Water-soluble transparent ceramide composition as well as preparation method and application method thereof

Abstract

The invention belongs to the technical direction of cosmetics, and relates to a water-soluble transparent ceramide composition as well as a preparation method and an application method thereof. The ceramide composition is prepared from ceramide, a solubilizer, a solvent and water, wherein the solubilizer is prepared from at least two of sucrose stearate, sucrose laurate, PEG-40 hydrogenated castor oil, PPG-26-butanol polyether-26, polyglycerol-6 octoate, poloxamer 184 and PEG-60 hydrogenated castor oil; the solvent is prepared from at least two of glycerol, butanediol, methylpropanediol, 1, 3-propylene glycol, 1, 2-pentanediol, dipropylene glycol, isosorbide dimethyl ether, diethoxy diethylene glycol and succinic acid diethoxy ethyl ester; the solvent is prepared from at least two of glycerol, butanediol, methylpropanediol, 1, 3-propylene glycol, 1, 2-pentanediol, dipropylene glycol, isosorbide dimethyl ether, diethoxy diethylene glycol and succinic acid diethoxy ethyl ester; the ceramide composition prepared according to the matching of the raw materials is water-soluble, colorless and transparent, also has excellent moisturizing performance, is good in skin delivery effect, and has a relatively good application prospect.

Description

Technical Field

[0001] The present invention belongs to the field of cosmetics technology and relates to a water-soluble transparent ceramide composition and a preparation method and an application method thereof. Background Art

[0002] Ceramide is composed of a sphingosine base (hydrophilic head) and a fatty acid (lipophilic tail) connected by an amide bond to form an "amphiphilic" molecule that can form a stable lipid film on the skin surface.

[0003] Ceramide can be exogenously supplemented into the intercellular lipid gaps to restore the integrity of the barrier and reduce transepidermal water loss, making it suitable for people with damaged barriers. Its lipophilic tail combines with water molecules to form a "hydration film", which, when combined with ingredients such as glycerol and hyaluronic acid, can achieve dual protection of outer film-forming and water-locking and inner moisture-absorbing and hydrating. It can also soften the stratum corneum, reduce desquamation and roughness, and reduce skin roughness. It can also block the NF-κB signaling pathway, reduce the release of inflammatory mediators such as IL-6 and TNF-α, relieve redness and itching, reduce damage to the skin caused by external stimuli, and reduce the frequency of sensitive skin attacks. It can also be compounded with antioxidants such as vitamin E and resveratrol to deeply scavenge free radicals and reduce collagen degradation. It can also promote cell renewal, regulate the differentiation cycle of keratinocytes, accelerate the generation of new cells, and improve fine lines and dullness.

[0004] The poor water solubility of ceramides is a core technical challenge in their application in cosmetics. This property directly impacts product stability, efficacy release, skin delivery, and formulation compatibility. Therefore, providing a water-soluble, transparent ceramide composition and its application in cosmetics to expand the functional strength of cosmetics is a currently unresolved technical challenge. Summary of the Invention

[0005] In response to the above technical problems, the present application proposes a water-soluble transparent ceramide composition and a preparation method and application method thereof.

[0006] In one aspect, the present invention provides a water-soluble transparent ceramide composition, the raw materials of which include: ceramide, a solubilizer, a solvent and water.

[0007] In a specific embodiment, the solubilizer includes at least two of sucrose stearate, sucrose laurate, PEG-40 hydrogenated castor oil, PPG-26-buteth-26, polyglyceryl-6 caprylate, poloxamer 184, and PEG-60 hydrogenated castor oil.

[0008] In a specific embodiment, the solvent includes at least two of glycerol, butylene glycol, methylpropylene glycol, 1,3-propylene glycol, 1,2-pentanediol, dipropylene glycol, dimethyl isosorbide, diethoxydiglycol, and diethoxyethyl succinate. The solvent described in the present invention is a non-aqueous solvent.

[0009] In a specific embodiment, the raw materials of the composition include, by weight percentage, 0.05-20% ceramide, 2-10% solubilizer, 5-40% solvent and the balance water.

[0010] In a specific embodiment, the weight percentage of ceramide can also be any value or range of 0.05%, 0.1%, 0.5%, 1%, 5%, 10%, 15%, or 20%.

[0011] In a specific embodiment, the weight percentage of the solubilizer can be any value or range of 2%, 4%, 5%, 7%, 8%, 9%, or 10%.

[0012] In a specific embodiment, the weight percentage of the solvent can also be any value or range of 5%, 10%, 20%, 25%, 30%, 35%, or 40%.

[0013] In one embodiment, the solubilizer includes 1-5% sucrose stearate and 1-4% polyglyceryl-6 caprylate. The combination of the two can effectively improve the solubility and stability of the ceramide in the composition, enhance its delivery to the skin, and impart excellent performance to the composition.

[0014] In a specific embodiment, the weight ratio of sucrose stearate to polyglyceryl-6 caprylate is 1:0.5-1.5. The selection of the ratio described in the present invention can further reduce the zeta potential of the composition and impart excellent stability to the composition.

[0015] Another aspect of the present invention provides a method for preparing a water-soluble transparent ceramide composition, comprising:

[0016] (1) heating and stirring the solvent and ceramide to obtain an oil phase;

[0017] (2) heating and stirring water and a solubilizing agent to obtain an aqueous phase;

[0018] (3) Add the oil phase to the water phase and stir to obtain a water-soluble transparent ceramide composition.

[0019] In a specific embodiment, the heating temperature in (1) is 35-55°C; and the heating temperature in (2) is 40-60°C.

[0020] The present invention also provides use of the water-soluble transparent ceramide composition in preparing cosmetics.

[0021] In a specific embodiment, the cosmetic contains 0.1-10 wt % of the water-soluble transparent ceramide composition.

[0022] The beneficial effects of the present invention are as follows:

[0023] The present invention uses ceramide, a solubilizer, a solvent and water to prepare a ceramide composition, wherein the solubilizer includes at least two of sucrose stearate, sucrose laurate, PEG-40 hydrogenated castor oil, PPG-26-butanediol-26, polyglyceryl-6 caprylate, poloxamer 184 and PEG-60 hydrogenated castor oil; the solvent includes at least two of glycerin, butylene glycol, methylpropanediol, 1,3-propylene glycol, 1,2-pentanediol, dipropylene glycol, dimethyl isosorbide, diethoxydiglycol and diethoxyethyl succinate; the ceramide composition prepared by combining the above raw materials is water-soluble, colorless and transparent, and also has excellent moisturizing properties and good skin delivery effect.

[0024] The composition prepared by the present invention has a zeta potential of -53.32 mV, a large absolute value, and excellent product stability. After high-temperature storage, the absolute value of the potential remains large, indicating high stability, high potential retention, and high stability in appearance and color.

[0025] The present invention uses sucrose stearate and polyglycerol-6 caprylate to synergistically enhance the stability of the composition at room temperature and high temperature. The present invention selects a composition with a ratio of sucrose stearate to polyglycerol-6 caprylate of 1:0.5-1.5, which has higher stability.

[0026] The composition prepared by the present invention exhibits a transparent appearance. The ceramide composition obtained by the present invention exhibits excellent moisturizing effects. Furthermore, the combination of sucrose stearate and polyglyceryl-6 caprylate influences the product's moisturizing properties. The combination of the two effectively delivers and promotes skin absorption, resulting in a product with enhanced moisturizing properties.

[0027] The use of methanol-extracted sea daffodil extract and ethanol-extracted verbena extract in cosmetics can significantly enhance the anti-aging effect. The combination of the two can produce a synergistic effect, giving the product excellent antioxidant properties. BRIEF DESCRIPTION OF THE DRAWINGS

[0028] Figure 1 : Comparison of appearance between water and composition 1 of the present invention.

[0029] Figure 2 : The water content T2 and T4 of the cheeks of each group before using the samples, two weeks and four weeks after using the samples (unit: au).

[0030] Figure 3: The increase rate of water content K2 and K4 (unit %) in each group after two weeks and four weeks of use compared with before use.

[0031] Figure 4 : DPPH radical scavenging efficiency. DETAILED DESCRIPTION

[0032] The present invention further illustrates the scheme of the present invention through the following specific implementation methods, so as to better explain and demonstrate the technology of the present invention.

[0033] In one aspect, the present invention provides a water-soluble transparent ceramide composition, the raw materials of which include: ceramide, a solubilizer, a solvent and water.

[0034] Furthermore, the solubilizer includes at least two of sucrose stearate, sucrose laurate, PEG-40 hydrogenated castor oil, PPG-26-buteth-26, polyglyceryl-6 caprylate, poloxamer 184, and PEG-60 hydrogenated castor oil.

[0035] Furthermore, the solvent includes at least two of glycerol, butylene glycol, methylpropylene glycol, 1,3-propylene glycol, 1,2-pentanediol, dipropylene glycol, dimethyl isosorbide, diethoxydiglycol, and diethoxyethyl succinate.

[0036] Furthermore, the raw materials of the composition include, by weight percentage, 0.05-20% ceramide, 2-10% solubilizer, 5-40% solvent and the balance water.

[0037] Furthermore, the weight percentage of ceramide can be any value or range including 0.05%, 0.1%, 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 8%, 10%, 12%, 15%, or 20%. The weight percentage of solubilizer can be any value or range including 2%, 4%, 5%, 7%, 8%, 9%, or 10%. The weight percentage of solvent can be any value or range including 5%, 10%, 20%, 25%, 30%, 35%, or 40%.

[0038] In one embodiment, the solubilizer comprises 1-5% sucrose stearate and 1-4% polyglyceryl-6 caprylate. This combination effectively improves the solubility and stability of the ceramide in the composition, enhancing its delivery to the skin and imparting excellent performance to the composition. The weight ratio of sucrose stearate to polyglyceryl-6 caprylate is 1:0.5-1.5. This ratio further reduces the zeta potential of the composition and imparts excellent stability.

[0039] Another aspect of the present invention provides a method for preparing a water-soluble transparent ceramide composition, comprising: (1) heating and stirring a solvent and ceramide to obtain an oil phase; (2) heating and stirring water and a solubilizing agent to obtain an aqueous phase; and (3) adding the oil phase to the aqueous phase and stirring to obtain the water-soluble transparent ceramide composition. Furthermore, the heating temperature in (1) is 35-55° C.; and the heating temperature in (2) is 40-60° C.

[0040] The present invention also provides use of the water-soluble transparent ceramide composition in preparing cosmetics. The cosmetic contains 0.1-10 wt% of the water-soluble transparent ceramide composition. Furthermore, the cosmetic may also contain 0.1-2% of sea daffodil extract, 0.1-2% of aloe vera extract, and 0.1-2% of verbena leaf extract.

[0041] In a specific embodiment, the aloe vera extract is obtained by pulping the flesh of the aloe vera leaves with water, heating and stirring, filtering, concentrating and freeze-drying. The sea daffodil extract is obtained by pulping the sea daffodil with water, adding methanol to adjust the methanol weight concentration to 15-30%, heating and stirring, centrifuging, filtering, concentrating and freeze-drying. The verbena leaf extract is obtained by pulping the leaves of verbena with water, adding ethanol to adjust the ethanol weight concentration to 20-35%, heating and stirring, centrifuging, filtering and concentrating, and freeze-drying. The sea daffodil extract obtained by the above-mentioned methanol extraction and the verbena extract obtained by the ethanol extraction are used in cosmetics to synergistically enhance the anti-aging effect of cosmetics.

[0042] Example 1

[0043] 1. Preparation of ceramide composition

[0044] The raw materials and amounts (weight percentages) of the ceramide composition are shown in Table 1.

[0045] Table 1: Ceramide composition

[0046]

[0047] In Table 1, sucrose stearate is sucrose stearate SE-16. Butylene glycol is 1,3-butylene glycol. Sucrose stearate, polyglyceryl-6 caprylate, PPG-26-buteth-26, and poloxamer 184 serve as solubilizers. Glycerin, butylene glycol, 1,2-pentanediol, and dipropylene glycol serve as solvents.

[0048] The preparation method of the above composition is as follows: (1) heating the solvent and ceramide to 50°C, maintaining the temperature and stirring at 300 rpm for 40 minutes to obtain an oil phase; (2) heating water and a solubilizer to 55°C and stirring at 200 rpm for 20 minutes to obtain an aqueous phase; (3) adding the oil phase to the aqueous phase, maintaining the temperature at 45°C and stirring at 350 rpm for 50 minutes, and sterilizing to obtain a ceramide composition.

[0049] Example 2

[0050] The potential Z1 of the water-soluble transparent ceramide composition prepared above was measured using nanoparticle size and zeta potential analysis and a titrator. Three replicate measurements were performed and the average value was calculated. After the water-soluble transparent ceramide composition was stored at 50°C for 14 days, its potential Z2 was measured again, and the average value was calculated for three replicate measurements. The potential retention rate was then calculated based on the Z2 / Z1 ratio. The stability parameters of the compositions are shown in Table 1. In Table 2, serial numbers 1-8 represent compositions 1-8, respectively.

[0051] Table 2: Composition stability

[0052]

[0053]

[0054] Combined with the test results in Table 2, it can be seen that the composition prepared by the present invention has a zeta potential of -53.32 mV, a large absolute value, and excellent product stability. After high-temperature storage, the absolute value of the potential remains large, indicating high stability, high potential retention, and high stability in appearance and color.

[0055] According to compositions 1, 8, it is known that after sucrose stearate and butylene glycol are omitted in the composition, the Zeta potential of the product changes significantly, and the composition stability is very poor. When the total amount of sucrose stearate and polyglycerol-6 caprylate in composition 1 is the same as the sucrose stearate or polyglycerol-6 caprylate dosage of the independent sucrose stearate or polyglycerol-6 caprylate of composition 4-5, the absolute value of the normal temperature and high temperature potential value of composition 1 and the potential retention rate are higher, indicating that the normal temperature and high temperature stability of composition 1 is better, and it can be seen that the present invention adopts sucrose stearate and polyglycerol-6 caprylate to coordinately enhance the normal temperature and high temperature stability of composition. And according to compositions 1, 6-7 test results, when keeping sucrose stearate and polyglycerol-6 caprylate collocation total amount unchanged, the effect of composition 6-7 of changing the ratio of the two is lower than composition 1, that is, the present invention selects sucrose stearate and polyglycerol-6 caprylate amount ratio to be 1: the stability of the composition when 0.5-1.5 is higher.

[0056] At the same time, the appearance of water and composition 1 were compared, and the results were shown in FIG. Figure 1( Figure 1 The left side is water, and the right side is composition 1 (3% ceramide). Visual inspection shows that the composition prepared by the present invention has a transparent appearance.

[0057] Example 3

[0058] 1. Purpose and Principle

[0059] 1.1. Purpose of the Test

[0060] The water content of the skin stratum corneum of the population was measured at the initial value before using the samples, and at 2 weeks and 4 weeks after using the samples.

[0061] 1.2 Test Principle

[0062] Water content of the skin stratum corneum: The larger the water content value of the skin stratum corneum, the higher the water content of the skin stratum corneum.

[0063] 2. Materials

[0064] 2.1 Sample Information

[0065] Table 3 Basic information of samples

[0066] Sample name Specification form Ceramide composition 100g / bottle liquid

[0067] 2.2. Subjects: A total of 20 female volunteers (divided into 4 groups, 5 people in each group), aged 30 to 55 years old, with an average age of 43±5 years old, met the subject selection criteria.

[0068] 3. Instruments

[0069] Stratum corneum hydration meter (MSC1201, Delfin).

[0070] 4. Testing environment

[0071] Test environment temperature: 20-22℃; humidity: 40-60%; dynamic monitoring.

[0072] 5. Test methods

[0073] 5.1. During the first visit, the subjects were given an explanation of the trial and signed the informed consent form.

[0074] 5.2. The subjects participating in the trial were screened according to the experimental requirements, and 20 people were selected to enter the experimental phase.

[0075] 5.3. On the day of the test, the subject should clean their face and equilibrate in the test environment for 20 minutes. Then, the stratum corneum hydration meter will be used to measure the observed area (five points on the cheek).

[0076] 5.4. After the measurement is completed, the sample usage instructions are given and the sample is distributed. Use once a day, morning and evening. Apply an appropriate amount of sample to the test area on the face each time. Confirm the sample weight at the beginning and end of the test.

[0077] 5.5. Use a stratum corneum hydration meter to measure the stratum corneum water content (au) at five points on the cheek at designated return visit time points.

[0078] 6. Test results

[0079] 6.1. Sample Completion Status

[0080] A total of 20 people were enrolled in the group, and 20 people finally completed the test.

[0081] 6.2 Product Usage and Tolerance Feedback

[0082] Each subject used the test sample as required within the specified time and no adverse reactions were observed.

[0083] 6.3 Instrument test results

[0084] The water content T2 and T4 (unit: au) of the cheeks of each group before using the samples, two weeks after using the samples and four weeks after using the samples are shown in the table. Figure 2 .

[0085] The increase in water content K2 and K4 (unit: %) after two weeks and four weeks of use in each group compared with before use is shown in the table. Figure 3 .

[0086] Combine Figure 2-3 The test results show that the ceramide composition obtained by the present invention has excellent moisturizing effects. The combination of sucrose stearate and polyglyceryl-6 caprylate affects the moisturizing performance of the product. The combination of the two can effectively deliver and promote skin absorption, making the product more moisturizing.

[0087] Example 4

[0088] Aloe extract: add 10 times the weight of water to the flesh of aloe leaves and beat into a pulp, heat to 45°C, keep warm and stir at 60 rpm for 1 hour, filter through 80 mesh gauze, concentrate under reduced pressure at 60°C to a weight of 13.6% of the filtrate, and freeze-dry at -50°C to a water content of 2.47% by weight.

[0089] Pancratium maritimum extract: The bulbs of Pancratium maritimum are pulped with 15 times their weight of water. Methanol is added to adjust the methanol concentration to 25% by weight. The extract is heated to 45°C and stirred at 100 rpm for 3.5 hours. The extract is then centrifuged at 800 rpm for 10 minutes to remove the precipitate. The extract is filtered through a 1μm filter membrane, and the filtrate is concentrated under reduced pressure at 50°C to 15.6% by weight. The extract is then freeze-dried at -50°C to a water content of 1.95% by weight.

[0090] Verbena leaf extract: Add 20 times the weight of water to the leaves of verbena to make a pulp, add ethanol to adjust the ethanol weight concentration to 30%, heat to 50°C and keep warm while stirring at 110 rpm for 3 hours, then centrifuge at 800 rpm for 10 minutes to remove the precipitate, filter through a 1 μm filter membrane, and concentrate the filtrate under reduced pressure at 55°C to 18.3% by weight of the filtrate, and then freeze-dry at -50°C to a water content of 2.38% by weight.

[0091] The ceramide composition and the above-mentioned raw materials were combined to prepare cosmetic products. The products were then tested for their ability to inhibit tyrosinase activity. The compositions of the products are shown in Table 4 below, measured in weight percentage.

[0092] Table 4: Product composition

[0093]

[0094]

[0095] The preparation method of the above product is as follows: heat water to 45°C, add ceramide composition 1, aloe extract, sea daffodil extract, and verbena leaf extract in sequence, stir at 120 rpm for 0.7 hours, sterilize, naturally cool to room temperature, and fill to obtain the product.

[0096] Example 5

[0097] The above products 1-5 were tested for their antioxidant effects, specifically testing their inhibition rates on DPPH free radicals.

[0098] Preparation of DPPH working solution: DPPH was dissolved in 9 wt % ethanol aqueous solution to a concentration of 0.15 mg / mL.

[0099] Preparation of test drugs: Products 1-5 were diluted with deionized water to a weight concentration of 0.04 mg / mL to obtain samples.

[0100] Group configuration: Mix 0.5 mL of the above sample with 2.5 mL of the working solution, and place it at room temperature in the dark for half an hour to obtain the experimental solution; replace the above sample with an equal volume of ethanol and mix it with 2.5 mL of the working solution, and place it at room temperature in the dark for half an hour to obtain the blank solution.

[0101] Test process: Before testing, use a UV-visible light photometer to zero the instrument with 50% ethanol water solution; then measure the absorbance OD of the experimental solution and the blank solution at 517nm, and calculate the scavenging efficiency S value of DPPH free radicals, where S = 100% × (OD 空白药液 -OD experimental solution) / OD blank solution; OD blank solution represents the absorbance value of blank solution at 517nm, and OD experimental solution represents the absorbance value of experimental solution at 517nm. Figure 4 .

[0102] according to Figure 4 The test results show that the use of sea daffodil extract obtained by methanol extraction and verbena extract obtained by ethanol extraction in cosmetics can significantly enhance the anti-aging effect. The combination of the two can produce a synergistic effect, giving the product excellent antioxidant properties.

Claims

1. A water-soluble transparent ceramide composition, characterized in that Ingredients include: Ceramide, solubilizer, solvent and water.

2. A water-soluble transparent ceramide composition according to claim 1, characterized in that The solubilizer includes at least two of sucrose stearate, sucrose laurate, PEG-40 hydrogenated castor oil, PPG-26-buteth-26, polyglyceryl-6 caprylate, poloxamer 184, and PEG-60 hydrogenated castor oil.

3. The water-soluble transparent ceramide composition according to claim 1, characterized in that: The solvent includes at least two of glycerol, butylene glycol, methylpropylene glycol, 1,3-propylene glycol, 1,2-pentanediol, dipropylene glycol, dimethyl isosorbide, diethoxydiglycol, and diethoxyethyl succinate.

4. The water-soluble transparent ceramide composition according to claim 1, characterized in that Calculated by weight percentage, the raw materials include: 0.05-20% ceramide, 2-10% solubilizer, 5-40% solvent and the balance water.

5. A water-soluble transparent ceramide composition according to claim 4, characterized in that: Solubilizers include 1-5% sucrose stearate and 1-4% polyglyceryl-6 caprylate.

6. The water-soluble transparent ceramide composition according to claim 4, characterized in that: The weight ratio of sucrose stearate to polyglyceryl-6 caprylate is 1:0.5-1.

5.

7. A method for preparing the water-soluble transparent ceramide composition according to any one of claims 1 to 6, characterized in that: include: (1) heating and stirring the solvent and ceramide to obtain an oil phase; (2) heating and stirring water and a solubilizing agent to obtain an aqueous phase; (3) Add the oil phase to the water phase and stir to obtain a water-soluble transparent ceramide composition.

8. The preparation method according to claim 7, characterized in that (1) The medium heating temperature is 35-55°C; (2) The medium heating temperature is 40-60°C.

9. Use of the water-soluble transparent ceramide composition according to any one of claims 1 to 6 in the preparation of cosmetics.

10. A cosmetic, characterized in that: Contains 0.1-10 wt% of the water-soluble transparent ceramide composition according to any one of claims 1-6.

Images