Carbon dioxide for promoting transdermal absorption and stabilization of active ingredients in cosmetics

Abstract

The invention relates to carbon dioxide for promoting transdermal absorption and stabilization of active ingredients in cosmetics. The invention provides an application of carbon dioxide in promoting transdermal absorption of an active component in cosmetics, wherein the active component is nicotinamide or vitamin C. The invention also provides a method for promoting transdermal absorption of nicotinamide or vitamin C in cosmetics, cosmetics, application of carbon dioxide in promoting vitamin C in cosmetics to maintain stability, and a method for facilitating vitamin C in cosmetics to maintain stability.

Description

Technical Field

[0001] This invention belongs to the field of cosmetics, and more specifically, this invention relates to carbon dioxide promoting the transdermal absorption and stabilization of active ingredients in cosmetics. Background Technology

[0002] CO2 in aqueous solution plays a crucial role in regulating skin pH and maintaining skin homeostasis, making it valuable for skin care and intervention in skin diseases. In skin care, Bock M et al. found that skin treated with CO2 solution showed a significant reduction in transepidermal water loss (TEWL) and pH. Fukagawa S et al., in their study on the effects and mechanisms of transepidermal CO2 solution on squamous xerosis, demonstrated through human experiments and 3D epidermal model experiments that transepidermal CO2 solution improved peeling in dry skin, accompanied by mild acidification of the stratum corneum, thus improving scaling. In the treatment of skin diseases, Schmidt J et al. pointed out that high-concentration CO2 solution can effectively promote wound and ulcer healing and inhibit the onset of Raynaud's syndrome. Furthermore, skin treated with CO2 solution showed an inhibition rate of ≥40% for scaling and wrinkle parameters, and continuous application of high-concentration CO2 solution had excellent skin repair and regeneration effects. Therefore, CO2 aqueous solution has significant biological significance for skin repair.

[0003] Research on carbon dioxide has demonstrated its role in skin care, repair, and wound healing. However, because carbon dioxide is a gas, conventional cosmetic formulations cannot effectively incorporate it into their formulations, limiting its application in cosmetics. In 2018, the inventors developed a carbon dioxide aerosol manufacturing system and process, making the application of carbon dioxide gas in cosmetics possible (CN201810645213.8).

[0004] The application of carbon dioxide gas in cosmetics also requires consideration of the transdermal absorption and stability of active ingredients. Skin has a natural protective barrier, and the transdermal absorption of active ingredients is directly related to their efficacy. Therefore, ensuring the safe and effective transdermal absorption of active ingredients is a crucial issue in cosmetic technology. Another common problem in cosmetic formulations is the stability of active ingredients. Many active ingredients have active groups that are easily oxidized and decomposed, causing instability in the formulation and significantly reducing product efficacy. For example, vitamin C, the most commonly used and effective whitening ingredient, is very unstable in solution and easily oxidized. Therefore, relatively stable vitamin C derivatives are currently used, such as vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, and magnesium ascorbate phosphate. However, these vitamin C derivatives are still easily oxidized and discolored when exposed to air, preventing them from fully exerting their effects.

[0005] Therefore, there is an urgent need to solve the above problems in this field. Summary of the Invention

[0006] This invention relates to carbon dioxide promoting transdermal absorption and stabilization of active ingredients in cosmetics.

[0007] A first aspect of the invention provides the use of carbon dioxide in promoting the transdermal absorption of an active ingredient in a cosmetic, wherein the active ingredient is niacinamide or vitamin C.

[0008] In one or more embodiments, the mass percentage of the carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

[0009] In one or more embodiments, the active ingredient is nicotinamide or a derivative thereof, or vitamin C or a derivative thereof.

[0010] In one or more embodiments, the nicotinamide derivative includes: nicotinamide adenine dinucleotide and isonicotinamide.

[0011] In one or more embodiments, the vitamin C derivative includes: vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, and magnesium ascorbate phosphate.

[0012] In one or more embodiments, the transdermal absorption is expressed as the cumulative release rate of the active ingredient through the skin per unit time.

[0013] A second aspect of the present invention provides a method for promoting transdermal absorption of niacinamide or vitamin C in cosmetics, the method comprising: adding carbon dioxide to the cosmetic.

[0014] In one or more embodiments, the mass percentage of the carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

[0015] A third aspect of the present invention provides a cosmetic product containing carbon dioxide, an active ingredient, and a cosmetically acceptable carrier, wherein the active ingredient is niacinamide or a derivative thereof, or vitamin C or a derivative thereof.

[0016] In one or more embodiments, the nicotinamide derivative includes: nicotinamide adenine dinucleotide and isonicotinamide.

[0017] In one or more embodiments, the vitamin C derivative includes: vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, and magnesium ascorbate phosphate.

[0018] In one or more embodiments, the mass percentage of the carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

[0019] In one or more embodiments, the mass percentages of the niacinamide or its derivatives, and vitamin C or its derivatives, based on the total weight of the cosmetic product, are: 0.001–10%, preferably 0.01–8%, 0.01–7%, 0.1–6%, 0.1–5%, 1–5%, or 3–5%, more preferably 5 ± 0.5%, 5 ± 0.3%, 5 ± 0.2%, or 5 ± 0.1%.

[0020] In one or more embodiments, the cosmetic is an aqueous product; preferably a lotion, essence water, toner, or makeup remover.

[0021] A fourth aspect of the invention provides the use of carbon dioxide in promoting the stability of vitamin C in cosmetics; wherein the vitamin C includes derivatives thereof.

[0022] In one or more embodiments, the mass percentage of the carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

[0023] In one or more embodiments, the vitamin C derivative includes: vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, and magnesium ascorbate phosphate.

[0024] In one or more embodiments, the stability includes: room temperature stability; preferably room temperature stability under light conditions.

[0025] A fifth aspect of the present invention provides a method for maintaining the stability of vitamin C in cosmetics, the method comprising: adding carbon dioxide to the cosmetic.

[0026] In one or more embodiments, the mass percentage of the carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

[0027] In one or more embodiments, the vitamin C includes vitamin C or a derivative thereof; preferably, the vitamin C derivative includes: vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, and magnesium ascorbate phosphate.

[0028] In one or more embodiments, the stability includes: room temperature stability; preferably room temperature stability under light conditions.

[0029] Other aspects of the invention will be apparent to those skilled in the art from the disclosure herein. Attached Figure Description

[0030] Figure 1 HaCat cell viability at CO2 concentrations of 33.82 mmol / L, 16.91 mmol / L, and 8.46 mmol / L. The group receiving PBS but without CO2 was designated as the PBS group, and the group receiving only cells was designated as the control group.

[0031] Figure 2 The cumulative release rate of niacinamide at different times was compared with that of niacinamide essence water without added CO2 as a control group.

[0032] Figure 3 The cumulative release rate of vitamin C at different times was compared with that of vitamin C essence water without added CO2 as a control group.

[0033] Figure 4 The cumulative release rate of arbutin at different times was compared with that of arbutin essence water without added CO2 as a control group.

[0034] Figure 5 The cumulative release rate of resveratrol at different times was compared with that of resveratrol essence water without added CO2 as a control group.

[0035] Figure 6 The cumulative release rate of tranexamic acid at different times was compared with that of tranexamic acid essence water without added CO2 as a control group.

[0036] Figure 7 The cumulative release rate of phenylethyl resorcinol at different times was compared with that of phenylethyl resorcinol essence water without added CO2 as a control group.

[0037] Figure 8 Results on the stability of vitamin C. (a) Initial state diagram of carbon dioxide under sunlight; (b) State diagram of carbon dioxide after 30 days under sunlight; (c) Initial state diagram of compressed air under sunlight; (d) State diagram of compressed air after 30 days under sunlight. Detailed Implementation

[0038] Through in-depth research, the inventors discovered that carbon dioxide is non-cytotoxic and can be used in cosmetic formulations. Unexpectedly, they found that carbon dioxide enhances the transdermal absorption of certain active ingredients in cosmetics, such as niacinamide and vitamin C, an effect that cannot be replicated with active ingredients such as arbutin, resveratrol, tranexamic acid, and phenylethyl resorcinol. Furthermore, the inventors also discovered that carbon dioxide helps maintain the stability of vitamin C in cosmetics.

[0039] This invention provides the application of carbon dioxide in promoting the transdermal absorption of active ingredients in cosmetics, wherein the active ingredient is niacinamide or vitamin C. Specifically, in the cosmetic, the mass percentage of carbon dioxide can be 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5 ± 0.5%, 2.5 ± 0.3%, 2.5 ± 0.2%, or 2.5 ± 0.1%.

[0040] In this invention, "promote" means significant "promotion", "enhancement" or "increase", for example, compared with the control group, it promotes, enhances or increases by more than 30%, more than 40%, more than 50%, more than 60%, more than 70% or higher.

[0041] As used in this invention, the "nicotinamide" mentioned above, also known as "vitamin B3," has the molecular formula C6H6N2O and the CAS number 98-92-0. The "nicotinamide" mentioned above also includes its derivatives. The term "nicotinamide derivative" refers to substances derived from naturally occurring nicotinamide that possess the biological functions of nicotinamide (e.g., antioxidant, anti-aging), such as, but not limited to, nicotinamide adenine dinucleotide and isonicotinamide.

[0042] As used in this invention, the "vitamin C" has the molecular formula C6H8O6 and the CAS number 50-81-7. The "vitamin C" also includes its derivatives. The term "vitamin C derivative" refers to substances derived from natural vitamin C and possessing the biological functions of vitamin C (e.g., ascorbic acid, antioxidant properties), such as, but not limited to: vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, and magnesium ascorbate phosphate.

[0043] As used in this invention, the "transdermal absorption enhancement effect" refers to the effect of carbon dioxide on the transdermal absorption of a certain active ingredient in cosmetics. This transdermal absorption enhancement effect can be expressed by the cumulative release rate of the active ingredient in the skin; a higher cumulative release rate indicates a stronger transdermal absorption effect. Exemplarily, the cumulative release rate can be measured using a standard curve method. In some specific embodiments, the transdermal absorption enhancement effect of carbon dioxide on niacinamide or vitamin C in cosmetics is more significant after 6 hours, for example, 8 hours, 10 hours, or 12 hours.

[0044] This invention provides a method for promoting the transdermal absorption of niacinamide or vitamin C in cosmetics, the method comprising: adding carbon dioxide to the cosmetic. Specifically, the mass percentage of carbon dioxide can be 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5 ± 0.5%, 2.5 ± 0.3%, 2.5 ± 0.2%, or 2.5 ± 0.1%.

[0045] The present invention also provides a cosmetic containing carbon dioxide, an active ingredient, and a cosmetically acceptable carrier, wherein the active ingredient is niacinamide or vitamin C.

[0046] In some specific embodiments, the mass percentage of carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

[0047] In some specific embodiments, the mass percentage of niacinamide or vitamin C in the cosmetic product, based on the total weight of the cosmetic product, can be 0.001–10%, for example 0.01–8%, 0.01–7%, 0.1–6%, 0.1–5%, 1–5%, or 3–5%, preferably 5 ± 0.5%, 5 ± 0.3%, 5 ± 0.2%, or 5 ± 0.1%.

[0048] In this invention, the cosmetic is preferably an aqueous product, such as, but not limited to, toner, essence water, lotion, and makeup remover.

[0049] The term "cosmetically acceptable carrier" refers to an applicable carrier in cosmetics, including various excipients and diluents, which are not essential active ingredients themselves and do not cause excessive toxicity after application. Suitable carriers are well known to those skilled in the art. A thorough discussion of cosmetically acceptable excipients can be found in the 2015 edition of the Cosmetic Hygiene Standard. These may include humectants, emulsifiers, thickeners, chelating agents, skin-moisturizing agents, pigments, etc. Examples, but not limited to, water, glycerin, phenoxyethanol, 1,3-butanediol, 1,2-hexanediol, p-hydroxyacetophenone, disodium EDTA, 1,3-propanediol, sodium hyaluronate, hydroxyethyl cellulose, xanthan gum, polyacrylate crosspolymer-6, tert-butanol, glyceryl stearate, cetearyl alcohol, cetearyl glucoside, plant squalane, caprylic / capric triglyceride, cetearyl alcohol, polydimethylsiloxane, tromethamine, ethylhexylglycerin, sorbitol, glyceryl polyether-26, p-hydroxyacetophenone, acrylates / C10-30 alkanol acrylate crosspolymers, butanediol, sodium stearoyl glutamate, p-hydroxyacetophenone, chlorophenoxyether, panthenol, dipotassium glycyrrhizate, arginine, dipropylene glycol, isononyl isononanoate. Betaine, glyceryl stearate / PEG-100 stearate, glyceryl stearate, carbomer, isohexadecane, isooctyl palmitate, cetearyl alcohol, polydimethylsiloxane, diisopropyl sebacate, citric acid or its salts, sorbitol, sorbitol polyether, cetyl alcohol polyether, pentaerythritol tetra(ethylhexanoate), sodium polyacrylamide dimethyl taurate, cetyl alcohol ethylhexanoate, PEG / PPG-17 / 6 copolymer, ammonium acryloyl dimethyl taurate / VP copolymer, PPG-26-butanol polyether-26, PEG-40 hydrogenated castor oil, decyl glucoside, fragrance, betaine, trisorbin PEG-20 esters, shea butter, cyclopentamethoxysiloxane, hydrogenated polydecene, phenyl polytrimethylsiloxane, etc.

[0050] In some specific embodiments of the present invention, the cosmetic further contains phenoxyethanol. Preferably, the mass percentage of phenoxyethanol, based on the total weight of the cosmetic, can be 0.1–5%, for example 0.1–2%, 0.1–1%, or 0.1–0.5%, more preferably 0.5 ± 0.1%, 0.5 ± 0.05%, 0.5 ± 0.02%, or 0.5 ± 0.01%.

[0051] This invention has discovered that carbon dioxide helps stabilize vitamin C in cosmetics. As used herein, "stability" includes, but is not limited to, room temperature stability. "Room temperature stability" refers to the stability of a sample after being placed at room temperature for an extended period. Typically, "an extended period" is 20 days or more, for example, 25 days or more, 28 days or more, 30 days or more, or longer. Typically, "room temperature" refers to 18°C ​​to 30°C. In a specific embodiment, because vitamin C oxidizes and turns orange-yellow under light, the stability test for vitamin C is performed under light conditions.

[0052] Therefore, the present invention also provides a method for maintaining the stability of vitamin C in cosmetics, the method comprising: adding carbon dioxide to the cosmetic. Specifically, the mass percentage of the carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

[0053] Carbon dioxide can be added to cosmetics using a carbon dioxide aerosol manufacturing system, for example, by referring to the method in the inventor's previous patent CN201810645213.8, the contents of which are incorporated herein by reference in their entirety.

[0054] While the numerical ranges and parameters used to define the broader scope of this invention are approximate values, the relevant values ​​in specific embodiments have been presented as precisely as possible. However, any value inevitably contains standard deviations due to individual testing methods. Here, "approximately" generally means that the actual value is within plus or minus 10%, 5%, 1%, or 0.5% of a particular value or range. Alternatively, the term "approximately" may mean that the actual value falls within the acceptable standard error of the mean, as determined by those skilled in the art. Except for experimental examples, or unless explicitly stated otherwise, it is understood that all ranges, quantities, values, and percentages used herein (e.g., to describe material usage, duration, temperature, operating conditions, quantity ratios, and others similar) are modified with "approximately". Therefore, unless otherwise stated, the numerical parameters disclosed in this specification and the accompanying claims are approximate values ​​and are subject to change as needed. At least these numerical parameters should be understood as the indicated significant digits and values ​​obtained by applying general rounding. The numerical ranges described in this invention include endpoint values. For example, 1 to 10% includes the endpoint values ​​of 1% and 10%.

[0055] Unless otherwise defined in this specification, scientific and technical terms used herein have the same meaning as understood and commonly used by those skilled in the art. Furthermore, unless conflicting with the context, singular nouns used herein include their plural forms, and vice versa.

[0056] The advantages of this invention are:

[0057] 1. Cell compatibility experiments show that carbon dioxide is non-cytotoxic and can be safely used in cosmetics.

[0058] 2. This invention discovers that carbon dioxide promotes the transdermal absorption of certain active ingredients in cosmetics, such as niacinamide and vitamin C. This transdermal absorption-promoting effect cannot be reproduced when the active ingredients are arbutin, resveratrol, tranexamic acid, or phenylethyl resorcinol.

[0059] 3. Carbon dioxide can help maintain the stability of vitamin C in cosmetics.

[0060] The present invention will be further illustrated below with reference to specific embodiments. It should be understood that these embodiments are for illustrative purposes only and are not intended to limit the scope of the invention. Experimental methods in the following embodiments, unless otherwise specified, are generally performed under conventional conditions or as recommended by the manufacturer.

[0061] Experimental materials

[0062] Active ingredients factory Item number Arbutin Adamas-beta P2039551 Resveratrol Rhine Biological PCE07 Tranexamic acid Source Leaf Bio T28D10F107066 Niacinamide Vibolai VBL062NTUA09 Vitamin C Adamas-beta P2234043 Phenethyl resorcinol Adamas-beta P2128291

[0063] Example

[0064] Example 1: HaCat cell compatibility experiment

[0065] HaCaT cells (from the Chinese Academy of Sciences) were incubated in a culture chamber until the confluence was approximately 90%, and then cell suspensions containing 33.82 mmol / L, 16.91 mmol / L, and 8.46 mmol / L CO2 samples were prepared. 100 μL of the cell suspension was seeded into each well of a 96-well plate, and the cell culture density with an absorbance of 1 at 450 nm was selected using a CCK-8 cell proliferation / cytotoxicity assay kit (Shanghai Beyotime Biotechnology Co., Ltd. C0038). The selected cell culture density was 2 × 10⁵ cells / mL.

[0066] At the selected cell densities, CO2 concentrations of 33.82 mmol / L, 16.91 mmol / L, and 8.46 mmol / L were added, respectively. After 48 h of cell adhesion culture, cell viability was assessed using the CCK-8 assay, and absorbance at 450 nm was measured using a microplate reader. The values ​​were recorded. The group receiving PBS without CO2 was designated as the PBS group, and the cell-only group served as the control group. HaCaT cell viability was calculated using the following formula:

[0067] Cell viability (%) = (A – A0) / (An – A0) × 100%

[0068] Where A represents the absorbance value of the well after adding CO2 with cells and CCK-8 solution, A0 represents the absorbance value of the well without cells, and An represents the absorbance value of the well with cells and CCK-8 solution but without CO2.

[0069] Table 1. Cell viability (%) of HaCaT

[0070]

[0071] like Figure 1 As shown in Table 1, when the CO2 concentration was 8.46–33.82 mmol / L, the cell viability of HaCaT was close to that of the control group and the PBS group, indicating that CO2 treatment was non-toxic to cells and had good biocompatibility with keratinocytes.

[0072] Example 2: The effect of carbon dioxide on promoting transdermal absorption of active ingredients in cosmetics

[0073] In this embodiment, arbutin, resveratrol, tranexamic acid, nicotinamide, vitamin C, and phenylethyl resorcinol were used as examples to investigate the effect of carbon dioxide on promoting the transdermal absorption of functional ingredients in cosmetics.

[0074] The inventors unexpectedly discovered that carbon dioxide could promote transdermal absorption only when the active ingredients were nicotinamide and vitamin C. This effect of promoting transdermal absorption could not be replicated in a large number of other active ingredients. For example, carbon dioxide could not promote the transdermal absorption of arbutin, resveratrol, tranexamic acid, and phenylethyl resorcinol.

[0075] Experimental methods:

[0076] 1. Experimental method for promoting transdermal absorption of water-soluble samples (tranexamic acid, nicotinamide, vitamin C):

[0077] Sample solutions of different concentrations were prepared using PBS solution, and the absorbance was measured using a UV spectrophotometer. The values ​​were recorded, and a standard curve was plotted.

[0078] Using pigskin as a permeable membrane, samples were prepared with PBS. A sample solution without CO2 was used as the control group, and a sample solution with CO2 was used as the experimental group. Both were placed in a diffusion cell, and an equal volume of PBS was added to the receiving cell. Samples were taken from the receiving cell at different time points, and their absorbance was measured under UV light. The concentration of the samples at different time points was obtained using a standard curve, and the cumulative release rate of the samples at different time points was calculated using the following formula:

[0079] Y = (C n V n +∑C K V K ) / CV

[0080] Y represents the cumulative release rate; Cn represents the sample concentration measured at the nth sampling point; CK represents the sample concentration measured at all sampling points before the nth sampling point; Vn represents the receiving liquid volume; VK represents the sampling volume corresponding to all sampling points before the nth sampling point; C represents the sample concentration in the initial diffusion chamber; and V represents the sample volume in the initial diffusion chamber.

[0081] 2. Experimental method for promoting transdermal absorption of water-insoluble samples (arbutin, resveratrol, phenylethyl resorcinol):

[0082] Solutions of active ingredients of different concentrations were prepared using ethanol and caprylic / capric triglycerides. The absorbance was measured using a UV spectrophotometer, the values ​​were recorded, and a standard curve for the samples was plotted.

[0083] Using pigskin as the permeation membrane, samples were prepared with receiving solution (PBS:ethanol = 6:4, volume ratio) and caprylic / capric triglycerides. A sample solution without CO2 was used as the control group, and a sample solution with CO2 was used as the experimental group. Both were placed in a diffusion cell, and an equal volume of receiving solution was added to the receiving cell. Samples were taken from the receiving cell at different time points, and their absorbance was measured under UV light. The concentration of the samples at different time points was obtained using a standard curve, and the cumulative release rate of the samples at different time points was calculated using the same formula as for the water-soluble samples. A higher cumulative release rate indicates better permeation performance.

[0084] Test Example 1: The effect of carbon dioxide on promoting transdermal absorption of nicotinamide

[0085] Sample Preparation: Niacinamide essence water samples were prepared according to the formula in Table 2. Vacuum sealing was required for sample sealing. Subsequently, CO2 was introduced into the essence water sample under constant pressure (25℃, 780 kPa, pressure maintained between 750 kPa and 800 kPa) until the pressure in the aerosol can reached equilibrium, resulting in an essence water sample containing CO2. The mass percentage of CO2 in the essence water sample was 2.5%.

[0086] The formula for the niacinamide essence water is shown in Table 2.

[0087] Table 2 Niacinamide Essence Water Formula

[0088]

[0089] Furthermore, using a sample solution without added CO2 as a control group, the effect of CO2 on promoting transdermal absorption of nicotinamide was investigated. The results are as follows: Figure 2 As shown in Table 3, CO2 has a good effect on promoting the transdermal absorption of niacinamide in whitening essence water.

[0090] Table 3. Effects of CO2 on the transdermal absorption of nicotinamide

[0091]

[0092] Test Example 2: The effect of carbon dioxide on promoting transdermal absorption of vitamin C

[0093] Sample Preparation: Vitamin C essence water samples were prepared according to the formula in Table 4. Vacuum sealing was required for sample sealing. Subsequently, CO2 was introduced into the essence water sample under constant pressure (25℃, 780 kPa, pressure maintained between 750 kPa and 800 kPa) until the pressure in the aerosol can reached equilibrium, resulting in an essence water sample containing CO2. The mass percentage of CO2 in the essence water sample was 2.5%.

[0094] The formula for Vitamin C essence water is shown in Table 4.

[0095] Table 4 Vitamin C Essence Water Formula

[0096]

[0097] Furthermore, using a sample solution without added CO2 as a control group, the effect of CO2 on promoting transdermal absorption of vitamin C was investigated. The results are as follows: Figure 3 As shown in Table 5, CO2 has a significant effect on promoting the transdermal absorption of vitamin C in the essence water.

[0098] Table 5. Effect of CO2 on promoting transdermal absorption of vitamin C

[0099]

[0100] Comparative Example 1: The effect of carbon dioxide on promoting transdermal absorption of arbutin

[0101] Sample Preparation: Arbutin essence water samples were prepared according to the formula in Table 6. Vacuum sealing was required for sample sealing. Subsequently, CO2 was introduced into the essence water sample under constant pressure (25℃, 780 kPa, pressure maintained between 750 kPa and 800 kPa) until the pressure in the aerosol can reached equilibrium, resulting in an essence water sample containing CO2. The mass percentage of CO2 in the essence water sample was 2.5%.

[0102] The formula for arbutin essence water is shown in Table 6.

[0103] Table 6 Arbutin Essence Water Formula

[0104]

[0105] Furthermore, using a sample solution without added CO2 as a control group, the effect of CO2 on promoting transdermal absorption of arbutin was investigated. The results are as follows: Figure 4 As shown in Table 7, CO2 cannot promote the penetration of arbutin in the essence water.

[0106] Table 7. Effect of CO2 on the transdermal absorption of arbutin

[0107]

[0108] Comparative Example 2: The effect of carbon dioxide on promoting transdermal absorption of resveratrol

[0109] Sample Preparation: Resveratrol essence water samples were prepared according to the formula in Table 8. Vacuum sealing was required for sample sealing. Subsequently, CO2 was introduced into the essence water sample under constant pressure (25℃, 780 kPa, pressure maintained between 750 kPa and 800 kPa) until the pressure in the aerosol can reached equilibrium, resulting in an essence water sample containing CO2. The mass percentage of CO2 in the essence water sample was 2.5%.

[0110] The formula for resveratrol essence water is shown in Table 8.

[0111] Table 8 Resveratrol Essence Water Formula

[0112]

[0113] Furthermore, using a sample solution without added CO2 as a control group, the effect of CO2 on promoting transdermal absorption of resveratrol was investigated. The results are as follows: Figure 5 As shown in Table 9, CO2 has almost no effect on the penetration of resveratrol in the essence water.

[0114] Table 9. Effect of CO2 on the transdermal absorption of resveratrol

[0115]

[0116] Comparative Example 3: The effect of carbon dioxide on promoting transdermal absorption of tranexamic acid

[0117] Sample Preparation: Tranexamic acid essence water samples were prepared according to the formula in Table 10. Vacuum sealing was required for sample sealing. Subsequently, CO2 was introduced into the essence water sample under constant pressure (25℃, 780 kPa, pressure maintained between 750 kPa and 800 kPa) until the pressure in the aerosol can reached equilibrium, obtaining an essence water sample containing CO2. The mass percentage of CO2 contained in the essence water sample was 2.5%.

[0118] The formula for tranexamic acid essence water is shown in Table 10.

[0119] Table 10. Formula for Tranexamic Acid Whitening Essence Water

[0120]

[0121] Furthermore, using a sample solution without added CO2 as a control group, the effect of CO2 on promoting the transdermal absorption of tranexamic acid was investigated. The results are as follows: Figure 6 As shown in Table 11, CO2 has no effect on the penetration of tranexamic acid in the essence water.

[0122] Table 11. Effect of CO2 on the transdermal absorption of tranexamic acid

[0123]

[0124] Comparative Example 4: The effect of carbon dioxide on promoting transdermal absorption of phenylethyl resorcinol

[0125] Sample Preparation: Phenethyl resorcinol essence water samples were prepared according to the formula in Table 12. Vacuum sealing was required for sample sealing. Subsequently, CO2 was introduced into the essence water sample under constant pressure (25℃, 780 kPa, pressure maintained between 750 kPa and 800 kPa) until the pressure in the aerosol can reached equilibrium, obtaining an essence water sample containing CO2. The mass percentage of CO2 contained in the essence water sample was 2.5%.

[0126] The formula for phenylethyl resorcinol essence water is shown in Table 12.

[0127] Table 12 Phenethylresorcinol Whitening Essence Water Formula

[0128]

[0129] Furthermore, using a sample solution without added CO2 as a control group, the transdermal absorption-promoting effect of CO2 on phenylethyl resorcinol was investigated. The results are as follows: Figure 7 As shown in Table 13, CO2 has almost no effect on promoting the transdermal absorption of phenylethyl resorcinol in the essence water.

[0130] Table 13 shows the effect of CO2 on promoting the transdermal absorption of phenylethyl resorcinol.

[0131]

[0132]

[0133] Example 3: Effect of carbon dioxide on the stability of vitamin C essence water samples

[0134] Vitamin C essence water samples were prepared according to the formula in Table 4. Carbon dioxide and compressed air were introduced separately, with compressed air serving as a control group. Vacuum sealing was required for each sample. Subsequently, under constant pressure (25℃, 780 kPa, pressure maintained between 750 kPa and 800 kPa), CO2 or compressed air was introduced into the essence water samples until the pressure in the aerosol can reached equilibrium, obtaining essence water samples containing either CO2 or compressed air. The CO2-containing essence water sample contained 2.5% CO2 by mass. The compressed air-containing essence water sample contained 1.20% compressed air by mass. Stability tests were conducted on the carbon dioxide and compressed air-containing essence water samples under outdoor sunlight.

[0135] Stability testing method: Essence water samples containing carbon dioxide and compressed air were left to stand for 30 days under outdoor sunlight, respectively. Since Vitamin C oxidizes upon exposure to light, turning orange-yellow, and the higher the degree of oxidation, the darker the color, the samples were photographed and observed after 30 days to compare the color and thus the degree of Vitamin C oxidation.

[0136] Figure 8 The results of the stability test show that carbon dioxide has a protective effect on vitamin C in the essence water, making it less susceptible to oxidation and inactivation compared to samples containing compressed air.

[0137] The embodiments described above are merely illustrative of several implementations of the present invention, and while the descriptions are relatively specific and detailed, they should not be construed as limiting the scope of the present invention. It should be noted that those skilled in the art can make various modifications and improvements without departing from the concept of the present invention, and these all fall within the scope of protection of the present invention. Therefore, the scope of protection of this patent should be determined by the appended claims. Furthermore, all documents mentioned in this invention are incorporated herein by reference as if each document were individually incorporated by reference.

Claims

1. The application of carbon dioxide in promoting transdermal absorption of active ingredients in cosmetics, wherein the active ingredient is niacinamide or vitamin C.

2. The application as described in claim 1, characterized in that, The mass percentage of carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

3. The application as described in claim 1, characterized in that, The active ingredient is nicotinamide or a derivative thereof, or vitamin C or a derivative thereof; Preferably, the nicotinamide derivative includes nicotinamide adenine dinucleotide and isonicotinamide, and the vitamin C derivative includes vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, and magnesium ascorbate phosphate.

4. The application as described in any one of claims 1 to 3, characterized in that, The term "transdermal absorption" is expressed as the cumulative release rate of active ingredients through the skin per unit time.

5. A method for promoting transdermal absorption of niacinamide or vitamin C in cosmetics, the method comprising: Carbon dioxide is added to the cosmetic product; Preferably, the mass percentage of the carbon dioxide is 0.1% to 10%, more preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, and even more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%.

6. A cosmetic product, characterized in that, The cosmetic contains carbon dioxide, an active ingredient, and a cosmetically acceptable carrier, wherein the active ingredient is niacinamide or a derivative thereof, or vitamin C or a derivative thereof; Preferably, the nicotinamide derivative includes nicotinamide adenine dinucleotide and isonicotinamide, and the vitamin C derivative includes vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, and magnesium ascorbate phosphate.

7. The cosmetic product as described in claim 6, characterized in that, The mass percentage of the carbon dioxide is 0.1% to 10%, preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%; and / or, The percentage by weight of the niacinamide or its derivatives, and vitamin C or its derivatives, based on the total weight of the cosmetic product, is 0.001–10%, preferably 0.01–8%, 0.01–7%, 0.1–6%, 0.1–5%, 1–5%, or 3–5%, more preferably 5 ± 0.5%, 5 ± 0.3%, 5 ± 0.2%, or 5 ± 0.1%.

8. The cosmetic product as described in claim 6 or 7, characterized in that, The cosmetic product is an aqueous product; preferably, it is a toner, essence, lotion, or makeup remover.

9. The application of carbon dioxide in promoting the stability of vitamin C in cosmetics; wherein the vitamin C includes its derivatives; Preferably, the mass percentage of the carbon dioxide is 0.1% to 10%, more preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%; and / or, Preferably, the vitamin C derivative comprises: Vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, magnesium ascorbate phosphate; And / or, Preferably, the stability includes: room temperature stability; more preferably, room temperature stability under light conditions.

10. A method for maintaining the stability of vitamin C in cosmetics, the method comprising: Carbon dioxide is added to the cosmetic product; Preferably, the mass percentage of the carbon dioxide is 0.1% to 10%, more preferably 0.1% to 9%, 0.2% to 8%, 0.3% to 7%, 0.5% to 6%, 0.8% to 5%, 1% to 4%, 1% to 3%, 1.2% to 3%, or 1.5% to 3%, more preferably 2.5±0.5%, 2.5±0.3%, 2.5±0.2%, or 2.5±0.1%; and / or, Preferably, the vitamin C comprises vitamin C or a derivative thereof; more preferably, the vitamin C derivative comprises: vitamin C ethyl ether, ascorbate glucoside, sodium ascorbate phosphate, magnesium ascorbate phosphate; and / or, Preferably, the stability includes: room temperature stability; more preferably, room temperature stability under light conditions.

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