Topical detergent composition based on ascorbyl glucoside and ascorbyl palmitate

Abstract

The present invention relates to a topical detergent composition comprising ascorbyl glucoside and ascorbyl palmitate, a matrix for washing and promoting transdermal absorption, said matrix comprising at least one nonionic surfactant, at least one anionic surfactant, and glycerol, in combination with suitable excipients and / or diluents.

Description

Technical Field

[0001] The present invention belongs to the technical field of external cleanser compositions and is based on ascorbyl glucoside and ascorbyl palmitate. Background Art

[0002] Skin aging is a complex process that includes various phenomena occurring in the dermal-epidermal region in response to endogenous and exogenous stimuli.

[0003] Specifically, at the epidermal level, sun exposure, long-term exposure to pollutants and allergens, dehydration of the intercorneal lipid matrix caused by aggressive detergents or impaired barrier lipid biosynthesis (atopic dermatitis, psoriasis, etc.), and chronic inflammatory states can accelerate skin aging and affect the integrity of the dermis. It is in the dermis, composed of connective tissue rich in collagen and elastic fibers and with an aqueous extracellular matrix, that the phenomena most closely associated with premature skin aging occur.

[0004] The scientific community is concerned about the following phenomena associated with skin aging: decreased connective tissue and extracellular matrix biosynthesis associated with mitochondrial damage (the "defective powerhouse model") [1]; fibroblast senescence with increased expression of genes for matrix-degrading enzymes [2]; telomere shortening [3]; and inadequate sun protection [4,5].

[0005] Various skin systemic approaches have been proposed in cosmetic medicine to reduce the progression of skin aging, including the use of cosmetics containing skin-nourishing and antioxidant substances (such as coenzyme Q10, ascorbic acid, ferulic acid, phloretin, various plant extracts rich in polyphenols, resveratrol, etc.). Among these substances, the one that has attracted the most attention and achieved great commercial success over the years is ascorbic acid (AA). Ascorbic acid is a lactone with acid function ( Figure 1 ), plays a key biological role in the aging of collagen fibers (procollagen) in the rough endoplasmic reticulum (RER) by activating lysine and proline hydroxylases (for which ascorbic acid is a cofactor) and by increasing the gene expression of new collagen synthases [6].

[0006] Ascorbic acid, derived from the vitamin C, is extracted from several citrus fruits and also synthesized. It is widely used in various concentrations in many successful cosmetic products and numerous food supplements. By this mechanism, ascorbic acid plays an important physiological role in maintaining the integrity of epithelial tissues, leading to the development of scurvy (impaired mucosal epithelial integrity, accompanied by gingival lesions and vascular endothelial damage) in individuals with a deficiency. This essential function, combined with its well-known antioxidant redox activity, has led to its widespread use in cosmetics and nutritional supplements.

[0007] Problems with existing technology

[0008] The first issue to be addressed is that, due to its antioxidant properties, ascorbic acid has poor stability in cosmetics and complex formulations, especially when aqueous solutions are involved or even just the presence of water in the formulation.

[0009] In fact, ascorbic acid can be oxidized by dissolved oxygen in water to form dehydroascorbic acid, which is no longer functional until it is rehydrogenated ( Figure 2 To solve the oxidation problem of this molecule, many ascorbic acid derivatives have been developed in recent years. Specifically, the most popular substances are enediol hydroxyphosphate derivatives: sodium ascorbyl phosphate and magnesium ascorbyl phosphate ( Figure 3 This chemical modification prevents the ascorbic acid radical from being oxidized by dehydrogenation, thus ensuring its high stability in the formulation.

[0010] On the other hand, this structural modification does not solve the problem of transdermal penetration. In fact, another factor limiting the use of ascorbic acid is its transdermal absorption, which is hindered by the high hydrophilicity of the compound. Pinnell et al. demonstrated that ascorbic acid can only effectively penetrate the skin when the concentration of ascorbic acid in the topical preparation is equal to or slightly higher than 20% and the pH is below 3.5 (generally lower than the pKA value of ascorbic acid, 4.2) [7]. At the same time, it is also true that under these conditions, it is very difficult to formulate a safe, non-sensitizing and cost-effective product. The ionized form of the molecule not only does not improve, but can paradoxically worsen the transfer of ascorbic acid into the epidermis and dermis, since this transfer physiologically involves diffusion through areas with a high lipid content (skin barrier, membrane phospholipid bilayer) [8,9].

[0011] Ascorbyl palmitate (AP), the ester of ascorbic acid and palmitic acid ( Figure 4 ), initially attracted attention due to its high lipophilicity, theoretically suitable for transdermal penetration. However, studies have shown that its ability to release ascorbic acid into the epidermis is low [8,9]. In addition, ascorbyl palmitate does not solve the problem of poor chemical stability [8,9]. Ascorbyl palmitate is used as an antioxidant and antiperoxidant (E 304) in the food, pharmaceutical, and cosmetic industries. Other ascorbic acid derivatives, such as ascorbyl isopalmitate and ascorbyl tetrapalmitate, have similar properties to the ascorbyl palmitate discussed above.

[0012] In general, other factors that increase the degradation rate of ascorbic acid include: high pH or temperature, the presence of dissolved oxygen, and catalytic amounts of metal ions.

[0013] Thus, although magnesium ascorbyl phosphate and ascorbyl palmitate are effective when taken orally, they are unable to increase tissue ascorbic acid levels when applied to the skin [7].

[0014] To reduce the degradation of ascorbic acid in topical formulations, various strategies have been employed, such as: reducing the amount of oxygen during the preparation process; using oxygen-impermeable packaging; designing technical encapsulation of ascorbic acid; low pH compositions; reducing water; and adding electrolytes and other antioxidants. In addition, skin treatments using techniques such as laser, microdermabrasion, or ultrasound transduction have been shown to significantly improve the release of topical vitamin C and its derivatives, which typically have poor dermal penetration [8].

[0015] Nevertheless, the stability of ascorbic acid remains a challenge, and some of these approaches may involve difficult and / or costly preparation.

[0016] Therefore, in view of the above considerations, it is necessary to design a topical composition that can, on the one hand, solve the oxidation problem of ascorbic acid in a topical form (preferably liquid or containing water); on the other hand, increase the transdermal permeability of ascorbic acid. Summary of the Invention

[0017] The applicant has developed an external cleaning composition comprising:

[0018] (i) ascorbyl glucoside and ascorbyl palmitate;

[0019] (ii) a matrix for washing and promoting percutaneous absorption, comprising:

[0020] - at least one nonionic surfactant;

[0021] - at least one anionic surfactant;

[0022] (iii) glycerol,

[0023] And combined with suitable excipients and / or diluents.

[0024] Advantages of the present invention

[0025] The topical cleanser composition of the present invention enhances the bioavailability of ascorbic acid by promoting the permeability of ascorbic acid precursors. This mechanism of promoting the permeability of such precursors operates simultaneously in multiple ways:

[0026] - Two active ingredients in the form of ascorbic acid precursors (i.e., ascorbyl glucoside ( Figure 5The combination of ascorbyl glucoside and ascorbyl palmitate promotes an increase in the bioavailability of ascorbic acid or ascorbate; specifically, the enediol hydroxyl group of ascorbyl glucoside is covalently bound to glucose, preventing oxidative dehydrogenation reactions; this stabilizes the molecule on the one hand and, on the other hand, promotes its penetration through the stratum corneum (SC) due to the lack of ionization. Ascorbyl glucoside is thus hydrolyzed in the epidermis by α-glucosidase

[10] , generating ascorbic acid in situ [11,12]. On the other hand, ascorbyl palmitate, due to its amphiphilic and surface-active properties (known in the literature

[13] ), can serve both as an auxiliary agent for the cleansing action described below and as a secondary source of ascorbic acid in the epidermis.

[0027] The cleansing matrix increases the permeability of ascorbic acid through the skin by altering the inter-cutaneous lipid structure and temporarily opening aqueous channels within the epidermis, without significantly altering the functionality of the stratum corneum (SC). Thus, the applicants have transformed the known "shortcomings" of traditional surfactants in their interactions with skin barrier components into a mechanism that promotes the transdermal passage of ascorbic acid precursors. Thus, in addition to its well-known cleansing effect on the skin surface, the cleansing action also promotes the transdermal penetration of ascorbyl glucoside, ensuring its good diffusivity and inherent chemical stability within the epidermis.

[0028] It should also be noted that excessive changes in skin barrier structure and functionality that may be induced by the washing matrix should be balanced by:

[0029] - Careful selection of the surfactants and their amounts in the composition to obtain a washing matrix that is mild or non-aggressive while facilitating the transdermal penetration of the ascorbic acid precursor;

[0030] - The glycerol that is necessarily present in the composition of the present invention forms hydrogen bonds with water, which reduces the thermodynamic activity of water and makes the washing matrix less reactive towards skin barrier components.

[0031] The topical cleanser composition can be effective without the need to use very high concentrations of ascorbic acid (e.g., close to or above 20%), nor without setting the pH of the composition to a value preferably ≤ 3.5 (below which the skin may be subject to irritation and alterations in barrier and immune function

[16] ).

[0032] Finally, although the topical cleanser composition is a rinse-off composition (as opposed to a leave-on composition such as a serum or lotion), i.e., it is applied and then rinsed off, it can effectively promote the absorption of ascorbic acid precursors, thereby increasing the bioavailability of ascorbic acid; this effect is particularly noteworthy considering that the composition, as a cleanser, does not require a dwell (or rest) time to function. BRIEF DESCRIPTION OF THE DRAWINGS

[0033] Figure 1 -L-ascorbic acid enediol-lactone structure;

[0034] Figure 2 -Redox reaction of L-ascorbic acid;

[0035] Figure 3 -Structure of sodium ascorbyl phosphate;

[0036] Figure 4 -Structure of ascorbyl palmitate;

[0037] Figure 5 -Structure of ascorbic acid 2-glucoside. DETAILED DESCRIPTION

[0038] Applicants describe the present invention and its advantages in more detail below.

[0039] External cleaning composition

[0040] An object of the present invention is to provide an external cleaning composition comprising:

[0041] (i) ascorbyl glucoside and ascorbyl palmitate;

[0042] (ii) a matrix for washing and promoting percutaneous absorption, comprising:

[0043] - at least one nonionic surfactant;

[0044] - at least one anionic surfactant;

[0045] (iii) glycerol,

[0046] And combined with suitable excipients and / or diluents.

[0047] It should be noted that the composition of the present invention is not in encapsulated form; preferably, the external cleanser composition is not in the form of an emulsion.

[0048] It should also be noted that the skin area to which the topical cleanser composition is applied need not be treated with techniques such as laser treatment, microdermabrasion, or ultrasound therapy before or after application.

[0049] Ascorbyl Glucoside and Ascorbyl Palmitate

[0050] Ascorbyl glucoside and ascorbyl palmitate are two active ingredients present in the external cleanser composition in the form of ascorbic acid precursors.

[0051] Preferably, the ascorbyl glucoside is present in an amount of about 0.01% to 12% by weight, preferably about 0.05% to 12%, preferably about 0.1% to 12%, preferably about 0.5% to 12%, preferably about 0.5% to 10%, preferably about 0.5% to 8%, preferably about 0.5% to 6%, preferably about 0.5% to 5%, preferably about 0.5% to 4%, preferably about 1% to 4%, preferably about 1%, 2%, 3% or 4% by weight of the total weight of the composition.

[0052] Preferably, the content of ascorbyl palmitate is from about 0.01% to 12% by weight, preferably from about 0.01% to 10%, preferably from about 0.01% to 5%, preferably from about 0.01% to 3%, preferably from about 0.05% to 3%, preferably from about 0.1% to 3%, preferably from about 0.2% to 3%, preferably from about 0.2% to 2%, preferably from about 0.2% to 1.5%, preferably from about 0.2% to 1%, preferably from about 0.2% to 0.7%, preferably from about 0.2% to 0.6%, preferably from about 0.4% to 0.6%, based on the total weight of the composition.

[0053] It should be noted that ascorbyl palmitate not only constitutes a source of ascorbic acid / ascorbate, but also enhances the cleaning action of the wash matrix.

[0054] Preferably, the ascorbyl glucoside and / or ascorbyl palmitate is not in encapsulated or vesicular form.

[0055] Preferably, the topical cleanser composition does not contain ascorbic acid itself or a phosphate derivative of ascorbic acid, such as sodium ascorbyl phosphate or magnesium ascorbyl phosphate.

[0056] Matrix that cleanses and promotes percutaneous absorption

[0057] The base for cleaning and promoting percutaneous absorption (or simply cleaning base) refers to a mixture of at least two surfactants of different chemical properties, which have a cleaning or cleansing effect on the skin surface and also have the effect of promoting percutaneous absorption of ascorbyl glucoside and / or ascorbyl palmitate.

[0058] Bases that cleanse and enhance transdermal absorption include:

[0059] - at least one nonionic surfactant;

[0060] - at least one anionic surfactant.

[0061] Preferably, the wash matrix comprises:

[0062] - at least two, preferably three, preferably four nonionic surfactants;

[0063] - at least one anionic surfactant, preferably 1 to 3 anionic surfactants.

[0064] According to another embodiment, which is preferred when the external cleanser composition is in liquid form, the washing matrix comprises:

[0065] - at least one nonionic surfactant, preferably 1 to 4;

[0066] - at least one anionic surfactant, preferably 1 to 3;

[0067] - At least one amphoteric surfactant, preferably one.

[0068] Preferably, whether the external cleanser composition is formulated in liquid or solid form, the washing matrix does not contain any cationic surfactants.

[0069] The level of cleaning substrate is preferably from about 10% to 60% by weight of the total composition, preferably from about 20% to 60%, preferably from about 30% to 60%, preferably from about 35% to 60%.

[0070] When the detergent composition is in solid form, the content of the washing matrix is ​​preferably from about 35% to 60% by weight of the total weight of the composition, preferably from about 40% to 60%, preferably from about 50% to 60%, preferably from about 55% to 60%, preferably from about 57% to 60%, preferably about 58%, 59% or 59.5%.

[0071] When the cleaning composition is in liquid form, the content of the cleaning matrix is ​​preferably from about 35% to 50% by weight, preferably from about 35% to 45% by weight, preferably about 36%, 37%, 38%, 39%, 40%, 41%, 42% or 43% by weight of the total weight of the composition.

[0072] Preferably, the nonionic surfactant is chosen from the group consisting of (expressed by the corresponding INCI names): Decyl Polyglucose, Lauryl Polyglucose, Decyl Glucoside, Coco Glucoside, Lauryl Glucoside, Capryl / Capryl Glucoside, Polyglyceryl-3 Cocoate, Polyglyceryl-6 Caprylate, Polyglyceryl-4 Caprate, Polyglyceryl-6 Ricinoleate, Polysorbate-20, Polysorbate-80, PEG-7 Glyceryl Cocoate and mixtures thereof.

[0073] Preferably, the ionic surfactant is selected from the group consisting of (represented by the corresponding INCI names): disodium laureth sulfosuccinate, disodium ricinoleamide MEA sulfosuccinate, sodium cocoyl glutamate, disodium cocoyl glutamate, sodium lauroyl glutamate, sodium methyl cocoyl taurate, sodium cocoyl isethionate, sodium cocoyl sarcosinate, potassium cocoyl hydrolyzed collagen, sodium cocoyl hydrolyzed wheat protein, sodium lauroyl sulfoacetate, sodium cocoyl polyglucose citrate, sodium cocoyl glucoside tartrate, oliveoyl fructoside, oliveoyl glutamic acid, and mixtures thereof.

[0074] Preferably, the amphoteric surfactant is chosen from the group consisting of (expressed by the corresponding INCI names): cocamidopropyl betaine, lauramidopropyl betaine, disodium cocoamphodiacetate, sodium cocoamphoacetate, sodium lauroamphoacetate, sodium oliveamphoacetate and mixtures thereof.

[0075] Preferably, the weight ratio of ascorbyl glucoside to washing matrix is ​​from 1:10 to 1:70, preferably from 1:10 to 1:65, preferably from 1:10 to 1:60, preferably from 1:12 to 1:60, preferably from 1:12 to about 1:59.5, preferably from 1:12 to 1:50, preferably from 1:12 to 1:40, preferably from 1:12 to 1:30, preferably from 1:12 to 1:25, preferably from 1:12 to 1:22, preferably from 1:12 to 1:21.5.

[0076] Preferably, applicants believe that such a weight ratio is effective to achieve penetration of ascorbic acid while minimizing changes in the lipid-protein structure of the stratum corneum.

[0077] glycerin

[0078] Preferably, the content of glycerol is about 1% to 10% by weight of the total weight of the composition, preferably about 1% to 8%, preferably about 1% to 7%, preferably about 2% to 7%, preferably about 3% to 6%, preferably about 3%, 4%, 6%.

[0079] It should be noted that glycerin acts as a humectant, preventing skin from becoming dehydrated.

[0080] Suitable excipients and / or diluents

[0081] The external cleanser composition includes suitable excipients and / or diluents; these excipients and / or diluents are substances known to those skilled in the art for preparing external cleanser compositions in liquid or solid form.

[0082] For example, the excipients and / or diluents may be selected from the group consisting of (expressed by the corresponding INCI names): gelling agents, pH adjusting agents, antifoaming agents, conditioning agents, preservatives, fragrances, coloring agents.

[0083] An example of a gelling agent is preferably selected from the group consisting of (represented by the corresponding INCI names): carbomer, hydroxyethylcellulose, xanthan gum, PEG-120 methyl glucose dioleate and mixtures thereof.

[0084] An example of a pH adjusting agent is preferably selected from the group consisting of (expressed by the corresponding INCI names): citric acid, ethanolamine, triethanolamine, L-arginine, sodium hydroxide and mixtures thereof.

[0085] An example of an antifoaming agent is preferably selected from the group consisting of (expressed by the corresponding INCI names) dimethicone, trimethicone, polydimethylsiloxane and mixtures thereof.

[0086] An example of a conditioning agent is preferably selected from the group consisting of (indicated by the corresponding INCI names): polyquaternium-10, polyquaternium-4, hydrolyzed collagen, hydrolyzed keratin, and mixtures thereof.

[0087] An example of a preservative is preferably selected from the group consisting of (indicated by the corresponding INCI names): phenoxyethanol, benzoic acid, dehydroacetic acid, capryloylglycine, undecylenic acid and mixtures thereof.

[0088] lipid-ceramide complex

[0089] The composition may also include a lipid-ceramide complex comprising:

[0090] at least one ceramide;

[0091] at least cholesterol or its derivatives;

[0092] A saturated or unsaturated amino alcohol precursor of at least one cell membrane sphingolipid.

[0093] The at least one ceramide is selected from the group consisting of ceramide NP, ceramide AP, ceramide EOP, and mixtures thereof.

[0094] At least cholesterol or a derivative thereof is selected from the group consisting of cholesterol, cholesterol sulfate, and mixtures thereof.

[0095] The carbon number of the saturated or unsaturated amino alcohol precursor of at least one cell membrane sphingolipid is C15 to C20, preferably C17 to C19, preferably C18. Preferably, it is selected from the group consisting of sphingosine, phytosphingosine, dihydrosphingosine and mixtures thereof, preferably phytosphingosine.

[0096] Preferably, the lipid-ceramide complex is present in an amount of about 0.01% to 5% by weight, preferably about 0.05% to 5%, preferably about 0.1% to 5%, preferably about 0.1% to 3%, preferably about 0.1% to 1.5%, preferably about 0.1% to 1%, preferably about 0.1% to 0.8%, preferably about 0.2% to 0.8%, based on the total weight of the composition.

[0097] Preferably, the lipid-ceramide complex comprises:

[0098] at least one ceramide;

[0099] at least cholesterol or its derivatives;

[0100] A saturated or unsaturated amino alcohol precursor of at least one cell membrane sphingolipid.

[0101] Anionic surfactants;

[0102] Thickeners and / or viscosity-increasing agents and / or

[0103] Stabilizer.

[0104] An example of a surfactant, preferably an anionic surfactant, is sodium lauroyl lactylate.

[0105] An example of a thickener, viscosity enhancer, or stabilizer is carbomer and / or xanthan gum.

[0106] Applicants believe that the lipid-ceramide complex possesses emollient properties that counteract skin barrier alterations caused by external agents and / or the washing matrix included in the compositions of the present invention. The lipid-ceramide complex also has a structure similar to that of the stratum corneum, meaning it mimics the composition of the human skin barrier, preferably stratum corneum lipids; in this sense, it further enhances the transdermal penetration of ascorbic acid in the form of glycosides and / or palmitates.

[0107] Possible active ingredients

[0108] Preferably, the topical cleanser composition may include an active ingredient selected from the group consisting of a moisturizer, a soothing agent, a re-epithelializing agent, a keratolytic agent, a whitening agent, a skin nourishing agent, and mixtures thereof.

[0109] Preferably, the external cleanser composition may comprise an active ingredient selected from the group consisting of (corresponding INCI names): panthenol, vitamin E acetate, urea, sodium PCA, hyaluronic acid, allantoin, glycolic acid, niacinamide, acetylglucosamine, oligopeptide-68, diacetyl boldine, retinyl palmitate, bakuchiol, and mixtures thereof.

[0110] Preferably, the external cleaning composition may include at least one active ingredient in an amount of about 0.1% to 7% by weight, preferably about 0.3% to 7%, preferably about 0.3% to 5%, preferably about 0.3%, 1.3%, 3%, 5% by weight of the total weight of the composition.

[0111] Other characteristics and forms of external cleanser compositions

[0112] The pH of the external cleanser composition is 5 to 6.

[0113] Applicants believe that the pH of the composition is also determined after taking into account the surfactants in the wash matrix.

[0114] It is well known that compositions or solutions with high pH (pH close to 10), even in the absence of surfactants, can cause swelling of the stratum corneum (SC) and alter lipid hardness, thereby inducing skin damage.

[0115] The external cleanser composition may be in liquid form or solid form.

[0116] According to a preferred embodiment, when the external cleansing composition is in liquid form, it may include water. Although water is not intentionally added to the formulation of the external cleansing composition in solid form, since water is naturally present in some of the raw materials used, water is also present in another embodiment (i.e., solid form) (although the content is small or at least negligible).

[0117] According to a liquid embodiment, the content of water in the external cleanser composition is preferably about 20% to 60% by weight of the total weight of the composition, preferably about 25% to 50%, preferably about 25% to 47%, preferably about 25% to 45%, preferably about 30% to 45%, preferably about 35% to 45%, preferably about 40% to 45%, preferably about 42% to 45%, preferably about 42%, 43%, 44%, 44.6% or 45%.

[0118] It should be noted that the liquid topical cleanser composition remains effective despite the relatively high water content.

[0119] According to a preferred form, when the external cleanser composition is in solid form, it comprises at least one hydrogenated vegetable oil, preferably a commercially available type.

[0120] The at least one hydrogenated vegetable oil is a vegetable oil extracted from a plant source, as is known to those skilled in the art, and which has undergone a hydrogenation process, i.e., a process of partially or fully saturating the unsaturation characteristic of the polyunsaturated fatty acids (preferably fatty acids having carbon atoms ranging from C12 to C24) contained in the vegetable oil. The hydrogenation process is typically carried out using a catalyst at a temperature of 120° C. to 210° C.

[0121] Preferably, the at least one hydrogenated vegetable oil is in solid or semi-solid form at room temperature (ie a temperature between 25°C and 27°C).

[0122] Preferably, the at least one hydrogenated vegetable oil is chosen from the group consisting of (INCI name): hydrogenated vegetable oil, hydrogenated rice bran oil and mixtures thereof.

[0123] The external cleanser composition can be prepared in the form of cosmetics or medical devices.

[0124] Cosmetics are any substance or mixture intended for application to the external surfaces of the human body (epidermis, hair system and hair, nails, lips, external genitalia), or to the teeth and oral mucosa, for the purpose of substantially altering and / or maintaining the aesthetic appearance, cleansing, enhancing fragrance, etc. Cosmetics do not have medical properties. Substances or mixtures intended for ingestion, inhalation, injection, or implantation into the human body are not considered cosmetics (reference legislation: Regulation (EC) No. 1223 / 2009).

[0125] “Medical device” means any instrument, apparatus, implant, substance or other product, whether used alone or in combination, intended by the manufacturer for use in human beings for the diagnosis, prevention, control, treatment or alleviation of disease; for the diagnosis, control, treatment, alleviation or compensation of injury or disability; for the study, replacement or modification of anatomical structures or physiological processes; or for intervention in conception, and the primary mode of action of the product in or on the human body is not through pharmacological, immunological or metabolic means, but its function may be assisted by such means (EU Regulation 745 / 2017).

[0126] Use of external cleaning composition

[0127] The compositions of the present invention are useful in treating skin diseases or altered skin conditions.

[0128] Preferably, the composition can be used to treat skin aging, melanin deposition or skin dermal-epidermal nutritional changes, or conditions in which skin aging, melanin deposition and skin dermal-epidermal nutritional changes coexist.

[0129] Skin dermal-epidermal nutritional changes refer to the following phenomena:

[0130] -Decreased connective tissue and extracellular matrix biosynthesis associated with mitochondrial damage;

[0131] -Fibroblast senescence is accompanied by increased expression of genes encoding matrix-degrading enzymes.

[0132] Preparation process of external cleaning agent composition

[0133] The preparation process of the liquid external cleaning composition comprises the following steps:

[0134] a) mixing a washing base, ascorbyl palmitate, suitable excipients and / or diluents, possibly adding at least one active ingredient, to obtain a first mixture;

[0135] b) separately mixing glycerol and water, optionally adding at least one active ingredient, and then heating to a temperature of 40° C. to 60° C., preferably 50° C., stirring for 10 to 20 minutes, preferably 15 minutes, to obtain a gel-like mixture, and then cooling;

[0136] c) mixing the cooled gel-like mixture with the first mixture under stirring to obtain a second mixture;

[0137] d) Ascorbyl glucoside is prepared separately, possibly with the addition of a lipid-ceramide complex, and then added to the second mixture, preferably together with water and other suitable excipients and / or diluents.

[0138] The preparation process of the solid external cleaning composition comprises the following steps:

[0139] a′) mixing the washing base, ascorbyl palmitate and at least one hydrogenated vegetable oil and melting them at a temperature preferably between 70° C. and 90° C., preferably 80° C., to obtain a first mixture, possibly adding at least one active ingredient once the temperature reaches 30° C. to 50° C., preferably 40° C.;

[0140] b') separately preparing glycerol and ascorbyl glucoside to obtain a second mixture;

[0141] c') mixing the second mixture with the first mixture and any excipients and / or diluents, preferably at a temperature between 30°C and 50°C, preferably 40°C, and possibly adding the lipid-ceramide complex.

[0142] Example

[0143] Applicants provide the following examples for illustrative purposes only and are not intended to be limiting.

[0144] Example 1 - External Cleanser Composition in Liquid Form

[0145]

[0146] Preparation process of the composition of Example 1:

[0147] Prepare Phases A, B, and C separately. Prepare Phase A by mixing the three surfactants and the gelling agent PEG-120 Methyl Glucose Dioleate in a glass beaker with very gentle stirring (avoiding foaming). Prepare Phase B by dispersing Vitamin E Acetate and Euxyl 701 in Tween 80 and stirring gently until a clear, homogeneous, amber-colored phase is obtained. Prepare Phase C by mixing glycerin and panthenol with water and stirring until a clear, colorless phase is obtained, then heating this phase to 50°C on a hot plate. Stir for at least 15 minutes, and once a gel-like, translucent, lump-free phase is obtained, cool to 25°C. Combine Phases B and A with gentle stirring (avoiding foaming), then mix Phase C with gentle stirring. Disperse the ingredients of Phase D one by one with gentle stirring, and finally mix Phase E. Adjust the pH to 5.3 to 5.5 with a citric acid and sodium citrate buffer (citrate buffer), and finally add the fragrance (Phase F).

[0148] Example 2 - External Cleanser Composition in Liquid Form

[0149]

[0150] Preparation process of the composition of Example 2:

[0151] Prepare Phases A, B, and C separately. Prepare Phase A by mixing the three surfactants and the gelling agent PEG-120 Methyl Glucose Dioleate in a glass beaker with very gentle stirring (avoiding foaming). Prepare Phase B by dispersing ubiquinone and Euxyl 701 in Tween 80 and stirring gently until a clear, homogeneous, amber-colored phase is obtained. Prepare Phase C by mixing glycerin and urea with water and stirring until a clear, colorless phase is obtained, then heating this phase to 50°C on a hot plate. Stir for at least 15 minutes, and once a gel-like, translucent, and lump-free phase is obtained, cool to 25°C. Combine Phases B and A with gentle stirring (avoiding foaming), then mix Phase C with gentle stirring. Disperse the ingredients of Phase D one by one with gentle stirring, and finally mix Phase E. Adjust the pH to 5.3 to 5.5 with a citric acid and sodium citrate buffer (citrate buffer). Finally, add the fragrance (Phase F).

[0152] Example 3 - External Cleanser Composition in Solid Form

[0153]

[0154] Preparation process of the composition of Example 3:

[0155] Phase A is melted at 80°C until a clear liquid phase is obtained. Once at 40°C, phase B is dispersed under stirring, followed by phase C. Finally, phases D and E are added and the mixture is allowed to solidify to room temperature.

[0156] References

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[0158] 2. Quan T, Qin Z, Xia W, Shao Y, Voorhees JJ, Fisher GJ. Matrix-degrading metalloproteinases in photoaging. J Investig Dermatol Symp Proc. 2009Aug; 14(1):20-4.doi:10.1038 / jidsymp.2009.8.

[0159] 3. Gilchrest BA, Eller MS, Yaar M. Telomere-mediated effects on melanogenesis and skin aging. J Investig Dermatol Symp Proc. 2009Aug; 14(1):25-31.doi:10.1038 / jidsymp.2009.9.

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Claims

1. An external cleaning composition comprising: (i) ascorbyl glucoside and ascorbyl palmitate; (ii) a matrix for washing and promoting percutaneous absorption, comprising: - at least one nonionic surfactant; - at least one anionic surfactant; (iii) glycerol, And combined with suitable excipients and / or diluents.

2. The composition according to claim 1, wherein the content of the ascorbyl glucoside is 0.01 to 12% by weight of the total weight of the composition.

3. The composition according to claim 1 or 2, wherein the content of ascorbyl palmitate is 0.01 to 12% by weight of the total weight of the composition.

4. The composition of any one of claims 1 to 3, wherein the weight ratio of the ascorbyl glucoside to the wash matrix is ​​from 1:10 to 1:

70.

5. The composition according to any one of claims 1 to 4, wherein the content of glycerol is 1 to 10% by weight of the total weight of the composition.

6. The composition according to any one of claims 1 to 5, further comprising a lipid-ceramide complex comprising: at least one ceramide; at least cholesterol or its derivatives; A saturated or unsaturated amino alcohol precursor of at least one cell membrane sphingolipid. The composition according to claim 6 , wherein the content of the lipid-ceramide complex is 0.01% to 5% by weight of the total weight of the composition.

8. The composition according to any one of claims 1 to 7, further comprising an active ingredient selected from the group consisting of a moisturizer, a soothing agent, a re-epithelializing agent, a keratolytic agent, a whitening agent, a skin nourishing agent, and mixtures thereof.

9. The composition according to any one of claims 1 to 8, wherein the pH is 5 to 6.

10. The composition according to any one of claims 1 to 9, in the form of a cosmetic or medical device.

11. The composition according to any one of claims 1 to 10, in liquid or solid form.

12. The composition according to claim 11, comprising water, preferably in an amount ranging from 20% to 60% by weight relative to the total weight of the composition.

13. A liquid composition according to claim 11 or 12, wherein the cleaning matrix further comprises at least one amphoteric surfactant.

14. The solid composition according to claim 11, comprising at least one hydrogenated vegetable oil.

15. The composition according to any one of claims 1 to 13 for use in treating a skin disease or altered state selected from skin aging, melanin pigmentation, skin dermal-epidermal nutritional changes or a combination thereof.

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