Whitening and freckle-removing composition, preparation method thereof and application of whitening and freckle-removing composition in cosmetics

Abstract

The invention belongs to the technical field of cosmetics, and particularly relates to a whitening and freckle-removing composition, a preparation method thereof and application of the whitening and freckle-removing composition in cosmetics. The whitening and freckle-removing composition provided by the invention is prepared from flavonoid essence, fat-soluble active oil, an active small molecule compound, a polysaccharide compound, camelina seed oil, shea butter, caprylic / capric triglyceride, cetostearyl olive oil ester, vitamin E, an emulsifier, glycerol, panthenol, xanthan gum, a skin feeling regulator, a preservative and water. The whitening and freckle-removing composition provided by the invention realizes high balance of safety and efficacy, shows an obvious whitening effect, effectively controls the potential skin irritation risk, and provides a milder and more reliable choice for consumers who pursue efficacy and pay attention to safety, especially crowds with sensitive skin.

Description

TECHNICAL FIELD

[0001] The present application belongs to the technical field of cosmetics, and particularly relates to a whitening and freckle-removing composition, a preparation method thereof and application thereof in cosmetics. BACKGROUND

[0002] At present, whitening and freckle-removing has gradually changed from "optional consumption" to "urgent consumption". Behind this trend, multiple factors jointly drive it: on the one hand, factors such as ultraviolet radiation, genetic factors, irregular life, accelerated rhythm, skin aging, and post-inflammatory pigmentation cause the problem of pigment deposition to intensify; on the other hand, more than 60% of the 25-45-year-old female group have skin dullness or freckle problems, which has given rise to huge consumer demand. In addition, the consumer's cognition of whitening products has been upgraded from "surface covering" to "root repair". The consumer's demand for freckle-removing and whitening products is changing. In the past, emergency products that pursued "short-term covering" were popular; now, consumers are more eager to obtain long-term solutions that "repair the root", and expect to improve skin problems from the physiological mechanism level of melanin generation and metabolism.

[0003] The current market demand for whitening and freckle-removing is strong, but existing products still face the following problems: safety and efficacy are difficult to balance. Traditional chemical synthesis whitening ingredients such as hydroquinone and kojic acid can effectively inhibit tyrosinase activity to achieve rapid whitening, but have high safety risks. Hydroquinone has cytotoxicity, and clinical data shows that long-term use of a concentration of more than 4% can damage the skin barrier, cause exogenous ochronosis, and cause skin redness, desquamation and other irritant reactions, especially in sensitive skin groups. Kojic acid can easily cause skin allergies, and its concentration and range are strictly limited in many countries. In contrast, natural ingredient products are safer, but their whitening and freckle-removing efficacy is poor due to technical limitations. Therefore, current whitening and freckle-removing cosmetics are still difficult to achieve the balance of safety and significant whitening and freckle-removing efficacy. SUMMARY

[0004] The purpose of the present application is to provide a whitening and freckle-removing composition, a preparation method thereof and application thereof in cosmetics. The whitening and freckle-removing composition provided by the present application achieves a high balance between safety and efficacy, and exhibits significant whitening efficacy while effectively controlling the potential skin irritation risk, providing a more gentle and reliable choice for consumers who pursue efficacy and safety, especially for sensitive skin groups.

[0005] In order to achieve the above-mentioned purpose, the present application provides the following technical solutions: The present application provides a whitening and freckle-removing composition, comprising the following components in mass percentage: Flavonoids essence 3~5%, fat-soluble active oil 1.5~2.5%, active small molecule compound 2~3%, polysaccharide compound 3~5%, camelina sativa seed oil 7~9%, shea butter 1~2%, caprylic / capric triglyceride 3~4%, cetearyl olivate 0.8~1.2%, vitamin E 0.4~0.6%, emulsifier 3.5~4.5%, glycerin 4~5%, panthenol 1.5~2%, xanthan gum 0.05~0.1%, skin feel modifier 1.5~2.5%, preservative 0.8~1.2%, water balance; The polysaccharide compound and the active small molecule compound are obtained by water extraction and enzymolysis of a first plant material in sequence, and the first plant material comprises Auricularia auricula, Lentinula edodes, Bletilla striata, Polygonatum sibiricum and Astragalus membranaceus; The flavonoids essence is obtained by low eutectic solvent extraction and alcohol elution of a second plant material in sequence, and the second plant material comprises Morus alba and Pinus densata; The fat-soluble active oil is obtained by supercritical CO2 fluid extraction of a third plant material, and the third plant material comprises Phellinus baumii, Atractylodes macrocephala and Angelica dahurica.

[0006] Preferably, the preparation method of the polysaccharide compound and the active small molecule compound comprises the following steps: The first plant material and water are mixed for reflux extraction to obtain an extraction liquid; The pH value of the extraction liquid is adjusted to be acidic to obtain an acidic extraction liquid, and the acidic extraction liquid and a composite enzyme are mixed for enzymolysis to obtain an enzymolysis liquid, and the composite enzyme comprises cellulase and pectinase; The enzymolysis liquid is sequentially subjected to enzyme inactivation and solid-liquid separation to obtain an enzymolysis filtrate, the enzymolysis filtrate is subjected to first ultrafiltration membrane separation to obtain a first retentate and a first permeate, the first retentate is sequentially subjected to concentration and drying to obtain the polysaccharide compound, and the first permeate is subjected to second ultrafiltration membrane separation to obtain a second retentate, and the second retentate is dried to obtain the active small molecule compound.

[0007] Preferably, the mass ratio of Auricularia auricula, Lentinula edodes, Bletilla striata, Polygonatum sibiricum and Astragalus membranaceus is (2~3):(1~2):(2~3):(2~3):(2~3); the solid-liquid ratio of the first plant material and water is 1:5~15; the temperature of the reflux extraction is 90~95℃, and the time is 1~3h; the mass percentage of the composite enzyme in the first plant material is 0.3~0.5%, and the mass ratio of cellulase and pectinase is 1~2:1~2; the temperature of the enzymolysis is 45~50℃, and the time is 2~3h; the molecular weight cut-off of the first ultrafiltration membrane separation is 100~120kDa, and the molecular weight cut-off of the second ultrafiltration membrane separation is 1~1.5kDa.

[0008] Preferably, the method for preparing the flavonoid extract includes the following steps: The second plant material was mixed with a eutectic solvent, which included choline chloride and lactic acid, and then subjected to ultrasonic extraction to obtain an extract. The extract was subjected to resin column separation to obtain an eluent, wherein the eluent used in the resin column separation included ethanol and water. The eluent was concentrated and dried sequentially to obtain the flavonoid extract.

[0009] Preferably, the mass ratio of mulberry bark to red pine mushroom is 1~2:1~2; the molar ratio of choline chloride to lactic acid is 1:2~4; the solid-liquid ratio of the second plant material to the eutectic solvent is 1:20~30; the ultrasonic extraction temperature is 45~55℃, the power is 350~450W, and the time is 20~40min; the resin column separation is performed using an AB-8 macroporous resin column, and the volume percentage of ethanol in the eluent is 70~75%.

[0010] Preferably, the method for preparing the fat-soluble active oil includes the following steps: The third plant material was subjected to supercritical CO2 fluid extraction to obtain the extract; The extract was post-processed to obtain the fat-soluble active oil.

[0011] Preferably, the mass ratio of Phellinus linteus, Atractylodes macrocephala, and Angelica dahurica is (2~3):(1~2):(1~2); the conditions for supercritical CO2 fluid extraction include: extraction pressure of 25~30 MPa, extraction temperature of 40~45℃, and cyclic extraction time of 2~3 h; the supercritical CO2 fluid extraction also uses an entrainer, which is ethanol; the post-treatment includes vacuum distillation at a temperature of 40~45℃.

[0012] Preferably, the emulsifier is Olivem 1000; the skin feel modifier is cyclopentamethoxysiloxane; and the preservative is pentylene glycol.

[0013] This invention provides a method for preparing the whitening and freckle-removing composition described in the above technical solution, comprising the following steps: Shea butter, cetearyl alcohol olive oil ester, linseed oil, caprylic / capric triglyceride, fat-soluble active oil, vitamin E and emulsifier are mixed to obtain the oil phase; Glycerol, panthenol, water, xanthan gum, active small molecule complex and polysaccharide complex were mixed to obtain an aqueous phase; The oil phase and the aqueous phase are homogenized to obtain an emulsion; The emulsion, flavonoid extract, skin feel modifier, and preservative are mixed to obtain the whitening and spot-removing composition.

[0014] This invention provides the application of the whitening and freckle-removing composition described in the above technical solution or the whitening and freckle-removing composition prepared by the preparation method described in the above technical solution in cosmetics.

[0015] This invention provides a whitening and freckle-removing composition comprising the following components in weight percentages: 3-5% flavonoid extract, 1.5-2.5% fat-soluble active oil, 2-3% active small molecule complex, 3-5% polysaccharide complex, 7-9% flaxseed oil, 1-2% shea butter, 3-4% caprylic / capric triglyceride, 0.8-1.2% cetearyl alcohol olive oil ester, 0.4-0.6% vitamin E, 3.5-4.5% emulsifier, 4-5% glycerin, 1.5-2% panthenol, 0.05-0.1% xanthan gum, and a skin-feeling... The composition comprises: regulator 1.5-2.5%, preservative 0.8-1.2%, and water as the balance. The polysaccharide complex and the active small molecule complex are obtained from a first plant material through sequential water extraction and enzymatic hydrolysis. The first plant material includes *Auricularia auricula-judae*, *Lentinula edodes*, *Bletilla striata*, *Polygonatum sibiricum*, and *Astragalus membranaceus*. The flavonoid extract is obtained from a second plant material through sequential eutectic solvent extraction and alcohol elution. The second plant material includes *Morus alba* bark and *Pinus massoniana*. The fat-soluble active oil is obtained from a third plant material through supercritical CO2 fluid extraction. The third plant material includes *Phellinus linteus*, *Atractylodes macrocephala*, and *Angelica dahurica*. The active phases in the whitening and freckle-removing composition provided by this invention include flavonoid extracts, fat-soluble active oils, active small molecule complexes, and polysaccharide complexes. The active phases in this invention employ a "barrier repair and targeted inhibition synergistic" method. The active small molecule complex and polysaccharide complex in the formula preferentially repair the skin's physical barrier, creating a healthier and more tolerable skin environment for the subsequent action of the flavonoid extract and fat-soluble active oil. This invention, through the design of its active phase, enables the product to demonstrate significant whitening efficacy in in vitro tests while effectively controlling potential skin irritation risks, providing a gentler and more reliable option for consumers seeking efficacy while prioritizing safety, especially those with sensitive skin. Simultaneously, the active phase in this invention constructs a network of action covering the entire pathway of melanin production, transport, and metabolism through multi-dimensional synergistic interventions, including barrier repair, tyrosinase inhibition, anti-inflammatory soothing, and keratinocyte metabolism promotion. In vitro cell experiments show that the whitening and spot-removing composition provided by this invention exhibits synergistic enhancement effects in multiple key pathways, with a comprehensive inhibitory effect superior to that of a single ingredient, thus providing a mechanistic basis for achieving more stable and lasting skin tone improvement. The clustered green extraction method used in this invention for the active phase can specifically enrich high-purity target active ingredients (such as ergothioneine and triterpenoids), minimizing ineffective impurities and degradation of heat-sensitive components. Furthermore, flaxseed oil in the formulation of this invention acts as a natural penetration enhancer, improving the transdermal delivery efficiency of lipid-soluble active ingredients. Finally, the formula of this invention, through the scientific combination of small molecule complexes and polysaccharide complexes (i.e. edible fungi polysaccharides) with flavonoid extracts and fat-soluble active oils, successfully endows the product with a delicate, silky, and non-sticky excellent skin feel while ensuring sufficient addition of effective ingredients.The cream is easy to spread and feels refreshing on the skin after absorption, significantly improving the heavy and greasy feeling often found in traditional functional skincare products. This helps to improve user compliance and ensures cumulative effects with long-term use. Detailed Implementation

[0016] This invention provides a whitening and freckle-removing composition, comprising the following components in weight percentages: Flavonoid extract 3-5%, fat-soluble active oil 1.5-2.5%, active small molecule complex 2-3%, polysaccharide complex 3-5%, flaxseed oil 7-9%, shea butter 1-2%, caprylic / capric triglyceride 3-4%, cetearyl alcohol olive oil 0.8-1.2%, vitamin E 0.4-0.6%, emulsifier 3.5-4.5%, glycerin 4-5%, panthenol 1.5-2%, xanthan gum 0.05-0.1%, skin feel modifier 1.5-2.5%, preservative 0.8-1.2%, water balance; The polysaccharide complex and the active small molecule complex are obtained by sequentially extracting and enzymatically hydrolyzing a first plant material, which includes Auricularia auricula-judae, Lentinus edodes, Bletilla striata, Polygonatum sibiricum, and Astragalus membranaceus. The flavonoid extract was obtained by sequentially extracting and eluting the second plant material with a eutectic solvent and an alcohol elution. The second plant material included mulberry bark and red pine mushroom. The fat-soluble active oil is obtained by supercritical CO2 fluid extraction from a third plant material, which includes Phellinus linteus, Atractylodes macrocephala, and Angelica dahurica.

[0017] In this invention, unless otherwise specified, all raw materials / components used in the preparation are commercially available products well known to those skilled in the art.

[0018] The whitening and freckle-removing composition provided by this invention comprises 3-5% flavonoid extract by weight percentage, and in the examples, it can be 3%, 4%, or 5%. In this invention, the flavonoid extract is obtained by sequentially extracting a second plant material using a eutectic solvent and eluting it with alcohol. The second plant material includes mulberry bark and red pine mushroom. The flavonoid extract contains alcohol-soluble active ingredients. Preferably, the flavonoid extract includes flavonoids and mulberry root ketone C. The flavonoid extract is a brownish-yellow refined powder. The function of the flavonoid extract is as a tyrosinase inhibitor.

[0019] In this invention, the method for preparing the flavonoid extract includes the following preferred steps: The second plant material was mixed with a eutectic solvent, which included choline chloride and lactic acid, and then subjected to ultrasonic extraction to obtain an extract. The extract was subjected to resin column separation to obtain an eluent, wherein the eluent used in the resin column separation included ethanol and water. The eluent was concentrated and dried sequentially to obtain the flavonoid extract.

[0020] This invention involves ultrasonic extraction of a second plant material and a eutectic solvent (DES), wherein the eutectic solvent comprises choline chloride and lactic acid, to obtain an extract. In this invention, the preferred mass ratio of mulberry bark to red pine mushroom is 1-2:1-2, and in the examples, it can be 1:1. The preferred molar ratio of choline chloride to lactic acid is 1:2-4, and in the examples, it can be 1:2. The preferred solid-liquid ratio of the second plant material to the eutectic solvent is 1:20-30, more preferably 1:25. The solid-liquid ratio of the second plant material to the eutectic solvent is the ratio of the mass (g) of the second plant material to the volume (mL) of the eutectic solvent. The preferred method for preparing the DES includes: heating and stirring choline chloride and lactic acid until a clear liquid is obtained; the preferred heating and stirring temperature is 50-60°C. The ultrasonic extraction is preferably performed in an ultrasonic extractor. The preferred ultrasonic extraction temperature is 45-55°C, and in the examples, it can be 50°C. The preferred ultrasonic extraction power is 350-450W, and in the examples, it can be 400W. The preferred time for ultrasonic extraction is 20-40 minutes, and in the example, it can be 30 minutes.

[0021] After obtaining the extract, the present invention performs resin column separation to obtain an eluent. The eluent used in the resin column separation includes ethanol and water. In the present invention, before performing the resin column separation, it is preferable to dilute the extract with water, and then perform the resin column separation on the diluted extract. The resin column separation is performed using an AB-8 macroporous resin column. The resin column separation preferably includes sequential pre-elution and elution. The eluent used in the pre-elution is preferably water, and the present invention removes impurities through pre-elution. The eluent used in the elution is preferably ethanol and water. The volume percentage of ethanol in the eluent used in the elution is preferably 70-75%. The eluent is collected after elution.

[0022] After obtaining the eluent, the present invention sequentially concentrates and dries the eluent to obtain the flavonoid extract. The concentration is preferably vacuum concentration. The drying is preferably freeze-drying.

[0023] The whitening and freckle-removing composition provided by this invention comprises 1.5-2.5% fat-soluble active oil, which can be 1.5%, 2%, or 2.5% in the embodiments. In this invention, the fat-soluble active oil is obtained by supercritical CO2 fluid extraction from a third plant material, including *Sanghuang* (Phellinus linteus), *Atractylodes macrocephala* (Bai Zhu), and *Angelica dahurica* (Bai Zhi). The fat-soluble active oil preferably contains volatile oil, triterpenes, and coumarins. *Sanghuang* is extracted with supercritical CO2 fluid to obtain triterpenes, *Atractylodes macrocephala* is extracted with supercritical CO2 fluid to obtain volatile oil, and *Angelica dahurica* is extracted with supercritical CO2 fluid to obtain coumarins. The fat-soluble active oil is a brownish-red transparent oily extract.

[0024] In this invention, the method for preparing the fat-soluble active oil preferably includes the following steps: The third plant material was subjected to supercritical CO2 fluid extraction to obtain the extract; The extract was post-processed to obtain the fat-soluble active oil.

[0025] This invention involves supercritical CO2 fluid extraction of the third plant material to obtain an extract. In this invention, the preferred mass ratio of *Sanghuang*, *Baizhu*, and *Baizhi* is (2-3):(1-2):(1-2), and in the embodiment, it can be 2:1:1. The supercritical CO2 fluid extraction is preferably carried out in a supercritical extraction vessel. The reagent used in the supercritical CO2 fluid extraction is CO2. The supercritical CO2 fluid extraction also preferably uses an entrainer, which is preferably ethanol, and in the embodiment, anhydrous ethanol. The mass percentage of the entrainer relative to the mass of the third plant material is preferably 0.1-0.5%. In this invention, the preferred conditions for supercritical CO2 fluid extraction include: an extraction pressure of 25-30 MPa, and in the embodiment, 28 MPa; an extraction temperature of 40-45°C; and a circulation extraction time of 2-3 h, and in the embodiment, 2.5 h. The extract is preferably collected in a separation vessel.

[0026] After obtaining the extract, the present invention performs post-processing on the extract to obtain the fat-soluble active oil. In the present invention, the post-processing preferably includes vacuum distillation, and the temperature of the vacuum distillation is preferably 40~45°C. The present invention preferably removes residual entrainers from the extract through the post-processing.

[0027] The whitening and freckle-removing composition provided by the present invention comprises 2-3% active small molecule complex, which can be 2%, 2.5% or 3% in the examples.

[0028] The whitening and freckle-removing composition provided by the present invention comprises 3-5% polysaccharide complex, which can be 3%, 4% or 5% in the examples.

[0029] In this invention, the polysaccharide complex and the active small molecule complex are obtained from a first plant material through sequential water extraction and enzymatic hydrolysis. The first plant material includes *Auricularia auricula-judae*, *Lentinula edodes*, *Bletilla striata*, *Polygonatum sibiricum*, and *Astragalus membranaceus*. The polysaccharide complex and the active small molecule complex are clusters of water-soluble components. Preferably, the polysaccharide complex and the active small molecule complex include polysaccharides, ergothioneine, and saponins. *Auricularia auricula-judae* is sequentially extracted with water and enzymatically hydrolyzed to obtain ergothioneine and polysaccharides. *Lentinula edodes* is sequentially extracted with water and enzymatically hydrolyzed to obtain polysaccharides. *Bletilla striata* is sequentially extracted with water and enzymatically hydrolyzed to obtain glucomannan. *Polygonatum sibiricum* is sequentially extracted with water and enzymatically hydrolyzed to obtain polysaccharides. *Astragalus membranaceus* is sequentially extracted with water and enzymatically hydrolyzed to obtain polysaccharides and saponins.

[0030] In this invention, the preparation method of the polysaccharide complex and the active small molecule complex includes the following steps: The first plant material was mixed with water and refluxed to extract the extract. The pH of the extract is adjusted to acidic to obtain an acidic extract. The acidic extract is then mixed with a compound enzyme for enzymatic hydrolysis to obtain an enzymatic hydrolysate. The compound enzyme includes cellulase and pectinase. The enzymatic hydrolysate is subjected to enzyme inactivation and solid-liquid separation in sequence to obtain an enzymatic hydrolysate. The enzymatic hydrolysate is then subjected to a first ultrafiltration membrane to obtain a first retentate and a first permeate. The first retentate is then concentrated and dried in sequence to obtain the polysaccharide complex. The first permeate is then subjected to a second ultrafiltration membrane to obtain a second retentate. The second retentate is then dried to obtain the active small molecule complex.

[0031] This invention involves mixing a first plant material with water and then refluxing to extract the extract. In this invention, the preferred mass ratio of the following ingredients is (2-3):(1-2):(2-3):(2-3):(2-3), and in some examples, it can be 2:1:2:2:2. The water can be purified water. The preferred solid-liquid ratio of the first plant material to water is 1:5-15, and in some examples, it can be 1:10. The solid-liquid ratio is the ratio of the mass (g) of the first plant material to the volume (mL) of the water. Before mixing, the first plant material is preferably sieved, and the undersize material is then mixed. The sieve used for sieving is preferably 40 mesh. The reflux extraction is carried out in an extraction tank. The preferred temperature for the reflux extraction is 90-95℃, and the preferred time is 1-3 hours, and in some examples, it can be 2 hours.

[0032] After obtaining the extract, the present invention adjusts the pH of the extract to acidic to obtain an acidic extract. The acidic extract is then mixed with a complex enzyme for enzymatic hydrolysis to obtain an enzymatic hydrolysate. The complex enzyme includes cellulase and pectinase. Preferably, the extract is cooled to 45-50°C before adjusting the pH. In this invention, the pH of the acidic extract is preferably 5-5.5. The mass percentage of the complex enzyme in the extract is preferably 0.3-0.5%. The mass ratio of cellulase to pectinase is preferably 1-2:1-2, and in the examples, it can be 1:1. The enzymatic hydrolysis is performed at an isothermal temperature. The preferred temperature for the enzymatic hydrolysis is 45-50°C. The preferred time for the enzymatic hydrolysis is 2-3 hours.

[0033] After obtaining the enzymatic hydrolysate, the present invention sequentially performs enzyme inactivation and solid-liquid separation to obtain an enzymatic hydrolysate filtrate. The enzymatic hydrolysate filtrate is then subjected to a first ultrafiltration membrane separation to obtain a first retentate and a first permeate. The first retentate is sequentially concentrated and dried to obtain the polysaccharide complex. The first permeate is then subjected to a second ultrafiltration membrane separation to obtain a second retentate, which is then dried to obtain the active small molecule complex. In this invention, enzyme inactivation preferably includes heating the enzymatic hydrolysate to 85-90°C and holding it for 10-15 minutes to inactivate the enzyme. Solid-liquid separation is preferably performed using a filter cloth, preferably a 200-mesh filter cloth. The molecular weight cutoff of the first ultrafiltration membrane separation is preferably 100-120 kDa, and in the examples, it can be 100 kDa. The first ultrafiltration membrane separation preferably retains large-molecule polysaccharides from Bletilla striata and Polygonatum sibiricum. The drying method after concentration of the first retentate is preferably spray drying. The molecular weight cutoff of the second ultrafiltration membrane separation is preferably 1-1.5 kDa, and in the examples, it can be 1 kDa. The second ultrafiltration membrane separation preferably retains ergothioneine and astragaloside from *Auricularia auricula-judae*. The second retentate is preferably dried by freeze-drying.

[0034] The whitening and freckle-removing composition provided by the present invention comprises 7-9% flaxseed oil, preferably 8%, by weight percentage.

[0035] The whitening and freckle-removing composition provided by the present invention comprises 1-2% shea butter, preferably 1.5%, by weight percentage.

[0036] The whitening and freckle-removing composition provided by the present invention comprises 3-4% caprylic / capric triglyceride, preferably 3.5%, by weight percentage.

[0037] The whitening and freckle-removing composition provided by the present invention comprises 0.8-1.2% cetearyl alcohol olive oil ester, preferably 1%, by weight percentage.

[0038] The whitening and freckle-removing composition provided by the present invention comprises 0.4-0.6% vitamin E, preferably 0.5%, by weight percentage.

[0039] The whitening and freckle-removing composition provided by the present invention comprises 3.5-4.5% emulsifier, preferably 4%, by weight percentage. In the present invention, the emulsifier is preferably Olivem 1000.

[0040] The whitening and freckle-removing composition provided by the present invention comprises 4-5% glycerin, preferably 3.5%, by weight percentage.

[0041] The whitening and freckle-removing composition provided by the present invention comprises 1.5-2% panthenol, preferably 3.5%, by weight percentage.

[0042] The whitening and freckle-removing composition provided by the present invention comprises 0.05-0.1% xanthan gum, preferably 0.1%, by weight percentage.

[0043] The whitening and freckle-removing composition provided by the present invention comprises 1.5-2.5% skin feel modifier, preferably 2%, by weight percentage. In the present invention, the skin feel modifier is preferably cyclopentamethoxysiloxane.

[0044] The whitening and freckle-removing composition provided by the present invention comprises 0.8-1.2% preservative, preferably 1%, by weight percentage. In the present invention, the preservative is preferably pentylene glycol.

[0045] The whitening and freckle-removing composition provided by this invention comprises water as the remainder, by weight percentage. In this invention, the water may be deionized water.

[0046] This invention provides a method for preparing the whitening and freckle-removing composition described in the above technical solution, comprising the following steps: Shea butter, cetearyl alcohol olive oil ester, linseed oil, caprylic / capric triglyceride, fat-soluble active oil, vitamin E and emulsifier are mixed to obtain the oil phase; Glycerol, panthenol, water, xanthan gum, active small molecule complex and polysaccharide complex were mixed to obtain an aqueous phase; The oil phase and the aqueous phase are homogenized to obtain an emulsion; The emulsion, flavonoid extract, skin feel modifier, and preservative are mixed to obtain the whitening and spot-removing composition.

[0047] This invention involves mixing shea butter, cetearyl alcohol olive oil ester, linseed oil, caprylic / capric triglyceride, a fat-soluble active oil, vitamin E, and an emulsifier (hereinafter referred to as the first mixture) to obtain an oil phase. In this invention, the first mixture preferably comprises: heating and melting shea butter and cetearyl alcohol olive oil ester to obtain a molten material; mixing the molten material, linseed oil, caprylic / capric triglyceride, fat-soluble active oil, and vitamin E, and then stirring and mixing with the emulsifier to obtain a clarified product. The preferred heating and melting temperature is 75-78°C.

[0048] This invention involves mixing glycerol, panthenol, water, xanthan gum, an active small molecule complex, and a polysaccharide complex (hereinafter referred to as the second mixture) to obtain an aqueous phase. In this invention, the second mixture preferably comprises: heating and mixing a portion of glycerol, panthenol, and water to obtain an aqueous solution; premixing xanthan gum and the remaining glycerol to obtain a slurry; stirring and mixing the slurry and the aqueous solution, and then adding the active small molecule complex and the polysaccharide complex and continuing stirring and mixing.

[0049] After obtaining the oil phase and the aqueous phase, the present invention homogenizes the oil phase and the aqueous phase to obtain an emulsion. In the present invention, the temperature of the oil phase during homogenization is preferably 75-78°C, and the temperature of the aqueous phase is preferably 78-80°C. The rotation speed of the homogenization process is preferably 8000-10000 rpm. The homogenization time is preferably 5-8 minutes. The temperature of the emulsion is preferably 75-80°C.

[0050] After obtaining the emulsion, the present invention mixes the emulsion, flavonoid extract, skin feel modifier, and preservative (hereinafter referred to as the third mixture) to obtain the whitening and spot-removing composition. In the present invention, the third mixture preferably includes: cooling the emulsion to 45~47°C, adding the flavonoid extract for dispersion, then cooling to 40~42°C, adding the skin feel modifier for stirring and mixing, and then cooling to 35~38°C, adding the preservative for stirring and mixing.

[0051] In this invention, the initial product is obtained directly after the third mixing. Preferably, a pH adjuster is used to adjust the pH value of the initial product to 5.5-5.8, followed by vacuum degassing and filling. The vacuum degassing conditions preferably include: a vacuum degree of -0.05 MPa and a time of 10-15 min.

[0052] This invention provides the application of the whitening and freckle-removing composition described in the above technical solution or the whitening and freckle-removing composition prepared by the preparation method described in the above technical solution in cosmetics.

[0053] In this invention, the cosmetic product is preferably a cream or lotion, specifically a face cream.

[0054] To further illustrate the present invention, the technical solutions provided by the present invention will be described in detail below with reference to the embodiments, but they should not be construed as limiting the scope of protection of the present invention.

[0055] Example 1: Preparation of Clustered Extracts 1.1 Water-soluble component cluster extract (polysaccharide complex and the aforementioned active small molecule complex, denoted as extract A) Formula: Mix golden ear fungus, shiitake mushroom, Bletilla striata, Polygonatum sibiricum and Astragalus membranaceus in a mass ratio of 2:1:2:2:2, with a total feed of 500g.

[0056] Process: Hot water extraction: The mixed raw materials are crushed and passed through a 40-mesh sieve, 10 times the amount (5L) of purified water is added, and the mixture is refluxed at 90℃ for 2 hours to obtain the extract.

[0057] Enzymatic hydrolysis: Cool the extract to 50℃, adjust the pH to 5.5, add 0.5% of the extract mass of a compound enzyme (cellulase: pectinase mass ratio of 1:1), and hydrolyze at 50℃ for 2 hours.

[0058] Enzyme inactivation and coarse filtration: Inactivate enzymes at 90℃ for 10 min, filter through a 200-mesh filter cloth to obtain the filtrate.

[0059] Membrane separation and enrichment: The filtrate is passed through a 100 kDa ultrafiltration membrane, and the retentate is spray-dried to obtain a polysaccharide complex (denoted as extract A1). The permeate is then passed through a 1 kDa nanofiltration membrane, and the retentate is freeze-dried to obtain an active small molecule complex (denoted as extract A2, rich in ergothioneine and saponins).

[0060] 1.2 Extract of alcohol-soluble components (flavonoid essence, denoted as extract B) Formula: Mulberry bark and red pine mushroom are mixed in a 1:1 ratio by weight, with a total feed of 200g.

[0061] Process: DES preparation: Choline chloride and lactic acid are mixed in a 1:2 molar ratio and stirred at 60°C to form a clear liquid, thus obtaining DES.

[0062] Ultrasonic extraction: The raw material and DES were mixed at a ratio of 1g:25mL and ultrasonically extracted at 50℃ and 400W for 30min to obtain the extract.

[0063] Purification: The extract was adsorbed onto an AB-8 macroporous resin column, washed with water, and then eluted with an ethanol-water solution with a 70% v:v content to obtain the eluent.

[0064] Drying: The eluent was successively concentrated under reduced pressure and freeze-dried to obtain flavonoid extract (B, rich in flavonoids and morinone C).

[0065] 1.3 Extract of fat-soluble components (fat-soluble active oil, denoted as extract C) Formula: Mix Phellinus linteus, Atractylodes macrocephala, and Angelica dahurica in a mass ratio of 2:1:1, with a total feed amount of 200g.

[0066] Process: Supercritical CO2 extraction: The raw materials are put into the extraction vessel, the pressure is set to 28MPa, the temperature is 45℃, and anhydrous ethanol, accounting for 5% of the total mass of Sanghuang, Baizhu and Baizhi, is used as the entrainer for extraction for 2.5h.

[0067] Collection: The extract is collected in the separation vessel.

[0068] Post-processing: Residual ethanol was removed by rotary evaporation under reduced pressure at 40℃ to obtain a fat-soluble active oil (C, rich in volatile oils, triterpenes, and coumarins). Shea butter. Example 2: Preparation of a whitening and spot-removing complex face cream (100 kg batch) This embodiment provides a whitening and spot-removing composite face cream, the formula of which is shown in Table 1 below: Table 1. Formula of the whitening and spot-removing complex face cream provided in Example 2

[0069] Preparation process: Oil phase preparation: Shea butter and cetearyl alcohol olive oil were heated to 75-78°C and melted. Flaxseed oil, caprylic / capric triglycerides, fat-soluble active oil (i.e., extract C prepared in Example 1), and vitamin E were added and mixed well. Finally, emulsifier was added and stirred until clear to obtain the oil phase, which was then kept warm.

[0070] Aqueous phase preparation: Glycerin (total glycerin minus the glycerin used for premixing with xanthan gum) and panthenol were added to deionized water to obtain an aqueous solution, which was then heated to 78-80°C and stirred to dissolve. Xanthan gum and a portion of glycerin (xanthan gum:glycerin = 1:10) were premixed into a slurry and added to the aqueous solution, and stirred until transparent. The active small molecule complex (extract A2) and polysaccharide complex (extract A1) were added, stirred to dissolve, and the aqueous phase was kept at this temperature.

[0071] Primary emulsification: At a homogenization speed of 8000 rpm, the oil phase is slowly added to the aqueous phase and homogenized for 7 minutes to form a uniform paste.

[0072] Cooling and Adding: Cool to 47°C, add flavonoid extract (extract B prepared in Example 1), and disperse for 2 minutes with the aid of a hand-held homogenizer.

[0073] Cool to 40°C, add D5, and mix slowly until homogeneous.

[0074] Cool to 38°C, add pentylene glycol, and stir slowly until well mixed.

[0075] Quality control and filling: Adjust the pH of the system to 5.6 with 10% citric acid solution. After vacuum degassing (-0.05MPa, 10min), discharge and fill to obtain the whitening and freckle-removing compound face cream.

[0076] Example 3: Preparation of a whitening and spot-removing complex face cream (formula optimization) The difference between this embodiment and Embodiment 2 is that the ratio of the core active ingredient has been optimized to achieve the best synergistic effect. The specific formulation is as follows: Extract B (flavonoid extract): 5.0 kg; Extract C (lipid-soluble active oil): 1.5 kg; Extract A2 (active small molecule complex): 3.0 kg; Extract A1 (polysaccharide complex): 3.0 kg; The remaining components and preparation process are the same as in Example 2.

[0077] Example 4: Preparation of a whitening and spot-removing complex face cream (formula optimization) This embodiment provides another face cream with optimized proportions, the specific formula of which is as follows: Extract B (flavonoid extract): 3.0 kg; Extract C (lipid-soluble active oil): 2.5 kg; Extract A2 (active small molecule complex): 2.0 kg; Extract A1 (polysaccharide complex): 5.0 kg; The remaining components and preparation process are the same as in Example 2.

[0078] Example 5: Evaluation of the skin-whitening and freckle-removing effects Experimental Example 1: Cellular-level safety evaluation (prediction of skin irritation) 1. Sample preparation: The face cream samples (S2, S3, S4) prepared in Examples 2, 3, and 4 were diluted with DMEM medium to prepare test solutions of different concentrations.

[0079] 2. Experimental Methods: Human immortalized keratinocytes (HaCaT) were used, at a concentration of 1×10⁻⁶. 5 Cells were seeded at a density of [number] cells / mL in 96-well plates and cultured for 24 hours. The medium was then replaced with different concentrations of the test sample, and cultured for another 48 hours. Cell viability was determined using the MTT assay. (A cell viability >70% was considered a safe concentration).

[0080] 3. Results and conclusions: The experimental results are shown in Table 2.

[0081] Table 2. Safety evaluation results at the cellular level

[0082] Conclusion: Even at a high concentration of 10%, the HaCaT cell survival rate remained above 70% in all tested samples, indicating excellent safety at usage concentrations of 2%–5%. This demonstrates that the cream of this invention has no potential irritation at the cellular level and exhibits good safety.

[0083] Experimental Example 2: Evaluation of In Vitro Whitening Efficacy 1. Sample preparation: Dilute face cream samples S2, S3, and S4 to a test concentration of 2% using DMEM medium. Set up a blank control group, an α-MSH model control group, and a positive control group (1% arbutin).

[0084] 2. Results of the intracellular tyrosinase activity inhibition test are shown in Table 3.

[0085] Table 3 Results of intracellular tyrosinase activity inhibition test

[0086] Conclusion: The sample of this invention has a better inhibitory effect on tyrosinase than the classic ingredient arbutin.

[0087] 3. Results of intracellular melanin content measurement are shown in Table 4.

[0088] Table 4 Results of intracellular melanin content measurement

[0089] Conclusion: The melanin inhibition rate and tyrosinase inhibition rate showed the same trend, but the values ​​were slightly lower. However, both were superior to the classic ingredient arbutin.

[0090] 4. The results of the free radical scavenging experiment (DPPH method) are shown in Table 5.

[0091] Table 5 Results of free radical scavenging experiments

[0092] As can be seen from the above embodiments, based on a deep understanding of skin physiology, the beneficial effects of the present invention compared to the prior art are mainly reflected in the following three aspects: (1) In terms of product concept, it realizes the transformation from "single intervention" to "system conditioning": existing products mostly focus on strong inhibition of melanin pathway. This invention pays more attention to overall skin health. Through a systematic strategy of first strengthening the skin barrier function and then synergistically inhibiting melanin production, it aims to achieve a more lasting and stable whitening and spot removal effect, while improving skin tolerance.

[0093] (2) In terms of raw material processing, a new "clustered" green extraction method has been established: breaking through the traditional isolated extraction mode of single raw materials, multiple natural raw materials are scientifically classified and extracted in combination according to the chemical properties of the components (such as water solubility and fat solubility). This method significantly improves the extraction efficiency and purity of the target active ingredients, and the process is more environmentally friendly and energy-saving, providing a new path for obtaining high-quality raw materials.

[0094] (3) In terms of formulation system, a synergistic mechanism of "multi-target and time-sequential" has been constructed: In the formulation design, not only are the complementary effects of different active ingredients (such as inhibition, anti-inflammation and repair) considered, but also through a fine preparation process (such as staged and temperature-controlled addition) to ensure that various ingredients can play their roles in an orderly and stable manner, thereby achieving the synergistic effect of "1+1>2" and ultimately giving the product an excellent skin feel.

[0095] This invention achieves a high balance between safety and efficacy: Employing a "synergistic design of barrier repair and targeted inhibition," the formula prioritizes the repair of the skin's physical barrier through ingredients such as Bletilla striata polysaccharide and Auricularia auricula-judae gelatin, creating a healthier and more tolerable skin environment for the subsequent action of active ingredients like Morus alba root bark extract (Morus alba root ketone C) and Morus alba triterpenes. This scientific design of timing and target allows the product to demonstrate significant whitening effects in in vitro tests while effectively controlling potential skin irritation risks, providing a gentler and more reliable option for consumers seeking efficacy while prioritizing safety, especially those with sensitive skin.

[0096] This invention employs multi-target intervention for a more comprehensive and lasting mechanism of action: Breaking away from the single-component, single-pathway approach, this invention constructs a network of action covering the entire pathway of melanin production, transport, and metabolism through multi-dimensional synergistic interventions such as barrier repair, tyrosinase inhibition, anti-inflammatory soothing, and keratinocyte metabolism promotion. In vitro cell experiments demonstrate that this compound system exhibits synergistic enhancement effects in multiple key pathways, with a comprehensive inhibitory effect superior to that of a single component, thus providing a mechanistic basis for achieving more stable and lasting skin tone improvement.

[0097] The active ingredient enrichment and bioavailability of this invention are more efficient and stable: the clustered green extraction process (such as supercritical CO2 extraction and membrane separation enrichment) adopted in this invention can specifically enrich high-purity target active substances (such as ergothioneine and triterpenoids), minimizing ineffective impurities and degradation of heat-sensitive components. Simultaneously, flaxseed oil in the formulation acts as a natural penetration enhancer, improving the transdermal delivery efficiency of fat-soluble active substances.

[0098] The organic balance between efficacy and premium skin feel in this invention: Through the scientific compounding of edible fungus polysaccharides and refined oils, this product ensures sufficient addition of active ingredients while successfully giving it a delicate, silky, and non-sticky texture. The cream is easy to spread and leaves a refreshing feeling after absorption, significantly improving the heavy and greasy feeling often found in traditional functional skincare products. This helps to enhance user compliance and ensures cumulative effects with long-term use.

[0099] Although the above embodiments have provided a detailed description of the present invention, they are only some embodiments of the present invention, and not all embodiments. Other embodiments can be obtained based on these embodiments without creative effort, and these embodiments all fall within the protection scope of the present invention.

Claims

1. A skin whitening and freckle-removing composition, characterized by comprising: The components include the following mass percentages: flavonoid essence 3-5%, fat-soluble active oil 1.5-2.5%, active small molecule compound 2-3%, polysaccharide compound 3-5%, cameline seed oil 7-9%, shea butter 1-2%, caprylic / capric triglyceride 3-4%, cetyl stearyl alcohol olive oil ester 0.8-1.2%, vitamin E 0.4-0.6%, emulsifier 3.5-4.5%, glycerol 4-5%, panthenol 1.5-2%, xanthan gum 0.05-0.1%, skin feel modifier 1.5-2.5%, preservative 0.8-1.2%, and water in balance; the polysaccharide compound and the active small molecule compound are obtained by water extraction and enzymatic hydrolysis of a first plant material in sequence, and the first plant material includes Auricularia auricula, Lentinula edodes, Bletilla striata, Polygonatum sibiricum, and Astragalus membranaceus; the flavonoid essence is obtained by deep eutectic solvent extraction and alcohol elution of a second plant material in sequence, and the second plant material includes Morus alba bark and Pinus densata; the fat-soluble active oil is obtained by supercritical CO2 fluid extraction of a third plant material, and the third plant material includes Phellinus baumii, Atractylodes macrocephala, and Angelica dahurica.

2. The whitening and freckle-removing composition according to claim 1, characterized by, The preparation method of the polysaccharide compound and the active small molecule compound includes the following steps: mixing the first plant material and water to perform reflux extraction to obtain an extraction liquid; adjusting the pH value of the extraction liquid to be acidic to obtain an acidic extraction liquid, mixing the acidic extraction liquid and a composite enzyme to perform enzymatic hydrolysis to obtain an enzymatic hydrolysis liquid, and the composite enzyme includes cellulase and pectinase; performing enzyme inactivation and solid-liquid separation on the enzymatic hydrolysis liquid in sequence to obtain an enzymatic hydrolysis filtrate, performing first ultrafiltration membrane separation on the enzymatic hydrolysis filtrate to obtain a first retentate and a first permeate, performing concentration and drying on the first retentate in sequence to obtain the polysaccharide compound, and performing second ultrafiltration membrane separation on the first permeate to obtain a second retentate, and performing drying on the second retentate to obtain the active small molecule compound.

3. The whitening and freckle-removing composition according to claim 2, characterized by, The mass ratio of Auricularia auricula, Lentinula edodes, Bletilla striata, Polygonatum sibiricum, and Astragalus membranaceus is (2-3):(1-2):(2-3):(2-3):(2-3); the solid-liquid ratio of the first plant material and water is 1:5-15; the reflux extraction temperature is 90-95°C, and the reflux extraction time is 1-3h; the mass percentage of the composite enzyme in the first plant material is 0.3-0.5%, and the mass ratio of cellulase and pectinase is 1-2:1-2; the enzymatic hydrolysis temperature is 45-50°C, and the enzymatic hydrolysis time is 2-3h; the molecular weight cut-off of the first ultrafiltration membrane separation is 100-120kDa, and the molecular weight cut-off of the second ultrafiltration membrane separation is 1-1.5kDa.

4. The whitening and freckle-removing composition according to claim 1, characterized by, The preparation method of the flavonoid essence includes the following steps: mixing the second plant material and a deep eutectic solvent to perform ultrasonic extraction, the deep eutectic solvent includes choline chloride and lactic acid to obtain an extraction liquid; performing resin column separation on the extraction liquid to obtain an eluate, and the eluent used in the resin column separation includes ethanol and water; performing concentration and drying on the eluate in sequence to obtain the flavonoid essence.

5. The whitening and freckle-removing composition according to claim 4, characterized by, The mass ratio of the mulberry bark and red pine mushroom is 1-2:1-2; the molar ratio of the choline chloride and lactic acid is 1:2-4; the solid-liquid ratio of the second plant raw material and the deep eutectic solvent is 1:20-30; the temperature of the ultrasonic extraction is 45-55℃, the power is 350-450W, and the time is 20-40min; the resin column separation is carried out by using an AB-8 macroporous resin column, and the volume percentage of ethanol in the eluent is 70-75%.

6. The whitening and freckle-removing composition according to claim 1, wherein The preparation method of the fat-soluble active oil comprises the following steps: The third plant raw material is subjected to supercritical CO2 fluid extraction to obtain an extract; The extract is subjected to post-treatment to obtain the fat-soluble active oil.

7. The whitening and freckle-removing composition according to claim 6, characterized by, The mass ratio of the Phellinus baumii, Atractylodes macrocephala and Angelica dahurica is (2-3):(1-2):(1-2); the supercritical CO2 fluid extraction conditions include an extraction pressure of 25-30MPa, an extraction temperature of 40-45℃, and a cycle extraction time of 2-3h; the supercritical CO2 fluid extraction also uses an entrainer, and the entrainer is ethanol; the post-treatment comprises vacuum distillation, and the temperature of the vacuum distillation is 40-45℃.

8. The whitening and freckle-removing composition according to claim 1, wherein The emulsifier is Olivem 1000; the skin feel regulator is cyclopentasiloxane; and the preservative is pentylene glycol.

9. The method of preparing the whitening and freckle-removing composition according to any one of claims 1 to 8, characterized by, The preparation method comprises the following steps: The shea butter, cetearyl olivate, camelina sativa seed oil, caprylic / capric triglyceride, fat-soluble active oil, vitamin E and emulsifier are mixed to obtain an oil phase; The glycerol, panthenol, water, xanthan gum, active small molecule compound and polysaccharide compound are mixed to obtain an aqueous phase; The oil phase and the aqueous phase are subjected to homogenization treatment to obtain an emulsion; The emulsion, flavonoid extract, skin feel regulator and preservative are mixed to obtain the whitening and freckle-removing composition.

10. The whitening and freckle-removing composition of any one of claims 1-8 or prepared by the preparation method of claim 9 in cosmetics.

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