A whitening composition suitable for sensitive skin that improves skin resistance and self-healing ability and its application

Abstract

The present invention discloses a whitening composition and application thereof for enhancing skin resistance and self-healing power suitable for sensitive skin, belonging to the technical field of cosmetics; the whitening composition provided by the present invention includes the following components in parts by mass: 0.1-3 parts of mulberry root extract, 0.1-3 parts of golden camellia extract, 0.01-1 parts of wood apple extract, 0.1-3 parts of andrographis paniculata extract, and 0.01-1 parts of epigallocatechin gallate. The present invention is compounded by selecting components in an appropriate mass ratio, and the obtained whitening composition can effectively promote the production and secretion of human beta defensins in the skin barrier, thereby effectively enhancing the tight junction function of the skin barrier, improving the resistance of the skin, and can effectively promote the metabolism of the skin, activate the skin's self-healing power and gently whiten the skin.

Description

Technical Field

[0001] The present invention belongs to the technical field of cosmetics, and in particular relates to a whitening composition suitable for sensitive skin and capable of improving skin resistance and self-healing ability, and an application thereof. Background Art

[0002] The stratum corneum is the outermost layer of the epidermis and is the main permeability and protective barrier of the skin. The different components of the stratum corneum, including keratinocytes, natural moisturizing factors, various enzymes and their inhibitors, antimicrobial peptides and antimicrobial lipids, interact to maintain the barrier function. The main barrier properties of the stratum corneum are to prevent water loss from the skin, prevent infection, and prevent the skin from contacting potentially harmful exogenous factors. Simply put, a good skin barrier function reduces the loss of water from the skin, achieving a "water-locking" effect, which is beneficial for skin moisturization and preventing skin dryness. Externally, it can reduce the erosion of the skin by ultraviolet rays (UV waves), chemicals (inferior detergents, bath products and cosmetics, secondhand smoke, PM2.5, etc.), microorganisms (viruses, bacteria), and dust (pollen, dust, exhaust gas, etc.).

[0003] Disturbances in the barrier function of the stratum corneum can lead to various skin problems, such as dry skin, flaking, or skin sensitivity. Currently, skin care products on the market that address dry skin, damaged skin barriers, or sensitive skin only focus on replenishing lipids and natural moisturizing factors, such as adding large amounts of moisturizing ingredients like squalane and hyaluronic acid. They do not focus on enhancing the skin's own resistance or activating its self-healing ability. Furthermore, skin whitening generally requires strong efficacy, and most whitening skin care products or whitening ingredients on the market have irritation issues. Therefore, for sensitive skin, there is a lack of skin care products or ingredients that can repair sensitivity, barrier damage, and gently whiten the skin. Summary of the Invention

[0004] The purpose of the present invention is to overcome the shortcomings of the above-mentioned prior art and provide a whitening composition and application thereof suitable for sensitive skin that has excellent skin resistance and self-healing ability enhancement and good whitening effect.

[0005] To achieve the above objectives, in a first aspect of the present invention, the present invention provides a whitening composition for enhancing skin resistance and self-healing ability, wherein the whitening composition comprises the following components in parts by mass: 0.1-3 parts of mulberry root extract, 0.1-3 parts of camellia chrysantha extract, 0.01-1 parts of wood apple extract, 0.1-3 parts of andrographis paniculata extract, and 0.01-1 parts of epigallocatechin gallate.

[0006] A good skin barrier gives the skin strong resistance, and the tight junctions of the stratum corneum are a key defense mechanism within the skin barrier. The antimicrobial peptide human β-defensin-3 (HBD3) in the human skin barrier can improve the tight junction barrier function of keratinocytes, increasing the barrier's resistance to external stimuli and reducing discomfort in people with sensitive skin, including redness, stinging, and itching. Furthermore, HBD3 can activate cellular autophagy, promoting the phagocytosis of old, dead skin cells and boosting skin metabolism. This stimulates the skin's self-healing ability and promotes self-repair, shortening recovery time for those with skin damage, especially those with barrier damage and breakouts. Furthermore, because HBD3 is also an inhibitor of the melanocortin 1 receptor (MC1R), a gene that controls the production and distribution of melanin in melanocytes, promoting HBD3 production can also achieve a certain whitening effect. The present invention has found that by selecting specific components within a specific mass range in the whitening composition of the present invention for compounding, the components have excellent synergistic effects, which can effectively promote the production and secretion of human β-defensin (HBD3) in the skin barrier, thereby effectively improving the tight junction function of the skin barrier, enhancing the skin's resistance, and effectively promoting skin metabolism, activating the skin's self-healing ability and gently whitening the skin.

[0007] Specifically, mulberry root is the dried root bark of the mulberry plant (Morus alba L.) of the Moraceae family. It is one of the commonly used Chinese medicinal materials in clinical practice. It has the effects of clearing the lungs and relieving asthma, promoting diuresis and reducing swelling, and is often used to treat diseases such as lung heat, asthma, cough, and facial and skin edema. The chemical components of mulberry root extract are mainly flavonoids, stilbene, glycosides and other types of compounds. In the cosmetics field, it can be used for whitening, anti-oxidation, and moisturizing, and can also help improve rough skin and anti-inflammatory.

[0008] Camellia chrysantha extract is rich in tea polyphenols, tea polysaccharides, proteins, amino acids, multiple vitamins, selenium, iron, zinc and other trace elements. It can be used to enhance skin immunity, provide meticulous and complete nutritional supplements and repairs to the skin, promote DNA damage repair, and enhance skin health.

[0009] Wood apple, also known as "elephant orange / Thanaka", is a traditional medicinal plant in Southeast Asia and India. Its bark is ground into powder and made into "Thanaka", a traditional Myanmar cosmetic, which has the functions of covering, whitening, moisturizing and sun protection. In the cosmetic field, wood apple extract can resist aging, prevent photodamage, promote skin cell metabolism, and improve skin quality.

[0010] Andrographis paniculata, often called the "king of bitterness", has the main active ingredient andrographolide, which has anti-inflammatory, antibacterial, anti-tumor, anti-diabetic, antimalarial and liver-protective effects. Studies have shown that Andrographis paniculata extract has a strong anti-inflammatory and antibacterial effect on the skin and can reduce cellular inflammation caused by oxidative stress.

[0011] Epigallocatechin gallate (EGCG) is an ester formed by gallocatechin and gallic acid. It is a catechin purified from tea tree extract. As an antioxidant, it has strong antioxidant ability and can prevent skin aging to a certain extent.

[0012] The present invention has found that only when the above components are compounded according to the ratio of the present invention can excellent effects be achieved, effectively increasing the skin's resistance and self-healing ability, as well as enhancing the skin's metabolism, to achieve gentle skin whitening.

[0013] As a preferred embodiment of the whitening composition of the present invention, the whitening composition includes the following components in parts by mass: 1-2 parts of mulberry root extract, 1-2 parts of camellia chrysantha extract, 0.5-0.8 parts of wood apple extract, 1-1.8 parts of andrographis paniculata extract, and 0.5-0.8 parts of epigallocatechin gallate.

[0014] The present invention has found that the mass parts of the components in the whitening composition will also affect the overall performance of the product. When the mass parts of the components are further selected to be within the above-mentioned range, it can better promote the production and secretion of human β-defensins in the skin barrier, thereby improving the skin barrier capacity. At the same time, it can also enhance the skin's resistance, self-healing ability and metabolic capacity, thereby achieving gentle skin whitening.

[0015] As a preferred embodiment of the whitening composition of the present invention, the ratio of the sum of the mass of the mulberry root extract and the camellia chrysantha extract to the sum of the mass of the wood apple extract, andrographis paniculata extract and epigallocatechin gallate is 1:(0.75-1.05).

[0016] Exemplarily, the ratio of the sum of the masses of the mulberry root extract and the camellia chrysantha extract to the sum of the masses of the wood apple extract, andrographis paniculata extract and epigallocatechin gallate can be any point value or any two-point range value between 1:(0.75-1.05), such as 1:0.75, 1:78, 1:80, 1:82, 1:84, 1:86, 1:88, 1:90, 1:92, 1:94, 1:96, 1:0.98, 1:1.0, 1:1.05, etc.

[0017] The present invention has found that the ratio of the sum of the masses of mulberry root extract and camellia chrysantha extract to the sum of the masses of wood apple extract, andrographis paniculata extract and epigallocatechin gallate will affect the synergistic effect between the components. When the ratio of the sum of the masses of mulberry root extract and camellia chrysantha extract to the sum of the masses of wood apple extract, andrographis paniculata extract and epigallocatechin gallate is further selected to be within the above range, the comprehensive performance of the obtained whitening composition is better.

[0018] As a preferred embodiment of the whitening composition of the present invention, in the whitening composition, the mass percentage of the Andrographis paniculata extract is 18-30%.

[0019] Illustratively, in the whitening composition, the mass percentage of the Andrographis paniculata extract can be any point value or any two point range values between 18-30%, such as 18%, 20%, 22%, 24%, 26%, 28%, 30%, etc.

[0020] The present invention has found that the mass percentage of Andrographis paniculata extract in the whitening composition not only affects the production and secretion effect of the whitening composition on human β-defensin in the skin barrier, thereby affecting the improvement of the skin barrier capacity; it also affects the skin's self-healing ability and resistance, and also affects the skin's whitening effect.

[0021] As a preferred embodiment of the whitening composition of the present invention, the preparation method of the mulberry root extract comprises the following steps:

[0022] (1) drying and crushing the mulberry root, adding it to an ethanol aqueous solution for reflux extraction, then filtering and collecting the filtrate and concentrating it to obtain a mulberry root extract;

[0023] (2) adding water to dissolve the mulberry root extract and then adding β-glucosidase to carry out enzymatic hydrolysis reaction. After the reaction is completed, filtering is performed, and the enzymatic hydrolysis solution is collected, concentrated, and dried to obtain the mulberry root extract.

[0024] The present invention has found that when mulberry root extract is prepared by different methods, the types and contents of its effective ingredients are different. When the mulberry root extract is further selected to be prepared by the preparation method provided by the present invention and is compounded with other components, the comprehensive effect of the obtained whitening composition is better.

[0025] As a preferred embodiment of the whitening composition of the present invention, in step (1), the mass percentage of ethanol in the ethanol aqueous solution is 60-80%.

[0026] As a preferred embodiment of the whitening composition of the present invention, in step (1), the material-liquid ratio of the reflux extraction is 1 g: (5-20) mL, the reflux extraction temperature is 70-90° C., the time of a single reflux extraction is 1-3 h, and the number of reflux extractions is 1-3 times.

[0027] As a preferred embodiment of the whitening composition of the present invention, in the step (2), the mass ratio of the mulberry root extract to water is 1:(2-5).

[0028] As a preferred embodiment of the whitening composition of the present invention, in the step (2), the mass ratio of β-glucosidase to mulberry root extract is (0.5-2):1.

[0029] As a preferred embodiment of the whitening composition of the present invention, in the step (2), the enzymatic hydrolysis temperature is 30-50° C., and the enzymatic hydrolysis time is 8-12 h.

[0030] The present invention has no particular limitation on the preparation method of the Camellia chrysantha extract; conventional alcohol extraction can achieve the purpose of the present invention, or the extract can be purchased from conventional commercial sources.

[0031] In one embodiment, the preparation method of the camellia chrysantha extract of the present invention comprises the following steps: drying and crushing the flowers of camellia chrysantha and adding them to an ethanol aqueous solution for reflux extraction; filtering after the extraction is completed; collecting the filtrate and concentrating and drying it to obtain the camellia chrysantha extract.

[0032] Preferably, the mass volume ratio of the Camellia chrysantha flower to the ethanol aqueous solution is 1 g: (5-20) mL.

[0033] Preferably, the mass percentage of ethanol in the ethanol aqueous solution is 50-80%.

[0034] Preferably, the temperature of the reflux extraction is 60-80° C., and the time is 1-2 h.

[0035] The present invention has no particular limitation on the preparation method of the wood apple extract; conventional alcohol extraction can achieve the purpose of the present invention, or the wood apple extract can be purchased from conventional commercial sources.

[0036] In one embodiment, the preparation method of the wood apple extract includes the following steps: taking the dried bark of the wood apple and crushing it, adding it into an ethanol aqueous solution for reflux extraction, filtering it after the extraction is completed, collecting the filtrate, concentrating it, and drying it to obtain the wood apple extract.

[0037] Preferably, the mass volume ratio of the wood apple bark to the ethanol aqueous solution is 1 g: (5-20) mL.

[0038] Preferably, the mass percentage of ethanol in the ethanol aqueous solution is 50-80%.

[0039] Preferably, the reflux extraction temperature is 40-60° C. and the time is 1-3 h.

[0040] The present invention has no particular limitation on the preparation method of the Andrographis paniculata extract; conventional alcohol extraction can achieve the purpose of the present invention, or the Andrographis paniculata extract can be purchased from conventional commercial sources.

[0041] In one embodiment, the preparation method of the Andrographis paniculata extract comprises the following steps: collecting the aerial part of Andrographis paniculata, cleaning it, drying it and crushing it, then adding the crushed Andrographis paniculata to methanol for ultrasonic extraction, filtering and collecting the filtrate after the extraction, and concentrating and drying it to obtain the Andrographis paniculata extract.

[0042] Preferably, the mass volume ratio of Andrographis paniculata to methanol is 1 g: (5-20) mL.

[0043] Preferably, the ultrasonic extraction time is 1-3 hours.

[0044] In a second aspect of the present invention, the present invention provides use of the whitening composition in preparing cosmetics.

[0045] The whitening composition provided by the present invention has a good effect of promoting the production and secretion of human β-defensin, and therefore can effectively enhance the skin's resistance and self-healing ability. In addition, the whitening composition provided by the present invention can also effectively promote skin metabolism and achieve mild whitening.

[0046] In the third aspect of the present invention, the present invention provides an emulsion, which comprises the following components in mass percentage: 0.5-5% of the whitening composition of the present invention, 0.1-0.5% of a thickener, 3-10% of a moisturizer, 0.1-10% of an emulsifier, 0.5-5% of a preservative, 0.01-0.1% of an antioxidant, 0.05-0.5% of a pH regulator, and the balance water.

[0047] The present invention has found that the emulsion provided by the present invention includes the whitening composition of the present invention, and the obtained emulsion has good skin barrier repairing ability and whitening effect.

[0048] As a preferred embodiment of the emulsion of the present invention, the thickener includes polyacrylate cross-linked polymer 6.

[0049] As a preferred embodiment of the emulsion of the present invention, the antioxidant includes sodium metabisulfite and glucosylrutin.

[0050] Preferably, the mass ratio of the sodium metabisulfite to glucosylrutin is 1:(0.5-1.5).

[0051] More preferably, the mass ratio of the sodium metabisulfite to glucosylrutin is 1:1.

[0052] The present invention has found that when the whitening composition of the present invention is added to an emulsion, the storage stability of the emulsion is not high due to the components in the whitening composition. When the thickener is polyacrylate cross-linked polymer 6 and the antioxidants are sodium metabisulfite and glucosylrutin, the resulting emulsion has excellent storage stability and will not cause precipitation or discoloration problems even after long-term storage.

[0053] As a preferred embodiment of the emulsion of the present invention, the moisturizing agent includes at least one of glycerin, D-panthenol, vitamin B5, 1,3-butylene glycol, 1,2-hexanediol, 1,3-propylene glycol, sodium hyaluronate, tremella polysaccharide, trehalose, betaine, and squalane.

[0054] As a preferred embodiment of the emulsion of the present invention, the emulsifier includes at least one of ethylhexylglycerin, dimethicone, steareth-2, steareth, caprylic / capric triglyceride, polymethylsilsesquioxane, cetearyl glucoside, and C14-22 alcohol / C12-20 alkyl glucoside.

[0055] As a preferred embodiment of the emulsion of the present invention, the preservative includes p-hydroxyacetophenone and / or polyol.

[0056] As a preferred embodiment of the emulsion of the present invention, the pH regulator includes disodium edetate and / or arginine.

[0057] Compared with the prior art, the present invention has the following beneficial effects:

[0058] The present invention selects components in appropriate mass ratios for compounding, resulting in good interaction between the components. This effectively promotes the production and secretion of human beta defensin (HBD3) in the skin barrier, thereby effectively enhancing the tight junction function of the skin barrier and improving the skin's resistance. Furthermore, it can effectively promote skin metabolism, activate the skin's self-healing ability, and gently whiten the skin. Furthermore, the whitening composition provided by the present invention can be widely added to cosmetics, thereby achieving good skin barrier repair and whitening effects. BRIEF DESCRIPTION OF THE DRAWINGS

[0059] Figure 1 This is a comparison chart of the zebrafish barrier permeability test results in Effect Example 1;

[0060] Figure 2 This is a comparison chart of the test results of inhibiting melanin production in zebrafish in Effect Example 1;

[0061] Figure 3 This is a comparison picture of the volunteers before and after use in Effect Example 2. DETAILED DESCRIPTION

[0062] In order to better illustrate the purpose, technical solutions and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments.

[0063] Unless otherwise specified, the reagents, methods, and equipment used in the present invention are all conventional reagents, methods, and equipment in the art; and unless otherwise specified, the raw materials used in parallel experiments are from the same batch of raw materials.

[0064] Mulberry root extract 1: Homemade, the preparation method includes the following steps:

[0065] (1) Clean the mulberry root and peel off the root bark. Place the peeled root bark in a 50°C constant temperature oven and dry it to constant weight. Then grind it and pass it through a No. 5 sieve. Collect the sieve residue. Add the sieve residue to a 70% ethanol aqueous solution (the mass volume ratio of the sieve residue to the 70% ethanol aqueous solution is 1 g:10 mL). Then, reflux extract three times at 80°C, with a single reflux extraction time of 2 h. After the extraction is completed, filter and collect the filtrate, concentrate under reduced pressure, and dry it to obtain a mulberry root extract.

[0066] (2) dissolving the mulberry root extract in 40°C water with 4 times the amount (based on the mulberry root extract), then adding 0.5 times the amount (based on the mulberry root extract) of β-glucosidase, and enzymolyzing at 30°C for 10 hours; then filtering, collecting the filtrate, concentrating under reduced pressure, and drying to obtain mulberry root extract 1;

[0067] Mulberry root extract 2: Homemade, the preparation method includes the following steps:

[0068] (1) Clean the mulberry root and peel off the root bark. Place the peeled root bark in a 50°C constant temperature oven and dry it to constant weight. Then grind it and pass it through a No. 5 sieve. Collect the sieve underflow. Add the sieve underflow into a 60% ethanol aqueous solution (the mass volume ratio of the sieve underflow to the 70% ethanol aqueous solution is 1 g:20 mL). Then, reflux extract three times at 85°C, with a single reflux extraction time of 1 h. After the extraction, filter and collect the filtrate, concentrate under reduced pressure, and dry it to obtain a mulberry root extract.

[0069] (2) dissolving the mulberry root extract in 2 times the amount (based on the mulberry root extract) of water at 45°C, then adding 1.5 times the amount (based on the mulberry root extract) of β-glucosidase, and enzymolyzing at 45°C for 10 hours; then filtering, collecting the filtrate, concentrating under reduced pressure, and drying to obtain mulberry root extract 2;

[0070] Mulberry root extract 3: Homemade, the preparation method includes the following steps:

[0071] (1) Clean the mulberry root and peel off the root bark. Place the peeled root bark in a 50°C constant temperature oven and dry it to constant weight. Then grind it and pass it through a No. 5 sieve. Collect the sieve residue. Add the sieve residue to a 70% ethanol aqueous solution (the mass volume ratio of the sieve residue to the 70% ethanol aqueous solution is 1 g:10 mL). Then, reflux extract three times at 80°C, with a single reflux extraction time of 2 h. After the extraction is completed, filter and collect the filtrate, concentrate under reduced pressure, and dry it to obtain a mulberry root extract.

[0072] (2) Dissolve the mulberry root extract in 40°C water, then add 0.5 times the amount of cellulase (based on the mulberry root extract) and perform enzymolysis at 30°C for 10 hours; then filter, collect the filtrate, concentrate under reduced pressure, and dry to obtain mulberry root extract 3;

[0073] Mulberry root extract 4: Homemade, the preparation method includes the following steps:

[0074] The mulberry root was cleaned and the root bark was peeled off. The peeled root bark was placed in a constant temperature oven at 50°C and dried to constant weight. The material was then ground and passed through a No. 5 sieve, and the sieve underflow was collected. The sieve underflow was added to a 70% ethanol aqueous solution (the mass volume ratio of the sieve underflow to the 70% ethanol aqueous solution was 1g:10mL), and then refluxed and extracted three times at 80°C, with a single reflux extraction time of 2h. After the extraction, the filtrate was filtered and collected and concentrated under reduced pressure to dryness to obtain mulberry root extract 4.

[0075] Camellia chrysantha extract: Homemade, the preparation method includes the following steps:

[0076] Collect the flowers of Camellia chrysantha, clean them, and place them in a constant temperature oven at 50°C to dry to constant weight. Grind them and pass them through a No. 5 sieve. Take 1 g of the sieve residue, add 20 mL of 75% ethanol by volume, and reflux extract at 80°C for 1 hour. After the extraction is completed, filter, collect the filtrate, concentrate, and dry it to obtain the Camellia chrysantha extract.

[0077] Wood apple extract: Homemade, the preparation method includes the following steps:

[0078] The dried bark of the wood apple tree was collected, dried in a constant temperature oven at 50°C to constant weight, ground and crushed, and passed through a No. 5 sieve. The sieve residue was collected and 10 times the amount of 70% ethanol aqueous solution was added thereto. The mixture was refluxed at 50°C for 2 hours. After the extraction was completed, the mixture was filtered, and the filtrate was collected and concentrated under reduced pressure and dried to obtain the wood apple extract.

[0079] Andrographis paniculata extract: commercially available from Draco;

[0080] Epigallocatechin gallate (EGCG): commercially available from Givaudan.

[0081] Examples 1-9 and Comparative Examples 1-5

[0082] The embodiments and comparative examples of the present invention provide a whitening composition for improving skin resistance and self-healing ability. The components (parts by mass) of the whitening composition are shown in Table 1.

[0083] Table 1

[0084]

[0085]

[0086] The preparation method of the whitening composition provided in Example 1 is: mixing the components uniformly to obtain the whitening composition.

[0087] The preparation methods of the whitening compositions provided in Examples 2-9 and Comparative Examples 1-5 are consistent with that in Example 1.

[0088] Comparative Example 6

[0089] The comparative example of the present invention provides a whitening composition. The only difference between the whitening composition and Example 1 is that the jackfruit extract is used instead of the mulberry root extract.

[0090] Comparative Example 7

[0091] The comparative example of the present invention provides a whitening composition. The only difference between the whitening composition and Example 1 is that the camellia extract is replaced by the camellia chrysantha extract.

[0092] Comparative Example 8

[0093] The comparative example of the present invention provides a whitening composition, the only difference between the whitening composition and Example 1 is that lemon extract is used instead of wood apple extract.

[0094] Comparative Example 9

[0095] The comparative example of the present invention provides a whitening composition. The only difference between the whitening composition and Example 1 is that the Andrographis paniculata extract is replaced by the honeysuckle extract.

[0096] Comparative Example 10

[0097] The comparative example of the present invention provides a whitening composition, the only difference between the whitening composition and Example 1 is that nicotinamide is used instead of EGCG.

[0098] Application Example 1-14, Comparative Application Example 1-10

[0099] The application examples of the present invention and the comparative application examples provide an emulsion, the components (mass percentage) of the emulsion are shown in Table 2; wherein the whitening compositions used in application examples 1-9 are respectively the whitening compositions prepared in embodiments 1-9, the whitening compositions used in comparative application examples 1-10 are respectively the whitening compositions prepared in comparative examples 1-10; the whitening compositions used in application examples 10-14 are the whitening compositions prepared in embodiment 1;

[0100] A blank application example was also set up, wherein the only difference between the blank application example and application example 1 was that no whitening composition was added;

[0101] Table 2

[0102]

[0103]

[0104] The preparation method of the emulsion provided in Application Example 1 comprises the following steps:

[0105] The ingredients in phase A were sequentially added to water. After the thickener was fully swollen, the mixture was homogeneously mixed. The mixture and phase B were heated separately until the solid matter melted uniformly. The mixture was homogeneously emulsified at 80°C. Phase C was heated until the p-hydroxyacetophenone melted, and then added to the emulsion and stirred uniformly. After the temperature dropped to 40°C, phases D and E were added and stirred to form a uniform emulsion. Finally, arginine was added to adjust the pH to obtain an emulsion.

[0106] The preparation methods of the emulsions provided in Application Examples 2-14, Comparative Application Examples 1-10 and Blank Application Examples are consistent with that in Application Example 1.

[0107] Effect Example 1

[0108] The performance of the whitening compositions prepared in Examples 1-9 and Comparative Examples 1-10 was investigated, including the following aspects:

[0109] 1. Promoting effect on human β-defensin

[0110] The tight junctions of the stratum corneum are an important defense mechanism in the skin barrier. Studies have found that human β-defensin-3 (HBD3) in the human skin barrier can improve the tight junction barrier function of keratinocytes, increase the barrier's resistance, resist external stimuli, and reduce discomfort reactions in people with sensitive skin, including redness, stinging, and itching. External stimuli such as light can lead to a decrease in the secretion of HBD3, thereby slowing the recovery of skin damage. If the secretion of HBD3 in the skin increases, the skin's resistance is enhanced, and the skin can speed up its self-healing. Therefore, by studying the whitening composition's promotion of the secretion of human β-defensin HBD3 after light damage to keratinocytes, it is possible to determine the whitening composition's ability to enhance the skin's resistance and self-healing ability. The stronger the secretion-promoting effect of HBD3, the stronger the whitening composition's effect on enhancing the skin's resistance and self-healing ability.

[0111] The specific test includes the following steps:

[0112] Human keratinocytes HaCat were revived and cultured in MEM containing 10% FBS. 2 , 320nm irradiation; after irradiation with the light source, fresh culture medium was replaced, and the whitening composition was prepared into a 20μg / mL working solution with fish embryo culture medium. 20μL of different whitening composition working solutions were added to treat HaCaT cells for 24h, and the culture solution without the whitening composition suitable for sensitive skin and not irradiated by UVB was used as the blank control group, and the culture solution without the whitening composition after UVB irradiation was used as the UVB model group. Different whitening compositions were configured into sample solutions and co-cultured with HaCat cells, and the cells were harvested. The concentration of HBD3 in HaCaT cells was detected by ELISA kit. The absorbance was measured at a wavelength of 450nm;

[0113] Among them, the HBD3 concentrations of the model group were compared with those of the blank control group. The HBD3 concentration of the model group was significantly lower than that of the blank control group (P<0.05), indicating that the model group was successfully established.

[0114] Promotion rate (%) = (HBD3 content in the test group - HBD3 content in the model group) / HBD3 content in the model group × 100%; the results are shown in Table 3.

[0115] 2. Testing the effect of whitening composition on promoting zebrafish's resistance to external stimuli

[0116] Zebrafish are a commonly used animal model for in vivo studies of human efficacy, as their skin barrier is similar to that of humans. In this experiment, we administered the prepared whitening compositions to zebrafish culture medium, added the irritant lactic acid to establish a zebrafish barrier damage model, and then added a red fluorescent dye. The dye then entered the zebrafish through the damaged skin and was observed for penetration. Less fluorescence indicates a stronger effect of the test compound on the zebrafish's skin barrier resistance and self-healing ability, and vice versa.

[0117] The specific test includes the following steps:

[0118] Healthy zebrafish embryos 2 days after fertilization were selected, and a blank control group (fish embryo culture medium), a model control group (fish embryo culture medium + a 1:1 mixed solution of gentian violet and lactic acid (LA)) and a test group (fish embryo culture medium + a mixed solution of gentian violet and lactic acid (LA) + a whitening composition prepared in the examples / comparative examples) were set up. The specific operation was as follows: 63 fish embryos were randomly selected and placed in a 3 cm culture dish. The test solution was prepared by using fish embryo culture medium to prepare a 20 μg / mL working solution. 5 mL of the test solution was added to the test group. After being cultured in a constant temperature shaker at 28±1°C for 4 hours, the cells were washed twice with fish embryo culture medium. 5 mL of a 1:1 mixed solution of gentian violet and lactic acid (LA) was added to each well of the model group and the test group, and then placed in a constant temperature shaker at 28±1°C for 20 minutes. The fish embryos were placed sideways. The tail fins of the fish embryos were photographed under a fluorescent stereomicroscope according to uniform photographic parameters. The fluorescence area of the photographs was analyzed using Image J software.

[0119] Skin barrier permeability inhibition rate (%) = (fluorescent area of the tail fin of the model group - fluorescent area of the tail fin of the test group) / fluorescent area of the tail fin of the model group × 100%; the obtained data are shown in Table 3;

[0120] Among them, the fluorescence area of the model group was compared with that of the blank control group. The fluorescence area of the model group was significantly increased compared with that of the blank control group (P < 0.05), that is, the modeling of the model group was successful.

[0121] 3. Whitening test of whitening composition

[0122] Studies have shown that zebrafish produce melanin during the embryonic and larval stages, so they can be used to study the inhibitory effect of samples on melanin synthesis and evaluate the whitening effect of the samples.

[0123] Healthy zebrafish embryos, 6 to 8 hours post-fertilization (PFP), were selected. A blank control group (egg culture medium), a 100% melanin inhibition model group (egg culture medium + Phenylthiourea working solution), and a test group (egg culture medium + Phenylthiourea working solution + the whitening composition prepared in the Examples / Comparative Examples) were established. Sixty-three fish embryos were randomly selected and placed in a 96-well plate, with one fish embryo and 0.2 mL of fish embryo culture medium per well. The test substance was prepared at a 20 μg / mL working solution using fish embryo culture medium. 0.2 mL of Phenylthiourea working solution was added to each well of the model group, while 0.2 mL of the test substance working solution was added simultaneously with the 0.2 mL of Phenylthiourea working solution in the test group. The embryos were incubated in a 28°C ± 1°C incubator until 48 hours ± 1 hour post-fertilization (PFP). The embryos were covered with 2% to 4% methylcellulose and placed with their backs facing upwards. The heads and yolk areas were then photographed under a stereomicroscope. The photographs were analyzed for melanin content using Image J software.

[0124] Melanin inhibition rate (%) = (melanopic area of model group - melanin area of test group) / melanin area of model group × 100%. The obtained data are shown in Table 3;

[0125] Among them, the melanin area of the model group was compared with that of the blank control group. The melanin area of the model group was significantly increased compared with that of the blank control group (P < 0.05), that is, the modeling of the model group was successful.

[0126] Table 3

[0127]

[0128] As can be seen from Table 3, the whitening composition provided by the present invention can improve the reduced secretion of HBD3 caused by UVB, with a promotion rate of HBD3 of over 93.41%. At the same time, the whitening composition provided by the present invention also has excellent resistance to external stimuli. In the zebrafish experiment, the skin barrier permeability inhibition rate was over 39.03%. In addition, the whitening composition provided by the present invention also has a good whitening effect, with an inhibition rate of over 28.94% on the production of melanin in zebrafish.

[0129] As can be seen from Examples 1-6, the mass fractions of the components in the whitening composition affect the overall performance of the product. When the mass fractions of the components are further selected within the scope of the present invention and the mass ratio of component A to component B is within the scope of the present invention, the overall effect of the resulting whitening composition is better. Specifically, the promotion rate of HBD3 is greater than 109.63%, the skin barrier permeability inhibition rate in the zebrafish experiment is greater than 52.04%, and the inhibition rate of zebrafish melanin production in the whitening experiment is greater than 55.92%. As can be seen from Examples 1 and 7-9, the preparation method of mulberry root extract can also affect the overall performance of the product.

[0130] As can be seen from Example 1 and Comparative Examples 1-5, the components of the whitening composition provided by the present invention are indispensable. When any one of them is missing, the overall performance of the obtained product is significantly reduced. As can be seen from Example 1 and Comparative Examples 6-10, when other similar ingredients are used to replace the components in the whitening composition, the corresponding efficacy of the present invention cannot be achieved.

[0131] In addition, the test results of zebrafish in the model group, Example 1, Comparative Example 1 and Comparative Example 6 in the zebrafish permeability test are shown in FIG. Figure 1 As shown, from Figure 1 It can be seen intuitively that when the technical solution provided by the present invention is adopted, the tail fin fluorescence area can be significantly reduced compared with the model group, that is, it has an excellent skin barrier permeability inhibition effect. The test results of the zebrafish in the model group, Example 1, Comparative Example 1 and Comparative Example 6 in the zebrafish melanin synthesis inhibition test are shown in the figure below. Figure 2 As shown, from Figure 2 It can be seen that compared with the model group, the product of Example 1 obtained by adopting the technical solution provided by the present invention can significantly reduce the melanin of zebrafish and achieve a good whitening effect.

[0132] Effect Example 2

[0133] The present invention explores the performance of the emulsions prepared by application examples 1-14, comparative application examples 1-10 and blank application examples, specifically: recruited patients with skin barrier damage problems (TEWL ≥ 20g / hm 2 ) were recruited. On the day of their visit, the volunteers were not allowed to apply any products to the test area (face). After washing their faces, they were asked to sit quietly in an air-conditioned room at a temperature of 21±1°C and a humidity of 50±10% for 20 minutes. They were then randomly divided into 25 groups, with 3 people in each group. Each volunteer's initial TEWL and ITA° values on the left and right sides of their face were measured using the TM Hex (Courage+Khazaka) and a Colorimeter CL400 color probe, and the average was calculated. Each group of volunteers applied the same amount of lotion to their faces once in the morning and evening. The first group used the blank application example (lotion without the whitening composition), the second group used application example 1, and so on. Post-application TEWL and post-application ITA° values were measured again on days 14 and 28, and the average values were calculated. The respective improvement rates (%) were calculated using the following formula:

[0134] TEWL value improvement rate (%) = (initial TEWL value - TEWL value after use) / initial TEWL value × 100%;

[0135] ITA° value improvement rate (%) = (ITA° value after use - initial ITA° value) / initial ITA° value × 100%;

[0136] Among them, the greater the improvement rate of the TEWL value, the stronger the skin barrier damage repair ability of the lotion; the greater the improvement rate of the ITA° value, the stronger the ability of the lotion to improve skin whitening and brighten skin tone; the results are shown in Table 4.

[0137] Table 4

[0138]

[0139] As can be seen from Table 4, the emulsion provided by the present invention has excellent effects of repairing the skin barrier and whitening the skin. Specifically, on the 28th day, the TEWL value improvement rate was above 27.98%, and the ITA° value improvement rate was above 17.84%.

[0140] As can be seen from Application Examples 1-6, the weight percentage of the components in the whitening composition added to the emulsion affects the overall performance of the product. When the weight percentages of the components are further selected within the range of the present invention and the mass ratio of component A to component B is within the range of the present invention, the overall effect of the resulting emulsion is better. Specifically, on the 28th day, the TEWL value improvement rate is greater than 33.94%, and the ITA° value improvement rate is greater than 22.94%. As can be seen from Application Examples 1 and Application Examples 7-9, the preparation method of the mulberry root extract also affects the overall performance of the product.

[0141] As can be seen from Application Example 1 and Comparative Application Examples 1-5, the components of the whitening composition provided by the present invention are indispensable. When any one of them is missing, the overall performance of the obtained emulsion is significantly reduced. As can be seen from Application Example 1 and Comparative Application Examples 6-10, when other similar ingredients are used to replace the components in the whitening composition, the corresponding efficacy of the present invention cannot be achieved.

[0142] Among them, the photographs of volunteers before and after use of the emulsion in the blank application example, application example 1 and comparative application example 1 are as follows: Figure 3 As shown, from Figure 3 It can be seen intuitively that the emulsion provided by the present invention can effectively repair skin damage and whiten the skin.

[0143] Effect Example 3

[0144] The present invention investigates the stability of the emulsions prepared in Application Examples 1-2 and Application Examples 10-13, wherein the emulsions used are batches of emulsions prepared in parallel, specifically comprising the following steps:

[0145] 1. Place the samples in a constant temperature device at 50°C and -8°C for extreme environmental stability testing. Take out the samples on the 0th, 1st, 7th, 14th, 21st, and 30th day respectively to observe whether the product has obvious abnormal changes in appearance such as discoloration, delamination, precipitation, and precipitation;

[0146] 2. Place the sample in a UV light aging box with a 0.50w / m 2 The product was irradiated with a dose of UVA light (340 nm) for 24 hours, and then taken out to observe whether there were any abnormal changes in appearance such as obvious discoloration, stratification, precipitation, and precipitation.

[0147] The results are shown in Table 5;

[0148] Table 5

[0149]

[0150]

[0151] As can be seen from Table 5, the type of thickener and antioxidant affects the stability of the emulsion. When polyacrylate cross-linked polymer 6 is used as the thickener and sodium metabisulfite and glucosylrutin are used as the antioxidants, the resulting emulsion achieves even better stability. Specifically, when polyacrylate cross-linked polymer 6 is omitted, the formulation lacks sufficient pulling force on the whitening composition, which can lead to the precipitation of unstable components in the whitening component and separation of the oil and aqueous phases under extreme conditions. However, sodium metabisulfite and glucosylrutin stabilize the color of the active ingredient. The optimal emulsion stability is achieved when the mass ratio of sodium metabisulfite to glucosylrutin is 1:1.

[0152] Finally, it should be noted that the above embodiments are intended to illustrate the technical solutions of the present invention rather than to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that the technical solutions of the present invention may be modified or replaced by equivalents without departing from the essence and scope of the technical solutions of the present invention.

Claims

1. A whitening composition suitable for sensitive skin for enhancing skin resistance and self-healing ability, characterized in that: The whitening composition comprises the following components in parts by weight: 0.1-3 parts of mulberry root extract, 0.1-3 parts of camellia chrysantha extract, 0.01-1 parts of wood apple extract, 0.1-3 parts of andrographis paniculata extract, and 0.01-1 parts of epigallocatechin gallate.

2. The whitening composition according to claim 1, characterized in that The whitening composition comprises the following components in parts by mass: 1-2 parts of mulberry root extract, 1-2 parts of camellia chrysantha extract, 0.5-0.8 parts of wood apple extract, 1-1.8 parts of andrographis paniculata extract, and 0.5-0.8 parts of epigallocatechin gallate.

3. The whitening composition according to claim 1, characterized in that The ratio of the sum of the mass of the mulberry root extract and the camellia chrysantha extract to the sum of the mass of the wood apple extract, the andrographis paniculata extract and epigallocatechin gallate is 1:(0.75-1.05).

4. The whitening composition according to claim 1, characterized in that In the whitening composition, the mass percentage of the Andrographis paniculata extract is 18-30%.

5. The whitening composition according to claim 1, characterized in that The preparation method of the mulberry root extract comprises the following steps: (1) drying and crushing the mulberry root, adding it to an ethanol aqueous solution for reflux extraction, then filtering and collecting the filtrate and concentrating it to obtain a mulberry root extract; (2) adding water to dissolve the mulberry root extract and then adding β-glucosidase to carry out enzymatic hydrolysis reaction. After the reaction is completed, filtering is performed, and the enzymatic hydrolysis solution is collected, concentrated, and dried to obtain the mulberry root extract.

6. The whitening composition according to claim 5, characterized in that At least one of the following is met: a. In the step (1), the mass percentage of ethanol in the ethanol aqueous solution is 60-80%; b. In the step (1), the solid-liquid ratio of the reflux extraction is 1g: (5-20) mL, the reflux extraction temperature is 70-90 ℃, the single reflux extraction time is 1-3h, and the number of reflux extractions is 1-3 times; c. In the step (2), the mass ratio of mulberry root extract and water is 1: (2-5); d. In the step (2), the mass ratio of β-glucosidase and mulberry root extract is (0.5-2): 1; e. In the step (2), the enzymatic hydrolysis temperature is 30-50°C and the enzymatic hydrolysis time is 8-12h.

7. Use of the whitening composition according to any one of claims 1 to 6 in the preparation of cosmetics.

8. An emulsion, characterized in that The emulsion comprises the following components in percentage by weight: 0.5-5% of the whitening composition according to any one of claims 1 to 6, 0.1-0.5% of a thickener, 3-10% of a moisturizer, 0.1-10% of an emulsifier, 0.5-5% of a preservative, 0.01-0.1% of an antioxidant, 0.05-0.5% of a pH regulator, and the balance being water.

9. The emulsion according to claim 8, characterized in that The thickener includes polyacrylate crosspolymer-6; And / or, the antioxidant includes sodium metabisulfite and glucosylrutin.

10. The emulsion according to claim 8, characterized in that The moisturizing agent includes at least one of glycerin, D-panthenol, vitamin B5, 1,3-butylene glycol, 1,2-hexanediol, 1,3-propylene glycol, sodium hyaluronate, tremella polysaccharide, trehalose, betaine, and squalane; And / or, the emulsifier includes at least one of ethylhexylglycerin, dimethicone, stearyl alcohol polyether, caprylic / capric triglyceride, polymethylsilsesquioxane, cetearyl glucoside, and C14-22 alcohol / C12-20 alkyl glucoside; and / or, the preservative includes p-hydroxyacetophenone and / or a polyol; And / or, the pH adjuster includes disodium edetate and / or arginine.

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