A composition with whitening efficacy and application thereof

Abstract

The application discloses a composition with whitening effect, which comprises the following components in mass fraction: 47-51 parts of grape seed oil, 47-51 parts of pomegranate seed oil, 0.5-0.8 parts of 4-butyl resorcinol, 0.2-0.6 parts of VC-IP and 0.1-10 parts of isorhamnetin-3-O-neohesperidoside. The application further discloses a preparation method of the composition. The application further discloses an essence oil containing the composition, and a cream containing the composition. The application further discloses application of the composition in preparation of cosmetics for skin whitening, freckle lightening and skin yellowing reduction. The composition establishes multiple target point synergistic pathways: one is a black removal pathway, which reduces activation of melanocytes under oxidative stress such as ultraviolet rays; and the other is a yellow removal pathway, which inhibits lipid peroxidation and promotes lipofuscin clearance.

Description

TECHNICAL FIELD

[0001] The present application belongs to the technical field of cosmetics and skin external preparation, and particularly relates to a composition with whitening effect and application thereof. BACKGROUND

[0002] The standard of ideal skin color is not only "white", but also "uniform, bright and clean". Current skin pigment problems mainly fall into two categories: one is "black" caused by excessive production or uneven distribution of melanin, such as freckles and dullness; the other is "yellow" caused by accumulation of advanced glycation end products (AGEs), carotenemia and especially lipofuscin in the skin, which is manifested as yellowish skin and lack of luster. Lipofuscin is a non-degradable fluorescent pigment particle formed by lipid peroxidation and protein cross-linking, which accumulates in cells with age and is an important internal factor for skin yellowing.

[0003] Most of the existing whitening products focus on inhibiting tyrosinase activity to reduce melanin production, and common ingredients such as arbutin and niacinamide are used, but the effect on skin yellowing caused by lipofuscin deposition is limited. A few studies on anti-glycation or anti-oxidation to improve skin color are also often separated from the melanin regulation path, and there is a lack of a synergistic solution to the "black" and "yellow" problems. At the same time, high-efficiency active ingredients such as 4-butylresorcinol have strong whitening effect, but may be accompanied by irritation; and lipofuscin removal requires a strong lipid-phase antioxidant system. SUMMARY

[0004] The present application aims to overcome the deficiencies in the prior art and provide a composition with whitening effect and application thereof. The composition realizes dual inhibition and removal of melanin production and lipofuscin deposition by scientific compounding of a specific oil matrix and low-concentration high-activity ingredients, and has good skin compatibility.

[0005] To achieve the above-mentioned purpose, the present application adopts the following technical solutions:

[0006] In a first aspect, the present application provides a composition with whitening effect, comprising the following components in mass parts: 47-51 parts of grape seed oil, 47-51 parts of pomegranate seed oil, 0.5-0.8 parts of 4-butylresorcinol, 0.2-0.6 parts of VC-IP, and 0.1-10 parts of isorhamnetin-3-O-neohesperidoside.

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

[0008] Preferably, the composition comprises the following components by mass fraction: 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.

[0009] In a second aspect of the present application, a method for preparing the composition as described above is provided, comprising the following steps:

[0010] (1) Mix grape seed oil and pomegranate seed oil, heat to 35-40℃, and stir to mix evenly;

[0011] (2) Maintain the temperature, switch to homogenization mode, and sequentially add 4-butylresorcinol, VC-IP, and isorhamnetin-3-O-neohesperidoside, and maintain stirring until complete dissolution and dispersion after adding each component.

[0012] In a third aspect of the present application, an essence oil is provided, comprising the composition as described above.

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

[0014] In a fourth aspect of the present application, a cream is provided, comprising the composition as described above.

[0015] According to a preferred embodiment of the present application, 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.

[0016] 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.

[0017] The B-phase comprises glycerol 16 parts, sodium hyaluronate 0.3 parts, xanthan gum 0.65 parts, and deionized water 49 parts.

[0018] The C-phase comprises 4-butylresorcinol 0.8 parts and isorhamnetin-3-O-neohesperidoside 1 part.

[0019] The D-phase comprises phenoxyethanol 3 parts.

[0020] In a fifth aspect of the present application, the use of the composition as described above in the preparation of a cosmetic product for skin whitening, spot lightening, and reduction of skin yellowing is provided.

[0021] The beneficial effects of the present application are as follows:

[0022] 1. High proportion of grape seed oil and pomegranate seed oil are used as the lipid base of the composition. They are not only the carriers of the active ingredients, but also provide a strong lipid phase antioxidant network to resist the formation of lipofuscin and ensure the mildness and moisturizing properties of the formula.

[0023] 2. Three high-activity ingredients (4-butylresorcinol, VC-IP, and isorhamnetin-3-O-neohesperidoside) are controlled at low concentrations. On the one hand, this greatly reduces the risk of irritation of the formula, and on the other hand, in the specific oil matrix, the permeability and bioavailability of these ingredients are improved, and they can synergize with the oil matrix to achieve "low concentration, high efficiency".

[0024] 3. A multi-target synergistic pathway is established: one is the melanin removal pathway, which reduces the activation of melanocytes by oxidative stress such as ultraviolet light; the other is the yellow removal pathway, which inhibits lipid peroxidation and promotes the removal of lipofuscin. DETAILED DESCRIPTION

[0025] The technology of the present application is described in detail below in conjunction with specific embodiments. It should be understood that these embodiments are only used to illustrate the present application and not to limit the scope of the present application.

[0026] The experimental methods used in the following examples are conventional methods unless otherwise specified. The materials, reagents, etc. used in the following examples can be obtained through conventional commercial channels unless otherwise specified.

[0027] VC-IP appearing in the following examples is ascorbic acid tetraisopalmitate.

[0028] Example 1, Different Proportion Composition Configuration

[0029] This example provides the composition and preparation method of seven groups of different proportion compositions, and the specific composition is shown in Table 1.

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

[0031]

[0032] Preparation process:

[0033] 1. Under light-proof conditions, the formula amount of grape seed oil and pomegranate seed oil is added to the main mixing tank, the stirring is started (stirring rate 300 rpm) and heated to 38℃, and stirred at this temperature for 15 minutes to make the oil completely miscible and the system uniform.

[0034] 2. Keep the temperature at 38 °C, switch the stirring to homogenizing mode (homogenizing speed 1000 rpm). Slowly add the formula amount of 4-Butylresorcinol, VC-IP and Iso-rhamnetin-3-O-neohesperidoside one by one. After each active ingredient is added, maintain the homogenizing stirring for 8 minutes to ensure it is completely dissolved and dispersed evenly before adding the next one.

[0035] 3. After all the active ingredients are added, continue to homogenize stirring at 1000 rpm for 15 minutes. Then, under continuous stirring (300 rpm), cool the system at a rate of about 1.5 °C / min by circulating cooling water until the temperature drops to 28 °C.

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

[0037] Example 2, Double-Effect Anti-aging Essence Oil

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

[0039] Formula (in parts by mass):

[0040] 49 parts of grape seed oil, 49 parts of pomegranate seed oil, 0.8 parts of 4-Butylresorcinol, 0.2 parts of VC-IP, 1 part of Iso-rhamnetin-3-O-neohesperidoside, 1 part of tocopheryl acetate (antioxidant), 59 parts of squalane, 40 parts of jojoba seed oil.

[0041] The specific preparation process is as follows:

[0042] 1. Under light-proof conditions, add all the oil-soluble ingredients (grape seed oil, pomegranate seed oil, squalane, jojoba seed oil) to the main preparation tank, stir at 250 rpm and heat to 40 °C, maintain for 20 minutes to completely dissolve.

[0043] 2. Keep 40 °C and 250 rpm stirring, add 4-Butylresorcinol, VC-IP, Iso-rhamnetin-3-O-neohesperidoside and tocopheryl acetate one by one, stir for 5 minutes after each ingredient is added to completely dissolve.

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

[0045] 4. Finally, filter through a 0.45 μm PTFE filter membrane, fill with nitrogen, and the double-effect anti-aging essence oil is obtained.

[0046] Example 3, Double-Effect Repairing Cream

[0047] The application provides a formula of a double-effect repair cream and a preparation process thereof.

[0048] The formula (including phase A, phase B, phase C, phase D, and specific component proportion is recorded in mass parts) is as follows:

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

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

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

[0052] Phase D: phenoxyethanol: 3 parts.

[0053] The specific preparation process is as follows:

[0054] 1. Phase A and phase B are heated to 78℃ respectively, and stirred until completely uniform.

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

[0056] 3. Start stirring (300 rpm) to cool the emulsion, and when the temperature is reduced to below 45℃, add the pre-dispersed C phase ingredients.

[0057] 4. Continue stirring to 38℃, add the D phase preservative, adjust the pH to 5.8, and homogenize at 2000 rpm for 2 minutes before discharging, to obtain the double-effect repair cream.

[0058] Example 4, tyrosinase inhibition activity test

[0059] In this example, the tyrosinase inhibition activity of different samples is tested by the tyrosinase dopamine rate oxidation method to verify the "black removal" effect and synergy of the composition.

[0060] The specific test method is as follows:

[0061] In 96-well plates, 140 μL of 0.1 M phosphate buffer (pH 6.8), 20 μL of sample solution to be tested, and 20 μL of mushroom tyrosinase solution (50 U / mL) were sequentially added, and incubated at 37°C for 10 minutes; then 20 μL of 2 mM L-DOPA solution was added to start the reaction, and immediately placed in a multifunctional microplate reader to continuously monitor the change in absorbance with time at a wavelength of 475 nm, and the slope of the initial linear phase of the reaction was recorded. The reaction system without sample was used as a blank control, and the system without enzyme was subtracted from the sample itself. The tyrosinase inhibition rate was calculated according to the following formula:

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

[0063] Theoretical additive 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-neohesperidoside.

[0064] By testing different concentrations of samples, the half-inhibitory concentration (IC 50 ).

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

[0066] Table 2 Inhibition 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 No. 8 at a concentration of 0.1%.

[0069] As shown in Table 2, the inhibition rate of the composition of the present application (particularly Example 1-4) on tyrosinase was as high as 88.2%, which was significantly higher than that of any single component, binary combination, and the theoretical additive value of each component and the matrix (about 71.6%). This clearly demonstrates that the three active ingredients of 4-butylresorcinol, VC-IP, and isorhamnetin-3-O-neohesperidoside produce significant synergistic effects in a specific oil matrix, rather than simply adding up.

[0070] Example 5, Lipofuscin model clearance ability test

[0071] The present experimental example adopts an in vitro human skin fibroblast (HFF-1) UVA-induced aging model to evaluate the ability of different samples to remove intracellular lipofuscin-like fluorescent substances, thereby verifying the "anti-yellowing" efficacy and synergy 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 fluorescent substances. Subsequently, fresh medium containing different concentrations of the sample to be tested (dispersed in cell culture medium as appropriate) was added, and the cells were incubated for another 48 hours. After the cells were collected and lysed, the fluorescence intensity of the lysate was measured using a fluorescence spectrophotometer at a specific excitation / emission wavelength (Ex / Em = 340 / 440 nm). Untreated normal cells served as the blank control, and UVA-irradiated model cells served as the negative control. The clearance rate of lipofuscin-like fluorescent substances was calculated according to the following formula:

[0073] Clearance rate (%) = [(model group fluorescence value - sample group fluorescence value) / (model group fluorescence value - blank group fluorescence value)] x 100%.

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

[0075] Test samples: Examples 1-1 to 1-7, Example 2, Example 3, and single components, binary combinations, blank matrix, and positive controls as controls.

[0076] Table 3: Clearance effect of intracellular lipofuscin-like fluorescent substances by different test samples

[0077]

[0078] Note: The total weight of the sample is 0.1 mg, and the concentration of the treated cells is 0.01 mg / mL. In sample No. 2-10, the sample is supplemented with cell culture medium to 0.1 mg. The positive control is kojic acid at a concentration of 0.1% dissolved in the blank carrier oil base of sample No. 8.

[0079] As shown in Table 3, the clearance rate of intracellular lipofuscin-like fluorescent substances by the present composition (particularly Example 1-4) is as high as 52.3%, which is significantly better than the blank matrix, any single component, and binary combination alone, and is also better than the theoretical additive value (about 48.3%) of each component and the matrix. This demonstrates that there is a clear synergistic effect among the components of the present composition in removing lipofuscin, a key pigment that causes skin "yellowing".

[0080] Example 6, Human Efficacy Evaluation

[0081] This experiment example verifies the actual efficacy and safety of the composition of the present application in specific products (essence oil and cream) through a 12-week clinical test.

[0082] Test products: Example 2 (dual anti-aging essence oil) and Example 3 (dual protective cream).

[0083] Test period: 12 weeks.

[0084] Test subjects: 70 healthy Asian women volunteers aged 35-55 years old with visible facial spots and yellowish skin problems. Randomly divided into two groups, 35 people in each group, using essence oil or cream respectively.

[0085] Test method: In a constant temperature and humidity environment (temperature about 22℃, relative humidity about 50%), at 0thweek (baseline), 4thweek, 8thweek, 12thweek, quantitative detection was carried out using VISIA-CR complex image analysis system, skin colorimeter (measuring ITA° value), and self-evaluation questionnaire of the subjects was collected.

[0086] Table 4 Objective instrument measurement results (12-week mean change)

[0087]

[0088] Note: The efficiency is defined as the percentage of subjects whose parameter improvement is more than 10%.

[0089] Table 5 Results of self-evaluation questionnaire of subjects (12thweek)

[0090]

[0091] Table 6 Skin tolerance and safety records

[0092]

[0093] According to Tables 4, 5 and 6, we can know that:

[0094] Dual efficacy verification: Both products of the two dosage forms show significant "black removal" (significant reduction of UV and brown spots) and "yellow removal / lightening" (improvement of ITA° value and a* / b* ratio), and the objective data are highly consistent with subjective feelings.

[0095] Dosage form difference: Essence oil has a slight advantage in black removal (reduction of UV spots) and lightening, which may be related to the promotion of active substance penetration by oil matrix; cream gets higher subjective praise in improving skin texture and moisturizing.

[0096] Safety tolerance: all active ingredients show excellent safety at very low concentrations, with high proportion of plant oil, no serious adverse reactions reported, suitable for long-term use.

[0097] The above human efficacy data strongly support the use of the composition in "preparing a skin whitening, spot lightening, and / or reducing skin yellowing", especially verifying its effectiveness against lipofuscin-related yellowing problems.

[0098] The present application provides an innovative plant-derived composition, which creatively constructs a double-pathway targeting "melanin" and "lipofuscin" by scientifically compounding high-proportion grape seed oil and pomegranate seed oil as functional matrix with ultra-low concentrations of 4-butylresorcinol, VC-IP and isorhamnetin-3-O-neohesperidoside. The composition not only achieves excellent black and yellow removal effects through high-efficiency synergy, but also significantly improves the safety and mildness of the formula due to the ultra-low concentration of high-activity ingredients and the synergistic effect of oil wrapping, which is suitable for the development of various dosage forms of skin care products.

[0099] The above is only to explain the preferred embodiments of the present application, not intended to limit the present application in any form, so any modification or change related to the present application made under the same inventive spirit shall still be included in the scope intended to be protected by the present application.

Claims

1. A composition having whitening effects, characterized in that, The product comprises 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.

2. The composition according to claim 1, characterized in that, The product contains 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.

3. The composition according to claim 1, characterized in that, The components include the following 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.

4. A method for preparing the composition according to any one of claims 1 to 3, characterized in that, Includes the following steps: (1) Mix grape seed oil and pomegranate seed oil, heat to 35~40℃, and stir until well mixed; (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.

5. An essential oil, characterized in that, It comprises the composition according to any one of claims 1-3.

6. The essential oil according to claim 5, characterized in that, The components include the following 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.

7. A face cream, characterized in that, The composition comprises any one of claims 1 to 3.

8. The face cream according to claim 7, characterized in that, 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; 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. Phase B comprises 16 parts glycerol, 0.3 parts sodium hyaluronate, 0.65 parts xanthan gum, and 49 parts deionized water; Phase C comprises 0.8 parts 4-butylresorcinol and 1 part isorhamnetin-3-O-neohesperidin. Phase D comprises 3 parts of phenoxyethanol.

9. The use of the composition according to any one of claims 1 to 3 in the preparation of cosmetics for skin whitening, fading pigmentation, and reducing skin yellowing.

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