Composition for retarding discoloration of resorcinol derivative as well as preparation method and application of composition

Abstract

The composition is prepared from the following components in parts by weight: 4 to 6 parts of resorcinol derivatives, 8 to 15 parts of anti-photosensitizer, 4 to 6 parts of solvent and 40 to 60 parts of 2 percent fibroin aqueous solution, the invention further discloses a preparation method and application of the composition for retarding discoloration of the resorcinol derivative. The composition for retarding the discoloration of the resorcinol derivative has the advantages that the discoloration of the resorcinol derivative is obviously retarded, and the problem of discoloration of the resorcinol derivative added in a formula is solved.

Description

Technical Field

[0001] This invention relates to the field of cosmetic technology, and more specifically to a composition for slowing down the discoloration of resorcinol derivatives, its preparation method, and its application. Background Technology

[0002] In cosmetics, the development of whitening ingredients requires stabilization technologies to protect the active ingredients from external damage and to address the technical challenges of applying these ingredients in formulations. Resorcinol derivatives are highly effective whitening agents. Compared to the strong skin irritation of resorcinol, the derivative structure of resorcinol significantly reduces skin irritation. However, they are highly susceptible to discoloration under light and heat conditions. Electrons in their molecular structure absorb energy from light and heat, undergoing oxidative changes that drastically reduce their whitening efficacy. This noticeable color change affects the appearance stability and efficacy of the formulation.

[0003] Currently, the main solutions to the problem of discoloration caused by adding resorcinol derivatives to formulations are to add antioxidants and construct nano-encapsulation technology. However, these methods have limitations, including the limited functionality of antioxidants, safety issues with nanomaterials, and biocompatibility issues with the human body.

[0004] In view of the above technical problems, those skilled in the art are dedicated to researching a composition that slows down the discoloration of resorcinol derivatives, its preparation method and application. Summary of the Invention

[0005] In view of the shortcomings of the prior art, the purpose of this application is to provide a composition for slowing down the discoloration of resorcinol derivatives, a method for preparing the composition, and its application.

[0006] More specifically, in a first aspect, this application provides a composition for slowing down the discoloration of resorcinol derivatives, comprising, by weight, 4-6 parts of resorcinol derivatives, 8-15 parts of photosensitizer, 4-6 parts of solvent, and 40-60 parts of 2% silk protein aqueous solution.

[0007] Furthermore, the photosensitizer comprises an acrylate copolymer; the solvent is selected from one or more of caprylic / capric triglyceride, isononyl isononanoate, hydrogenated polyisobutylene, ethylhexanoate cetearyl stearate, pentaerythritol tetra(ethylhexanoate), and lauroyl sarcosinate isopropyl ester.

[0008] Furthermore, by weight, it includes 5 parts of resorcinol derivative, 10 parts of photosensitizer, 5 parts of solvent, and 50 parts of 2% silk protein aqueous solution.

[0009] Secondly, this application provides a method for preparing a composition that slows down the discoloration of resorcinol derivatives, comprising the following steps: First, the resorcinol derivative, photosensitizer, and solvent are dissolved evenly. Then, 2% fibroin aqueous solution is added to obtain a mixed solution. Next, the mixed solution is homogenized and finally processed by high-pressure microfluidic jet to obtain the composition.

[0010] Furthermore, the homogenization process involves using a homogenizer at a homogenization speed of 5000-6000 rpm for 2-4 minutes.

[0011] Furthermore, the high-pressure microjets process involves using a high-pressure microjets at a power of 75-85 kW and a pressure of 15,000-25,000 psi.

[0012] Thirdly, this application provides a whitening cosmetic, including the aforementioned composition for slowing down the discoloration of resorcinol derivatives.

[0013] Furthermore, the composition for slowing down the discoloration of resorcinol derivatives has a mass percentage of 1-3% in the whitening cosmetic.

[0014] Furthermore, it also includes humectants, preservatives, thickeners, and water; The moisturizer includes at least one of glycerin, 1,2-hexanediol, and 1,3-propanediol; The thickener includes at least one of ammonium acryloyldimethyl taurate / VP copolymer, polyacrylate crosspolymer-6, and dehydroxanthan gum; The preservative includes at least one of p-hydroxyacetophenone, phenoxyethanol, and chlorphenesin.

[0015] The technical solution of this application achieves the following technical effects: 1. The composition for slowing down the discoloration of resorcinol derivatives in this application uses silk core protein, a natural surface-active substance extracted from silk. Under the physical induction of high-pressure microjets, the protein is modified to form a spherical cavity, which encapsulates the lipid-soluble resorcinol derivative and photosensitizer, etc., in the cavity, protecting the resorcinol derivative from external damage. No emulsification is required, and this composition significantly slows down the discoloration of resorcinol derivatives.

[0016] 2. In this application, based on the skin affinity, nanoscale, repair / anti-aging, and efficient emulsification properties of silk core protein, it can be used as a carrier for whitening active ingredients, avoiding the safety and compatibility issues of nanomaterials, while playing a role in repairing the skin and anti-aging. The nanoscale internal phase particles also increase the permeability of active ingredients in the skin.

[0017] 3. The silk core protein forms a spherical cavity that encapsulates the lipid-soluble resorcinol derivative and photosensitizer, thus slowing down the discoloration of the resorcinol derivative without affecting its whitening effect.

[0018] The following will further explain the concept, specific structure and technical effects of this application in conjunction with the accompanying drawings, so as to fully understand the purpose, features and effects of this application. Attached Figure Description

[0019] Figure 1 This is a nanoparticle size distribution diagram of the composition of this application.

[0020] Figure 2 These are color comparison photos of an embodiment and a comparative example of this application after being added to whitening cosmetics and exposed to light for one month at 4°C, 50°C, and light.

[0021] Figure 3 These are color comparison photos of an embodiment and a comparative example of this application, showing the color of the product added to a whitening cosmetic at 50°C for one month.

[0022] Figure 4 This is a comparison chart of tyrosinase inhibition rates at concentrations of 0.1% and 0.01% in one embodiment and a comparative example of this application. Detailed Implementation

[0023] The following specific examples illustrate the implementation of this application. Those skilled in the art can easily understand other advantages and effects of this application from the content disclosed in this specification. This application can also be implemented or applied through other different specific embodiments, and various details in this specification can also be modified or changed based on different viewpoints and applications without departing from the spirit of this application. It should be noted that, unless otherwise specified, the following embodiments and features in the embodiments can be combined with each other.

[0024] Some exemplary embodiments of this application have been described for illustrative purposes. It should be understood that this application may be implemented in other ways not specifically shown in the accompanying drawings.

[0025] Silk-core protein, as a high-molecular-weight repair protein, is one of the naturally skin-friendly proteins. Its content of glycine, alanine, and serine is 85%, which can replenish epidermal structural proteins and has combined repair / anti-aging effects. It is an FDA-approved ingredient for medical implants, cosmetic surgery, and high-end skincare. Silk-core protein's skin-friendliness, nanoscale size, repair / anti-aging properties, and efficient emulsification make it suitable as a carrier for whitening active ingredients, avoiding the safety and compatibility issues of nanomaterials. It simultaneously repairs the skin and has anti-aging effects, while the nanoscale internal phase particles also increase the permeability of active ingredients in the skin. Therefore, this application provides a composition for slowing down the discoloration of resorcinol derivatives, prepared by compounding silk-core protein, an anti-photosensitizer, and a resorcinol derivative, and its application in cosmetics.

[0026] This application discloses a composition for slowing down the discoloration of resorcinol derivatives, comprising, by weight, 4-6 parts of resorcinol derivative, 8-15 parts of photosensitizer, 4-6 parts of solvent, and 40-60 parts of 2% silk protein aqueous solution. The photosensitizer includes an acrylate copolymer, and the solvent is selected from one or more of caprylic / capric triglyceride, isononyl isononanoate, hydrogenated polyisobutylene, ethylhexanoate cetearyl stearate, pentaerythritol tetra(ethylhexanoate), and lauroyl sarcosinate isopropyl ester.

[0027] The composition includes 4-6 parts of resorcinol derivative, 8-15 parts of photosensitizer, 4-6 parts of solvent, and 40-60 parts of 2% silk protein aqueous solution. For example, the weight percentages could be 5 parts of resorcinol derivative, 8 parts of photosensitizer, 5 parts of solvent, and 50 parts of 2% silk protein aqueous solution, or 6 parts of resorcinol derivative, 12 parts of photosensitizer, 6 parts of solvent, and 60 parts of 2% silk protein aqueous solution. It should be understood that the listed proportions do not constitute a limitation of this application. Those skilled in the art can select from the range of 4-6 parts of resorcinol derivative, 8-15 parts of photosensitizer, 4-6 parts of solvent, and 40-60 parts of 2% silk protein aqueous solution, or adjust according to the actual situation.

[0028] The photosensitizer, solvent, and 2% fibroin aqueous solution used in this application were purchased directly from the market.

[0029] This application also discloses a method for preparing a composition that slows down the discoloration of resorcinol derivatives, comprising the following steps: first, dissolving the resorcinol derivative, photosensitizer and solvent evenly according to the weight parts, then adding 2% silk protein aqueous solution to obtain a mixed solution, then homogenizing the mixed solution, and finally obtaining the composition by high-pressure microfluidic treatment.

[0030] The preparation method of this application is as follows: First, the resorcinol derivative, photosensitizer and solvent are mixed and dissolved evenly according to the weight parts, and then 2% silk protein aqueous solution is added to obtain a mixed solution; then the above mixed solution is homogenized by homogenizing at a homogenization speed of 5000-6000 rpm for 2-4 min; finally, it is treated at least three times by a high-pressure microfluidic instrument under the conditions of 75-85 kW power and 15000-25000 psi pressure to obtain a composition that slows down the discoloration of resorcinol derivative.

[0031] It should be understood that those skilled in the art can adjust the homogenization speed and processing time of the homogenizer according to the actual situation, as long as the purpose of mixing the material evenly is achieved; the power and pressure parameters of the high-pressure microfluidic instrument can be selected as long as the purpose of forming a spherical cavity that can be enclosed under the physical induction of the high-pressure microfluidic jet is achieved.

[0032] This application also discloses a skin-whitening cosmetic, comprising the aforementioned composition for slowing down the discoloration of resorcinol derivatives. Furthermore, the composition for slowing down the discoloration of resorcinol derivatives constitutes 1-3% by mass in the skin-whitening cosmetic.

[0033] The whitening cosmetic disclosed in this application also includes moisturizers, preservatives, thickeners, and water; wherein the moisturizers include at least one of glycerin, 1,2-hexanediol, and 1,3-propanediol; the thickeners include at least one of ammonium acryloyldimethyl taurate / VP copolymer, polyacrylate crosspolymer-6, and dehydroxanthan gum; and the preservatives include at least one of p-hydroxyacetophenone, phenoxyethanol, and chlorphenesin.

[0034] It should be understood that those skilled in the art can adjust the dosage of materials. When it is necessary to prepare a larger quantity of composition or whitening cosmetics, the above-mentioned raw materials can be increased proportionally.

[0035] In this application, the compounded composition is processed by a high-pressure microfluidic process, utilizing the self-assembly of fibroin to form microspheres that encapsulate oil-soluble substances within the inner phase, protecting resorcinol derivatives from external damage. After the composition is added to the experimental formulation for testing, the composition of this application has a significant effect in slowing down the discoloration of resorcinol derivatives.

[0036] Example 1: Preparation of a composition for slowing down the discoloration of resorcinol derivatives According to the weight proportions, weigh 5 parts of 4-butylresorcinol, 10 parts of acrylic (ester) copolymer, 5 parts of caprylic / capric triglyceride and 1 part of lauroyl sarcosine isopropyl ester, mix them thoroughly and evenly, and then add 50 parts of 2% silk protein aqueous solution; use a homogenizer to homogenize at 5000 rpm for 3 min, and finally use a high-pressure microfluidic instrument to treat the above-mentioned mixed substances three times at a power of 85kW and a pressure of 25000psi to obtain a composition that slows down the discoloration of resorcinol derivatives.

[0037] The composition obtained in this example that slows down the resorcinol derivative was subjected to three parallel tests, yielding the following results: Figure 1 The particle size distribution of the prepared composition is shown in the figure. It can be seen from the figure that the particle size of the composition is between 400-500 nm.

[0038] Example 2: Preparation of a composition for slowing down the discoloration of resorcinol derivatives According to the weight proportions, 6 parts of 4-butylresorcinol, 12 parts of acrylic (ester) copolymer, 6 parts of isononyl isononanoate and hydrogenated polyisobutylene were weighed and mixed thoroughly and evenly. Then, 60 parts of 2% silk protein aqueous solution were added. After homogenizing with a homogenizer at a speed of 5500 rpm for 3 minutes, the mixture was finally treated three times with a high-pressure microfluidic instrument at a power of 80 kW and a pressure of 20000 psi to obtain a composition that slows down the discoloration of resorcinol derivatives.

[0039] Example 3: Preparation of a composition for slowing down the discoloration of resorcinol derivatives According to the weight proportions, 5 parts of phenylethyl resorcinol, 10 parts of acrylic (ester) copolymer, and 5 parts of caprylic / capric triglyceride were weighed and mixed thoroughly and evenly. Then, 50 parts of 2% silk protein aqueous solution were added. After homogenizing for 2 minutes at 5500 rpm using a homogenizer, the mixture was finally treated three times using a high-pressure microfluidic instrument at a power of 85 kW and a pressure of 25000 psi to obtain a composition that slows down the discoloration of resorcinol derivatives.

[0040] Example 4: Preparation of a composition for slowing down the discoloration of resorcinol derivatives (Part 4) According to the weight proportions, 6 parts of phenylethyl resorcinol, 8 parts of acrylic (ester) copolymer, 6 parts of cetearyl stearate ethylhexanoate and pentaerythritol tetra(ethylhexanoate) ester were weighed and mixed thoroughly and dissolved evenly. Then, 60 parts of 2% silk protein aqueous solution were added. After homogenizing with a homogenizer at a speed of 6000 rpm for 4 min, the mixture was finally treated three times with a high-pressure microfluidic instrument at a power of 85 kW and a pressure of 25000 psi to obtain a composition that slows down the discoloration of resorcinol derivatives.

[0041] Example 5: Preparation of a composition for slowing down the discoloration of resorcinol derivatives According to the weight proportions, weigh 4 parts of phenylethyl resorcinol, 15 parts of acrylic (ester) copolymer, and 4 parts of caprylic / capric triglyceride, mix them thoroughly and evenly, and then add 40 parts of 2% silk protein aqueous solution. After homogenizing with a homogenizer at a speed of 6000 rpm for 3 min, the mixture is finally treated three times with a high-pressure microfluidic instrument at a power of 75 kW and a pressure of 15000 psi to obtain a composition that slows down the discoloration of resorcinol derivatives.

[0042] Example 6 Preparation of whitening cosmetics The compositions obtained in Examples 1-4 were added according to the formulations in Table 1 below to prepare whitening cosmetics; wherein the mass percentage of the composition in the whitening cosmetics was 2%.

[0043] Table 1 Comparative Example 1 According to the weight proportions, 5 parts of 4-butylresorcinol, 5 parts of caprylic / capric triglyceride, 1 part of lauroyl sarcosine isopropyl ester, 0.5 parts of 1,2-hexanediol, 0.5 parts of p-hydroxyacetophenone, and 88 parts of deionized water were weighed and mixed evenly. The mixture was then homogenized at 6000 rpm for 3 minutes to obtain the composition of Comparative Example 1. This composition of Comparative Example 1 was then used to prepare cosmetics according to the formulation in Table 1, wherein the composition of Comparative Example 1 constituted 2% by weight in the whitening cosmetic.

[0044] Comparative Example 2 According to the weight proportions, 5 parts of 4-butylresorcinol, 10 parts of acrylate copolymer, 5 parts of caprylic / capric triglyceride, 1 part of lauroyl sarcosine isopropyl ester, 0.5 parts of 1,2-hexanediol, 0.5 parts of p-hydroxyacetophenone, and 78 parts of deionized water were weighed and mixed evenly. The mixture was then homogenized at 6000 rpm for 3 minutes to obtain the composition of Comparative Example 2. This Comparative Example 2 composition was then used to prepare cosmetics according to the formulation in Table 1, wherein the composition of Comparative Example 2 constituted 2% by weight in the whitening cosmetic.

[0045] Comparative Example 3 According to the weight proportions, 5 parts of 4-butylresorcinol, 5 parts of caprylic / capric triglyceride, 1 part of lauroyl sarcosine isopropyl ester, 0.5 parts of 1,2-hexanediol, 0.5 parts of p-hydroxyacetophenone, and 38 parts of deionized water were weighed and mixed evenly. Then, 50 parts of 2% silk protein aqueous solution were added. The mixture was homogenized at 6000 rpm for 3 minutes using a homogenizer. Finally, the mixture was treated three times using a high-pressure microfluidic apparatus at a power of 85 kW and a pressure of 25000 psi to obtain the composition of Comparative Example 3. This composition of Comparative Example 3 was then used to prepare cosmetics according to the formula in Table 1, wherein the composition of Comparative Example 3 accounted for 2% by mass in the whitening cosmetics.

[0046] Comparative Example 4 According to the weight proportions, 5 parts of phenylethyl resorcinol, 5 parts of caprylic / capric triglyceride, 1 part of lauroyl sarcosine isopropyl ester, 0.5 parts of 1,2-hexanediol, 0.5 parts of p-hydroxyacetophenone, and 88 parts of deionized water were weighed and mixed evenly. The mixture was then homogenized at 6000 rpm for 3 minutes to obtain the composition of Comparative Example 4. This Comparative Example 4 composition was then used to prepare cosmetics according to the formulation in Table 1, wherein the composition of Comparative Example 4 constituted 2% by weight in the whitening cosmetic.

[0047] Comparative Example 5 According to the weight proportions, 5 parts of phenylethyl resorcinol, 10 parts of acrylate copolymer, 5 parts of caprylic / capric triglyceride, 1 part of lauroyl sarcosine isopropyl ester, 0.5 parts of 1,2-hexanediol, 0.5 parts of p-hydroxyacetophenone, and 78 parts of deionized water were weighed and mixed evenly. The mixture was then homogenized at 6000 rpm for 3 minutes to obtain the composition of Comparative Example 5. This Comparative Example 5 composition was then used to prepare cosmetics according to the formulation in Table 1, wherein the composition of Comparative Example 5 constituted 2% by weight in the whitening cosmetic.

[0048] Comparative Example 6 According to the weight proportions, 5 parts of phenylethyl resorcinol, 5 parts of caprylic / capric triglyceride, 1 part of lauroyl sarcosine isopropyl ester, 0.5 parts of 1,2-hexanediol, 0.5 parts of p-hydroxyacetophenone, and 38 parts of deionized water were weighed and mixed evenly. Then, 50 parts of 2% silk protein aqueous solution were added. The mixture was homogenized at 6000 rpm for 3 minutes using a homogenizer. Finally, the mixture was treated three times using a high-pressure microfluidic apparatus at a power of 85 kW and a pressure of 25000 psi to obtain the composition of Comparative Example 6. This Comparative Example 6 composition was then used to prepare cosmetics according to the formula in Table 1, wherein the mass percentage of the Comparative Example 6 composition in the whitening cosmetic was 2%.

[0049] Test Example 1 The cosmetics prepared from the compositions of Example 1 and Comparative Examples 1-3 were placed at 4°C, 50°C, and under light, respectively. After one month, photographs were taken to compare the changes in appearance and color. The results are as follows: Figure 2 As shown in the figure, the degree of color change reduction under light is: Example 1 > Comparative Example 2 > Comparative Example 1 > Comparative Example 3. That is, the color difference between Comparative Example 1 and Comparative Example 3 is not significant, indicating that the silk core protein has no obvious effect on reducing the color change of the composition of this application. Although a photosensitizer was added in Comparative Example 2, its ability to reduce color change is relatively limited. The slow color change in Example 1 of this application indicates that the composition of lipid-soluble 4-butylresorcinol and anti-photosensitizer, which is encapsulated by silk core protein, has a better effect on reducing color change. The addition of silk core protein can further consolidate the effect of the anti-photosensitizer.

[0050] Test Example 2 The cosmetics prepared from the compositions of Example 3 and Comparative Examples 4-6 were placed at 50°C for one month, and the changes in appearance and color were compared by taking photographs. The results are as follows: Figure 3 As shown in the figure, the degree of color reduction under light exposure is greater in Example 3 than in Comparative Example 4, which is approximately equal to that in Comparative Example 5, which is approximately equal to that in Comparative Example 6. This indicates that the composition containing lipid-soluble phenylethyl resorcinol encapsulated in silk protein and a photosensitizer has a superior effect in reducing color discoloration.

[0051] Test Example 3 The compositions prepared in Example 1 and Comparative Example 1 were used to prepare samples with volume fractions of 0.1% and 0.01%, respectively, for tyrosinase inhibition tests. The test results are as follows: Figure 4 As shown in the figure, the comparison shows that the cosmetics prepared in Example 1 and Comparative Example 1 did not show a significant difference in tyrosinase inhibition rate at concentrations of 0.1% and 0.01%, indicating that the encapsulation of the silk core protein does not affect the whitening effect of 4-butylresorcinol.

[0052] The above embodiments are merely illustrative of the principles and effects of this application and are not intended to limit this application. Any person skilled in the art can modify or alter the above embodiments without departing from the spirit and scope of this application. Therefore, all equivalent modifications or alterations made by those skilled in the art without departing from the spirit and technical concept disclosed in this application should still be covered by the claims of this application.

Claims

1. A composition for slowing down the discoloration of resorcinol derivatives, characterized in that, By weight, it includes 4-6 parts of resorcinol derivative, 8-15 parts of photosensitizer, 4-6 parts of solvent, and 40-60 parts of 2% silk protein aqueous solution.

2. The composition for slowing down the discoloration of resorcinol derivatives according to claim 1, characterized in that, The photosensitizer includes an acrylic (ester) copolymer; the solvent is selected from one or more of the following: caprylic / capric triglyceride, isononyl isononanoate, hydrogenated polyisobutylene, ethylhexanoate cetearyl stearate, pentaerythritol tetra(ethylhexanoate), and lauroyl sarcosinate isopropyl ester.

3. The method for preparing the composition for slowing down the discoloration of resorcinol derivatives according to claim 1, characterized in that, By weight, it includes 5 parts of resorcinol derivative, 10 parts of photosensitizer, 5 parts of solvent, and 50 parts of 2% silk protein aqueous solution.

4. A method for preparing the composition for slowing down the discoloration of resorcinol derivatives according to any one of claims 1-3, characterized in that, Includes the following steps: First, the resorcinol derivative, photosensitizer, and solvent are dissolved evenly. Then, 2% fibroin aqueous solution is added to obtain a mixed solution. Next, the mixed solution is homogenized and finally processed by high-pressure microfluidic jet to obtain the composition.

5. The method for preparing the composition for slowing down the discoloration of resorcinol derivatives according to claim 4, wherein the homogenization step is to use a homogenizer to homogenize at a speed of 5000-6000 rpm for 2-4 min.

6. The method for preparing the composition for slowing down the discoloration of resorcinol derivatives according to claim 4, characterized in that, The high-pressure microjets process involves using a high-pressure microjets at a power of 75-85 kW and a pressure of 15,000-25,000 psi.

7. A whitening cosmetic product, characterized in that, Compositions that slow down the discoloration of resorcinol derivatives as described in any one of claims 1-3.

8. The whitening cosmetic according to claim 7, characterized in that, The composition for slowing down the discoloration of resorcinol derivatives has a mass percentage of 1-3% in whitening cosmetics.

9. The whitening cosmetic according to claim 7, characterized in that, It also includes humectants, preservatives, thickeners, and water; The moisturizer includes at least one of glycerin, 1,2-hexanediol, and 1,3-propanediol; The thickener includes at least one of ammonium acryloyldimethyl taurate / VP copolymer, polyacrylate crosspolymer-6, and dehydroxanthan gum; The preservative includes at least one of p-hydroxyacetophenone, phenoxyethanol, and chlorphenesin.

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