Whitening composition with after-sun repair effect, application of whitening composition, cosmetic and preparation method of cosmetic

Abstract

The invention discloses a whitening composition with an after-sun repair effect, application of the whitening composition, cosmetics and a preparation method of the cosmetics. The whitening composition is prepared from 4-butyl resorcinol liposome, rice fermentation liquor and hothorax Atlantianus oil, and the mass ratio of the 4-butyl resorcinol liposome to the rice fermentation liquor to the hothorax Atlantianus oil is (0.1-2%): (0.1-10%): (0.1-10%). According to the whitening composition with the after-sun repair effect, the application of the whitening composition, the cosmetic and the preparation method of the whitening composition, the bioavailability and the absorption efficiency can be improved, irritation to the skin is reduced, the whitening composition can be used for sensitive and fragile after-sun skin, and the whitening requirement of the after-sun skin is met.

Description

Technical Field

[0001] The invention belongs to the technical field of compositions, and relates to a whitening composition, and in particular to a whitening composition with after-sun repairing effect, an application thereof, a cosmetic and a preparation method thereof. Background Art

[0002] Ultraviolet (UV) in sunlight is the main source of UV exposure for organisms on Earth. UV is non-ionizing radiation, and its photon energy can cause electron energy level transitions after being absorbed by atoms or molecules, thereby triggering a variety of biological effects in the cells of organisms. According to different wavelengths, ultraviolet rays can be divided into four types: UVA (320-400nm), UVB (275-320nm), UVC (200-275nm), and UVD (100-200nm). Among them, UVC is almost completely absorbed by the ozone layer and cannot reach the earth's surface. Among the UV that can reach the earth's surface, 5% of UVB can penetrate the surface of the skin, and 95% of UVA can penetrate the dermis.

[0003] The skin is one of the largest organs in the human body, and its main function is to protect the body's internal tissues and organs from external stimuli. The skin is mainly composed of three parts: the epidermis, dermis, and subcutaneous tissue. The epidermis mainly contains keratinocytes (KC), a small amount of Langerhans cells (LC), melanocytes, and Merkel cells (MC), which have the functions of preventing fluid loss and repairing wounds. The dermis is the main component of the skin, mainly composed of collagen and elastin, which supports the epidermis and provides skin elasticity. The subcutaneous tissue is composed of fat cells, connecting the dermis and muscles, and plays a role in regulating temperature and buffering.

[0004] UV mainly affects the skin by inducing oxidative stress, DNA damage, immunosuppression, photoaging and inflammation. When human skin is exposed to ultraviolet rays, it will cause cells to release a variety of inflammatory mediators such as interleukin (IL), tumor necrosis factor-α (TNF-α), etc. and increase the level of reactive oxygen species (ROS) in skin cells, eventually showing symptoms such as redness, desquamation, itching, and stinging. Under strong sunlight, ordinary sunscreen methods cannot completely avoid the damage caused by ultraviolet rays to the skin, so it is particularly important to repair the skin after sun exposure. In addition, after ultraviolet rays irradiate the skin, arachidonic acid, prostaglandin D2, prostaglandin E2 and some reduction products increase significantly, increase the number of melanocytes, enlarge melanocytes and their dendrites, and increase the ability of cells to synthesize melanin and the activity of tyrosinase.

[0005] Currently, whitening cosmetics on the market mainly achieve whitening effects by protecting against ultraviolet rays, inhibiting the production and transport of melanocytes, and promoting the renewal of the stratum corneum. Among them, inhibiting the production and transport of melanin is widely used because it can accurately and effectively achieve whitening effects. Tyrosinase is a key enzyme for synthesizing melanin, so inhibiting the activity or amount of tyrosinase is the key to whitening. Currently commonly used tyrosinase inhibitors such as vitamin C, kojic acid and its derivatives mainly reduce the reduction of dopaquinone to dopa, reduce the raw materials for the production of melanin and block the catalytic reaction of tyrosinase to reduce the final production of melanin.

[0006] At present, related inventions in the field of skin whitening, such as Chinese invention patent CN202410417799.8, mainly use niacinamide, arbutin, tranexamic acid, etc. as whitening ingredients, and achieve whitening effects by inhibiting the production and transport of melanocytes. However, they have the disadvantages of being highly irritating to the skin, unstable ingredients, and difficult to be absorbed and utilized by the skin. Compared with normal skin, sun-exposed skin has a more urgent need for whitening, and sun-exposed skin is more sensitive and fragile, so ordinary whitening products cannot meet the whitening needs of sun-exposed skin.

[0007] At the same time, there have been many studies on skin repair after sun exposure, but existing technologies such as Chinese invention patent CN202010321379.1 mainly focus on alleviating the inflammatory response and redness, swelling, itching and other discomforts after sun exposure to repair the skin. There is no related invention that targets the darkening of skin after sun exposure and takes into account both whitening and repair effects.

[0008] In addition, existing sunscreen products cannot provide long-term sun protection and can easily increase the burden on the skin, causing clogged pores. Post-sun repair solutions, such as Chinese invention patent CN202211154512.4, can only repair existing skin damage and cannot play a preventive role.

[0009] In view of this, there is an urgent need to design a new whitening composition so as to overcome at least part of the above-mentioned defects of the existing whitening compositions. Summary of the invention

[0010] The present invention provides a whitening composition with after-sun repairing effect and its application, cosmetics and preparation method thereof, which can improve bioavailability and absorption efficiency, reduce irritation to skin, can be used for sensitive and fragile after-sun skin, and meet the whitening needs of after-sun skin.

[0011] To solve the above technical problem, according to one aspect of the present invention, the following technical solution is adopted:

[0012] A whitening composition with after-sun repair effect, the whitening composition comprises: 4-butylresorcinol liposome, rice fermentation liquid and Atlantic snapper oil, the mass ratio of the 4-butylresorcinol liposome, rice fermentation liquid and Atlantic snapper oil is (0.1-2%): (0.1-10%): (0.1-10%).

[0013] As an embodiment of the present invention, the mass ratio of the 4-butylresorcinol liposome, rice fermentation broth and Atlantic snapper oil is (0.1% to 1%): (0.1% to 5%): (0.1% to 5%).

[0014] According to another aspect of the present invention, the following technical solution is adopted: an application of the above-mentioned whitening composition with after-sun repairing effect in the preparation of cosmetics with after-sun repairing effect.

[0015] According to another aspect of the present invention, the following technical solution is adopted: a cosmetic comprising the above-mentioned whitening composition with after-sun repairing effect.

[0016] As an embodiment of the present invention, the cosmetic is a facial cream, a lotion, an essence, a freeze-dried powder, or a skin care lotion.

[0017] As an embodiment of the present invention, the cosmetic is a facial cream; the facial cream further comprises phase A auxiliary material, phase B auxiliary material, phase C auxiliary material and phase D auxiliary material;

[0018] Based on 100 parts by weight of the facial cream, the phase A auxiliary materials include 0.1 to 25 parts of thickener A, 0.1 to 30 parts of skin conditioner A and 1 to 30 parts of moisturizer A; the phase B auxiliary materials include 0.1 to 25 parts of thickener B, 0.1 to 30 parts of emulsifier and 1 to 15 parts of skin conditioner B; the phase C auxiliary materials include 0.1 to 5 parts of pH regulator; the phase D auxiliary materials include 0.1 to 5 parts of fragrance and 0.01 to 1 part of preservative.

[0019] As an embodiment of the present invention, the phase A auxiliary material also includes water, and the amount of water used is such that the weight parts of the cream reaches 100 parts.

[0020] As an embodiment of the present invention, the thickener A and the thickener B each independently include at least one of acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer, polyacrylamide, xanthan gum, propylene glycol, behenyl alcohol, carbomer, laureth-7, cetyl alcohol, stearyl alcohol and hydroxyethyl cellulose.

[0021] As an embodiment of the present invention, the skin conditioner A and the skin conditioner B each independently include at least one of glycerin, isohexadecane, olive oil, sodium hyaluronate, lauryl alcohol, avocado butter, allantoin, butylene glycol, squalane, panthenol, lactic acid, tocopherol and dipotassium glycyrrhizinate.

[0022] As an embodiment of the present invention, the moisturizing agent A includes at least one of hyaluronic acid, allantoin, glycerin, ceramide, sodium lactate, butylene glycol, hydrogenated grape seed oil, olive oil and shea butter.

[0023] As an embodiment of the present invention, the emulsifier includes at least one of glyceryl stearate citrate, cetearyl glucoside (and) cetearyl alcohol, behenyl trimethyl ammonium methyl sulfate, coconut oil glycerides and sorbitan olivate.

[0024] As an embodiment of the present invention, the pH regulator includes at least one of arginine and lactic acid; the fragrance includes essence; and the preservative includes at least one of phenoxyethanol, ethylhexylglycerin and pentylene glycol.

[0025] According to another aspect of the present invention, the following technical solution is adopted: a method for preparing the above-mentioned cosmetics, the preparation method comprising:

[0026] Step a, obtaining a water phase: placing water in a container with a stirring device and stirring, fully wetting and mixing the other parts of the auxiliary materials in phase A except water, adding them into the water, stirring them fully until they are completely dissolved, and heating them to 75-80°C;

[0027] Step b, obtaining an oil phase; mixing the auxiliary materials of phase B, heating to 75-80°C, and stirring until completely dissolved;

[0028] Step c, emulsification: add the mixture of step b to the aqueous phase of step a, stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes;

[0029] Step d, add phase C auxiliary material, stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes, and stir and cool to 40-45°C;

[0030] Step e, adding the whitening composition, stirring at 250-350 rpm for 3-5 minutes and homogenizing at 2500-3500 rpm for 3-10 minutes;

[0031] Step f: After the temperature is lowered to 35-38° C., add the auxiliary material of phase D, stir at 250-350 rpm and homogenize at 2500-3500 rpm for 3-10 minutes to obtain the cosmetics.

[0032] As an embodiment of the present invention, the cosmetics are filtered and sterilized before being filled, and the bacterial content is detected and the toxins, immunogenicity, etc. are quality controlled to obtain the desired whitening cream with after-sun repair effect.

[0033] The beneficial effects of the present invention are as follows: the whitening composition with after-sun repairing effect and its application, cosmetics and preparation method thereof proposed in the present invention can improve bioavailability and absorption efficiency, reduce irritation to the skin, can be used for sensitive and fragile after-sun skin, and meet the whitening needs of after-sun skin.

[0034] The whitening composition of the present invention can not only inhibit tyrosinase activity through 4-butylresorcinol and reduce melanin production to achieve the purpose of whitening, but also can promote cell metabolism and collagen synthesis through the synergistic effect of rice fermentation liquid and Atlantic sea bream oil, by up-regulating the expression of skin water retention and barrier-related genes, and helping to lastingly moisturize, soothe, and promote skin repair, thereby achieving an after-sun repair effect. At the same time, the component cytosine in the rice fermentation liquid can protect the skin and prevent UVB from causing skin damage.

[0035] The 4-butylresorcinol liposomes prepared by the preferred nanoliposome encapsulation technology of the present invention greatly improve their bioavailability and absorption efficiency, reduce irritation to the skin, and can be used for sensitive and fragile sun-sunned skin to meet the whitening needs of sun-sunned skin.

[0036] The present invention repairs sunburned skin from the perspective of promoting ATP generation, reducing the expression of pro-inflammatory factors, and the synergistic effect of multiple functional ingredients. α-KG promotes the generation of cellular energy factor ATP and the proliferation of keratinocytes; ω-3PUFAs can reduce the expression of pro-inflammatory factors and reduce the generation of a large number of free radicals. The present invention specifically uses 4-butylresorcinol nanoliposomes and Atlantic snapper oil, and adds multi-functional ingredient rice fermentation liquid to promote the penetration of other functional ingredients, further ensuring the repair and whitening effect of the composition on sunburned skin. The combined use is significantly better than the effect of each ingredient used alone.

[0037] The present invention emphasizes the UVB protection effect of the composition. Cytosine in the rice fermentation liquid and ω-3 PUFAs in the Atlantic bream oil can prevent UVB from damaging the skin through high cell membrane resistance to ultraviolet rays and absorption of ultraviolet rays in the band of about 274 nm, thereby preventing and reducing sun damage.

[0038] The present invention selects raw materials, taking into full consideration the raw material stability, color, odor and other issues. The composition obtained by the invention has good light and heat stability and solubility, low irritation, and is easy to formulate. It can be added as a raw material to finished cosmetics for preparing whitening cosmetics with after-sun repair effect. BRIEF DESCRIPTION OF THE DRAWINGS

[0039] Figure 1 Flow chart of a method for preparing cosmetics in one embodiment of the present invention. DETAILED DESCRIPTION

[0040] The preferred embodiments of the present invention are described in detail below with reference to the accompanying drawings.

[0041] In order to further understand the present invention, preferred embodiments of the present invention are described below in conjunction with examples. However, it should be understood that these descriptions are only for further illustrating the features and advantages of the present invention, rather than limiting the claims of the present invention.

[0042] The description in this section is only for several typical embodiments, and the present invention is not limited to the scope of the embodiments. The same or similar prior art means and some technical features in the embodiments are mutually replaced within the scope of the present invention.

[0043] Unless otherwise indicated, implied from the context, or customary in the prior art, all parts and percentages in this application are based on weight, and the test and characterization methods used are all current as of the filing date of this application. Where applicable, the contents of any patent, patent application or publication referred to in this application are fully incorporated herein by reference, and their equivalent patent families are also incorporated by reference, especially the definitions of synthesis techniques, product and processing designs, polymers, comonomers, initiators or catalysts disclosed in these documents in the art. If the definition of a specific term disclosed in the prior art is inconsistent with any definition provided in this application, the definition of the term provided in this application shall prevail.

[0044] Numerical ranges in this application are approximate values, so unless otherwise specified, they may include numerical values ​​outside the range. Numerical ranges include all numerical values ​​from the lower limit to the upper limit increased by 1 unit, provided that there is an interval of at least 2 units between any lower value and any higher value. For example, if the recorded component, physical or other properties (such as molecular weight, melt index, etc.) are 100 to 1000, it means that all single values ​​are clearly listed, such as 100, 101, 102, etc., and all sub-ranges, such as 100 to 166, 155 to 170, 198 to 200, etc. For a range containing a numerical value less than 1 or containing a fraction greater than 1 (such as 1.1, 1.5, etc.), 1 unit is appropriately regarded as 0.0001, 0.001, 0.01 or 0.1. For a range containing a single digit less than 10 (such as 1 to 5), 1 unit is usually regarded as 0.1. These are only specific examples of what is intended to be expressed, and all possible combinations of values ​​between the lowest and highest values ​​listed are considered to be clearly recorded in this application. It should also be noted that the terms "first", "second", etc. in this article do not limit the order of precedence, but are only used to distinguish substances with different structures.

[0045] When used with respect to chemical compounds, unless expressly specified otherwise, the singular includes all isomeric forms and vice versa (e.g., "hexane" includes all isomers of hexane, individually or collectively). In addition, nouns using "a," "an," or "the" also include their plural forms unless expressly specified otherwise.

[0046] The terms "comprising", "including", "having" and their derivatives do not exclude the presence of any other components, steps or processes, and are irrelevant to whether these other components, steps or processes are disclosed in this application. To eliminate any doubt, unless explicitly stated, all compositions using the terms "comprising", "including", or "having" in this application may include any additional additives, adjuvants or compounds. On the contrary, except for those necessary for operating performance, the term "essentially consisting of..." excludes any other components, steps or processes from the scope of any description of the term below. The term "consisting of..." does not include any components, steps or processes that are not specifically described or listed. Unless explicitly stated, the term "or" refers to the listed individual members or any combination thereof.

[0047] The description of the steps in each embodiment in the specification is only for the convenience of explanation, and the implementation method of the present application is not limited by the order of implementation of the steps.

[0048] The invention discloses a whitening composition with after-sun repairing effect. The whitening composition comprises: 4-butylresorcinol liposome, rice fermentation liquid and Atlantic snapper oil. The mass ratio of the 4-butylresorcinol liposome, rice fermentation liquid and Atlantic snapper oil is (0.1-2%): (0.1-10%): (0.1-10%).

[0049] In one embodiment of the present invention, the mass ratio of the 4-butylresorcinol liposome, rice fermentation broth and Atlantic snapper oil is (0.1%-1%): (0.1%-5%): (0.1%-5%).

[0050] The present invention also discloses an application of the whitening composition with after-sun repairing effect in preparing cosmetics with after-sun repairing effect.

[0051] The present invention also discloses a cosmetic, which comprises the above-mentioned whitening composition with after-sun repairing effect. In one embodiment of the present invention, the cosmetic can be a face cream, a lotion, a serum, a freeze-dried powder or a skin care lotion.

[0052] In one embodiment, the cosmetic is a face cream (of course, the cosmetic can also be other cosmetic categories, such as eye cream, moisturizing cream, and body cream). The face cream also includes A phase auxiliary material, B phase auxiliary material, C phase auxiliary material, and D phase auxiliary material.

[0053] Based on 100 parts by weight of the facial cream, the phase A auxiliary materials include 0.1 to 25 parts of thickener A, 0.1 to 30 parts of skin conditioner A and 1 to 30 parts of moisturizer A; the phase B auxiliary materials include 0.1 to 25 parts of thickener B, 0.1 to 30 parts of emulsifier and 1 to 15 parts of skin conditioner B (which may be an excipient); the phase C auxiliary materials include 0.1 to 5 parts of pH regulator; the phase D auxiliary materials include 0.1 to 5 parts of fragrance and 0.01 to 1 part of preservative.

[0054] In one embodiment of the present invention, the phase A auxiliary material also includes water, and the amount of water used is such that the weight parts of the cream reaches 100 parts.

[0055] The thickener A and the thickener B each independently include at least one of acrylates / C10-30 alkyl acrylate crosspolymer, polyacrylamide, xanthan gum, propylene glycol, behenyl alcohol, carbomer, laureth-7, cetyl alcohol, stearyl alcohol and hydroxyethyl cellulose.

[0056] The skin conditioning agent A and the skin conditioning agent B each independently include at least one of glycerin, isohexadecane, olive oil, sodium hyaluronate, lauryl alcohol, shea butter, allantoin, butylene glycol, squalane, panthenol, lactic acid, tocopherol and dipotassium glycyrrhizinate.

[0057] The moisturizing agent A comprises at least one of hyaluronic acid, allantoin, glycerin, ceramide, sodium lactate, butylene glycol, hydrogenated grape seed oil, olive oil and shea butter.

[0058] The emulsifier includes at least one of glyceryl stearate citrate, cetearyl glucoside (and) cetearyl alcohol, behentrimonium methylsulfate, cocoglycerides and sorbitan olivate.

[0059] The pH regulator includes at least one of arginine and lactic acid; the fragrance includes essence; and the preservative includes at least one of phenoxyethanol, ethylhexylglycerin and pentylene glycol.

[0060] The present invention further discloses a method for preparing the above cosmetics. Figure 1 is a flow chart of a cosmetic preparation method according to an embodiment of the present invention; please refer to Figure 1 , the preparation method comprises:

[0061] Step a. Obtaining an aqueous phase: Place water in a container with a stirring device and stir, fully wet and mix the other parts of the phase A auxiliary materials, add them to the water, stir until completely dissolved, and heat to 75-80°C;

[0062] Step b. Obtaining the oil phase; heating the mixture of phase B excipients to 75-80°C and stirring until completely dissolved;

[0063] Step c. Emulsification: Add the mixture of step b to the aqueous phase of step a, stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes;

[0064] Step d. Add phase C auxiliary material, stir at 250-350rpm for 3-5 minutes and homogenize at 2500-3500rpm for 3-10 minutes, and stir and cool to 40-45°C;

[0065] Step e. Add the whitening composition (other active ingredients may also be added), stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes;

[0066] Step f. After the temperature is lowered to 35-38°C, add the phase D auxiliary material, stir at 250-350 rpm and homogenize at 2500-3500 rpm for 3-10 minutes to obtain the cosmetics.

[0067] In one embodiment of the present invention, the cosmetics are filtered and sterilized before being filled, and the bacterial content is detected and the toxins, immunogenicity, etc. are quality controlled to obtain the desired whitening cream with after-sun repair effect.

[0068] The present invention sets up each group of experiments by taking the face cream as an example, but is not limited to the use of the face cream. The composition can also be applied to various skin care products such as lotions, essences, freeze-dried powders, and skin care water. The face cream is the above key combination and an emollient, a thickener, a chelating agent, and a pH regulator. Preferably, the raw materials for preparing the whitening face cream with after-sun repairing effect also include any one or a combination of at least two of a preservative and a flavor.

[0069] Table 1 Proportions of components in Example 1

[0070]

[0071] In some embodiments, based on 100 parts by weight of the facial cream, the phase A excipients include 0.1 to 15 parts of xanthan gum, 0.1 to 20 parts of carbomer, 0.01 to 1 part of sodium hyaluronate, 0.1 to 10 parts of allantoin, 5 to 25 parts of glycerin, and 1 to 10 parts of butylene glycol;

[0072] Based on 100 parts by weight of the facial cream, the phase B auxiliary materials include 1-15 parts of cetyl alcohol, 1-15 parts of stearyl alcohol, 1-15 parts of behenyl alcohol, 0.1-15 parts of cetearyl glucoside (and) cetearyl alcohol, 1-40 parts of squalane, 1-30 parts of avocado tree (BUTYROSPERMUMPARKII) fruit fat, 0.1-10 parts of tocopherol acetate, 1-40 parts of hydrogenated polyisobutene, and 1-30 parts of polydimethylsiloxane;

[0073] Based on 100 parts by weight of the facial cream, the C-phase auxiliary material includes 0.1 to 5 parts of arginine;

[0074] Based on 100 parts by weight of the facial cream, the phase D auxiliary material includes 0.1 to 1 part of phenoxyethanol, 0.05 to 1 part of ethylhexylglycerin and 0.1 to 2 parts of fragrance.

[0075] One or more embodiments of the present invention provide a method for preparing a facial cream, comprising the following steps:

[0076] a. Obtaining the aqueous phase: Place water in a container with a stirring device and stir, fully wet and mix the other parts of the phase A excipients, add them to the water, stir until completely dissolved, and heat to 75-80°C;

[0077] b. Obtain the oil phase; mix the B phase excipients and heat to 75-80°C, stirring until completely dissolved;

[0078] c. Emulsification: Add the mixture of step b to the aqueous phase of step a, stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes;

[0079] d. Add phase C auxiliary material, stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes, and cool to 40-45°C with stirring;

[0080] e. Add the whitening composition, stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes;

[0081] f. After the temperature drops to 35-38°C, add phase D auxiliary material, stir at 250-350 rpm and homogenize at 2500-3500 rpm for 3-10 minutes to obtain cosmetics.

[0082] In one embodiment of the present invention, the cosmetics are filtered and sterilized before being filled, and the bacterial content is detected and the toxins, immunogenicity, etc. are quality controlled to obtain the desired whitening cream with after-sun repair effect.

[0083] Characterization data and effect data of the products of the embodiments and comparative examples

[0084] Examples 2-3 and Comparative Examples 1-3

[0085] The difference between Example 2 and Example 1 is only the increase of each effective ingredient, and the difference between Example 3 and Example 1 is only the reduction of each effective ingredient.

[0086] The difference between Control Examples 1-3 and Example 1 is the lack of one key composition component, the difference between Control Examples 4-6 and Example 1 is the lack of two key composition components, and the difference between Control Example 7 and Example 1 is that no composition component is added.

[0087] The specific proportions of Examples 2-3 and Comparative Examples 1-3 refer to Table 2, and the preparation method is consistent with that of Example 1.

[0088] Table 2 Specific proportions of components in Examples 1-3 and Comparative Examples 1-7

[0089]

[0090]

[0091] Efficacy evaluation test

[0092] 1. Determination of tyrosinase activity in mouse melanoma B16 cells

[0093] Test product: the creams obtained in Examples 1 to 3 and Control Examples 1 to 7 were diluted to 100 mg / mL with ethanol solution.

[0094] Model: Mouse melanoma B16 cells

[0095] Test method:

[0096] 1) B16 cell culture and grouping

[0097] Mouse melanoma B16 cells were placed in a medium containing 10% fetal bovine serum and penicillin-streptomycin (100 kU·L -1 ) in DMEM high-glucose medium (pH=7.2) at 37°C, 5% CO2 and relative saturated humidity, and cells in the logarithmic growth phase were used for subsequent experiments;

[0098] 2) Determination of intracellular tyrosinase activity

[0099] B16 cells were taken at 5×10 7 ·L -1 Inoculate in 12-well plates, 1 mL per well, and culture for 24 h. Add 0.2 μmol·L -1α-MSH was used to induce and construct a melanin high-expression cell model, and then different test samples were added, with 4 replicate wells in each group. After 48 hours of culture, the supernatant was discarded, and the cells were washed 3 times with PBS. 500 μL of PBS buffer containing 1% TritonX-100 was added to each well, and the cells were placed in a -80°C refrigerator and frozen for 1 hour, then thawed at room temperature. The cell lysate was centrifuged at 12000 r·min-1 and 4°C for 20 minutes, and the supernatant was collected. 60 μL of the supernatant was taken in a 96-well plate, and 140 μL of 5 mmol·L -1 L-Dopa, incubate at 37℃ for 1h, and measure the absorbance of each well at 405nm. The protein content in the solution was determined by Bradford method. The relative activity of intracellular tyrosinase was calculated according to the following formula: relative activity of intracellular tyrosinase / % = tyrosinase activity per gram of protein in the experimental group / tyrosinase activity per gram of protein in the α-MSH model group × 100%.

[0100] 2. Free radical (DPPH) scavenging test

[0101] Test product: the facial creams obtained in Examples 1 to 3 and Comparative Examples 1 to 7.

[0102] Experimental methods:

[0103] (1) Prepare 0.1 mmol / L DPPH solution and store it in the dark; prepare 100 mg / mL solutions of different samples;

[0104] (2) Place on a plate and allow to react for 30 minutes at room temperature in the dark.

[0105] Sample group: sample solution 100 μL + DPPH solution 100 μL;

[0106] Blank group: 100 μL sample solution + 100 μL anhydrous ethanol;

[0107] Control group: 100 μL DPPH solution + 100 μL water;

[0108] (3) Detect the absorbance at 517 nm, take the average value, and calculate the DPPH clearance rate of each sample, where the DPPH clearance rate calculation formula is: (1-(A sample -A blank ) / A control )×100%

[0109] Table 3 Comparison of the performance of the creams obtained in Examples 1-3 and Comparative Examples 1-7

[0110] Test Project Tyrosinase inhibition rate (%) Free radical DPPH scavenging rate (%) Example 1 90.23 86.83 Example 2 85.71 82.15 Example 3 80.23 75.72 Comparative Example 1 60.76 72.76 Comparative Example 2 66.74 65.37 Comparative Example 3 64.93 70.03 Comparative Example 4 58.72 65.79 Comparative Example 5 67.03 65.75 Comparative Example 6 58.69 59.37 Comparative Example 7 53.02 54.11

[0111] As shown in Table 3, Examples 1-3 have a significant inhibitory effect on tyrosinase and can reduce the formation of melanin. Compared with Control Examples 2, 3, and 5, Examples 1-3 have more significant inhibitory effects on tyrosinase and the ability to scavenge free radicals. From the comparison of the results, it can be seen that compared with not using the composition and only using one or two of 4-butylresorcinol nanoliposomes, rice fermentation broth, and Atlantic snapper oil, the inhibitory effect of tyrosinase and the ability to scavenge free radicals using 4-butylresorcinol nanoliposomes, rice fermentation broth, and Atlantic snapper oil are more significant, indicating that the composition of 4-butylresorcinol nanoliposomes, rice fermentation broth, and Atlantic snapper oil has a synergistic effect, and the facial cream prepared from the composition has good whitening and free radical scavenging abilities.

[0112] 3. Transepidermal water loss (TWEL) and skin stratum corneum moisture content test

[0113] Test sample: facial cream obtained in Example 1

[0114] Test equipment: TWEL( Combo), Cornermeter( Combo)、VISIA-CR(Canfield, system)

[0115] Test results:

[0116] (1) Demographic information of subjects: A total of 32 subjects were included, all of whom were female. The average age was 30 years old, including 17 subjects aged 18-25 years, 7 subjects aged 26-30 years, 7 subjects aged 36-40 years, and 1 subject aged 41-45 years.

[0117] (2) Statistics of adverse events during the test: None

[0118] (3) Skin physical and chemical data analysis results

[0119] Table 4 Analysis of changes in stratum corneum water content over time

[0120] Time Averages and standard deviations Variationpercentage BL 211.23±37.19 - W1 230.74±51.52 9.27％ W2 235.07±39.83 11.28％ W4 239.24±36.11 13.26％

[0121] As can be seen from Table 4, the water content of the stratum corneum of the subjects increased significantly by 13.26% after using the product for 4 weeks. The above results indicate that under the test conditions, the test product can significantly increase the water content level of the stratum corneum of the skin and has a moisturizing effect.

[0122] Table 5 Analysis of changes in TWEL values ​​of subjects' skin over time

[0123] Time Averages and standard deviations Variationpercentage BL 17.23±4.12 - W1 17.05±5.51 -1.04％ W2 14.56±3.65 -15.50％ W4 13.55±4.02 -21.36％

[0124] As can be seen from Table 5, the subjects' skin TWEL value decreased significantly by 15050% after using the product for 2 weeks; after using the product for 4 weeks, TWEL continued to decrease, significantly decreasing by 21.36%. The above results indicate that under the test conditions, the test product can significantly reduce the skin TWEL value and has a repairing effect.

[0125] 3. Security Testing

[0126] Test sample: Example 1

[0127] Test method: Select a suitable patch with an area of ​​no more than 50mm2 and a depth of about 1mm. Use the closed patch test method to add about 0.02-0.025mL (g) of the test substance into the patch tester. Stick the patch tester on the curved side of the subject's forearm, remove the test substance after 24 hours, observe the skin reaction at 0.5h, 24h, and 48h after removal, and record the results according to the skin reaction grading standards in the "Cosmetic Safety Technical Regulations 2015".

[0128] Table 6 Patch test results

[0129]

[0130] Note: Skin reaction grading standards

[0131] Grade 0: negative reaction;

[0132] Grade 1: Suspicious reaction; only slight erythema;

[0133] Grade 2: weak positive reaction (erythema reaction); erythema, infiltration, edema, and papules may be present;

[0134] Grade 3: Strong positive reaction (herpes reaction); erythema, infiltration, edema, papules; herpes; the reaction may extend beyond the tested area;

[0135] Grade 4: Very strong reaction (confluent herpes reaction); obvious erythema, severe infiltration, edema, confluent herpes, and the reaction exceeds the test area.

[0136] As can be seen from Table 6 above, the prepared cream showed no irritation and passed the safety test.

[0137] 4. Stability test

[0138] Test sample: Example 1

[0139] Test method: Internal control standard, observe the appearance color, viscosity, and pH within three months.

[0140] Table 7 Stability test results

[0141]

[0142]

[0143] As can be seen from Table 7 above, the color, viscosity and pH of the prepared cream did not change significantly under high and low temperature conditions or light exposure within three months, indicating that the cream has good stability.

[0144] 4-Butylresorcinol is a new type of antioxidant and the strongest tyrosinase inhibitor discovered so far. It can effectively inhibit melanin synthesis by enhancing the proteolysis of tyrosinase and inhibiting the activity of tyrosinase and tyrosinase-related protein-1 (TRP-1), thereby achieving whitening and brightening effects: in vitro experiments have also shown that the whitening effect is 5 times stronger than kojic acid and 500 times stronger than arbutin, and can effectively inhibit melanin synthesis. However, its shortcomings such as being slightly soluble in water, easy to volatilize, easy to oxidize, easy to change color, and highly irritating to the skin limit its application in cosmetics. The invention adopts nano-liposome encapsulation technology, utilizes nano-transmission system (NDS) to develop nano-active substances with a particle size of less than 50 nm, and stably encapsulates 4-butylresorcinol in nano-carriers to form a novel 4-butylresorcinol nano-liposome preparation (Nano-Liposomal4-Butylresorcinol), which greatly improves the bioavailability and absorption efficiency of 4-butylresorcinol. In addition, nano-liposome encapsulation increases hydrophilicity, lipophilicity and stability, so that 4-butylresorcinol can be more widely used in cosmetic formulations.

[0145] Mitochondria are a multifunctional organelle in cells, which are mainly responsible for life processes such as energy production and cell apoptosis, and play a role in the entire injury repair process. On the one hand, mitochondria provide the ATP energy basis required for cell growth; on the other hand, they provide the material basis such as oxygen and nutrition, promote capillary regeneration, improve the microenvironment, and remove necrotic tissue. At the same time, the Ca2+ stored in mitochondria can upregulate the activity of nitric oxide synthase (NOS), induce angiogenesis, accelerate matrix remodeling, and induce the proliferation of fibroblasts, endothelial cells, etc. In addition, mitochondria participate in regulating the release of growth factors such as VEGF, bFGF and PDGF, thereby promoting endothelial division and angiogenesis, and accelerating injury repair.

[0146] Rice fermentation liquid is a natural active extract obtained by fermenting selected extraordinary yeast species (Saccharomyces veronae) with high-quality rice produced at 40 degrees north latitude. It contains more than 90 substances such as amino acids, sugars, fruit acids, polyamines, nucleic acids, etc. Among them, cytosine has characteristic absorption in the band around 274nm, so it has ultraviolet protection ability and can prevent UVB in the environment from causing damage to the skin. Applying it to the skin can produce a cool feeling and quickly relieve the burning sensation of the skin after sun exposure.

[0147] In particular, the ingredient α-KG can promote the production of cellular energy factor ATP, help promote the proliferation of keratinocytes, strengthen the skin barrier function, improve the skin's water retention capacity, enhance the expression of barrier-related genes (FLG, SPT and IVL), and help quickly soothe and repair the skin after sun exposure.

[0148] In addition, experiments have confirmed that rice fermentation liquid has a penetration-enhancing effect. Based on the technology of nanoliposome encapsulation of 4-butylresorcinol adopted in the present invention, it is further ensured that the effective ingredients can quickly penetrate into the bottom layer of the skin, so as to achieve rapid soothing, repairing and whitening of the skin after sun exposure, and the synergistic effect is better.

[0149] Atlantic Hoplostethus ATLANTICUS oil is fish oil refined from the skin and body parts of Atlantic Hoplostethus altitus. It is rich in ω-3 polyunsaturated fatty acids (ω-3 PUFAs) and has a fatty acid composition very close to that of human sebum. Therefore, it has good skin affinity and is easily absorbed. It has excellent water-locking and moisturizing capabilities, can promote skin barrier repair, reduce skin irritation, and increase skin softness.

[0150] ω-3PUFAs are important components of human skin cell membranes, and therefore can improve the resistance of cell membranes to ultraviolet rays, thereby preventing and reducing skin damage after sun exposure. ω-3PUFAs can competitively prevent the metabolism of AA by replacing arachidonic acid (AA, dodecatetraenoic acid) in cell membrane phospholipids, reduce AA metabolites, reduce the production of proinflammatory factors such as prostaglandin 2 (PGE2) and leukotriene 4 (LBT4), and promote the phagocytic function of macrophages, thereby reducing the body's inflammatory response. In addition, ω-3PUFAs counteract the generation of a large number of free radicals, delay the progression of oxidative stress, strengthen the body's antioxidant system, and synergize with the first two functional ingredients described in the present invention to promote after-sun repair.

[0151] In summary, the whitening composition with after-sun repair effect and its application, cosmetics and preparation method thereof proposed in the present invention can improve bioavailability and absorption efficiency, reduce irritation to the skin, and can be used for sensitive and fragile after-sun skin to meet the whitening needs of after-sun skin.

[0152] The whitening composition of the present invention can not only inhibit tyrosinase activity through 4-butylresorcinol and reduce melanin production to achieve the purpose of whitening, but also can promote cell metabolism and collagen synthesis through the synergistic effect of rice fermentation liquid and Atlantic sea bream oil, by up-regulating the expression of skin water retention and barrier-related genes, and helping to lastingly moisturize, soothe, and promote skin repair, thereby achieving an after-sun repair effect. At the same time, the component cytosine in the rice fermentation liquid can protect the skin and prevent UVB from causing skin damage.

[0153] The 4-butylresorcinol liposomes prepared by the preferred nanoliposome encapsulation technology of the present invention greatly improve their bioavailability and absorption efficiency, reduce irritation to the skin, and can be used for sensitive and fragile sun-sunned skin to meet the whitening needs of sun-sunned skin.

[0154] The present invention repairs sunburned skin from the perspective of promoting ATP generation, reducing the expression of pro-inflammatory factors, and the synergistic effect of multiple functional ingredients. α-KG promotes the generation of cellular energy factor ATP and the proliferation of keratinocytes; ω-3PUFAs can reduce the expression of pro-inflammatory factors and reduce the generation of a large number of free radicals. The present invention specifically uses 4-butylresorcinol nanoliposomes and Atlantic snapper oil, and adds multi-functional ingredient rice fermentation liquid to promote the penetration of other functional ingredients, further ensuring the repair and whitening effect of the composition on sunburned skin. The combined use is significantly better than the effect of each ingredient used alone.

[0155] The present invention emphasizes the UVB protection effect of the composition. Cytosine in the rice fermentation liquid and ω-3 PUFAs in the Atlantic bream oil can prevent UVB from damaging the skin through high cell membrane resistance to ultraviolet rays and absorption of ultraviolet rays in the band of about 274 nm, thereby preventing and reducing sun damage.

[0156] The present invention selects raw materials, taking into full consideration the raw material stability, color, odor and other issues. The composition obtained by the invention has good light and heat stability and solubility, low irritation, and is easy to formulate. It can be added as a raw material to finished cosmetics for preparing whitening cosmetics with after-sun repair effect.

[0157] The technical features of the above-described embodiments may be arbitrarily combined. To make the description concise, not all possible combinations of the technical features in the above-described embodiments are described. However, as long as there is no contradiction in the combination of these technical features, they should be considered to be within the scope of this specification.

[0158] The description and application of the present invention here are illustrative, and it is not intended to limit the scope of the present invention to the above-mentioned embodiments. The effects or advantages involved in the embodiments may not be embodied in the embodiments due to interference from various factors, and the description of the effects or advantages is not used to limit the embodiments. The deformation and change of the embodiments disclosed here are possible, and the replacement of the embodiments and the various equivalent parts are well known to those of ordinary skill in the art. It should be clear to those skilled in the art that the present invention can be implemented in other forms, structures, arrangements, proportions, and with other components, materials and parts without departing from the spirit or essential features of the present invention. Other deformations and changes can be made to the embodiments disclosed here without departing from the scope and spirit of the present invention.

Claims

1. A whitening composition with after-sun repair effect, characterized in that: The whitening composition comprises: 4-butylresorcinol liposome, rice fermentation liquid and Atlantic snapper oil, and the mass ratio of the 4-butylresorcinol liposome, rice fermentation liquid and Atlantic snapper oil is (0.1-2%): (0.1-10%): (0.1-10%).

2. The whitening composition with after-sun repair effect according to claim 1, characterized in that: The mass ratio of the 4-butylresorcinol liposome, rice fermentation liquid and Atlantic snapper oil is (0.1% to 1%): (0.1％～5％)：(0.1％～5％)。 3. Use of the whitening composition with after-sun repairing effect according to any one of claims 1 to 2 in the preparation of cosmetics with after-sun repairing effect.

4. A cosmetic, characterized in that: The cosmetic comprises the whitening composition with after-sun repairing effect as claimed in any one of claims 1 to 2.

5. The cosmetic according to claim 4, characterized in that: The cosmetics are face cream, lotion, essence, freeze-dried powder or skin care lotion.

6. The cosmetic according to claim 5, characterized in that: The cosmetic is a facial cream; the facial cream further comprises phase A auxiliary material, phase B auxiliary material, phase C auxiliary material and phase D auxiliary material; Based on 100 parts by weight of the facial cream, the phase A auxiliary materials include 0.1 to 25 parts of thickener A, 0.1 to 30 parts of skin conditioner A and 1 to 30 parts of moisturizer A; the phase B auxiliary materials include 0.1 to 25 parts of thickener B, 0.1 to 30 parts of emulsifier and 1 to 15 parts of skin conditioner B; the phase C auxiliary materials include 0.1 to 5 parts of pH regulator; the phase D auxiliary materials include 0.1 to 5 parts of fragrance and 0.01 to 1 part of preservative.

7. The cosmetic according to claim 6, characterized in that: The phase A auxiliary material also includes water, and the amount of water used is such that the weight parts of the cream reaches 100 parts.

8. The cosmetic according to claim 6, characterized in that: The thickener A and the thickener B each independently include at least one of acrylic acid (esters) / C10-30 alkyl acrylate crosspolymer, 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 at least one of glycerin, isohexadecane, olive oil, sodium hyaluronate, lauryl alcohol, avocado butter, allantoin, butylene glycol, squalane, panthenol, lactic acid, tocopherol and dipotassium glycyrrhizinate; The moisturizing agent A comprises at least one of hyaluronic acid, allantoin, glycerin, ceramide, sodium lactate, butylene glycol, hydrogenated grape seed oil, olive oil and shea butter; The emulsifier includes at least one of glyceryl stearate citrate, cetearyl glucoside (and) cetearyl alcohol, behenyl trimethyl ammonium methyl sulfate, cocoglycerides and sorbitan olivate; The pH regulator includes at least one of arginine and lactic acid; the fragrance includes essence; and the preservative includes at least one of phenoxyethanol, ethylhexylglycerin and pentylene glycol.

9. A method for preparing the cosmetic according to any one of claims 6 to 8, characterized in that: The preparation method comprises: Step a, obtaining a water phase: placing water in a container with a stirring device, fully moistening and mixing the other parts of the auxiliary materials in phase A except water, adding them into the water, stirring them fully until they are completely dissolved, and heating them to 75-80°C; Step b, obtaining an oil phase; mixing the auxiliary materials of phase B, heating to 75-80°C, and stirring until completely dissolved; Step c, emulsification: add the mixture of step b to the aqueous phase of step a, stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes; Step d, add phase C auxiliary material, stir at 250-350 rpm for 3-5 minutes and homogenize at 2500-3500 rpm for 3-10 minutes, and stir and cool to 40-45°C; Step e, adding the whitening composition, stirring at 250-350 rpm for 3-5 minutes and homogenizing at 2500-3500 rpm for 3-10 minutes; Step f: After the temperature is lowered to 35-38° C., add the auxiliary material of phase D, stir at 250-350 rpm and homogenize at 2500-3500 rpm for 3-10 minutes to obtain the cosmetics.

10. The preparation method according to claim 9, characterized in that: Before filling the cosmetics, they are filtered and sterilized, and the bacterial content is tested and quality control is performed on toxins, immunogenicity, etc., so that the desired whitening cream with after-sun repair effect can be obtained.

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