A water-oil double-layer penetration-enhancing cosmetic composition and a method for preparing the same

Abstract

The application provides a water-oil double-layer penetration-promoting cosmetic composition and a preparation method thereof, and relates to the cosmetic field. The raw materials of the water-oil double-layer penetration-promoting cosmetic composition include 5-30% of an oil phase and 70-95% of an aqueous phase according to a total mass of 100%. The raw materials of the aqueous phase include dipropylene glycol, glycerol glucoside and water. The raw materials of the oil phase include caprylic capric triglyceride and isosorbide dioctanoate. The isosorbide dioctanoate in the water-oil double-layer penetration-promoting cosmetic composition constructs a lipid microchannel, the dipropylene glycol enhances the hydration of the stratum corneum, and the glycerol glucoside activates AQP3 water channel protein. The three channels synergistically improve the penetration efficiency without damaging the integrity of the skin barrier. The penetration-promoting agent has strong broad-spectrum penetration-promoting ability for different polar functional ingredients, the penetration-promoting effect is stable, and the penetration-promoting agent can be stably distributed in the oil and water phases.

Description

Technical Field

[0001] This application relates to the field of cosmetics, and more particularly to a water-oil bilayer penetration-enhancing cosmetic composition and its preparation method. Background Technology

[0002] The transdermal penetration ability of cosmetic active ingredients is a key factor determining product efficacy. Currently, commonly used penetration enhancers in commercially available cosmetics include azones, alcohols, and exfoliating agents, but these have problems such as high irritation, narrow applicability, and damage to the skin barrier.

[0003] Water-oil dual-layer cosmetic systems are highly favored for their visual appeal, engaging application, and ability to simultaneously dissolve active ingredients of different polarities. However, this system faces the following technical challenges: 1. Traditional penetration enhancers have uneven distribution coefficients in two-layer systems, resulting in unstable penetration enhancement effects and an inability to stably distribute in the oil-water two-phase system; 2. Single penetration enhancers have limited broad-spectrum penetration-enhancing capabilities for active ingredients of different polarities; 3. High concentrations of penetration enhancers can easily cause skin irritation and formula instability, exhibiting high irritation and a narrow safety window; 4. Lack of broad-spectrum and efficient synergistic penetration-enhancing solutions.

[0004] Therefore, there is an urgent need to provide a water-oil dual-layer penetration-enhancing cosmetic system to solve the above problems. Summary of the Invention

[0005] The purpose of this application is to provide a water-oil dual-layer penetration-enhancing cosmetic composition and its preparation method to solve the above-mentioned problems.

[0006] To achieve the above objectives, the first aspect of this application provides a water-oil dual-layer penetration-enhancing cosmetic composition, wherein the raw materials, based on a total mass of 100%, include: 5%-30% oil phase, 70-95% aqueous phase; The raw materials for the aqueous phase include dipropylene glycol, glycerol glucoside, and water; The raw materials for the oil phase include caprylic / capric triglyceride and isosorbide dicaprylate.

[0007] Optionally, the mass ratio of isosorbide dioctanoate, dipropylene glycol, and glyceryl glucoside is 0.2-2:0.2-4:0.2-4.

[0008] Optionally, the mass ratio of the caprylic / capric triglyceride to the isosorbide dicaprylate is 3-29.8:0.2-2.

[0009] Optionally, the aqueous phase may further include disodium ethylenediaminetetraacetate and a preservative.

[0010] Optionally, the preservative includes p-hydroxyacetophenone and / or 1,2-hexanediol.

[0011] A second aspect of this application provides a method for preparing the aforementioned water-oil bilayer penetration-enhancing cosmetic composition, comprising: The raw materials in the aqueous phase are first mixed to obtain the aqueous phase; The raw materials for the oil phase are mixed a second time to obtain the oil phase; The aqueous phase and the oil phase are mixed for a third time and allowed to stand for separation to obtain a water-oil bilayer penetration-enhancing cosmetic composition.

[0012] Optionally, the temperatures of the first mixture and the second mixture are each independently 75-80°C.

[0013] Compared with the prior art, the beneficial effects of this application include: The water-oil bilayer penetration-enhancing cosmetic composition provided in this application uses isosorbide dicaprylate to construct lipid microchannels, dipropylene glycol to enhance stratum corneum hydration, and glyceryl glucoside to activate AQP3 aquaporin. These three pathways synergistically improve penetration efficiency without damaging the skin barrier integrity. The penetration enhancer has a broad-spectrum penetration-enhancing ability for ingredients with different polarities, and the penetration-enhancing effect is stable, allowing for stable distribution in both the oil and water phases.

[0014] The method for preparing the water-oil two-layer penetration-enhancing cosmetic composition provided in this application is simple to operate and the raw materials are readily available. Attached Figure Description

[0015] To more clearly illustrate the technical solutions of the embodiments of this application, the accompanying drawings used in the embodiments will be briefly described below. It should be understood that the following drawings only show some embodiments of this application and should not be regarded as a limitation on the scope of this application.

[0016] Figure 1 This is a photograph of the water-oil dual-layer penetration-enhancing cosmetic composition provided in Example 1. Detailed Implementation

[0017] First, the solution provided in this application will be explained in more detail as follows: The first aspect of this application provides a water-oil dual-layer penetration-enhancing cosmetic composition, wherein the raw materials, based on a total mass of 100%, include: 5%-30% oil phase, 70%-95% aqueous phase; Optionally, the raw materials of the water-oil bilayer penetration-enhancing cosmetic composition, based on a total mass of 100%, may have an oil phase of any value between 5%, 10%, 15%, 20%, 25%, 30%, or 5-30%, and an aqueous phase of any value between 70%, 75%, 80%, 85%, 90%, 95%, or 70-95%. Preferably, the oil phase is 15%-20% and the aqueous phase is 80%-85%; The raw materials for the aqueous phase include dipropylene glycol, glycerol glucoside, and water; The raw materials for the oil phase include caprylic / capric triglyceride and isosorbide dicaprylate.

[0018] It is important to note that isosorbide dicaprylate is a mild bipolar ester compound with surface-active properties; dipropylene glycol, as a solvent and humectant, can enhance stratum corneum hydration; and glyceryl glucoside can activate aquaporin AQP3. When used individually, these three compounds have limited penetration-enhancing effects, and there are no reports of their combination in water-oil bilayer systems achieving synergistic broad-spectrum penetration enhancement.

[0019] Glyceryl glucoside (GG) has two configurations: 2-αGG and 2-βGG. Its structure is rich in multiple free hydroxyl groups, which can act as a broad-spectrum multi-hydroxyl hydrogen bond donor (HBD). The hydroxyl hydrogen atoms can not only form a main network with DPG and IDC, but also form secondary hydrogen bond pairings with the carbonyl, hydroxyl or amino groups of most polar active substances (including but not limited to nicotinamide, polyphenols, polysaccharides, alkaloids and peptides). This makes the active substance itself a participating component in the NADES-like structure on the skin surface. This solvent system blurs the solute-solvent boundary and avoids phase separation and crystallization in traditional carriers.

[0020] Isosorbide dioctanoate (IDC) contains a rigid bicyclic structure. The ether bond in the bicyclic structure can bind to HBD. Its octanoate chain can insert into the hydrophobic acyl chain region of the stratum corneum phospholipid bilayer, generating slight and continuous phospholipid spatial perturbation. At the same time, this structure can increase the solubility of oil-soluble components. The central ether bond oxygen atom in the dipropylene glycol (DPG) molecule can act as a hydrogen bond acceptor (HBA), forming a dynamic hydrogen bond network with αGG and active ingredients. This can more effectively prevent the excessive aggregation of active ingredient molecules. At the same time, DPG acts as a two-phase co-solvent, allowing water, lipids, and active ingredients to coexist in a single system on the skin surface, avoiding phase separation and achieving synchronous penetration.

[0021] The three work synergistically: isosorbide dicaprylate improves cellular lipid pathways, dipropylene glycol creates a hydration environment, and glyceryl glucoside, as a broad-spectrum HBD, makes the active ingredients more uniform on the skin surface and activates aquaporins. The three pathways work in parallel to achieve broad-spectrum penetration enhancement through a synergistic mechanism of forming a hydrogen bond network, lipid perturbation, and biphasic cosolubility, thereby significantly improving the transdermal delivery efficiency of active ingredients.

[0022] In some embodiments, the synergistic index CI of the oil-based double-layer penetration-enhancing cosmetic composition provided in this application is 1.93-2.12, and the penetration enhancement rate is 4.3-4.7 times higher than that without any added penetration enhancer, achieving a strong synergistic effect at a low total concentration (2.5%).

[0023] In some embodiments, the mass ratio of isosorbide dioctanoate, dipropylene glycol, and glyceryl glucoside is 0.2-2:0.2-4:0.2-4.

[0024] Optionally, the mass ratio of isosorbide dicaprylate, dipropylene glycol, and glyceryl glucoside can be any value between (0.2:0.2:0.2), (0.5:0.2:0.2), (1:0.2:0.2), (1.5:0.2:0.2), (2:0.2:0.2), (0.2:0.5:0.2), (0.2:1:0.2), (0.2:1.5:0.2), (0.2:2:0.2), (0.2:3:0.2), (0.2:4:0.2), (0.2:0.2:1), (0.2:0.2:2), (0.2:0.2:4) or 0.2-2:0.2-4:0.2-4.

[0025] In some embodiments, the mass ratio of caprylic / capric triglyceride to isosorbide dicaprylate is 3-29.8:0.2-2.

[0026] Optionally, the mass ratio of caprylic / capric triglyceride to isosorbide dicaprylate can be (3:0.2), (5:0.2), (10:0.2), (20:0.2), (29.8:0.2), (28:2) or any value between 3 and 29.8:0.2-2.

[0027] In some embodiments, the aqueous phase further includes disodium ethylenediaminetetraacetate and a preservative.

[0028] In some embodiments, the preservative includes p-hydroxyacetophenone and / or 1,2-hexanediol.

[0029] A second aspect of this application provides a method for preparing the aforementioned water-oil bilayer penetration-enhancing cosmetic composition, comprising: The raw materials in the aqueous phase are first mixed to obtain the aqueous phase; The raw materials for the oil phase are mixed a second time to obtain the oil phase; The aqueous phase and the oil phase are mixed for a third time and allowed to stand for separation to obtain a water-oil bilayer penetration-enhancing cosmetic composition.

[0030] In some embodiments, the temperatures of the first mixture and the second mixture are each independently 75-80°C.

[0031] Optionally, the temperatures of the first mixture and the second mixture can be independently any value between 75°C, 76°C, 77°C, 78°C, 79°C, 80°C, or 75°C-80°C.

[0032] A third aspect of this application provides a cosmetic product, comprising the aforementioned water-oil dual-layer penetration-enhancing cosmetic composition.

[0033] In some embodiments, the cosmetic product further includes active ingredients; The active ingredients include at least one of nicotinamide, tocopheryl acetate, acetyl glycosamine, and carnosine.

[0034] In some embodiments, the active ingredient accounts for 0.5%-2% of the mass of the cosmetic product.

[0035] The implementation schemes of this application will be described in detail below with reference to specific embodiments. However, those skilled in the art will understand that the following embodiments are only for illustrating this application and should not be regarded as limiting the scope of this application. Unless otherwise specified in the embodiments, conventional conditions or conditions recommended by the manufacturer shall apply. Reagents or instruments used without specified manufacturers are all conventional products that can be purchased commercially.

[0036] Example 1 The first aspect of this embodiment provides a water-oil bilayer penetration-enhancing cosmetic composition, the raw materials of which include: 15g oil phase and 85g water phase; The aqueous phase consists of 0.05g EDTA-2Na, 0.5g p-hydroxyacetophenone, 0.5g 1,2-hexanediol, 1g dipropylene glycol, 1g glyceryl glucoside and 81.95g water; The oil phase raw materials are 14.5g caprylic / capric triglyceride and 0.5g isosorbide dicaprylate.

[0037] The mass ratio of isosorbide dicaprylate, dipropylene glycol, and glyceryl glucoside is 1:1:1, and the mass ratio of caprylic / capric triglyceride and isosorbide dicaprylate is 14.5:0.5.

[0038] The second aspect of this embodiment provides a method for preparing a water-oil bilayer penetration-enhancing cosmetic composition, the specific steps of which are as follows: S1. Aqueous phase preparation: Dissolve the penetration enhancer (dipropylene glycol, glyceryl glucoside) in deionized water, then add EDTA-2Na, p-hydroxyacetophenone and 1,2-hexanediol, heat to 80℃ and stir until homogeneous; S2. Oil phase preparation: Caprylic / capric triglyceride and isosorbide dicaprylate are mixed, heated to 80°C, and stirred until homogeneous; S3. Mixing: Slowly add the oil phase to the aqueous phase; S4. Settling and Layering: Stop stirring, cool to 25°C, and let stand for 24 hours to form a stable double layer; S5. Filling: Fill directly while keeping the container still.

[0039] The actual photograph of the water-oil dual-layer penetration-enhancing cosmetic composition provided in this embodiment is shown below. Figure 1 As shown.

[0040] Example 2 This embodiment provides a water-oil bilayer penetration-enhancing cosmetic composition, the raw materials of which include: 15g oil phase and 85g water phase; The aqueous phase consists of 0.05g EDTA-2Na, 0.5g p-hydroxyacetophenone, 0.5g 1,2-hexanediol, 3g dipropylene glycol, 3g glyceryl glucoside, and 77.95g water. The oil phase raw materials are 13.5g caprylic / capric triglyceride and 1.5g isosorbide dicaprylate.

[0041] The mass ratio of isosorbide dicaprylate, dipropylene glycol, and glyceryl glucoside is 1.5:3:3, and the mass ratio of caprylic / capric triglyceride and isosorbide dicaprylate is 13.5:1.5.

[0042] The preparation method of the water-oil dual-layer penetration-enhancing cosmetic composition in this embodiment is the same as that in the previous embodiment.

[0043] Example 3 This embodiment provides a water-oil bilayer penetration-enhancing cosmetic composition, the raw materials of which include: 15g oil phase and 85g water phase; The aqueous phase consists of 3g dipropylene glycol, 3g glyceryl glucoside, and 79g water. The oil phase raw materials are 13.5g caprylic / capric triglyceride and 1.5g isosorbide dicaprylate.

[0044] The mass ratio of isosorbide dicaprylate, dipropylene glycol, and glyceryl glucoside is 1.5:3:3, and the mass ratio of caprylic / capric triglyceride and isosorbide dicaprylate is 13.5:1.5.

[0045] The preparation method of the water-oil dual-layer penetration-enhancing cosmetic composition in this embodiment is the same as that in the previous embodiment.

[0046] Examples 4-8 In addition, to verify different ratios of oil and water phases, this application also provides Examples 4-8, which are shown in Table 1.

[0047] Table 1. Types and amounts of raw materials used in Examples 4-8

[0048] Comparative Examples 1-7 This application also provides comparative examples 1-7, whose raw materials and amounts are different from those in example 2, as shown in Table 2.

[0049] Table 2. Types and amounts of raw materials used in Comparative Examples 1-7

[0050] This application conducted single-efficacy component tests on Examples 1-2 and Comparative Examples 1-7. The efficacy components included nicotinamide, tocopheryl acetate, acetylglucosamine, and carnosine. These four efficacy components were added to Examples 1-2 and Comparative Examples 1-7, respectively. The tested mass concentrations after adding nicotinamide were 2.0%, tocopheryl acetate was 0.5%, acetylglucosamine was 1.0%, and carnosine was 0.5%. Six parallel experiments (n=6) were conducted independently for each efficacy component. Only one component was tested on each excised pig skin sample. The cumulative permeation over 24 hours (μg / cm³) was measured. 2 The results for the enhancement rate (ER) are shown in Table 3.

[0051] Table 3 Single-function ingredient test

[0052] Note: Data are expressed as mean ± standard deviation (n=6), and only one component was tested for each excised pig skin sample.

[0053] Table 3 shows that the coefficient of variation (CV) for the penetration-enhancing effect of Example 1 on different polarity components (water / oil-soluble) is <5%, confirming its broad-spectrum nature and independence from the polarity of the active ingredient. Comparative Examples 2-4, using a single penetration enhancer component, demonstrated an enhancement rate of 4.27-4.55 times for water-soluble components such as nicotinamide, acetyl glucosamine, and carnosine, and an enhancement rate of 4.73 times for oil-soluble components such as tocopheryl acetate, with a CV <5% between polarities.

[0054] This application also conducted synergy index (CI) tests on Example 1 (with the addition of isosorbide dioctanoate (A), dipropylene glycol (B), and glyceryl glucoside (C) as three penetration enhancers), Comparative Examples 5-7 (with only two penetration enhancer components added), and the active ingredients (nicotinamide, tocopheryl acetate, acetyl glucosamine, and carnosine). The Loewe equivalent model was used, and a concentration correction factor was introduced to calculate CI = (A+B+C actual ER) / (A theoretical ER + B theoretical ER + C theoretical ER); where a higher CI indicates a more significant synergy; the specific test results are shown in Table 4.

[0055] Table 4 Collaborative Testing

[0056] This application also tested the steady-state permeation flux Jss and skin accumulation of the active ingredients (nicotinamide, tocopheryl acetate, acetyl glucosamine, and carnosine) in Example 1 and Comparative Example 1 (penetration enhancer blank group). The steady-state permeation flux Jss mainly measures the speed at which the active ingredient penetrates the skin barrier, characterizing the speed and ease with which the active ingredient enters the skin. The skin accumulation mainly measures the total amount of ingredients remaining in the skin, indicating how much of the effective ingredient ultimately remains in the skin. The test results of steady-state permeation flux Jss and skin accumulation are shown in Table 5.

[0057] Table 5. Steady-state osmotic flux Jss and skin accumulation

[0058] Note: Tocopheryl acetate is an oil-soluble component, and the difference between its accumulation in the skin and its penetration is consistent with its distribution characteristics.

[0059] To further verify the effect of the ratio of aqueous phase to oil phase on the penetration enhancement effect, this application also tested the 24-hour cumulative penetration of the active ingredient nicotinamide in Examples 1 and 4-8. The specific test results are shown in Table 6.

[0060] Table 6. Cumulative 24-hour permeation of nicotinamide

[0061] Note: Overall evaluation value The optimal oil phase mass ratio is 15%-20%, at which the penetration-enhancing effect reaches its peak. Within the entire range of 5%-30% oil phase mass ratio, the enhancement rate is >3.0 times, which is significantly better than Comparative Example 1 (p<0.05). An excessively high oil phase ratio (>30%) will reduce the penetration-enhancing efficiency due to increased viscosity and the oil film barrier effect.

[0062] The above tests show that when the water-oil bilayer penetration-enhancing cosmetic compositions provided in Comparative Examples 2-4 contain only one or two of dipropylene glycol, glyceryl glucoside, and isosorbide dicaprylate, the ER of the single penetration enhancer component in Comparative Examples 2-4 is much lower than that in Example 1 (the three components of dipropylene glycol, glyceryl glucoside, and isosorbide dicaprylate); when the water-oil bilayer penetration-enhancing cosmetic compositions provided in Comparative Examples 5-7 contain only two of dipropylene glycol, glyceryl glucoside, and isosorbide dicaprylate, the synergistic index CI is much lower than that in Example 1.

[0063] The water-oil bilayer penetration-enhancing cosmetic composition provided in this application has a significant synergistic effect: the addition of dipropylene glycol, glyceryl glucoside and isosorbide dioctanoate makes the synergistic index CI reach 1.93-2.12, achieving the effect of "1+1+1>3"; The water-oil bilayer penetration-enhancing cosmetic composition provided in this application exhibits excellent broad-spectrum properties: the penetration enhancement rate for water-soluble (nicotinamide, acetyl glucosamine, carnosine) and oil-soluble (tocopheryl acetate) components remains stable at 4.3-4.7 times, and the coefficient of variation (CV) between polarities is <5%. The water-oil dual-layer penetration-enhancing cosmetic composition provided in this application is mild and safe: according to TEWL and skin erythema index tests, there was no significant difference between all experimental groups and the blank group (p>0.05), and it does not damage the skin barrier; The water-oil bilayer penetration-enhancing cosmetic composition system provided in this application has strong compatibility: it is effective in a wide range of oil phase ratios from 5% to 30%, and is suitable for various water-oil bilayer formulations. The cost optimization of the water-oil bilayer penetration-enhancing cosmetic composition provided in this application: the optimal concentration (isosorbide dioctanoate 0.5%, dipropylene glycol 1.0%, glyceryl glucoside 1.0%) achieves the best effect, and higher concentrations do not provide significant benefits.

[0064] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of this application, and are not intended to limit them. Although this application has been described in detail with reference to the foregoing embodiments, those skilled in the art should understand that modifications can still be made to the technical solutions described in the foregoing embodiments, or equivalent substitutions can be made to some or all of the technical features therein. Such modifications or substitutions do not cause the essence of the corresponding technical solutions to deviate from the scope of the technical solutions of the embodiments of this application.

[0065] Furthermore, those skilled in the art will understand that although some embodiments herein include certain features included in other embodiments but not others, combinations of features from different embodiments are intended to be within the scope of this application and form different embodiments. For example, any of the claimed embodiments can be used in any combination. The information disclosed in this background section is intended only to enhance the understanding of the general background of this application and should not be construed as an admission or in any way implying that such information constitutes prior art known to those skilled in the art.

Claims

1. A water-oil dual-layer penetration-enhancing cosmetic composition, characterized in that, Its raw materials, calculated on a 100% basis by total mass, include: 5%-30% oil phase, 70%-95% aqueous phase; The raw materials for the aqueous phase include dipropylene glycol, glycerol glucoside, and water; The raw materials for the oil phase include caprylic / capric triglyceride and isosorbide dicaprylate.

2. The water-oil dual-layer penetration-enhancing cosmetic composition according to claim 1, characterized in that, The mass ratio of isosorbide dioctanoate, dipropylene glycol, and glyceryl glucoside is 0.2-2:0.2-4:0.2-4.

3. The water-oil dual-layer penetration-enhancing cosmetic composition according to claim 1, characterized in that, The mass ratio of the caprylic / capric triglyceride to the isosorbide dicaprylate is 3-29.8:0.2-2.

4. The water-oil dual-layer penetration-enhancing cosmetic composition according to claim 1, characterized in that, The aqueous phase also includes disodium ethylenediaminetetraacetate and preservatives.

5. The water-oil dual-layer penetration-enhancing cosmetic composition according to claim 4, characterized in that, The preservatives include p-hydroxyacetophenone and / or 1,2-hexanediol.

6. A method for preparing the water-oil bilayer penetration-enhancing cosmetic composition according to any one of claims 1-5, characterized in that, include: The raw materials in the aqueous phase are first mixed to obtain the aqueous phase; The raw materials for the oil phase are mixed a second time to obtain the oil phase; The aqueous phase and the oil phase are mixed for a third time and allowed to stand for separation to obtain a water-oil bilayer penetration-enhancing cosmetic composition.

7. The method for preparing the water-oil bilayer penetration-enhancing cosmetic composition according to claim 6, characterized in that, The temperatures of the first mixture and the second mixture are each independently 75-80°C.

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