentle agitation for 3 hours at room temperature. The arrays were washed three times with TBS-T. The arrays were then treated with 70 ml of an antibody mixture containing one biotinylated antibody corresponding to the capture antibody for each array. The arrays were incubated with gentle agitation for 1 hour at room temperature. The arrays were washed three times with TBS-T. The arrays were then incubated with 70 ml of a solution containing streptavidin-Cy5 conjugates with gentle agitation for 1 hour at room temperature. The arrays were washed three times with TBS-T, rapidly rinsed in deionized water, and dried.
[0179] The slides can be imaged using the PERKIN-ELMER SCANARRAY 4000 confocal fluorescence imaging system. Array images can be saved and analyzed using IMAGING RESEARCH ARRAYVISION software. In short, spot intensity is determined by subtracting the background signal. Spot replicates from each sample condition can be averaged and then compared with appropriate controls.
[0180] Endothelial tubule formation: Endothelial tubule formation involves angiogenesis and microvascular capillary formation. Capillary formation and angiogenesis can lead to skin redness and rosacea. The ability of endothelial cells to form tubes in the presence or absence of test extracts and compounds can be determined using a capillary disruption assay in a cell culture system with pre-formed primary human umbilical vein endothelial cells (HUVECs).
[0181] In short, HUVECs are cultured in vitro on an extracellular matrix that stimulates endothelial cell attachment and tubular morphogenesis to form capillary-like luminal structures. These in vitro-formed capillary tubes resemble human vascular capillaries in many ways. Capillary tube assays are based on this phenomenon and are used to evaluate potential vascular system targets.
[0182] HUVEC cultures were grown in a 5% CO2 incubator at 37°C. The complete growth medium for HUVECs was endothelial cell basal medium (EBM) supplemented with 2% fetal bovine serum (FBS), 12 μg / ml bovine brain extract, 1 μg / ml hydrocortisone, and 1 μg / ml GA-1000 (gentamicin-amphotericidal). All assays could be performed using HUVEC cultures between passage 3 and passage 8.
[0183] HUVECs were pre-labeled with the fluorescent reagent Calcein AM and seeded in extracellular matrix-coated 96-well culture plates using their full growth medium. Endothelial capillaries should form approximately four hours after the morphogenesis process. Then, 50 μl of the designed dose of the test reagent was applied to the formed capillary culture as a treatment condition. An untreated control could be added to the test reagent medium. SUTENT®, an FDA-approved anti-angiogenic drug, was included at one concentration as a performance control. Approximately six hours after treatment, the morphology of the endothelial tubules in each well was examined under a microscope, imaged, and the capillary-disrupting activity under the treatment condition could be quantitatively analyzed. Each test condition was performed in duplicate wells, including a control.
[0184] * * * * * * * * * * * * * *
[0185] All compositions and / or methods disclosed and claimed herein can be prepared and carried out without excessive experimentation, in view of this disclosure. While the compositions and methods of the invention have been described by way of preferred embodiments, it will be apparent to those skilled in the art that variations can be made to the compositions and / or methods, and the steps or sequence of steps of the methods described herein, without departing from the concept, spirit, and scope of the invention. More specifically, it will be apparent that certain chemically and physiologically relevant agents can be substituted for the agents described herein while achieving the same or similar results. All such similar substitutions and modifications that are apparent to those skilled in the art are considered to be within the spirit, scope, and concept of the invention as defined by the appended claims.
Claims
1. A method for protecting skin, the method comprising topically applying to human skin a composition free of decamethylcyclopentasiloxane (D5), the composition comprising: Black willow bark extract; Nicotinamide; and Octocrylin, The composition described herein does not contain D5.
2. The method of claim 1, wherein the D5-free composition comprises: Black willow bark extract, 0.0001% to 3% by weight; Nicotinamide, 0.01% to 5% by weight; and Octocrylene, 1% to 20% by weight.
3. The method of claim 1, wherein the D5-free composition further comprises polydimethylsiloxane.
4. The method of claim 3, wherein the D5-free composition comprises 2 to 20% by weight of polydimethylsiloxane.
5. The method of claim 1, wherein the D5-free composition further comprises: Magnesium sulfate; glycerin; Xanthan gum; Butylene glycol; Ascorbate glucoside; Octyl polymethylsiloxane; Butyl octyl salicylate; Ethylhexyl salicylate; and Silicon dioxide.
6. The method of claim 5, wherein the D5-free composition comprises: Magnesium sulfate, 0.01% to 3% by weight; 1% to 10% glycerin by weight; Xanthan gum, 0.01% to 3% by weight; 1% to 20% by weight of butanediol; 0.01% to 3% by weight of ascorbate glucoside; 1% to 10% by weight of octyl polymethylsiloxane; 1% to 15% by weight of butyl octyl salicylate; 1% to 15% by weight of ethylhexyl salicylate; and 0.01% to 3% by weight of silicon dioxide.
7. The method of claim 1, wherein the D5-free composition further comprises milk thistle fruit extract.
8. The method of claim 1, wherein the D5-free composition further comprises one or more additional ingredients selected from one or more colorants, chelating agents, surfactants, viscosity control agents, film-forming agents, humectants, foaming agents, pH adjusters, moisturizers, antioxidants, fragrances, skin conditioning agents, structuring agents, exfoliating agents, preservatives, and solvents.
9. The method of claim 1, wherein the D5-free composition is formulated as an emulsion, cream, lotion, oil, gel, water-in-oil emulsion, or ointment.
10. The method of claim 1, wherein the D5-free composition is formulated to be sweat-resistant and / or moisture-resistant.
11. The method of claim 1, wherein the D5-free composition protects the skin from ultraviolet (UV) radiation.
12. The method of claim 1, wherein the D5-free composition reduces the immune response in the skin triggered by heat exposure compared to the second composition, and the second composition is identical to the D5-free composition except that the second composition contains D5 and / or does not contain black willow bark extract, nicotinamide, and / or octocrylene.
13. A topical skin composition free of decamethylcyclopentasiloxane (D5), comprising: Black willow bark extract; Nicotinamide; and Octocrylin, The composition described herein does not contain D5.
14. The D5-free topical skin composition of claim 13, wherein the D5-free topical skin composition comprises: Black willow bark extract, 0.0001% to 3% by weight; Nicotinamide, 0.01% to 5% by weight; and Octocrylene, 1% to 20% by weight.
15. The D5-free topical skin composition of claim 13, wherein the D5-free topical skin composition further comprises polydimethylsiloxane.
16. The D5-free topical skin composition of claim 15, wherein the D5-free topical skin composition comprises 2% to 20% by weight of polydimethylsiloxane.
17. The D5-free topical skin composition of claim 14, wherein the D5-free topical skin composition further comprises: Magnesium sulfate; glycerin; Xanthan gum; Butylene glycol; Ascorbate glucoside; Octyl polymethylsiloxane; Butyl octyl salicylate; Ethylhexyl salicylate; and Silicon dioxide.
18. The D5-free topical skin composition of claim 13, wherein the D5-free topical skin composition comprises: Magnesium sulfate, 0.01% to 3% by weight; 1% to 10% glycerin by weight; Xanthan gum, 0.01% to 3% by weight; 1% to 20% by weight of butanediol; 0.01% to 3% by weight of ascorbate glucoside; 1% to 10% by weight of octyl polymethylsiloxane; 1% to 15% by weight of butyl octyl salicylate; 1% to 15% by weight of ethylhexyl salicylate; and 0.01% to 3% by weight of silicon dioxide.
19. The D5-free topical skin composition of claim 13, wherein the D5-free topical skin composition is formulated as an emulsion, cream, lotion, oil, gel, water-in-oil emulsion, or ointment, and further comprises one or more additional ingredients selected from one or more colorants, chelating agents, surfactants, viscosity control agents, film-forming agents, humectants, foaming agents, pH adjusters, moisturizers, antioxidants, fragrances, skin conditioning agents, structuring agents, exfoliating agents, preservatives, and solvents.
20. The D5-free topical skin composition of claim 13, wherein the D5-free topical skin composition further comprises milk thistle fruit extract.
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