Composition with whitening effect and application thereof

Abstract

The invention discloses a composition with a whitening effect. The composition is prepared from the following components in parts by mass: 47 to 51 parts of grape seed oil, 47 to 51 parts of pomegranate seed oil, 0.5 to 0.8 part of 4-butylresorcinol, 0.2 to 0.6 part of VC-IP (Vitamin C-IP) and 0.1 to 10 parts of isorhamnetin-3-O-neohesperidin. The invention also discloses a preparation method of the composition. The invention also discloses an essence oil containing the composition. The invention also discloses a face cream containing the composition. The invention also discloses application of the composition in preparation of cosmetics for skin whitening, spot fading and skin yellowing reduction. The composition provided by the invention establishes a multi-target synergistic pathway: 1, a blackness removal pathway for reducing the activation of oxidative stress such as ultraviolet rays on melanocytes; and 2, a jaundice removal pathway: inhibiting lipid peroxidation and promoting lipofuscin removal.

Description

Technical Field

[0001] This invention belongs to the field of cosmetics and topical skin preparations, specifically relating to a composition with whitening effects and its application. Background Technology

[0002] The ideal skin tone is not only about being "white," but also about being "even, bright, and clear." Current skin pigmentation problems mainly fall into two categories: one is "darkness" caused by excessive melanin production or uneven distribution, such as age spots and dullness; the other is "yellowness" caused by the accumulation of advanced glycation end products (AGEs), carotenemia, and especially the long-term deposition of lipofuscin in the skin, manifesting as a sallow complexion and lack of luster. Lipofuscin is a non-degradable fluorescent pigment particle formed by lipid peroxidation and protein cross-linking. It accumulates in cells with age and is a significant intrinsic factor in skin yellowing.

[0003] Most existing skin-whitening products focus on inhibiting tyrosinase activity to reduce melanin production, commonly using ingredients such as arbutin and niacinamide. However, their effectiveness is limited for skin yellowing caused by lipofuscin deposition. A few studies targeting anti-glycation or anti-oxidation to improve skin tone often operate separately from melanin regulation pathways, lacking a synergistic solution for both "dark" and "yellow" skin issues. Furthermore, while highly effective active ingredients like 4-butylresorcinol have strong whitening power, they may be irritating; and lipofuscin removal requires a robust lipid-phase antioxidant system. Summary of the Invention

[0004] The purpose of this invention is to overcome the shortcomings of existing technologies and provide a composition with whitening effects and its application. This composition, through the scientific compounding of a specific oil matrix and low-concentration, highly active ingredients, achieves dual inhibition and removal of melanin production and lipofuscin deposition, and exhibits good skin compatibility.

[0005] To achieve the above objectives, the present invention adopts the following technical solution:

[0006] In a first aspect, the present invention provides a composition having whitening effects, comprising the following components in parts by weight: 47-51 parts grape seed oil, 47-51 parts pomegranate seed oil, 0.5-0.8 parts 4-butylresorcinol, 0.2-0.6 parts VC-IP, and 0.1-10 parts isorhamnetin-3-O-neohesperidin.

[0007] According to a preferred embodiment of the present invention, the composition comprises the following components in parts by weight: 48-50 parts grape seed oil, 48-50 parts pomegranate seed oil, 0.6-0.8 parts 4-butylresorcinol, 0.2-0.4 parts VC-IP, and 0.1-5 parts isorhamnetin-3-O-neohesperidin.

[0008] Preferably, the composition comprises the following components in parts by weight: 49 parts grape seed oil, 49 parts pomegranate seed oil, 0.8 parts 4-butylresorcinol, 0.2 parts VC-IP, and 1 part isorhamnetin-3-O-neohesperidin.

[0009] A second aspect of the present invention provides a method for preparing the composition as described above, comprising the following steps:

[0010] (1) Mix grape seed oil and pomegranate seed oil, heat to 35~40℃, and stir until well mixed;

[0011] (2) Maintain the temperature, switch to homogenization mode, and add 4-butylresorcinol, VC-IP and isorhamnetin-3-O-neohesperidin in sequence. After each ingredient is added, keep stirring until completely dissolved and dispersed.

[0012] A third aspect of the invention provides an essential oil comprising the composition described above.

[0013] According to a preferred embodiment of the present invention, the essential oil comprises the following components in parts by weight: 49 parts grape seed oil, 49 parts pomegranate seed oil, 0.8 parts 4-butylresorcinol, 0.2 parts VC-IP, 1 part isorhamnetin-3-O-neohesperidin, 1 part tocopheryl acetate, 59 parts squalane, and 40 parts jojoba seed oil.

[0014] A fourth aspect of the invention provides a face cream comprising the composition described above.

[0015] According to a preferred embodiment of the present invention, the face cream comprises an A-phase oil phase, a B-phase aqueous phase, a C-phase active ingredient phase, and a D-phase preservative phase;

[0016] Phase A comprises 49 parts grape seed oil, 49 parts pomegranate seed oil, 16 parts shea butter, 13 parts cetearyl alcohol, 0.2 parts VC-IP, and 0.65 parts tocopherol.

[0017] Phase B comprises 16 parts glycerin, 0.3 parts sodium hyaluronate, 0.65 parts xanthan gum, and 49 parts deionized water;

[0018] The C phase comprises 0.8 parts of 4-butylresorcinol and 1 part of isorhamnetin-3-O-neohesperidin;

[0019] Phase D comprises 3 parts of phenoxyethanol.

[0020] A fifth aspect of the invention provides the use of the composition described above in the preparation of cosmetics for skin whitening, fading pigmentation, and reducing skin yellowing.

[0021] The beneficial effects of this invention are as follows:

[0022] 1. The lipid base of the composition is formed by a high proportion of grape seed oil and pomegranate seed oil. They not only carry the active ingredients, but their own powerful lipid-phase antioxidant network provides a basic environment for resisting the formation of lipofuscin and ensures the gentleness and moisturizing properties of the formula.

[0023] 2. The three highly active ingredients (4-butylresorcinol, VC-IP, and isorhamnetin-3-O-neohesperidin) are controlled at low concentrations. This significantly reduces the risk of irritation in the formulation. Furthermore, in the specific oil matrix, the permeability and bioavailability of these ingredients are enhanced, allowing them to synergize with the oil matrix and achieve "low concentration, high efficiency".

[0024] 3. A multi-target synergistic pathway was established: first, the de-melanin pathway: reducing the activation of melanocytes by oxidative stress such as ultraviolet radiation; second, the de-yellowing pathway: inhibiting lipid peroxidation and promoting the clearance of lipofuscin. Detailed Implementation

[0025] The present invention will be described in detail below with reference to specific embodiments. It should be understood that these embodiments are for illustrative purposes only and are not intended to limit the scope of the invention.

[0026] Unless otherwise specified, the experimental methods used in the following examples are conventional methods. Unless otherwise specified, the materials and reagents used in the following examples are all available through conventional commercial channels.

[0027] The VC-IP mentioned in the following examples is ascorbate tetraisopalmitate.

[0028] Example 1: Preparation of compositions in different proportions

[0029] This embodiment provides the composition and preparation method of seven different proportions of the composition, and the specific composition is shown in Table 1.

[0030] Table 1. Composition of the composition described in Example 1 (by parts by mass)

[0031]

[0032] Preparation process:

[0033] 1. Under light-protected conditions, add the prescribed amounts of grape seed oil and pomegranate seed oil to the main mixing tank, turn on the stirrer (stirring speed 300 rpm) and heat to 38°C. Stir at this temperature for 15 minutes to ensure that the oils are completely mixed and the system is homogeneous.

[0034] 2. Maintain the temperature at 38℃ and switch the stirring to homogenization mode (homogenization rate 1000 rpm). Slowly add the formulated amounts of 4-butylresorcinol, VC-IP, and isorhamnetin-3-O-neohesperidin in sequence. After adding each active ingredient, maintain homogenization stirring for 8 minutes to ensure complete dissolution and uniform dispersion before adding the next one.

[0035] 3. After all active ingredients have been added, continue homogenizing and stirring at 1000 rpm for 15 minutes. Then, while continuing to stir (300 rpm), cool the system at a rate of approximately 1.5°C / minute using cooling water circulation until the temperature drops to 28°C.

[0036] 4. The obtained composition is filtered through a polytetrafluoroethylene (PTFE) filter membrane with a pore size of 0.45 μm. The collected filtrate is the clear and transparent target composition.

[0037] Example 2: Dual-Effect Anti-Aging Essence Oil

[0038] This embodiment provides a dual-effect anti-aging essence oil formula and its preparation process.

[0039] Formula (by weight):

[0040] 49 parts grape seed oil, 49 parts pomegranate seed oil, 0.8 parts 4-butylresorcinol, 0.2 parts VC-IP, 1 part isorhamnetin-3-O-neohesperidin, 1 part tocopheryl acetate (antioxidant), 59 parts squalane, and 40 parts jojoba seed oil.

[0041] The specific preparation process is as follows:

[0042] 1. Under light-protected conditions, add all oil-soluble components (grape seed oil, pomegranate seed oil, squalane, jojoba seed oil) to the main mixing tank, stir at 250 rpm and heat to 40°C, maintain for 20 minutes to ensure complete mixing.

[0043] 2. While maintaining a temperature of 40°C and a stirring speed of 250 rpm, add 4-butylresorcinol, VC-IP, isorhamnetin-3-O-neohesperidin and tocopheryl acetate in sequence. Stir for 5 minutes after each ingredient is added until completely dissolved.

[0044] 3. After all the ingredients have been added, cool the system to 25°C at a rate of 1°C / min, and then stir at 400 rpm for 10 minutes at this temperature to homogenize it.

[0045] 4. Finally, the product is filtered through a 0.45 μm PTFE membrane, filled with nitrogen, and then the dual-effect anti-aging essence oil is obtained.

[0046] Example 3: Dual-Effect Repairing Face Cream

[0047] This invention provides a formula and preparation process for a dual-effect repair face cream.

[0048] Formula (including phases A, B, C, and D, with specific component proportions listed in parts by mass):

[0049] Phase A (oil phase): 49 parts grape seed oil, 49 parts pomegranate seed oil, 16 parts shea butter, 13 parts cetearyl alcohol, 0.2 parts VC-IP, and 0.65 parts tocopherol.

[0050] Phase B (aqueous phase): 16 parts glycerin, 0.3 parts sodium hyaluronate, 0.65 parts xanthan gum, and 49 parts deionized water.

[0051] Phase C (active phase): 0.8 parts of 4-butylresorcinol (pre-dissolved in a small amount of propylene glycol) and 1 part of isorhamnetin-3-O-neohesperidin (pre-dissolved in a small amount of ethanol).

[0052] Phase D: Phenoxyethanol: 3 parts.

[0053] The specific preparation process is as follows:

[0054] 1. Heat phase A and phase B to 78°C respectively, and stir until completely homogeneous.

[0055] 2. Under high-speed homogenization (2000 rpm), slowly add phase A to phase B and homogenize for 5 minutes to form a uniform emulsion.

[0056] 3. Turn on the stirring (300 rpm) to cool the emulsion. When the temperature drops below 45°C, add the pre-dispersed C phase component.

[0057] 4. Continue stirring until 38°C, add phase D preservative, adjust pH to 5.8, homogenize at 2000 rpm for 2 minutes, and then discharge to obtain the dual-effect repair cream.

[0058] Example 4: Tyrosinase Inhibition Activity Test

[0059] In this embodiment, the tyrosinase dopa rate oxidation method was used to test the tyrosinase inhibitory activity of different samples to verify the "blackening" efficacy and synergistic effect of the composition.

[0060] The specific testing method is as follows:

[0061] In a 96-well plate, 140 µL of 0.1 M phosphate buffer (pH 6.8), 20 µL of the test sample solution, and 20 µL of mushroom tyrosinase solution (50 U / mL) were added sequentially, and the plate was incubated at 37 °C for 10 minutes. Then, 20 µL of 2 mM L-DOPA solution was added to initiate the reaction. The plate was immediately placed in a multi-microplate reader, and the absorbance was continuously monitored over time at 475 nm. The slope of the initial linear phase of the reaction was recorded. The reaction system without the sample served as a blank control, and the background of the sample was subtracted from the enzyme-free system. The tyrosinase inhibition rate was calculated using the following formula:

[0062] Inhibition rate (%) = [1 - (slope of sample group / slope of blank control group)] × 100%.

[0063] Theoretical summation inhibition rate (%) = Inhibition rate of blank carrier oil matrix (grape seed oil + pomegranate seed oil) + Inhibition rate of 4-butylresorcinol + Inhibition rate of VC-IP + Inhibition rate of isorhamnetin-3-O-neohesperidin.

[0064] By testing samples of different concentrations, their half-maximal inhibitory concentration (IC50) can be calculated. 50 ).

[0065] The test samples were: Examples 1-1 to 1-7, Example 2, Example 3, and as comparisons, single components, binary combinations, blank matrix (grape seed oil + pomegranate seed oil) and positive control (kojic acid).

[0066] Table 2. Inhibitory effect of each test sample on tyrosinase activity

[0067]

[0068] The positive control was kojic acid dissolved in the blank carrier oil matrix of sample number 8, with a kojic acid concentration of 0.1%.

[0069] As shown in Table 2, the compositions of the present invention (especially Examples 1-4) exhibited an inhibition rate of up to 88.2% against tyrosinase, significantly higher than the theoretical summation of any single component, binary combination, and components and matrix (approximately 71.6%). This clearly demonstrates that the three active ingredients—4-butylresorcinol, VC-IP, and isorhamnetin-3-O-neohesperidin—exhibited a significant synergistic effect in a specific oil matrix, rather than a simple additive effect.

[0070] Example 5: Lipofuscin model clearance ability test

[0071] This experiment used an in vitro human skin fibroblast (HFF-1) UVA-induced aging model to evaluate the ability of different samples to clear intracellular lipofuscin-like fluorescent substances, in order to verify the "de-yellowing" efficacy and synergistic effect of the composition.

[0072] Test Method: HFF-1 cells were seeded in culture plates and repeatedly irradiated with UVA (wavelength 365 nm, irradiation dose 2 J / cm²) to induce the deposition of intracellular lipofuscin-like fluorescent substances. Subsequently, the culture medium was replaced with fresh medium containing different concentrations of the test sample (appropriately dispersed in cell culture medium), and cultured for another 48 hours. After cell collection and lysis, the fluorescence intensity of the lysate was measured using a fluorescence spectrophotometer at specific excitation / emission wavelengths (Ex / Em = 340 / 440 nm). Untreated normal cells served as a blank control, and model cells irradiated only with UVA served as a negative control. The clearance rate of the lipofuscin-like fluorescent substances was calculated using the following formula:

[0073] Sweep rate (%) = [(Model group fluorescence value - Sample group fluorescence value) / (Model group fluorescence value - Blank group fluorescence value)] × 100%.

[0074] Theoretical summation clearance rate (%) = clearance rate of blank carrier oil matrix (grape seed oil + pomegranate seed oil) + clearance rate of 4-butylresorcinol + clearance rate of VC-IP + clearance rate of isorhamnetin-3-O-neohesperidin.

[0075] The test samples were: Examples 1-1 to 1-7, Example 2, Example 3, and single components, binary combinations, blank matrix and positive control as comparisons.

[0076] Table 3. Scavenging effect of each test sample on intracellular lipofuscin-like fluorescent substances

[0077] Note: The total weight of all samples was 0.1 mg, and the cell concentration was 0.01 mg / mL. For samples 2-10, cell culture medium was used to replenish the sample to 0.1 mg. The positive control was kojic acid dissolved in the blank carrier oil matrix of sample 8, with a kojic acid concentration of 0.1%.

[0078] As shown in Table 3, the compositions of the present invention (especially Examples 1-4) achieved a clearance rate of up to 52.3% for intracellular lipofuscin-like fluorescent substances, which is significantly better than that of the carrier matrix alone, any single component, and binary combinations, and also better than the theoretical sum of the individual components and the matrix (approximately 48.3%). This demonstrates a clear synergistic enhancement effect among the components in clearing lipofuscin, a key pigment causing skin "yellowing".

[0079] Example 6: Evaluation of Human Efficacy

[0080] This experimental example verifies the actual efficacy and safety of the composition of the present invention in specific products (essence oil and face cream) through a 12-week clinical trial.

[0081] Test products: Example 2 (Dual-Effect Anti-Aging Essence Oil) and Example 3 (Dual-Effect Repair Cream).

[0082] Testing period: 12 weeks.

[0083] Test subjects: 70 healthy Asian female volunteers aged 35-55 with visible age spots and dull skin tone. They were randomly divided into two groups of 35 each, with one group using a facial oil and the other a face cream.

[0084] Test method: In a constant temperature and humidity environment (temperature approximately 22℃, relative humidity approximately 50%), quantitative detection was performed at weeks 0 (baseline), 4, 8 and 12 using the VISIA-CR complex image analysis system and a skin colorimeter (measuring ITA° values), and self-assessment questionnaires were collected from the subjects.

[0085] Table 4. Objective instrument measurement results (12-week mean change)

[0086]

[0087] Note: The effectiveness rate is defined as the percentage of subjects whose parameter improves by more than 10%.

[0088] Table 5. Results of the participants' self-assessment questionnaire (Week 12)

[0089]

[0090] Table 6 Skin Tolerance and Safety Records

[0091]

[0092] According to Tables 4, 5, and 6:

[0093] Dual efficacy verification: Both dosage forms of the product showed significant dual efficacy of "removing dark spots" (significantly reducing UV and brown spots) and "removing yellow spots / brightening" (increasing ITA° value and improving the a* / b* ratio), with objective data and subjective feelings being highly consistent.

[0094] Differences in formulation: Facial oils have a slight advantage in reducing dark spots (UV spots) and improving radiance, possibly due to the oil matrix promoting the penetration of active ingredients; face creams receive higher subjective praise for improving skin texture and moisturizing.

[0095] Safety and Tolerability: All active ingredients, at extremely low concentrations, combined with a high proportion of plant oils, demonstrate excellent safety, with no reports of serious adverse reactions, making it suitable for long-term use.

[0096] The above human efficacy data strongly support the use of the composition in "preparing skin whitening, fading pigmentation, and / or reducing skin yellowing", and in particular, verify its effectiveness in addressing lipofuscin-related yellowing problems.

[0097] This invention provides an innovative plant-derived composition that uses a high proportion of grape seed oil and pomegranate seed oil as functional matrices, scientifically combined with ultra-low concentrations of 4-butylresorcinol, VC-IP, and isorhamnetin-3-O-neohesperidin, creatively constructing a dual-effect pathway that simultaneously targets melanin and lipofuscin. This composition not only achieves highly efficient synergy, resulting in excellent effects in removing dark spots and yellowing skin, but also significantly enhances the safety and gentleness of the formulation due to the extremely low concentration of highly active ingredients and the synergistic effect of oil encapsulation, making it suitable for the development of various skincare product formulations.

[0098] The above description is merely a preferred embodiment for explaining the present invention and is not intended to limit the present invention in any way. Therefore, any modifications or changes made to the present invention under the same inventive spirit should still be included within the scope of protection intended by the present invention.

Claims

1. A composition having whitening efficacy, characterized by, The composition comprises the following components by mass: grape seed oil 47-51 parts, pomegranate seed oil 47-51 parts, 4-butylresorcinol 0.5-0.8 parts, VC-IP 0.2-0.6 parts, and isorhamnetin-3-O-neohesperidoside 0.1-10 parts.

2. The composition of claim 1, wherein, The composition comprises the following components by mass: grape seed oil 48-50 parts, pomegranate seed oil 48-50 parts, 4-butylresorcinol 0.6-0.8 parts, VC-IP 0.2-0.4 parts, and isorhamnetin-3-O-neohesperidoside 0.1-5 parts.

3. The composition of claim 1, wherein, The composition comprises the following components by mass: grape seed oil 49 parts, pomegranate seed oil 49 parts, 4-butylresorcinol 0.8 parts, VC-IP 0.2 parts, and isorhamnetin-3-O-neohesperidoside 1 part.

4. A process for the preparation of a composition according to any one of claims 1 to 3, characterised in that, The method comprises the following steps: (1) Mix grape seed oil and pomegranate seed oil, and heat to 35-40°C, and stir to mix evenly; (2) Maintain the temperature, switch to the homogenization mode, and sequentially add 4-butylresorcinol, VC-IP, and isorhamnetin-3-O-neohesperidoside, and maintain stirring after adding each component until complete dissolution and dispersion.

5. An essential oil characterized in that, The composition comprises the following components by mass: grape seed oil 49 parts, pomegranate seed oil 49 parts, 4-butylresorcinol 0.8 parts, VC-IP 0.2 parts, and isorhamnetin-3-O-neohesperidoside 1 part.

6. The serum oil of claim 5, wherein, The composition comprises the following components by mass: grape seed oil 49 parts, pomegranate seed oil 49 parts, 4-butylresorcinol 0.8 parts, VC-IP 0.2 parts, and isorhamnetin-3-O-neohesperidoside 1 part.

7. A face cream characterized in that, The cream comprises an A-phase oil phase, a B-phase water phase, a C-phase active substance phase, and a D-phase preservative phase; 8. The face cream according to claim 7, characterized in that, The A-phase comprises grape seed oil 49 parts, pomegranate seed oil 49 parts, shea butter 16 parts, cetylstearyl alcohol 13 parts, VC-IP 0.2 parts, and tocopherol 0.65 parts; The B-phase comprises glycerol 16 parts, sodium hyaluronate 0.3 parts, xanthan gum 0.65 parts, and deionized water 49 parts; the C-phase comprises 4-butylresorcinol 0.8 parts and isorhamnetin-3-O-neohesperidoside 1 part; The D-phase comprises phenoxyethanol 3 parts.

9. Use of the composition of any one of claims 1-3 in the preparation of a cosmetic product for skin whitening, spot lightening, and reduction of skin yellowing. ​

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