Composition with whitening effect and application thereof

Abstract

The invention relates to the technical field of skin care products, in particular to a composition with a whitening effect, which is prepared from the following components in percentage by weight: 15 to 40.0 percent of tranexamic acid, 20.0 to 30.0 percent of hydroxyethyl piperazine ethanesulfonic acid, 1.0 to 10.0 percent of carnosine and 0.01 to 0.1 percent of nonapeptide-1. According to the composition disclosed by the invention, tranexamic acid, carnosine and nonapeptide-1 are compounded according to a specific proportion and have a synergistic effect, the activity of tyrosinase is inhibited, and then cutin is mildly exfoliated through hydroxyethyl piperazine ethanesulfonic acid, so that the composition can whiten skin more quickly and mildly. In addition, the composition with the whitening effect has the effect of temporarily brightening the skin color, has the whitening effect after being used for a long time, and is mild and non-irritant to the skin, safe to use and good in stability.

Description

Technical Field

[0001] The invention relates to the technical field of skin care products, and more particularly to a composition with whitening effect and application thereof. Background Art

[0002] Exogenous stimuli such as working overtime and staying up late, ultraviolet radiation, long-term exposure to electronic screens such as mobile phones and computers, and skin inflammatory reactions can easily cause melanocytes to accelerate the production of melanin. Melanin then moves to the stratum corneum of the skin through the inner layer of cell metabolism, gradually forming the skin problems we see such as dull skin tone, spots, uneven skin tone, etc.

[0003] There are thousands of ways to whiten your skin. In addition to physical methods such as laser, medical beauty, and sunscreen, within the cosmetics industry, using skin care products containing whitening ingredients to accelerate the whitening of problem skin is also a common method.

[0004] Because whitening ingredients are different, they can be divided into the following five categories according to different whitening pathways:

[0005] ①Reduce or avoid the activation of melanocytes

[0006] To reduce the stimulation of ultraviolet rays, the most important thing is sun protection. In addition to physical sun protection such as holding an umbrella and wearing clothes, applying sunscreen is a whitening method in the cosmetic category. The main ingredients of sunscreen are titanium dioxide, zinc oxide, octocrylene, benzophenone-4, etc.

[0007] ②Inhibit tyrosinase activity or inhibit melanocyte activation

[0008] Inhibit tyrosinase activity. Related ingredients include: arbutin, tranexamic acid, nonapeptide-1, 4-butylresorcinol, phenethylresorcinol, licorice extract, etc.

[0009] ③Prevent further oxidation of DOPA and reduce melanin formation

[0010] Related ingredients include: vitamin C and its derivatives, tranexamic acid, 4-methoxysalicylic acid potassium salt, glutathione, etc.

[0011] ④ Prevent melanin from being transported to keratinocytes

[0012] Related ingredients include: niacinamide, thyme extract, ellagic acid, etc.

[0013] ⑤ Accelerate melanin shedding

[0014] Related ingredients include: fruit acid, glycolic acid, salicylic acid, azelaic acid, glycolic acid, retinoic acid, etc.

[0015] As mentioned above, although there are many whitening raw materials to choose from, the whitening products on the market still generally have problems such as slow effect, poor effect, poor material stability, and high product irritation. For example, acid whitening products can quickly peel off the stratum corneum and accelerate whitening, but they will make the stratum corneum thinner, destroy the skin barrier, and make the skin sensitive; resorcinol whitening agents can strongly inhibit the activity of tyrosinase, but they are prone to cause skin allergies. In addition, some unscrupulous manufacturers on the market illegally add cosmetics in order to achieve fast and good results. Although they can quickly whiten and rejuvenate the skin, long-term use will seriously affect skin health. Therefore, it is very necessary to develop a safe and effective product with good product stability, which can moisturize the stratum corneum to achieve a temporary brightening effect and have whitening effects. Summary of the invention

[0016] In view of the deficiencies in the prior art, the object of the present invention is to provide a safe and effective composition with good product stability, which can instantly moisturize the stratum corneum to achieve a temporary brightening effect and has a whitening effect and its application.

[0017] To achieve the above object, the present invention is implemented through the following technical solutions:

[0018] A composition with whitening effect comprises the following components in weight percentage: 15%-40.0% tranexamic acid, 20.0%-30.0% hydroxyethylpiperazineethane sulfonic acid, 1.0%-10.0% carnosine, and 0.01%-0.1% nonapeptide-1.

[0019] Studies have found that tranexamic acid is more stable than traditional whitening ingredients, is resistant to acid and alkalinity, and is not easily affected by temperature and environment. Its whitening mechanism is to inhibit the activity of tyrosinase and melanocytes, reduce the production of melanin from the basal layer of the epidermis, and completely cut off the path of melanin formation due to ultraviolet radiation. Nonapeptide-1 is a biomimetic peptide that can competitively prevent the binding of α-MSH to the MC1 R receptor. When α-MSH reaches the extracellular binding site of melanocytes, the site has been occupied by nonapeptide-1, thereby reducing the binding of α-MSH to MC1-R and preventing tyrosinase from being further activated to produce melanin. As a natural biological molecule, carnosine can achieve the purpose of removing yellowness by inhibiting free radicals, protecting elastin, and preventing the formation of glycation end products. Its anti-inflammatory properties help to reduce inflammatory responses; it has an inhibitory effect on tyrosinase; and it also has a photoprotective effect on human skin. Hydroxyethylpiperazine ethane sulfonic acid is a zwitterionic buffer that gently exfoliates and promotes epidermal metabolism. It can smooth and soften the skin, brighten the skin tone, and achieve the effect of whitening. It also helps penetration and can promote the absorption of other ingredients.

[0020] The inventors have found that the whitening efficacy composition of the present invention covers multiple whitening pathways, and multiple whitening pathways can achieve faster whitening efficacy. The whitening composition of the present invention also has the effect of instantly and temporarily brightening the skin color. The content of the components in the composition is at a safe and mild dosage, which is milder and more stable than other components.

[0021] Preferably, the composition of the present invention comprises the following components in weight percentage: 20%-40.0% tranexamic acid, 22.0%-28.0% hydroxyethylpiperazineethanesulfonic acid, 2.0%-8.0% carnosine, and 0.02%-0.08% nonapeptide-1.

[0022] Preferably, the composition of the present invention comprises the following components in weight percentage: 20%-35.0% tranexamic acid, 23.0%-27.0% hydroxyethylpiperazineethanesulfonic acid, 3.0%-7.0% carnosine, and 0.03%-0.07% nonapeptide-1.

[0023] Preferably, the composition of the present invention further comprises other active ingredients.

[0024] Preferably, the active ingredient includes at least one of a moisturizing ingredient, an antioxidant ingredient, and a whitening ingredient.

[0025] Moisturizing ingredients include but are not limited to inositol, mannitol, and erythritol.

[0026] Antioxidant ingredients include but are not limited to ergothioneine, ectoine, and taurine.

[0027] Whitening ingredients include but are not limited to glutathione, niacinamide, and arbutin.

[0028] In order to further broaden the application scope of the composition of the present invention, it can be prepared into a cosmetic comprising the above-mentioned composition with whitening effect.

[0029] Preferably, the dosage form of the cosmetic can be selected as needed, such as any one of cream, lotion, mask, essence, lotion, spray, facial cleanser or shower gel or others.

[0030] Preferably, the cosmetic further comprises a matrix commonly used in the art, such as at least one of water, a pH regulator, a fragrance, a thickener, an emulsifier, a chelating agent, a colorant, and a preservative; the type and content of the matrix can be conventionally selected according to the type of cosmetic.

[0031] The above embodiments of the present invention have the following beneficial effects:

[0032] The whitening efficacy composition of the present invention covers a variety of whitening pathways, and tranexamic acid, carnosine, and nonapeptide-1 synergize with each other to inhibit tyrosinase activity. Compared with traditional whitening ingredients, tranexamic acid is more stable, resistant to acid and alkalinity, not easily affected by temperature environment, and effectively inhibits tyrosinase activity. Nonapeptide-1 competes with α-MSH for MC1 R receptors to prevent further activation of tyrosinase. Carnosine can achieve the purpose of removing yellowing by inhibiting free radicals, protecting elastin, preventing the formation of glycation end products, and inhibiting tyrosinase activity. Hydroxyethylpiperazineethane sulfonic acid gently exfoliates keratin, making the composition faster and milder whitening. In addition, the whitening efficacy composition of the present invention has the effect of temporarily brightening the skin color, has whitening efficacy when used for a long time, is mild and non-irritating to the skin, is safe to use, and has good stability. DETAILED DESCRIPTION

[0033] The technical scheme of the present invention is further described below in conjunction with the embodiments. Obviously, the described embodiments are only part of the embodiments of the present invention, rather than all of the embodiments. Based on the embodiments in the present invention, all other embodiments obtained by ordinary technicians in the field without creative work are within the scope of protection of the present invention. The methods or operations used in the embodiments, unless otherwise specified, are conventional methods or conventional operations in the art.

[0034] The present application provides a general and / or specific description of the materials and test methods used in the experiments. In the following examples, unless otherwise specified, % means wt%, i.e., weight percentage. The reagents or instruments used without indicating the manufacturer are all conventional reagent products that can be obtained commercially.

[0035] The invention provides a composition with whitening effect, comprising tranexamic acid, hydroxyethylpiperazineethane sulfonic acid, carnosine and nonapeptide-1.

[0036] The tranexamic acid, hydroxyethylpiperazineethane sulfonic acid, carnosine, nonapeptide-1 and other active ingredients in the examples and comparative examples are all commercially available, conform to the general definition in the art, and are widely used in the cosmetics field as cosmetic raw materials.

[0037] The composition contains other active ingredients. Preferably, a moisturizer is selected, and inositol is used as the other active ingredient in the examples and comparative examples.

[0038] Examples 1-6 and Comparative Examples 1-4 are compositions with whitening effects of the present invention. The components and percentages of the compositions of Examples 1-6 and Comparative Examples 1-4 are shown in Table 1 below:

[0039] Table 1 Composition formula of examples and comparative examples

[0040]

[0041] Example 5 20 25 3 0.01 margin Example 6 40 20 7 0.07 margin Comparative Example 1 0 25 3 0.05 margin Comparative Example 2 20 0 3 0.05 margin Comparative Example 3 20 25 0 0.05 margin Comparative Example 4 20 25 3 0 margin

[0042] Weigh each component according to the proportion in Table 1, sieve each component with a 60-mesh sieve, and stir evenly with a powder blender to obtain the corresponding composition with whitening effect.

[0043] For the convenience of application and experimental needs, the present invention provides a whitening essence containing the above-mentioned whitening efficacy composition, and its formula is as follows:

[0044] Table 2: Formula of the Examples and Comparative Examples

[0045] Components Raw material name content(%) Composition Corresponding to the embodiment or comparative example 5 Thickener Carbomer 0.15 Moisturizer glycerin 8 pH Adjusters Aminomethyl propanol Adjust pH to 6.0 preservative p-Hydroxyacetophenone, 1,2-hexanediol (mass ratio is 1:1) 1 Chelating agents EDTA-Disodium 0.03 Solvents water Top up to 100

[0046] The preparation method of the above essence is:

[0047] (1) Weigh water, chelating agent, preservative, thickener and humectant in proportion, heat to 80-85°C, stir until completely dissolved, and keep warm for 15 minutes.

[0048] (2) Cooling to 45° C., adding the composition and pH adjuster, stirring evenly, and filtering the material with a 200-mesh filter cloth to obtain the corresponding whitening essence containing the whitening effect composition.

[0049] Unless otherwise specified in the following experiments, the test samples in the experimental methods generally refer to the whitening essence containing the whitening efficacy composition.

[0050] 1. Tyrosinase inhibition rate experiment

[0051] The tyrosinase inhibition experiment was used to verify the tyrosinase inhibition ability of Examples 1-6 and Comparative Examples 1-4.

[0052] Tyrosinase is a key enzyme in the synthesis of melanin. Inhibiting it can effectively reduce the synthesis of melanin and play a whitening role.

[0053] Test samples: Examples 1-6 and Comparative Examples 1-4.

[0054] Experimental methods:

[0055] 1.1 Sample preparation

[0056] The sample was prepared at a ratio of 0.45 mg sample to 1 mL serum-free culture medium.

[0057] 1.2 Cell culture

[0058] Mouse B16 melanoma cells were grown to a confluent state, digested with trypsin-EDTA for 5 minutes, and then dispersed by blowing. The cell suspension was aspirated into a centrifuge tube and centrifuged at 1000r / min for 5 minutes. The supernatant was discarded and culture medium was added to obtain a cell suspension. The cell suspension was diluted to a certain concentration with culture medium. B16 cells in the logarithmic growth phase were inoculated in a 96-well plate at a cell density of 7×10 4 CFU / mL, 100 μL per well, mark the top cover of the cell plate after laying the plate, and culture in the incubator for 24 hours.

[0059] After 24 hours of culture, the cell plate was carefully aspirated with a pipette to remove the supernatant and divided into a blank group and a sample group. The prepared sample was added to the sample group, and serum-free medium without drugs was added to the blank group. The addition amount was 100 μL / well, and 4 replicates were made for each concentration. After addition, the cells were placed in an incubator for 72 hours of culture.

[0060] 1.3 Determination of intracellular tyrosinase inhibition rate

[0061] After incubation for 72 hours, the supernatant was discarded, 150 μL of 1% TritonX-100 solution was added to each well, and the cells were quickly frozen at 80°C for 30 minutes, then thawed at room temperature to completely rupture the cells, and 60 μL of 0.5% L-DOPA solution was added after preheating at 37°C for 5 minutes, reacted at 37°C for 2 hours, and the absorbance (OD) value was measured at 490 nm on an enzyme reader. The tyrosinase activity inhibition rate was calculated, and the results are shown in Table 3.

[0062] The calculation formula is: tyrosinase activity inhibition rate (%) = (1-average absorbance value of sample / average absorbance value of blank) × 100%.

[0063] Table 3 Tyrosine inhibition rate of the embodiments and comparative examples

[0064] Group Tyrosine inhibition rate (%) Example 1 60.12 Example 2 61.35 Example 3 51.44 Example 4 55.89 Example 5 52.76 Example 6 63.45 Comparative Example 1 25.48 Comparative Example 2 59.17 Comparative Example 3 20.95 Comparative Example 4 26.19

[0065] From the data of Examples 1-6 and Comparative Examples 1, 3, and 4 in Table 3, it can be seen that the composition of the present invention has a good effect of inhibiting the activity of tyrosinase, and tranexamic acid, carnosine, and nonapeptide-1 synergize with each other; from the data of Examples 1-6 and Comparative Example 2, hydroxyethylpiperazineethanesulfonic acid does not affect the activity of tyrosinase in the composition. However, since whitening requires solving multiple pathway problems, it is further speculated that hydroxyethylpiperazineethanesulfonic acid acts on other pathways to achieve whitening effects. In order to verify this conjecture, further experiments are needed.

[0066] 2. Melanin presence test

[0067] Epidermal melanin can intuitively reflect whether the composition has whitening effect. If the melanin content of the sample is reduced compared with the initial value after using it for a period of time, it means that the composition has whitening effect.

[0068] Test samples: Examples 1-6 and Comparative Examples 1-4

[0069] Experimental method: 10 groups of experimenters used Examples 1-6 and Comparative Examples 1-4 respectively, and used the samples once in the morning and evening after cleansing every day for 4 consecutive weeks. During this period, other cosmetics were prohibited. Then, the amount of melanin in the same part of the face was measured using the JC08 SHM100 Skin Melanin Tester produced by Beijing Beixin Keyi Analytical Instrument Co., Ltd. for three consecutive times, and the average value was taken. The results are shown in Table 4.

[0070] The calculation formula is: Melanin quantity (%) = ((OD 空白 -OD 测试 ) / OD 空白 )×100%.

[0071] Table 4 Melanin presence rate of the examples and comparative examples

[0072]

[0073]

[0074] As shown in Table 4, the whitening composition provided by the present invention can well reduce the presence of melanin. Comparing the results of Examples 1-2 and Comparative Example 2 and the conjecture of the above tyrosinase inhibition rate experiment, it can be seen that although hydroxyethylpiperazineethanesulfonic acid has no effect on the inhibition of tyrosinase, the increase in the content of hydroxyethylpiperazineethanesulfonic acid can effectively reduce the presence of melanin, which may be related to the characteristics of its raw materials, which have the function of mild exfoliation and accelerate the metabolism of the generated melanin.

[0075] 3. Facial brightness L* value and ITA° value test experiment

[0076] The facial brightness L* value and ITA° value can test the brightening effect of the composition on the skin after a short period of use.

[0077] Experimental method: 100 healthy women aged 20-45 were selected and randomly divided into 10 groups, with 10 people in each group. After cleaning their faces, they sat quietly for 30 minutes in a constant temperature and humidity environment (temperature 25±1°C, relative humidity 50±10%). Each group used the compositions of Examples 1-6 and Comparative Examples 1-4 to apply for 15 minutes and then removed them. The L* value and ITA° value of the skin were detected using a CK skin tester and a VISIA skin tester. The test time was before application (blank value), 0min, 5min, 30min, 60min and 120min after removing the film patch. The higher the L* value, the brighter the skin, and the larger the ITA° value, the lighter the skin color. The average value of each group was recorded and calculated. The results are shown in Tables 5-6.

[0078] The calculation formulas are:

[0079] △L* value change rate (%) = ((L* 测试 -L* 空白 ) / L* 空白 )×100%

[0080] △ITA° value change rate (%) = ((ITA° 测试 -ITA° 空白 ) / I TA° 空白 )×100%.

[0081] Table 5 Facial brightness L* value change rate of the embodiment and the comparative example

[0082]

[0083] Table 6 Facial brightness I TA° value change rate of the embodiment and the comparative example

[0084]

[0085]

[0086] It can be seen from Table 5 and Table 6 that the use of the whitening composition provided by the present invention can have a good effect of brightening the skin tone in a short period of time. Combining the △L* value change rate and △I TA° value change rate data of Examples 1-6, it can be concluded that the △L* value change rate is within 0min-30min, and the value is large, which means that the skin lightening effect is more obvious. As time goes by, the skin lightening effect becomes weaker, and the △I TA° value change rate value has not been significant, which means that there is no very big difference in skin color before and after use, indicating that brightening the skin tone is only for a short time, and the real skin tone does not change much. This also shows that the composition provided by the present invention does not whiten in a short period of time, but only brightens the skin tone in a short period of time, which is in line with the concept of healthy whitening. Whitening is a subject that can only be improved by long-term persistence, and healthy whitening can create a good market environment.

[0087] 4. Patch test

[0088] Using the 2022 "Technical Specifications for Safety of Cosmetics" as a reference standard, the whitening compositions of Examples 1-6 were evaluated for cosmetic irritation. The test method was a skin patch test, and 60 people randomly distributed between the ages of 16 and 65 were tested.

[0089] Test method: Prepare the composition into a 10% aqueous solution and put it into a patch tester, the dosage is 0.020-0.025g, cover the patch tester with the test substance on the back or forearm of the subject with a non-irritating cloth-based tape, and gently press it with the palm to make it evenly adhere to the skin surface for 24 hours. After removing the test patch tester, observe the skin reaction 30 minutes after the indentation disappears. If the result is negative, observe again 24 hours and 48 hours after the patch test.

[0090] Evaluation criteria:

[0091] Grade 0: negative reaction;

[0092] Grade 1: Suspicious reaction, only slight erythema;

[0093] Grade 2: weak positive reaction, erythema, infiltration, edema, and papules may be present;

[0094] Grade 3: Strong positive reaction, erythema, infiltration, edema, papules, and the reaction may extend beyond the test area;

[0095] Grade 4: Very strong positive reaction, obvious erythema, severe infiltration, edema, confluent herpes, and the reaction exceeds the test area.

[0096] Test results: Skin reactions were negative in all subjects.

[0097] The above test results show that the whitening composition provided by the present invention is mild and non-irritating to the skin and is safe to use.

[0098] 5. Material stability test

[0099] Stability test: A test method to examine how an item changes over time under the influence of temperature, humidity, light, etc.

[0100] Due to the characteristics of their raw materials, whitening products are very prone to problems such as poor material stability, discoloration and taste change, so it is very necessary to examine the stability.

[0101] Experimental methods:

[0102] The whitening essence containing the whitening efficacy composition was packed into four small bottles, which were placed in an environment of 50°C, 26°C, and -18°C under light, respectively, and the changes in the material were observed after one month.

[0103] Test results: Except for a slight discoloration at 50°C, there was no discoloration or odor change in the other three environments, and the temperature was stable and excellent.

[0104] In summary, the whitening efficacy composition of the present invention covers a variety of whitening pathways, and tranexamic acid, carnosine, and nonapeptide-1 synergize with each other to inhibit tyrosinase activity. Compared with traditional whitening ingredients, tranexamic acid is more stable, resistant to acid and alkalinity, not easily affected by temperature environment, and effectively inhibits tyrosinase activity. Nonapeptide-1 competes with α-MSH for MC1 R receptors to prevent further activation of tyrosinase. Carnosine can achieve the purpose of removing yellowing by inhibiting free radicals, protecting elastin, preventing the formation of glycation end products, and inhibiting tyrosinase activity. Hydroxyethylpiperazineethane sulfonic acid gently exfoliates keratin, making the composition faster and milder whitening. In addition, the whitening efficacy composition of the present invention has the effect of temporarily brightening the skin color, has whitening efficacy when used for a long time, is mild and non-irritating to the skin, is safe to use, and has good stability.

[0105] The above is only a preferred embodiment of the present invention, and the protection scope of the present invention is not limited to the above embodiments. All technical solutions under the concept of the present invention belong to the protection scope of the present invention. It should be pointed out that for ordinary technicians in this technical field, some improvements and modifications without departing from the original material of the present invention should also be regarded as the protection scope of the present invention.

Claims

1. A composition with whitening effect, characterized in that: The invention comprises the following components in weight percentage: 15%-40.0% of tranexamic acid, 20.0%-30.0% of hydroxyethylpiperazineethanesulfonic acid, 1.0%-10.0% of carnosine and 0.01%-0.1% of nonapeptide-1.

2. The composition with whitening effect according to claim 1, characterized in that: The invention comprises the following components in weight percentage: 20%-40.0% of tranexamic acid, 22.0%-28.0% of hydroxyethylpiperazineethanesulfonic acid, 2.0%-8.0% of carnosine and 0.02%-0.08% of nonapeptide-1.

3. The composition with whitening effect according to claim 1, characterized in that: The invention comprises the following components in weight percentage: 20%-35.0% of tranexamic acid, 23.0%-27.0% of hydroxyethylpiperazineethanesulfonic acid, 3.0%-7.0% of carnosine and 0.03%-0.07% of nonapeptide-1.

4. The composition with whitening effect according to any one of claims 1 to 3, characterized in that: Other active ingredients are also included.

5. The composition with whitening effect according to claim 4, characterized in that: The active ingredient includes at least one of a moisturizing ingredient, an antioxidant ingredient, and a whitening ingredient.

6. The composition with whitening effect according to claim 5, characterized in that: The moisturizing ingredient includes at least one of inositol, mannitol and erythritol.

7. The composition with whitening effect according to claim 5, characterized in that: The antioxidant component includes at least one of ergothioneine, ectoine and taurine.

8. The composition with whitening effect according to claim 5, characterized in that: The whitening ingredient includes at least one of glutathione, niacinamide and arbutin.

9. A cosmetic, characterized in that: The invention comprises the composition with whitening effect as described in any one of claims 1 to 8.

10. The cosmetic according to claim 9, characterized in that: The cosmetic is any one of a facial cream, a lotion, a facial mask, an essence, an aqueous solution, a spray, a facial cleanser or a shower gel.

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