Whitening and spot-fading active composition and application thereof in cosmetics

Abstract

The invention belongs to the technical field of cosmetics, and provides a whitening and spot-fading active composition, application of the whitening and spot-fading active composition in cosmetics, a skin care product containing the whitening and spot-fading active composition and a preparation method of the whitening and spot-fading active composition. The whitening and spot-fading active composition is prepared by compounding the following components in percentage by mass: 15%-25% of nicotinamide, 15%-25% of tranexamic acid, 0.1%-0.4% of beta-glucan, 0.5%-1% of nano-coated phenylethyl resorcinol and the balance of water. The skin care product prepared by the invention has both product safety and whitening and spot-fading effectiveness, and meanwhile, the cost investment is effectively reduced.

Description

Technical Field

[0001] The invention belongs to the technical field of cosmetics, and particularly relates to a whitening and spot-lightening active composition and application thereof. Background Art

[0002] The whitening effect of cosmetics is one of the most important effects. More and more research is being conducted on raw materials and formulas that can bring whitening effects. Due to ultraviolet radiation, genetic levels, improper living habits, and aging, people's skin often loses its brightness and even develops spots. The market demand for whitening and spot-removing products is growing.

[0003] Skin color is mainly determined by the content of melanin in the skin. Skin melanin is a ubiquitous biological pigment. The synthesis, transport and metabolism of melanin in melanocytes are complex biochemical processes involving multiple enzymes. Skin whitening needs to start from melanin synthesis, melanosome transport, metabolism, oxidative stress, ultraviolet stimulation and other environmental stimuli to achieve the desired effect. Skin whitening is mainly carried out from the following three aspects: inhibiting the synthesis of melanin, regulating the melanin metabolic pathway, and promoting melanin metabolism.

[0004] Whitening products contain ingredients with whitening effects. To achieve the whitening effect, these ingredients often need to be added to the effective concentration. If a single ingredient is added in too much, it will cause greater irritation to the skin, and some people will experience tingling and tight skin during or after use. Even if a combination of multiple whitening ingredients can reduce the irritation caused by a single ingredient, due to the synergistic effect of whitening ingredients, different consumers have different tolerance levels to different ingredients, and the number of skin intolerances after use has also increased. In addition, some products will add physical ingredients such as titanium dioxide to achieve an immediate whitening effect. These ingredients will adhere to the surface of the skin and are not easy to clean thoroughly. Long-term use will cause skin problems such as clogged pores and acne. There are also a considerable number of whitening products with heavy effects, which are combined with acidic ingredients to peel off waste keratin. They can bring obvious whitening effects in the short term, but consumers cannot use them for a long time, and after discontinuation due to factors such as living habits and ultraviolet radiation, they will "return to black".

[0005] Therefore, it is of great practical significance to develop a safe, mild, non-irritating whitening and spot-removing active composition with strong whitening and spot-removing effects and use it in skin care products. Summary of the invention

[0006] The purpose of the present invention is to provide a safe and effective whitening and freckle-removing active composition, which is mild and non-irritating and has good whitening and freckle-removing effects, and is suitable for the preparation of whitening and freckle-removing skin care products.

[0007] The technical solution of the present invention is:

[0008] The invention provides a whitening and freckle-removing active composition, which is compounded from the following four raw materials: niacinamide, tranexamic acid, nano-encapsulated phenethyl resorcinol and beta-glucan.

[0009] Nicotinamide, also known as vitamin B3, has a high purity and reduces the irritation caused by niacin. It can inhibit melanin deposition, reduce the melanin that has been generated and precipitated, and block its transfer to the surface cells. Tranexamic acid, also known as tranexamic acid and tranexamic acid, can indirectly inhibit the activity of tyrosinase and melanocytes, block the path of melanin formation, and thus achieve a whitening effect. At the same time, tranexamic acid, as a protease inhibitor, can also prevent pigmentation caused by ultraviolet rays. Nano-encapsulated phenylethyl resorcinol can inhibit the activity of tyrosinase, effectively reduce the production of melanin, improve uneven skin color, have a strong whitening and spot-lightening effect, and reduce the darkening of skin color caused by ultraviolet radiation. β-Glucan, derived from highland barley oats, can promote the proliferation of Langerhans cells, repair damaged skin, has significant anti-inflammatory and anti-allergic activity, and can also form a moisturizing film on the skin surface to effectively lock in skin moisture.

[0010] On one hand, the present invention provides a whitening and spot-lightening active composition, which is made of the following raw materials by mass percentage: 15%-25% niacinamide, 15%-25% tranexamic acid, 0.1%-0.4% β-glucan, 0.5%-1% nano-encapsulated phenylethyl resorcinol, and the balance is water. The composition is scientifically and rationally proportioned, and the components have different functions but complement each other, so that it has significant whitening and antioxidant effects, and is mild and safe.

[0011] In one or more embodiments, the mass percentage of nicotinamide is 15%-25%, for example, 15%, 20% or 25%, preferably 15%-20%, and more preferably 20%.

[0012] In one or more embodiments, the mass percentage of tranexamic acid is 15%-25%, for example, 15%, 20%, 25%, preferably 20%-25%, and more preferably 25%.

[0013] In one or more embodiments, the mass percentage of the nano-encapsulated phenethyl resorcinol is 0.5%-1%, for example, it can be 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1%, and more preferably 0.7%.

[0014] In one or more embodiments, the mass percentage of β-glucan is 0.1%-0.4%, for example, 0.1%, 0.2%, 0.3%, 0.4%; more preferably 0.4%.

[0015] As a further technical solution, in the whitening and spot-removing active composition, the mass percentage of niacinamide: the mass percentage of tranexamic acid is ≤1.25, for example, the ratio between the two is 25:20, 25:25, 20:25, 20:20, 15:15; more preferably, the mass percentage of niacinamide: the mass percentage of tranexamic acid is ≤1, for example, 20:20, 20:25 or 15:15.

[0016] As a further technical solution, the whitening and spot-lightening active composition has a nano-encapsulated phenethyl resorcinol content of 0.5%-0.7% by mass.

[0017] As a further technical solution, the mass percentage of β-glucan in the whitening and spot-removing active composition is 0.1-0.2%.

[0018] Another aspect of the present invention provides a whitening and freckle-removing skin care product, which comprises the above-mentioned whitening and freckle-removing active composition and a skin care product base substance.

[0019] The skin care product is one of lotion, cream, mask, toner and essence.

[0020] Preferably, the mass percentage of the whitening and spot-lightening active composition in the whitening and spot-lightening skin care product is ≤10%. By adding the whitening and spot-lightening active composition of the present invention, the prepared skin care product has both good whitening and spot-lightening effects and is mild and non-irritating.

[0021] Preferably, when the skin care product is an essence, the basic substance of the skin care product includes 5-15% moisturizer, 0.2-5% thickener, 0.5-5% emulsifier, 1-15% oil, 0.05-0.9% preservative, 0.05-0.5% fragrance and the balance water.

[0022] Preferably, the moisturizing agent includes at least one of glycerin, propylene glycol, butylene glycol, 1,3-propanediol, sodium hyaluronate, sugars, and polyethylene glycol.

[0023] Preferably, the thickener includes at least one of xanthan gum, carbomer, cellulose, carrageenan, gellan gum, polyacrylic acid copolymer, and magnesium aluminum silicate.

[0024] Preferably, the emulsifier includes at least one of PEG-100 stearate, glyceryl stearate, polysorbate-20, and polyglyceryl-6 distearate.

[0025] Preferably, the oil comprises at least one of squalane, isopropyl palmitate, caprylic / capric triglyceride, and tocopherol acetate.

[0026] Preferably, the preservative includes at least one of benzyl alcohol and phenoxyethanol.

[0027] Preferably, the flavor includes at least one of Morgelbert daisy and chamomile flavor.

[0028] Another aspect of the present invention provides use of the above-mentioned whitening and spot-lightening active composition for preparing whitening and spot-lightening skin care products.

[0029] Another aspect of the present invention further provides a method for preparing the above-mentioned whitening and spot-lightening skin care product, comprising the following steps:

[0030] (1) Add moisturizer, thickener, emulsifier and oil into the main pot, heat to 60-70℃, homogenize and disperse evenly, and keep warm for 30 minutes;

[0031] (2) cooling the product of (1) to 40-45° C., adding the whitening and spot-lightening active composition, preservatives and essence, and stirring to mix evenly;

[0032] The product of (2) is cooled to 38°C to obtain a whitening and spot-removing skin care product.

[0033] Compared with the prior art, the present invention has the following beneficial effects: by combining nicotinamide, tranexamic acid, β-glucan and nano-encapsulated phenylethyl resorcinol within a specific mass ratio to prepare a whitening and freckle-removing active composition, the four components cooperate with each other to give full play to their functions, which not only reduces the content of effective ingredients that easily cause skin irritation, but also maintains or even enhances the whitening and freckle-removing effect of the composition. The obtained whitening and freckle-removing skin care product has both product safety and whitening and freckle-removing effectiveness, while effectively reducing cost investment. DETAILED DESCRIPTION

[0034] After extensive and in-depth research, the present invention has developed a whitening and spot-removing active composition, which is mild and non-irritating and has a strong whitening effect. It is easy to add to the formula of skin care products and can effectively solve the problems of safety, irritation and efficacy of skin care products.

[0035] Unless otherwise specified, the raw materials, reagents or devices used in the following examples can be purchased from conventional commercial sources or obtained by existing known methods.

[0036] The whitening and freckle-removing active composition of Examples 1-5 of the present invention is obtained by compounding: niacinamide (trade name: Fantelus), nano-encapsulated phenethyl resorcinol (purchased from: Purui Biopharmaceuticals, NanoActive 377), β-glucan (purchased from: Shanghai Lanhai Biotechnology Co., Ltd.), and tranexamic acid (purchased from: Boying). The formula (mass percentage) of the whitening and freckle-removing active composition of Examples 1-5 is as follows;

[0037] Table 1. Formula of the whitening and spot-lightening active composition of Examples 1-5 (mass percentage %)

[0038]

[0039] The four substances in Table 1 are added into water in order according to the formula amount, heated and stirred evenly at a temperature not exceeding 50° C., and compounded to obtain a whitening and spot-lightening active composition.

[0040] Example 6 Essence prepared from whitening and spot-lightening active composition and preparation method

[0041] Table 2. Formula for preparing whitening essence using the whitening and spot-lightening active composition of Examples 1-5 (mass percentage %)

[0042]

[0043] *The whitening and spot-lightening active compositions are the whitening and spot-lightening active compositions obtained in Examples 1-5, respectively.

[0044] The preparation method of the essence is as follows:

[0045] 1) Add raw materials 1-6 in Table 2 into the main pot, heat to 60-70°C, homogenize and disperse evenly, and keep warm for 30 minutes;

[0046] 2) When the temperature of the product in 1) drops to 40-45°C, add raw materials 7-9 and stir to mix evenly;

[0047] 3) Cool the product in 2) to below 38°C and discharge.

[0048] Effect Example 1 Animal Safety Evaluation of Whitening and Spot-Removing Active Compositions of Examples 1-5

[0049] Test samples: the whitening and spot-removing active compositions of Examples 1-5, and two positive controls (two commercially available whitening essences: Commercially available product 1 (Comparative Example 1): Water-based Whitening Essence (main whitening active ingredients: 5% niacinamide, 0.05% to 5% hexyldecanol, 0.2% to 2% undecylenoyl phenylalanine, inositol, and ascorbyl glucoside, see CN104768525B); Commercially available product 2 (Comparative Example 2): Bright Diamond Whitening Essence Milk, whose main whitening active ingredients include: Zhenbaiyin Pro (see CN111850073B, hydrolyzed conchiolin and calcium lactate), encapsulated 377 (phenylethyl resorcinol), glycyrrhizin, niacinamide).

[0050] (1) Experimental animals: The experimental animals were New Zealand rabbits; the grade was ordinary; female animals were selected from non-pregnant and non-fertile animals; the animal weight was 2.0kg to 3.0kg; the animals were sourced from Pizhou Dongfang Breeding Co., Ltd. Also attached: Experimental Animal Production License No.: SCXK (Su) 2022-0004; Quality Certificate No.: B202401040357.

[0051] (2) Skin irritation test

[0052] There are 4 rabbits in each group. The hair on both sides of the rabbit's spine is shaved off, covering an area of ​​3cm×3cm. 0.5ml of the test sample is applied to the left skin, covering an area of ​​2.5cm×2.5cm. The skin on the other side is used as a control and applied once a day for 14 consecutive days. Starting from the second day, shave the hair before each application, and use warm water to remove the residual test substance. Observe the results after one hour and score according to P491 of the "Technical Specification for Safety of Cosmetics" (2015 Edition) (hereinafter referred to as the specification). The skin on both sides is treated in the same way. The average score of each animal per day is calculated according to the formula, and the skin irritation intensity is determined according to P492 in the specification.

[0053] Table 3 Skin irritation reaction scores

[0054]

[0055] Table 4 Multiple skin irritation test in rabbits

[0056]

[0057] The results of multiple skin irritation tests on rabbits show that the whitening and spot-lightening active compositions of Examples 1-5 are non-irritating and safer than commercially available products.

[0058] (3) Rabbit acute eye irritation test

[0059] Before the experiment, the animals must adapt to the experimental animal room environment for at least 3 days; both eyes of the experimental animals must be examined (using sodium fluorescein) within 24 hours before the start of the experiment; animals with symptoms of eye irritation, corneal defects and conjunctival damage cannot be used for experiments.

[0060] Three rabbits were selected from each group. 0.1 mL of the test sample was dropped into the left conjunctival sac to make the upper and lower eyelids passively closed for 1 second. The right eye was left untreated as a self-control. At the 30th second, the eyes were rinsed with sufficient water at a fast flow rate that would not cause damage to the animals' eyes for 30 seconds. Then the eyes were inspected and scored according to the Cosmetic Safety Technical Specification P107.

[0061] Table 5 Results of rabbit eye irritation test

[0062]

[0063]

[0064]

[0065] The results of the rabbit acute eye irritation experiment show that the whitening and spot-lightening active compositions of Examples 1-5 are non-irritating and are superior to commercially available products.

[0066] Effect Example 2 Skin Patch Test

[0067] Test samples: the whitening and spot-lightening active compositions of Examples 1-5, and two comparative examples (two commercially available whitening essences).

[0068] Test method: 35 subjects were tested, all of whom met the criteria for subjects. Test samples were placed in the small chamber of the spot tester, with a dosage of about 0.020mL-0.025mL. The control well was a blank control (no substance was placed). The spot tester with the test sample was applied to the back or curved side of the forearm of the subject with a low-allergenic tape, and the palm of the hand was gently pressed to evenly apply it to the skin for 24 hours. The skin reaction was observed according to the standards in the table below 30 minutes (after the indentation disappears), 24 hours and 48 hours after the removal of the test sample spot tester, and the observation results were recorded.

[0069] Table 6 Skin reaction grading standards for skin occlusion patch test

[0070]

[0071] Table 7 Skin patch test results

[0072]

[0073] The results of human skin patch tests showed that the whitening and freckle-removing active composition had no irritation to the skin and was superior to two commercially available whitening essence samples.

[0074] Effect Example 3 Antioxidant Capacity Test

[0075] Test samples: The whitening and spot-removing active compositions of Examples 1-5 were prepared into essence samples using Formula Example 1 in Table 2, namely Essence 1-1, Essence 1-2, Essence 1-3, Essence 1-4 and Essence 1-5, as well as the above two commercially available products (Comparative Examples 1 and 2).

[0076] Test method: 6 ml of 2 mg / mL DPPH methanol solution absorbance (1 ± 0.02) was mixed with the test samples prepared from essences 1-1 to 1-5 and two commercially available whitening essences. The reaction mixture was shaken at room temperature, kept in the dark for 20 minutes, and the absorbance value (A) was measured at a wavelength of 517 nm. 测试样品 ). Methanol was used as a blank control sample instead of the sample solution (A 对照样品 ), the scavenging performance of DPPH free radicals is calculated according to the formula:

[0077] DPPH clearance rate % = (A 对照样品 -A 测试样品 ) / A 对照样品 ×100%

[0078] The linear regression analysis of the dose-effect curve between DPPH free radical scavenging performance and sample concentration was performed, and the results were expressed as IC 50 Indicates. IC 50 Refers to the mass concentration of the sample required to reduce the DPPH free radical concentration by 50% (mg / ml), IC 50 The lower the value, the higher the free radical scavenging activity.

[0079] Table 8 DPPH removal rate%

[0080]

[0081] From the above antioxidant capacity test results, it can be seen that the antioxidant capacity of essences 1-1 to 1-5 is significantly better than that of the two commercially available whitening essence samples.

[0082] Effect Example 4 Tyrosinase Inhibition Experiment

[0083] Polyphenol oxidase, also known as tyrosinase, is a key enzyme in the synthesis of melanin in organisms. It can catalyze L-dopa to produce dopachrome. Its product has a characteristic absorption peak at λ=475nm, and then the activity of tyrosinase is measured and the inhibition rate of tyrosinase activity of the sample is calculated.

[0084] Phosphate buffer solution (pH=6.86): Mix 0.1 mol / l sodium phosphate solution and 0.1 mol / l potassium hydrogen phosphate solution in a ratio of about 1:2 and stir evenly.

[0085] Levodopa test solution: Weigh 39.4 mg of Levodopa powder and dissolve it in 100 mL of phosphate buffer (pH=6.86) to prepare a 2 mmol / L test solution.

[0086] Tyrosinase test solution: Weigh 2 mg of tyrosinase powder and dissolve it in 12.4 mL of phosphate buffer (pH=6.86) to prepare 200 U / L tyrosinase test solution.

[0087] Test samples: The whitening and spot-lightening active composition samples of Examples 1-5 and 2% α-arbutin as a positive control were diluted with deionized water to 4 times and 16 times, respectively, and together with the original concentrations formed 3 concentration gradients to be tested, as shown in Table 9, and the experimental grouping settings are shown in Table 10.

[0088] Table 9 Tyrosinase activity inhibition test sample solution concentration gradient setting (%)

[0089]

[0090] Table 10 Tyrosinase activity inhibition test group settings

[0091]

[0092] According to Tables 9 and 10, the test sample solutions of each gradient concentration, the corresponding phosphate buffer solution, and the tyrosinase test solution were added to a 96-well plate, mixed and incubated at 25°C for 5 minutes, then the levodopa test solution was added, mixed and incubated at 25°C for 10 minutes, and the absorbance A was measured at λ = 475 nm using an enzyme reader. 475 , set up 3 replicate wells in each group, and take A after detection 475 The tyrosinase inhibition rate of each group of test samples was calculated according to the following formula:

[0093] Tyrosinase inhibition rate = 1- ×100%

[0094] Table 11 Tyrosinase activity inhibition rate of test samples and positive controls

[0095]

[0096] Preliminary experiments have shown that within the specified proportion range of the composition, if any component is removed, the whitening and freckle removal effect will be weakened.

[0097] It can be seen from the above experimental results that the whitening and freckle-removing active composition of the present invention has a strong antioxidant capacity and can bring about whitening and freckle-removing effects after long-term use.

[0098] This specification selects and specifically describes the above embodiments in order to better explain the principles and practical applications of the present invention, so that those skilled in the art can better understand and use the present invention. All details are not described in detail, nor is the invention limited to the specific implementation methods described. Obviously, modifications and changes can be made according to the content of this specification, and these equivalent forms also fall within the scope defined by the claims attached to this application.

Claims

1. A whitening and spot-lightening active composition, Features: The invention is prepared from the following raw materials by mass percentage: 15%-25% niacinamide, 15%-25% tranexamic acid, 0.1%-0.4% beta-glucan, 0.5%-1% nano-encapsulated phenylethyl resorcinol, and the balance is water.

2. The whitening and spot-lightening active composition according to claim 1, Features: Nicotinamide mass: Tranexamic acid mass ≤1.

25.

3. The whitening and spot-lightening active composition according to claim 2, Features: Niacinamide mass: Tranexamic acid mass ≤1.

4. The whitening and spot-lightening active composition according to claim 1, Features: The mass percentage of the beta-glucan in the raw material is 0.1%-0.2%, and the mass percentage of the nano-encapsulated phenylethyl resorcinol in the raw material is 0.5-0.7%.

5. A skin care product for whitening and lightening spots. It is characterized in that Contains the whitening and spot-lightening active composition as claimed in any one of claims 1 to 4.

6. The whitening and spot-lightening skin care product according to claim 5, It is characterized in that The mass percentage of the whitening and spot-lightening active composition in the skin care product is ≤10%.

7. The whitening and spot-lightening skin care product according to claim 5, It is characterized in that The skin care product is a whitening essence, which also includes the following components: a moisturizer, a thickener, an emulsifier, a preservative and a fragrance; the moisturizer includes at least one of glycerin, propylene glycol, methylpropanediol, butylene glycol, sodium hyaluronate, sugars and polyethylene glycol; the thickener includes at least one of biosaccharide gum, xanthan gum, carbomer, cellulose, carrageenan, gellan gum, polyacrylic acid copolymer and magnesium aluminum silicate; the preservative includes at least one of benzyl alcohol and phenoxyethanol.

8. Use of the whitening and spot-lightening active composition according to any one of claims 1 to 4 in the preparation of whitening and spot-lightening skin care products.

9. The preparation process of the whitening and spot-lightening skin care product according to claim 7, Features: The following steps are involved: (1) Add moisturizer, thickener, emulsifier and oil into the main pot, heat to 60-70°C, homogenize and disperse evenly, and keep warm for 30 minutes; (2) cooling the product of (1) to 40-45° C., adding the whitening and spot-lightening active composition, preservatives and essence, and stirring to mix evenly; (3) Cooling the product of (2) to 38° C. to obtain a whitening and spot-removing skin care product.

Images