Composition with functions of uniformizing skin color, brightening and whitening as well as preparation method and application of composition

By using compositions of α-arbutin liposomes, grape seed extract and nicotinamide, the existing whitening technology is difficult to solve the problem of yellowing, redness and excessive melanin at the same time, and the effect of whitening, even skin tone and brightening skin tone is achieved, meeting consumers' needs for "healthy whiteness" and "even-formal whiteness".

CN120168375APending Publication Date: 2025-06-20MAGELINE BIOLOGY TECH CO LTD
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Patent Information

Application Number
CN202510317495.9
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-03-18
Publication Date
2025-06-20

AI Technical Summary

Technical Problem

Existing whitening technologies are difficult to solve the problems of yellowing, redness and excessive melanin at the same time, and cannot meet consumers' needs for "healthy whiteness" and "even-formal whiteness".

Method used

Using a composition of α-arbutin liposomes, grape seed extract and nicotinamide, the effect of whitening, even skin tone and brighten skin tone by reducing skin inflammation, inhibiting melanocyte activation, improving skin barrier function and anti-saccharification.

Benefits of technology

It achieves the effect of reducing the expression of melanin on the skin while improving the dull yellowness and redness of the skin, achieving whitening, even skin tone and brighten the skin tone, meeting consumers' needs for "healthy whiteness" and "even-formal whiteness".

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention relates to a composition capable of uniformizing skin color, brightening and whitening as well as a preparation method and application of the composition. The composition comprises alpha-arbutin liposome, a grape seed extract and nicotinamide in a mass ratio of (0.1-2): (0.1-10): (0.1-5). Compared with the prior art, the composition disclosed by the invention is complementary in action mechanism and is jointly applied to reduce skin melanin expression and improve dull yellow and red skin at the same time, so that the effects of whitening, homogenizing and brightening the skin color are achieved, and the specific requirements of different consumers on whitening are met.
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Description

Technical Field

[0001] The present invention relates to the field of cosmetics, and in particular to a composition with skin tone even - ing, brightening and whitening effects, and its preparation method and application. Background Art

[0002] Since ancient times, "bright, fair and flawless" skin has been regarded as a symbol of beauty and health. This aesthetic concept has been dominant from ancient Greece and ancient China until before sun - tanning became fashionable. For many people, the meaning of whitening is not only about pursuing beauty, but more about pursuing freedom and confidence. Nowadays, whitening is still one of the main demands of consumers. However, with the transformation of consumers' cognition and needs, the blind pursuit of "extremely white" has changed to a rational pursuit of whitening combined with their own skin types and scenarios. The dull skin color caused by staying up late and other scenarios, and the flushing accompanied by inflammatory reactions have gradually attracted attention to the needs of "removing yellowing" and "fading redness", and the "healthy white" with natural and bright skin color has become the new pursuit of whitening.

[0003] The color of normal skin depends on the amounts of melanin, carotene, oxyhemoglobin and deoxyhemoglobin in the skin, and is also closely related to many factors such as the thickness and water content of the stratum corneum, blood flow, and oxygen content in the blood. Melanin is the most important pigment that determines the color of human skin. It is synthesized in melanocytes located in the basal layer of the epidermis, and then is transferred to adjacent keratinocytes through the dendritic processes of melanocytes, and moves towards the upper layer of the epidermis along with keratinocytes, thus affecting the color of the skin.

[0004] Skin yellowing is mainly caused by glycation reaction of the skin and excessive sebum secretion. As people age, the pressure of life and work increases, and coupled with irregular living and eating habits, the human body begins to age, the metabolism slows down, and excessive sugars (such as glucose, fructose, galactose, etc.) accumulate in the body. These sugars will combine with proteins in the body to form brown glycated proteins inside the skin. When this substance accumulates to a certain amount inside the skin, the skin will turn yellow. In addition, when the skin produces too much oil, the secreted sebum and sweat mix together to form a thick oil film on the skin surface, which will reduce the ability to reflect light, making the skin color dull and yellow. In addition, the excessive sebum secreted by the skin is oxidized, which will also make the skin turn yellow. These sebum will also mix with exfoliated dandruff, a large amount of dust, heavy metals and other pollutants in the air, and various powders in makeup, making the skin dull.

[0005] There are many reasons for skin flushing, such as excessive cleansing, damage to the skin barrier caused by external stimuli, thinning of the stratum corneum; acne, rosacea, which cause capillary dilation in order to resist inflammation. In addition, there is also long-term sun exposure, and the compensatory dilation of blood vessels on the plateau leads to a decrease in the elasticity of the blood vessel wall and the inability to contract. The dilation and congestion of small blood vessels and capillaries on the skin surface are the fundamental reasons for skin flushing.

[0006] At present, there have been many studies and applications in the field of skin whitening. However, the relevant research mainly focuses on inhibiting the activity of tyrosinase and hindering the maturation of tyrosinase (the main active ingredients used include tranexamic acid, arbutin, 377, etc.); reducing intermediate melanin products and hindering melanin oxidation (the main active ingredients used include VC, glutathione, astaxanthin, etc.); hindering melanin transport, so that the generated melanin cannot be transported to keratinocytes (the main active ingredient used is niacinamide), and accelerating the shedding of melanin that has been transferred to keratinocytes (the main active ingredients used include A-alcohol, fruit acids, salicylic acid components, etc.). However, using such whitening ingredients alone cannot solve the problems of skin yellowing and flushing, and cannot meet consumers' advanced needs for whitening.

[0007] For example, in patent CN202410289874.7, the whitening effect is mainly achieved through plant extracts, and there are problems such as a single action pathway, unclear action mechanism, and insignificant whitening effect.

[0008] For example, in patent CN202311130400.X, the whitening effect is mainly achieved by regulating the generation, metabolism, and transport of melanin, and it cannot solve the problems of skin dullness, yellowing, and flushing after staying up late. Simply reducing melanin in the skin cannot meet today's consumers' pursuit of "healthy white" and "even white" skin color. Summary of the Invention

[0009] The purpose of the present invention is to overcome the above-mentioned defects existing in the prior art and provide a composition with the functions of skin tone uniformity, brightening, and whitening, as well as its preparation method and application.

[0010] The purpose of the present invention can be achieved through the following technical solutions: A composition with the functions of skin tone uniformity, brightening, and whitening, which comprises α-arbutin liposomes, grape seed extract, and niacinamide in a mass ratio of (0.1-2):(0.1-10):(0.1-5).

[0011] Furthermore, the mass ratio of the α-arbutin liposomes, grape seed extract, and niacinamide is (0.1-1):(0.1-7):(0.1-2.5).

[0012] Furthermore, the α-arbutin liposomes are prepared by the following method:

[0013] (1) Dissolve cholesterol and non-ionic surfactant fully in chloroform. After stirring until fully dissolved, transfer it to a rotary evaporator and remove the solvent chloroform by vacuum distillation (under vacuum distillation at a certain temperature, such as 50 - 60 °C), so that the lipid components form a uniform lipid film on the inner wall of the container;

[0014] (2) Add PBS buffer to the container containing the lipid film and stir (a common stirrer can be used, such as a magnetic stirrer) to fully mix the lipid film and the PBS buffer to form a liposome suspension;

[0015] (3) Stir and mix PBS buffer and α - arbutin evenly;

[0016] (4) Slowly add the mixed solution obtained in step (3) to the liposome suspension obtained in step (2), and stir and mix evenly;

[0017] (5) Place the liposome suspension containing α - arbutin obtained in step (4) in an ice bath device, quickly cool it to near the freezing point (about 0 °C) and keep it for 25 - 35 min, then take it out, thaw it at room temperature for 30 min - 60 min, and then perform ultrasonic treatment and filtration to obtain α - arbutin liposomes.

[0018] Further, the non - ionic surfactant in step (1) is Tween 20 and Span 20 with a molar ratio of 1:1, the molar ratio of the non - ionic surfactant to cholesterol is 2:1, and the volume ratio of the sum of the mass of cholesterol and the non - ionic surfactant to chloroform is (40 - 500):(4 - 40) mg / ml;

[0019] Further, the rotation speed of the rotary evaporator in step (1) is 150 rpm;

[0020] In step (2), the pH of the PBS buffer is 6.5, and the mass - to - volume ratio of the lipid film to the PBS buffer is (20 - 30):(1 - 2) mg / ml;

[0021] Further, the rotation speed of stirring in step (2) is 120 rpm;

[0022] In step (3), the mass - to - volume ratio of α - arbutin to the PBS buffer is (100 - 400):(20 - 50) mg / mL;

[0023] In step (5), the ultrasonic power is 200 W, the frequency is 40 kHz, and the ultrasonic time is 5 minutes;

[0024] Further, the particle size of the obtained α - arbutin liposomes is between 0.1 - 1 μm.

[0025] The present invention also provides a skin care product containing the composition, and the dosage of the composition in the skin care product is 1-14 parts by weight.

[0026] Further, the skin care product includes lotion, facial mask liquid, cream, essence, freeze-dried powder or skin care lotion.

[0027] Further, the skin care product is facial mask liquid, and the facial mask liquid further includes A-phase auxiliary materials, B-phase auxiliary materials, C-phase auxiliary materials and D-phase auxiliary materials;

[0028] Based on 100 parts by weight of the facial mask liquid,

[0029] The A-phase auxiliary materials include 0.1 part - 25 parts of thickener, 0.15 part - 6 parts of skin conditioner A and 1 part - 30 parts of humectant A;

[0030] The B-phase auxiliary materials include 0.2 part - 25 parts of skin conditioner B, 0.1 part - 15 parts of emulsifier and 1 part - 15 parts of esterifying agent;

[0031] The C-phase auxiliary materials include 0.1 part - 5 parts of pH regulator;

[0032] The D-phase auxiliary materials include 0.1 part - 1 part of fragrance and 0.15 part - 1 part of preservative.

[0033] Further, the thickener includes one or more of acrylate / C10-30 alkyl acrylate cross-linked polymer, polyacrylamide, xanthan gum, propylene glycol, behenyl alcohol, carbomer, laureth-7, cetyl alcohol, stearyl alcohol and hydroxyethyl cellulose;

[0034] The skin conditioner A and the skin conditioner B each independently include one or more of glycerol, isocetane, olive oil, sodium hyaluronate, lauryl alcohol, shea butter, allantoin, butylene glycol, squalane, panthenol, lactic acid, tocopherol and dipotassium glycyrrhizate;

[0035] The humectant A includes one or more of hyaluronic acid, allantoin, glycerol, ceramide, sodium lactate, butylene glycol, ethylhexylglycerin, hydrogenated grape seed oil, olive oil and shea butter;

[0036] The emulsifier includes one or more of glyceryl stearate citrate, cetearyl glucoside (and) cetearyl alcohol, behenyl trimethyl ammonium methyl sulfate, coconut oil glycerides and sorbitan oleate;

[0037] The pH regulator includes one or more of arginine and lactic acid;

[0038] The fragrance includes essence;

[0039] The preservative includes one or more of phenoxyethanol, ethylhexylglycerin, and pentylene glycol.

[0040] The present invention also provides a method for preparing a skin care product, which includes the following steps:

[0041] a. Aqueous phase: Each component of the excipients in Phase A is fully wetted and mixed, then added to water, stirred thoroughly until completely dissolved, and heated.

[0042] b. Oil phase: The excipients in Phase B are mixed and heated, stirred until completely dissolved.

[0043] c. Emulsification: The mixture in step b is added to the aqueous phase in step a, stirred and homogenized.

[0044] d. Add the excipients in Phase C, stir and homogenize, and stir to cool down to 40 - 50 °C.

[0045] e. Add the excipients in Phase D, stir and homogenize.

[0046] f. Wait until the temperature is stirred down to 35 - 38 °C, add the functional ingredient composition E, stir and homogenize, and then the mask liquid is obtained.

[0047] Further, the heating temperature in steps a - b is 75 - 80 °C;

[0048] The stirring speed in steps c - f is 200 - 400 rpm, and the stirring time is 3 - 5 minutes;

[0049] The homogenization speed in steps c - f is 2000 - 4000 rpm, and the homogenization time is 3 - 5 minutes.

[0050] Compared with the prior art, the present invention has the following beneficial effects:

[0051] 1. In the present invention, through the synergistic effect of α - arbutin liposomes, grape seed extract, and niacinamide, among which α - arbutin liposomes can reduce skin inflammation, accelerate cell metabolism, slow down skin oxidation; grape seed extract can inhibit the expression of c - Kit protein, block signals, reduce the activation of melanocytes, inhibit the activity of tyrosinase, and increase the autophagy activity of melanocytes; niacinamide can improve the barrier function, resist skin aging, anti - glycation, and reduce sebum production. The three act synergistically from different pathways, while reducing the expression of skin melanin, improving skin sallow and flushing, achieving the effects of whitening, even skin tone, and brightening skin tone, meeting the specific whitening needs of different consumers. Compared with the existing inventions, the whitening mechanism is more perfect and can better meet the needs of consumers.

[0052] 2. The present invention wraps α - arbutin using liposome - like encapsulation technology, enhancing its stability, encapsulation efficiency, skin permeability, sustained - release performance, biocompatibility, biodegradability and reducing its irritation. Compared with existing inventions, it solves the problems that α - arbutin is vulnerable to light and cannot be completely absorbed by the skin, reducing the risk of arbutin being converted into hydroquinone under external influence, thereby increasing the usability and safety of the composition. BRIEF DESCRIPTION OF THE DRAWINGS

[0053] Figure 1 Photographs of skin glossiness on the 0th, 14th, and 28th days using the product obtained in Example 3;

[0054] Figure 2 Photographs of skin transparency on the 0th, 14th, and 28th days using the product obtained in Example 3. DETAILED DESCRIPTION OF THE INVENTION

[0055] The present invention will be described in detail below with reference to specific embodiments.

[0056] The present invention selects specific proportions of α - arbutin liposome - like, grape seed extract, and niacinamide to act synergistically. By reducing skin inflammation, accelerating cell metabolism, slowing down skin oxidation, inhibiting the expression of c - Kit protein, blocking signals, reducing the activation of melanocytes, inhibiting tyrosinase activity, and increasing the autophagy activity of melanocytes, etc., they act synergistically to reduce the expression of skin melanin while improving skin sallowness and flushing, achieving the effects of whitening, skin tone evenness, and skin brightening, meeting the specific whitening needs of different consumers. Compared with existing inventions, the whitening mechanism is more perfect and can better meet consumer needs. The specific description is as follows:

[0057] Arbutin, namely 4-hydroxyphenyl-β-D-glucopyranoside, also known as arbutoside and arbutin, is mainly extracted from the leaves of arbutus plants and is divided into α-type and β-type. The whitening effect of α-arbutin is 10 to 15 times that of β-arbutin. It can inhibit the tyrosinase activity of melanocytes and melanoma cells by increasing the activity of superoxide dismutase (SOD) in local skin tissues, significantly reducing the contents of tyrosine and malondialdehyde (MDA), thus promoting the redox reaction of skin cells, reducing free radical production, and inhibiting melanin formation. Secondly, arbutin has significant anti-inflammatory activity and shows strong anti-inflammatory effects in multiple experimental models. Arbutin also enhances autophagy by activating Sirt1, thereby effectively inhibiting inflammation and apoptosis. Through the Sirt1 / Nrf2 / NF-κBp65 pathway, α-arbutin can reduce the levels of inflammatory cytokines such as tumor necrosis factor α (TNF-α), interleukin 1β (IL-1β), and interleukin 6 (IL-6). α-Arbutin can also reduce the levels of oxidative stress markers (such as MDA) and increase the activity of superoxide dismutase (SOD), indicating its dual effects of antioxidant and anti-inflammatory.

[0058] At present, α-arbutin has been widely used in cosmetics. However, affected by factors such as acidity, temperature, light, and microorganisms, there is a risk of conversion into hydroquinone. Hydroquinone has a stimulating effect on the skin, can cause erythema, desquamation, pain, damage human DNA, is toxic to germ cells, and is also a potential carcinogen. In this invention, the safety and stability of α-arbutin are improved through niosome encapsulation technology. Niosomes are single or multi-layer vesicles composed of non-ionic surfactants and cholesterol, so they are also called non-ionic surfactant vesicles. Compared with liposomes, niosomes show excellent stability, encapsulation efficiency, skin permeability, sustained release performance, biocompatibility, biodegradability, and low irritation, and have a lower cost. Niosomes can effectively deliver compositions, reduce oxidation, photosensitivity / thermosensitivity and other effects, and improve the stability and transdermal absorption rate of active ingredients.

[0059] Grape seed extract (VITIS VINIFERA (GRAPE) SEED EXTRACT) is used as an antioxidant and astringent in cosmetics. It has a significant ROS scavenging effect, reflecting antioxidant effects and anti-inflammatory and soothing effects. It can reduce skin inflammatory reactions and lipid oxidation, thereby reducing skin flushing and sallowness, brightening, and evening out skin tone. In addition, grape seed extract can significantly inhibit the expression of c-Kit. The c-Kit protein is a transmembrane receptor tyrosine kinase. Binding to its specific ligand can activate melanocytes, increasing the proliferation, differentiation of melanocytes, and the synthesis of melanin. Grape seed extract can block the signal by inhibiting the expression of c-Kit protein in B16 cells, reducing the activation of melanocytes, and can significantly inhibit the activity of tyrosinase, increasing the autophagy activity of melanocytes, promoting the degradation of melanosomes in melanocytes, and clearing melanin, thus making the skin tone more uniform, delicate, and shiny.

[0060] Niacinamide, also known as nicotinamide, is the amidated product of niacin and belongs to the B vitamins. Its whitening mechanism is mainly to inhibit the formation of melanin and the transfer of melanin to keratinocytes. When some melanin inevitably reaches the surface skin, niacinamide can promote the shedding of epidermal cells containing melanin by accelerating the renewal rate of skin cells. In addition, niacinamide is a component of coenzyme I-NAD (nicotinamide adenine dinucleotide) and coenzyme II-NADP (nicotinamide adenine dinucleotide phosphate) which are essential in the process of ATP production, and plays an important role in DNA repair and maintaining skin homeostasis. Some studies have shown that niacinamide has good effects in improving barrier function, resisting skin aging, anti-glycation, and reducing sebum production.

[0061] The following is a detailed description through specific examples. The raw materials and detection means involved in the present invention are common raw materials and detection means in the art unless otherwise specified.

[0062] In the present invention, groups of experiments are set up taking the facial mask liquid as an example, but it is not limited to the use of facial mask liquid. This composition can also be applied to various skin care products such as lotions, creams, essence, freeze-dried powder, skin care water, etc. The composition of the facial mask liquid of the present invention includes the above key combination, as well as thickeners, chelating agents, and pH regulators. Preferably, the raw materials for preparing the whitening facial mask liquid for evening out skin tone and brightening also include any one or at least two combinations of preservatives and fragrances. Specifically, the composition of the facial mask liquid is shown in Table 1 below:

[0063] Table 1 Composition of the facial mask liquid

[0064]

[0065]

[0066] The α - arbutin liposomes used in the following examples were prepared by the following method:

[0067] (1) Mix Tween 20 and Span 20 with a molar ratio of 1:1. The resulting non - ionic surfactant and cholesterol are fully dissolved in chloroform. The total mass of cholesterol and non - ionic surfactant is 400 mg (where the molar ratio of non - ionic surfactant to cholesterol is 2:1), and the volume of chloroform is 40 ml. After stirring until fully dissolved, transfer it to a rotary evaporator and remove the solvent chloroform under reduced pressure at 60 °C with a rotation speed of 150 rpm, so that the lipid components form a uniform lipid film on the inner wall of the container.

[0068] (2) Add 20 ml of PBS buffer solution with a pH of 6.5 to the container containing the lipid film, and place it on a magnetic stirrer. Stir at a rotation speed of 120 rpm to fully mix the lipid film and the PBS buffer solution to form a liposome suspension.

[0069] (3) Dissolve 400 mg of α - arbutin in 30 ml of PBS buffer solution and stir evenly.

[0070] (4) Slowly add the mixed solution obtained in step (3) to the liposome suspension obtained in step (2), and continue to stir and mix evenly.

[0071] (5) Place the liposome suspension containing α - arbutin obtained in step (4) in an ice - bath device, quickly cool it to near the freezing point (about 0 °C) and keep it for 30 min, then take it out and thaw it at room temperature for 45 min. Subsequently, perform ultrasonic treatment with an ultrasonic power of 200 W, a frequency of 40 kHz, and an ultrasonic time of 5 minutes. Finally, obtain α - arbutin liposomes by filtration. The particle size of the obtained α - arbutin liposomes is between 0.1 - 1 μm and is evenly distributed.

[0072] The following takes the facial mask liquid as an example for detailed description, that is, the skin - care products of each example, control example, and blank example are facial mask liquids, and the specific formulations are shown in the following table

[0073] Table 2 Raw material component formulations of Examples 1 - 5, Control Examples 1 - 7, and Blank Example 1 (weight percentage %)

[0074]

[0075]

[0076] In Table 2 above, the only difference between Control Example 7 and Example 3 is that the α - arbutin liposomes added in Example 3 are replaced with α - arbutin, and the preparation method is the same as that of Example 3.

[0077] (2) According to the dosage of each component in Examples 1-3, Comparative Examples 1-7 and Blank Example 1 in Table 2, the following method was used to prepare the facial mask liquid:

[0078] a. Aqueous phase: Place water in a container with a stirring device and stir. After fully wetting and mixing the other components of the excipients in Phase A, add them to the water and stir thoroughly until completely dissolved. Heat to 75-80 °C;

[0079] b. Oil phase: Mix the components of the excipients in Phase B, heat to 75-80 °C, and stir until completely dissolved;

[0080] c. Emulsification: Add the oil phase obtained in step b to the aqueous phase obtained in step a, stir at 250-400 rpm for 3-5 min, and then homogenize at 2000-4000 rpm for 3-5 minutes;

[0081] d. Add the excipients in Phase C, stir at 250-350 rpm for 3-5 min, then homogenize at 2000-4000 rpm for 3-5 minutes, and stir to cool down to 40-50 °C;

[0082] e. Add the excipients in Phase D, stir at 250-350 rpm for 3-5 min, then homogenize at 2000-4000 rpm for 3-5 minutes to obtain the required soothing facial mask liquid for sensitive skin after medical aesthetics treatment.

[0083] g. Immerse the facial mask matrix in the facial mask liquid to obtain a whitening facial mask with uniform skin color and brightening effect. Filter and sterilize before packaging, and detect the bacterial content and conduct quality control on toxins, immunogenicity, etc.

[0084] Efficacy evaluation test

[0085] I. Detection of skin gloss and transparency

[0086] Subjects: A total of 110 people, including 50 males and 60 females, aged 18 to 60 years old, meeting the volunteer selection criteria for subjects. They were divided into 11 groups, with 10 people in each group. Sign a written informed consent form. Before enrollment, a series of questions about medical history, health status, etc. were asked according to the inclusion and exclusion criteria. At the same time, a compliance assessment and skin color test screening were conducted on the skin of the test site and recorded;

[0087] Environmental conditions: During the test, the visual assessment and instrument test were carried out in an environment with a temperature of 21±1 °C and a relative humidity of 50±10% RH. The visual assessment was carried out under constant illumination (daylight lamp or LED light with a color temperature of 5500-6500 K). The subjects needed to adapt to this environment for at least 30 minutes before the assessment and test could be carried out.

[0088] Test products: Products obtained from Examples 1-3, Comparative Examples 1-7 and Blank Example 1

[0089] Experimental methods and results: A facial image analyzer VISIA-CR was used to detect the skin glossiness after 0 days, 7 days, 28 days, and 56 days of use; the transparency after 0 days, 7 days, and 28 days of use was measured to obtain the glossiness and transparency measurement values. The change rates of glossiness and transparency relative to 0 days were calculated respectively. Among them, the change rate = (average measurement value after using the product - average measurement value before using the product) ÷ average measurement value before using the product × 100%. The glossiness change rates are shown in Table 3, and the transparency change rates are shown in Table 4. An increase in the glossiness measurement value indicates an increase in skin glossiness, and an increase in the transparency measurement value indicates an increase in skin transparency.

[0090] Table 3 Skin glossiness change rates

[0091]

[0092]

[0093] As shown in Table 3 and Figure 1 It can be seen that after all the subjects used the products in Examples 1-3 and Comparative Examples 1-7, the skin glossiness of all subjects generally improved compared to before use. It is worth noting that for the subjects using Examples 1-3, the improvement ratio of their skin glossiness was significantly higher than that of other comparative examples, and as the use time extended, the improvement effect of glossiness became more significant. The total dosage of the active ingredients in Example 3 was equal to the total dosage of the active ingredients in Comparative Examples 1-7, but the effect of Example 3 was significantly better than the cases containing only one (Comparative Examples 4-6) or two active ingredient components (1-3). This result indicates that the synergistic effect of the three active ingredients, namely α-arbutin liposomes, grape seed extract, and niacinamide, in the present invention shows excellent effects in improving skin glossiness. Further analysis found that when the proportion of the three active ingredients in the cosmetics is higher, the whitening and brightening effect is more significant. In contrast, the effects of the comparative examples containing only one or two active ingredients (such as Comparative Examples 1-2) were significantly inferior to those of Examples 1-3, further proving the synergistic effect of the three active ingredients of the present invention.

[0094] It is particularly worth mentioning that although Comparative Example 7 used the same dosage of active ingredients as Example 3, but only replaced α-arbutin liposomes with commercially available α-arbutin, its effect was weakened at the same initial concentration as Example 3. This comparison not only highlights the advantages of the liposome encapsulation technology in improving the stability and skin permeability of α-arbutin, but also further confirms that through this technology, the active ingredients can be more effectively absorbed by the skin, thereby exerting a more significant whitening and brightening effect.

[0095] Figure 1Intuitively shows the changes in the skin glossiness of the subjects on the 0th, 14th, and 28th days after using the product of Example 3. Especially after 28 days of use, there is an obvious improvement in skin glossiness.

[0096] Table 4 Skin transparency change rate

[0097]

[0098]

[0099] As shown in Table 4 and Figure 2 It can be seen that after all the subjects used the test products of Examples 1-3 and Comparative Examples 1-7, the average value of their skin transparency generally increased compared with that before use. It is worth noting that for the subjects using the samples of Examples 1-3, the improvement ratio of their skin transparency is significantly higher than that of other comparative examples, and with the extension of the use time, the improvement effect becomes more significant. This result strongly proves that the three active ingredients of α-arbutin liposomes, grape seed extract and niacinamide in the present invention have a significant synergistic effect in promoting the improvement of skin transparency.

[0100] Further analysis found that when the proportion of these three active ingredients in the product increases, the improvement effect on skin transparency also increases. The total amount of the active ingredients in Example 3 is equal to the total amount of the active ingredients in Comparative Examples 1-7, but the effect of Example 3 is significantly better than the cases containing only one (Comparative Examples 4-6) or two active components (1-3), which further verifies the synergistic mechanism of the components of the present invention.

[0101] It is particularly noteworthy that although Comparative Example 7 used the same dose of active ingredients as Example 3, but only replaced α-arbutin liposomes with commercially available α-arbutin, the effect of improving skin transparency was weakened under the same initial concentration as Example 3. This contrast clearly reflects the unique value of the liposome encapsulation technology in enhancing the bioavailability of α-arbutin and promoting skin absorption, and also further confirms the key role of this technology in achieving the significant skin transparency improvement effect of the present invention.

[0102] Figure 2 Are the photos of skin transparency on the 0th, 14th, and 28th days of using the product obtained in Example 3; It can be seen from Figure 1 that the skin transparency is significantly improved after 28 days of use.

[0103] II. Detection of skin L* value and ITA* value

[0104] Subjects: A total of 110 people, including 50 males and 60 females, aged 18 to 60 years old, meeting the volunteer inclusion criteria for subjects. They were divided into 11 groups with 10 people in each group. A written informed consent form was signed. Before enrollment, a series of questions regarding medical history, health status, etc. were asked of the subjects according to the inclusion and exclusion criteria. At the same time, a compliance assessment and skin color test screening were conducted on the skin of the test site and recorded;

[0105] Environmental conditions: During the test process, the visual assessment and instrument testing were carried out in an environment with a temperature of 21 ± 1°C and a relative humidity of 50 ± 10% RH. The visual assessment was carried out under constant illumination (daylight fluorescent tubes or LED lights with a color temperature of 5500 - 6500K). The subjects needed to adapt to this environmental condition for at least 30 minutes before the assessment and testing could be carried out.

[0106] Experimental instrument: CHROMA METER CR - 400 skin detector

[0107] Experimental method: Use the skin color measuring instrument CHROMA METER CR - 400 to detect the skin color after 0 days, 7 days, 28 days, and 56 days of use, obtaining the L* value and ITA value °. Calculate the change rates of the L* value and ITA value ° at 7 days, 28 days, and 56 days relative to 0 days. Among them, the change rate = (average value measured after using the product - average value measured before using the product) ÷ average value measured before using the product × 100%. The change rate of the L* value is shown in Table 5, and the change rate of the ITA value ° is shown in Table 6. Among them, the L* value represents the brightness of the skin. The larger the value, the more the color tends to be white; the larger the ITA° value, the brighter the skin. On the contrary, the darker the skin.

[0108] The specific results are shown in the following table:

[0109] Table 5 Change rate of skin L* value

[0110]

[0111]

[0112] Table 6 Change rate of skin ITA° value

[0113]

[0114] As can be seen from Table 5-6 above: After the subjects used the test products in Examples 1-3 and Comparative Examples 1-7, both the change rate of the L* value and the change rate of the ITA value ° of the subjects increased. Among them, the change rate of the L* value and the change rate of the ITA value ° were more obvious when using the samples in Examples 1-3. Moreover, the higher the content of the active ingredients, the better the effect. When the sum of the dosages of the active ingredients in Example 3 was equal to the sum of the dosages of the active ingredients in Comparative Examples 1-7, the effect of Example 3 (containing three active ingredients simultaneously) was significantly better than the cases containing only one of them (Comparative Examples 4-6) or two active ingredients (1-3). Therefore, it is proved that the three active ingredients of the present invention have a synergistic effect.

[0115] In summary, it can be seen that compared with before use, after 7 days, 28 days, and 56 days of using the product of Example 1, the skin gloss and transparency increased significantly. The increase in skin color and gloss of using Example 2 was lower than that of Example 1, and the increase in skin color and gloss of using Example 3 was lower than that of Example 2, indicating that within this range, with the increase of the composition concentration, the whitening effect of the composition improved. It can be speculated that the whitening effect brought by the mask products of the examples is dependent on this composition. The active ingredients in Comparative Example 7 were not protected by liposome encapsulation. Under the condition that the initial concentration was the same as that of Example 3, the effect was weaker than that of Example 3. It can be speculated that the liposome encapsulation technology also helps the active ingredients to be absorbed by the skin and play the whitening and brightening effect. There were no active ingredients in Blank Example 1, and its effect was far inferior to other examples and comparative examples.

[0116] After using the mask liquids of Comparative Examples 1 to 7, the improvement degrees of skin color and gloss in each group were inferior to those of Examples 1 to 3. Example 1 contained α-arbutin liposome, grape seed extract, and niacinamide simultaneously, and had a better effect, while Comparative Examples 1 to 6 contained only two or one of the three ingredients. Therefore, it is proved that the composition containing α-arbutin liposome, grape seed extract, and niacinamide has a synergistic effect.

[0117] III. Subjective Evaluation Questionnaire

[0118] Subjects: 33 subjects were enrolled, and finally 33 subjects were counted, including 5 males and 28 females, aged 29 to 49 years, with an average age of 38.61 ± 0.89 years.

[0119] After the subjects used the product of Example 1 twice a week for 7 days, 28 days, and 56 days, they filled out a self-evaluation questionnaire. The evaluation is shown in Table 7.

[0120] Table 7 Evaluation of the subjects after using the product of Example 1 twice a week for 7 days, 14 days, and 28 days

[0121]

[0122]

[0123] As can be seen from the results in Table 7 above, the test product has the effects of moisturizing, brightening, and evening out skin tone. After using the product of Example 1 twice a week for 7 days, 28 days, and 56 days, 100.00% of the subjects felt that the product was mild and non-irritating, and thus it was considered that the product was mild (non-irritating).

[0124] The above-described embodiments only represent several implementation manners of the present invention, and the description thereof is relatively specific and detailed. However, it should not be construed as a limitation on the scope of the invention patent. It should be noted that for those of ordinary skill in the art, without departing from the concept of the present invention, several modifications and improvements can still be made, and these all belong to the protection scope of the present invention. Therefore, the protection scope of the present invention patent shall be subject to the appended claims.

Claims

1. A composition for brightening and whitening a uniform skin tone, characterized in that: The composition comprises alpha-arbutin liposome, grape seed extract and nicotinamide in a mass ratio of (0.1-2):(0.1-10):(0.1-5).

2. A composition for brightening and whitening skin with uniform skin tone according to claim 1, characterized in that: The mass ratio of the α-arbutin liposome, grape seed extract and nicotinamide is (0.1-1): (0.1-7): (0.1-2.5).

3. A composition for brightening and whitening skin tone according to claim 1 or 2, characterized in that: The α-arbutin liposome is prepared by the following method: (1) fully dissolving cholesterol and nonionic surfactant in chloroform, stirring until fully dissolved, and then transferring to a rotary evaporator, distilling under reduced pressure to remove the solvent chloroform, so that the lipid components form a uniform lipid film on the inner wall of the container; (2) adding PBS buffer to the container containing the lipid film and stirring to fully mix the lipid film and the PBS buffer to form a liposome suspension; (3) Stir and mix PBS buffer and α-arbutin; (4) slowly adding the mixed solution obtained in step (3) to the liposome suspension obtained in step (2), stirring and mixing uniformly; (5) placing the α-arbutin-containing liposome suspension obtained in step (4) in an ice bath, rapidly cooling to near freezing point and maintaining for 25 to 35 minutes, taking out, thawing at room temperature for 30 to 60 minutes, performing ultrasonic treatment, and filtering to obtain α-arbutin liposomes.

4. The method for preparing α-arbutin liposomes according to claim 3, characterized in that: The nonionic surfactant in step (1) is Tween 20 and Span 20 in a molar ratio of 1:1, the molar ratio of the nonionic surfactant to cholesterol is 2:1, and the volume ratio of the sum of the mass of cholesterol and the nonionic surfactant to chloroform is (40-500):(4-40) mg / ml; Further, the rotation speed of the rotary evaporator in step (1) is 150 rpm; In step (2), the pH of the PBS buffer is 6.5, and the mass volume ratio of the lipid film to the PBS buffer is (20-30): (1-2) mg / ml; Further, the rotation speed in step (2) is 120 rpm; In step (3), the mass volume ratio of α-arbutin to PBS buffer is (100-400): (20-50) mg / mL; In step (5), the ultrasonic power is 200 W, the frequency is 40 kHz, and the ultrasonic time is 5 minutes; The particle size of the obtained α-arbutin liposome is between 0.1 and 1 μm.

5. A skin care product containing the composition according to any one of claims 1 to 4, characterized in that: The composition is used in skin care products in an amount of 1-14 parts by weight.

6. The skin care product according to claim 5, characterized in that The skin care products include facial mask liquid, emulsion, facial cream, essence, freeze-dried powder or skin care water.

7. The skin care product according to claim 6, characterized in that The skin care product is a facial mask liquid, which also includes phase A auxiliary materials, phase B auxiliary materials, phase C auxiliary materials and phase D auxiliary materials; Taking the weight of the facial mask liquid as 100 parts, The phase A auxiliary material includes 0.1 to 25 parts of a thickener, 0.15 to 6 parts of a skin conditioner A, and 1 to 30 parts of a moisturizer A; The phase B auxiliary material includes 0.2-25 parts of skin conditioning agent B, 0.1-15 parts of emulsifier and 1-15 parts of excipient; The phase C auxiliary material includes 0.1 to 5 parts of a pH adjuster; The phase D auxiliary materials include 0.1 to 1 part of fragrance and 0.15 to 1 part of preservative.

8. The skin care product according to claim 7, characterized in that: The thickener includes one or more of acrylic acid (esters) / C10-30 alkyl acrylate cross-linked polymer, polyacrylamide, xanthan gum, propylene glycol, behenyl alcohol, carbomer, laureth-7, cetyl alcohol, stearyl alcohol and hydroxyethyl cellulose; The skin conditioning agent A and the skin conditioning agent B each independently include one or more of glycerin, isohexadecane, olive oil, sodium hyaluronate, lauryl alcohol, shea butter, allantoin, butylene glycol, squalane, panthenol, lactic acid, tocopherol and dipotassium glycyrrhizinate; The moisturizing agent A comprises one or more of hyaluronic acid, allantoin, glycerin, ceramide, sodium lactate, butylene glycol, ethylhexylglycerin, hydrogenated grape seed oil, olive oil and shea butter; The emulsifier includes one or more of glyceryl stearate citrate, cetearyl glucoside (and) cetearyl alcohol, behenyl trimethyl ammonium methyl sulfate, cocoglycerides and sorbitan olivate; The pH regulator includes one or more of arginine and lactic acid; The aromatic agent includes essence; The preservative includes one or more of phenoxyethanol, ethylhexylglycerin and pentylene glycol.

9. The method for preparing a skin care product according to claim 7, characterized in that: The steps include: a. Water phase: After fully moistening and mixing the components of phase A excipients, add them into water, stir thoroughly until completely dissolved, and heat; b. Oil phase; mix and heat the B phase excipients, stirring until completely dissolved; c. Emulsification: Add the mixture of step b to the aqueous phase of step a, stirring and homogenizing; d. Add phase C auxiliary materials, stir and homogenize, and cool to 40-50℃; e. Add phase D auxiliary materials, stir and homogenize; f. After stirring and cooling to 35-38°C, add the effective ingredient composition E, stir and homogenize to obtain the mask liquid.

10. The method for preparing a skin care product according to claim 9, characterized in that: The heating temperature in steps a to b is 75 to 80° C. The stirring speed in steps c to f is 200 to 400 rpm, and the stirring time is 3 to 5 minutes; The homogenization speed in steps c to f is 2000 to 4000 rpm, and the homogenization time is 3 to 5 minutes.

Citation Information

Patent Citations

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