Composition with skin whitening and spot fading effects and skin care product thereof

Abstract

The invention relates to the field of cosmetics, and discloses a composition with skin whitening and spot fading effects and a skin care product of the composition. Kojic acid; an angelica dahurica extract; a licorice extract; a cortex moutan extract; a pearl powder extract; an octyl glucoside; a vegetable oil phase; the skin care product comprises the composition, the skin care product is cream, emulsion, essence, facial mask, water aqua or gel, preferably emulsion, and the skin care product is prepared through the following steps that an oil phase containing vegetable oil and octyl glucoside is prepared; mixing the oil phase and the water phase to form a microemulsion; the microcapsule is used as a carrier and is matched with fullerene for preparation; and adding the microcapsule into the microemulsion, and uniformly stirring. The fullerene is introduced into the composition in a microcapsule embedding form, so that a stable controlled release system is effectively constructed, the stability of the fullerene in illumination and high-temperature environments is greatly improved, and the problems of difficulty in controlled release and easiness in degradation of the fullerene in practicability are solved.

Description

Technical Field

[0001] The present invention relates to the technical field of cosmetics, and specifically relates to a composition with skin whitening and freckle-reducing effects and skin care products thereof. Background Art

[0002] In the prior art, skin care products often use ingredients such as fullerene, kojic acid, and arbutin to improve skin color and reduce melanin deposition. Fullerene has been applied in many beauty products due to its excellent antioxidant properties, especially in the fields of anti-aging and whitening, and has become a key ingredient in many high-end formulations. Kojic acid and arbutin, as classic tyrosinase inhibitors, have been widely used in whitening products, and they improve skin pigmentation by inhibiting melanin synthesis. To enhance the effects of these ingredients, many formulations adopt forms such as lotions and serums, combining different plant extracts and other excipients in order to achieve comprehensive skin care effects. With the development of technology, some products have tried to compound fullerene and plant extracts and utilize their synergistic effects to enhance antioxidant and whitening effects.

[0003] However, there are still some problems in the prior art that restrict the further improvement of its effects. Although fullerene has strong antioxidant effects, due to its poor water solubility and susceptibility to light and heat, conventional dispersion methods are difficult to ensure its stability and sustained release on the skin. In addition, traditional emulsification techniques often use low-energy emulsification methods, which are difficult to effectively control the particle size distribution, resulting in unstable emulsion structures and prone to precipitation or stratification, affecting the user experience. For whitening ingredient formulations, a single tyrosinase inhibitor often cannot provide continuous effects, and although the compounding of plant extracts has certain effects, its permeability and bioavailability are relatively low, and the deep delivery of active ingredients cannot be achieved. Therefore, there is still room for improvement in the prior art in terms of stability, permeability, and effect persistence. Summary of the Invention

[0004] In view of the deficiencies of the prior art, the present invention provides a composition with skin whitening and freckle-reducing effects and skin care products thereof, solving the problems of insufficient stability, permeability, and effect persistence of fullerene and whitening ingredients in existing skin care formulations.

[0005] To achieve the above objectives, the present invention is realized through the following technical solutions: A composition with skin whitening and freckle-reducing effects, comprising the following component materials in parts by mass:

[0006] Fullerene: 0.1 - 2 parts;

[0007] Kojic acid: 0.1 - 1 part;

[0008] Angelica dahurica extract: 1 - 2 parts;

[0009] Licorice extract: 0.5 - 2 parts;

[0010] Moutan cortex extract: 0.3 - 1 part;

[0011] Pearl powder extract: 0.5 - 1 part;

[0012] Octyl glucoside: 0.5 - 2 parts;

[0013] Vegetable oil phase: 5 - 15 parts;

[0014] Microcapsules: 0.1 - 2 parts;

[0015] Furthermore, as a free radical scavenger, fullerene is added in a proportion of 0.1 - 2 parts, and its role in skin antioxidant and reducing melanin formation has been widely verified. In the present invention, fullerene is encapsulated in the form of microcapsules, significantly enhancing its stability in the water - oil system and improving its active release behavior on the skin surface through a sustained - release manner. This structural design not only reduces the photosensitivity problem of fullerene but also improves its efficiency in penetrating the stratum corneum;

[0016] As a commonly used tyrosinase inhibitor, kojic acid is added in a proportion of 0.1 - 1 part. Its main function is to interfere with the tyrosine oxidation reaction in the process of melanin synthesis, inhibiting melanin production from the source. The synergistic antioxidant mechanism of kojic acid and fullerene can act on different nodes of the melanin production pathway, achieving a more comprehensive whitening effect;

[0017] The active ingredients of Angelica dahurica extract include angelicol, angelicoside and volatile oil, with a mass ratio of 2 - 3:1 - 2:1 - 2. This extract is widely used in traditional Chinese medicine for skin color conditioning and improving blood circulation, and its components have been confirmed to have multiple effects such as anti - inflammation and promoting cell renewal in modern research. Especially the volatile oil part has a mild penetration effect, which helps the absorption of other active ingredients, providing a penetration - promoting platform for the compound formula;

[0018] Licorice extract contains glycyrrhizic acid, liquiritin and licorice flavonoids, with a mass ratio of 3 - 4:2 - 3:1 - 2. Glycyrrhizic acid has excellent soothing and anti - allergic abilities for the skin, liquiritin has anti - inflammatory effects, and licorice flavonoids have whitening and antioxidant functions. The three cooperate with each other to form a composite mechanism that can not only regulate the immune response but also participate in the reduction and metabolism of melanin, improving the balance of the overall skin metabolic environment;

[0019] The paeonol, paeoniflorin and polysaccharides in the Moutan cortex extract, with a mass ratio of 2 - 3:1 - 2:1 - 2, have good anti - inflammatory, antioxidant and blood - circulation - promoting effects. As a small - molecule structure, paeonol can quickly penetrate the skin barrier, activating microcirculation and promoting pigment metabolism, while paeoniflorin and polysaccharides form an anti - inflammatory sustained - release system, reducing skin dullness and pigmentation caused by environmental stress;

[0020] The pearl powder extract includes pearl amino acids, pearl polysaccharides and calcium, and the mass ratio is 2 - 3:1 - 2:1 - 2. Pearl amino acids have good skin affinity and can promote the repair of the stratum corneum; pearl polysaccharides have moisturizing and barrier repair effects; calcium ions play an important regulatory function in the process of epidermal differentiation. The three work together to contribute to skin regeneration and even skin tone;

[0021] The above components are introduced into the system with octyl glucoside as an emulsifier, and the proportion is 0.5 - 2 parts, constructing a stable oil-in-water emulsion structure. Octyl glucoside is a non-ionic green emulsifier, with low irritation and good emulsifying ability, especially suitable for sensitive skin, ensuring the stability and uniformity of the system during long-term storage or use, and avoiding stratification or precipitation.

[0022] Preferably, the fullerene in the microcapsules exists in an embedded form, the particle size of the microcapsules is between 200 - 500 nanometers, and the microcapsule carrier is poly(lactic-co-glycolic acid).

[0023] Preferably, the Angelica dahurica extract includes angelol, angelinoside and volatile oil, and the mass ratio of angelol:angelinoside:volatile oil is 2 - 3:1 - 2:1 - 2;

[0024] The Glycyrrhiza glabra extract includes glycyrrhizic acid, liquiritin, and licorice flavonoids, and the mass ratio of glycyrrhizic acid:liquiritin:licorice flavonoids is 3 - 4:2 - 3:1 - 2.

[0025] Preferably, the Paeonia suffruticosa extract includes paeonol, paeoniflorin, and polysaccharides, and the mass ratio of paeonol:paeoniflorin:polysaccharides is 2 - 3:1 - 2:1 - 2;

[0026] The pearl powder extract includes pearl amino acids, pearl polysaccharides, and calcium, and the mass ratio of pearl amino acids:pearl polysaccharides:calcium is 2 - 3:1 - 2:1 - 2.

[0027] Application of a composition with skin whitening and freckle lightening effects in the preparation of skin care products.

[0028] A skin care product, which contains a composition with skin whitening and freckle lightening effects.

[0029] Preferably, the skin care product is a cream, emulsion, essence, mask, aqueous solution or gel, and preferably an emulsion.

[0030] Preparation method of skin care products, including the following steps:

[0031] Prepare an oil phase containing vegetable oil and octyl glucoside, and an aqueous phase containing Angelica dahurica extract, Glycyrrhiza glabra extract, Paeonia suffruticosa extract and pearl powder extract;

[0032] Use a high-shear homogenizer to mix the oil phase and the water phase to form a microemulsion;

[0033] Use the microcapsules as carriers and prepare them by an embedding technique in combination with fullerene;

[0034] Add the microcapsules into the microemulsion and stir evenly to ensure that the microcapsules are evenly dispersed in the emulsion;

[0035] Furthermore, in terms of the preparation method, first mix vegetable oil and octyl glucoside to form an oil phase, and at the same time prepare extracts of Angelica dahurica, licorice, moutan bark, and pearl powder as the water phase. Mix the oil and water phases by high-shear homogenization technology to form a microemulsion. This process not only improves the particle size uniformity of the emulsion (controlled between 50 - 200 nm), but also enhances the stability of the oil-water interface, enabling the plant active ingredients to be well dispersed, thereby improving the transport efficiency of the active substances;

[0036] In the step of embedding fullerene, use poly(lactic-co-glycolic acid) (PLGA) as the microcapsule material, dissolve fullerene in carbon tetrachloride solvent, and form an embedding structure by solvent evaporation method. This technology can form nano-microcapsules with a particle size of 200 - 500 nm, and the embedding rate reaches 90% - 95%. The application of microcapsules not only significantly improves the stability of fullerene in the system, but also makes its release in the skin more controllable, prolongs the action time, and reduces irritation;

[0037] Introduce the prepared fullerene microcapsules into the above microemulsion system and stir evenly to ensure the stable distribution of the microcapsules. This structure enables the composition to form an emulsion film with a controlled release function on the skin surface, promotes the gradual penetration of the active ingredients through the stratum corneum, and continuously exerts its efficacy in the epidermis or dermis layer, thereby achieving long-term stable effects of whitening, freckle reduction, and skin tone balance.

[0038] Preferably, the oil phase is heated to 50 - 60 °C, and after completely dissolving octyl glucoside in the vegetable oil, it is mixed with the water phase to form an emulsion;

[0039] The particle size of the microemulsion is 50 - 200 nm after being treated by a high-shear homogenizer.

[0040] Preferably, the preparation steps of the embedding technique include:

[0041] Dissolve fullerene in carbon tetrachloride solvent;

[0042] Perform solvent evaporation embedding of fullerene together with the poly(lactic-co-glycolic acid) of the microcapsules;

[0043] The embedding rate of fullerene in the microcapsules is 90% - 95%.

[0044] The present invention provides a composition with skin whitening and freckle lightening effects and skin care products containing the same.

[0045] It has the following beneficial effects:

[0046] 1. In the present invention, fullerene is introduced into the composition in the form of PLGA microcapsules, effectively constructing a stable controlled release system, which greatly improves the stability of fullerene in the presence of light and high temperature. Different from the prior art where fullerene is directly dissolved in the system, which easily leads to the inactivation of its activity, this solution significantly extends the action time of fullerene on the skin surface, solving the problems of difficult controlled release and easy degradation in the practical application of fullerene.

[0047] 2. In the present invention, high-shear homogenization and non-ionic emulsifiers cooperate to form a nano-scale microemulsion structure, constructing a skin-friendly encapsulation environment, which not only ensures the stability of the emulsion system but also improves the penetration efficiency of active ingredients. Compared with the traditional emulsification method relying only on stirring, this solution shows better performance in terms of particle size control and dispersion uniformity, overcoming the formulation problem of easy precipitation of large particles in emulsions.

[0048] 3. In the present invention, kojic acid is added to the composition and synergistically combined with fullerene and various plant extracts to form a three-dimensional action mechanism, exerting multiple effects on the path of inhibiting melanin production. Compared with the conventional idea of relying solely on kojic acid or plant extracts in existing formulations, this compounding path improves the overall freckle lightening efficiency, avoids the bottleneck of single-component action, and shows an unexpected whitening enhancement effect.

[0049] 4. In the present invention, the extracts of Angelica dahurica, Glycyrrhiza glabra, Paeonia suffruticosa, and pearl powder are compounded in a scientific ratio, and their synergistic release is enhanced through the microemulsion system, maximizing the utilization of the mildness and functional superposition of plant-derived ingredients. Different from the common problems of poor dispersion and separated effects of herbal ingredients in existing skin care products, this solution successfully realizes a composite whitening mechanism of ingredient synergy and integrated action, improving the overall bioavailability and skin feel experience of the product. BRIEF DESCRIPTION OF THE DRAWINGS

[0050] Figure 1 It is a flowchart of the preparation method steps of the skin care products of the present invention. DETAILED DESCRIPTION OF THE EMBODIMENTS

[0051] The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the accompanying drawings of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all of the embodiments. All other embodiments obtained by those of ordinary skill in the art based on the embodiments of the present invention without creative efforts shall fall within the protection scope of the present invention.

[0052] Please refer to the attached Figure 1 :

[0053] Example 1: High-content ratio plan of the composition (maximum value of the interval)

[0054] Raw material composition (parts by mass):

[0055] Fullerene: 2;

[0056] Kojic acid: 1;

[0057] Angelica dahurica extract: 2 (by angelicol: angelicinoside: volatile oil = 3:2:2);

[0058] Licorice extract: 2 (by glycyrrhizic acid: liquiritin: licorice flavonoids = 4:3:2);

[0059] Moutan cortex extract: 1 (by paeonol: paeoniflorin: polysaccharide = 3:2:2);

[0060] Pearl powder extract: 1 (by pearl amino acid: pearl polysaccharide: calcium = 3:2:2);

[0061] Octyl glucoside: 2;

[0062] Vegetable oil (jojoba oil + sweet almond oil, 1:1): 15;

[0063] Microcapsules (containing fullerene, embedded with PLGA, particle size 300 nm, embedding rate 95%): 2;

[0064] Preparation steps:

[0065] Preparation of the oil phase: Heat the vegetable oil to 60 °C and add octyl glucoside, stir until completely dissolved;

[0066] Preparation of the water phase: Dissolve the extracts of Angelica dahurica, licorice, moutan cortex, and pearl powder in deionized water at 60 °C respectively and stir evenly;

[0067] Emulsification: Slowly add the water phase to the oil phase, homogenize at 10000 rpm for 10 minutes to form a microemulsion with a particle size of about 150 nm;

[0068] Preparation of microcapsules: Dissolve fullerene in carbon tetrachloride, add the PLGA copolymer solution, and prepare microcapsules with a particle size of 300 nm by the solvent evaporation method;

[0069] Compound: Add the microcapsules to the microemulsion and stir at low speed (800 rpm) for 15 minutes;

[0070] Cooling and packaging: Cool to room temperature, adjust the pH to 5.5, and then filter and package.

[0071] Example 2: Medium ratio plan of the composition (median value of the interval)

[0072] Raw material composition (parts by mass):

[0073] Fullerene: 1;

[0074] Kojic acid: 0.5;

[0075] Angelica dahurica extract: 1.5 (bydalenol: angelicoside: volatile oil = 2.5:1.5:1.5);

[0076] Licorice extract: 1.25 (glycyrrhizic acid: liquiritin: licorice flavonoids = 3.5:2.5:1.5);

[0077] Moutan bark extract: 0.65 (paeonol: paeoniflorin: polysaccharide = 2.5:1.5:1.5);

[0078] Pearl powder extract: 0.75 (pearl amino acids: pearl polysaccharide: calcium = 2.5:1.5:1.5);

[0079] Octyl glucoside: 1.25;

[0080] Vegetable oil (coconut oil + grape seed oil, 1:1): 10;

[0081] Microcapsules (containing fullerene, embedded with PLGA, particle size 250 nm, embedding rate 93%): 1;

[0082] Preparation steps:

[0083] Preparation of oil phase: Heat the vegetable oil to 55 °C and add octyl glucoside, then stir well;

[0084] Preparation of water phase: Dissolve and mix each extract in water at 55 °C;

[0085] Emulsification: Homogenize the oil and water phases under high shear (8000 rpm) for 8 minutes to form an emulsion with a particle size of about 120 nm;

[0086] Preparation of microcapsules: Dissolve fullerene in carbon tetrachloride, mix it with PLGA copolymer, and carry out the solvent diffusion method to form microcapsules;

[0087] Compound stirring: Slowly add the microcapsules to the emulsion and stir evenly;

[0088] Final product treatment: Cool naturally, adjust the pH to 5.8, and filter and bottle.

[0089] Example 3: Low-content formulation plan of the composition (minimum value of the interval)

[0090] Raw material composition (parts by mass):

[0091] Fullerene: 0.1;

[0092] Kojic acid: 0.1;

[0093] Angelica dahurica extract: 1 (angelicol: angelicoside: volatile oil = 2:1:1);

[0094] Licorice extract: 0.5 (glycyrrhizic acid: liquiritin: licorice flavonoids = 3:2:1);

[0095] Moutan cortex extract: 0.3 (paeonol: paeonoside: polysaccharide = 2:1:1);

[0096] Pearl powder extract: 0.5 (pearl amino acids: pearl polysaccharide: calcium = 2:1:1);

[0097] Octyl glucoside: 0.5;

[0098] Vegetable oil (olive oil): 5;

[0099] Microcapsule (containing fullerene, embedded with PLGA, particle size 200 nm, embedding rate 90%): 0.1;

[0100] Preparation steps:

[0101] Preparation of oil phase: Heat olive oil to 50 °C and add octyl glucoside, stir to dissolve;

[0102] Preparation of water phase: Add each plant extract to water at 50 °C and mix evenly;

[0103] Emulsification: Homogenize the water phase and the oil phase at 6000 rpm for 6 minutes to form an emulsion with a particle size of about 100 nm;

[0104] Preparation of microcapsules: Dissolve fullerene in carbon tetrachloride and form microcapsules with PLGA copolymer by solvent evaporation method;

[0105] Combination: Add microcapsules at low speed and stir slowly for 10 minutes;

[0106] Finishing: Adjust the pH to 6.0, filter to remove impurities and then fill.

[0107] Comparative example 1:

[0108] Compared with Example 1, the difference is that fullerene microcapsules are not used, and fullerene is directly added to the system in a free state, and the rest are the same.

[0109] Comparative example 2:

[0110] Compared with Example 1, the difference is that octyl glucoside is not added, and other formulations and processing conditions remain unchanged, and the rest are the same.

[0111] Comparative example 3:

[0112] Compared with Example 1, the difference is that kojic acid is not added, and the other components and their contents remain consistent.

[0113] Comparative Example 4:

[0114] Compared with Example 1, the difference lies in that a high-shear homogenizer was not used in the oil-water mixing stage, and only magnetic stirring was used to mix the oil phase and the water phase, and the other conditions were the same.

[0115] Experiment 1:

[0116] Experiment purpose:

[0117] Verify the difference in photothermal stability of fullerene in the embedded and unembedded states in the emulsion system of the present invention, and clarify the effect of the microcapsule technology on improving its retention rate and anti-degradation ability.

[0118] Experiment materials and instruments:

[0119] Samples: emulsions obtained in Example 1 and Comparative Example 1;

[0120] Instruments: high performance liquid chromatograph (HPLC), light incubator (40 °C, stable illuminance of about 4500 LUX);

[0121] Fullerene standard, carbon tetrachloride (for dissolution), methanol (for elution);

[0122] Experiment steps:

[0123] Take 5 g of each of the two groups of samples (Example 1 and Comparative Example 1), place them in transparent glass bottles respectively, and open the bottle caps to simulate air contact.

[0124] Place the samples in the light incubator, set the temperature to 40 °C, and irradiate continuously for 7 days.

[0125] Take 0.5 g of samples every 1 day, extract the fullerene in the system with carbon tetrachloride, and centrifuge to remove the emulsion impurities.

[0126] The extract was analyzed by HPLC, the wavelength of the ultraviolet detector was set at 335 nm, the peak area was recorded and the fullerene concentration was calculated.

[0127] Calculate the retention rate of fullerene after 7 days and evaluate the degradation rate (the detailed data is shown in Table 1).

[0128] Table 1

[0129]

[0130]

[0131] Experiment summary:

[0132] As an antioxidant with a highly active double-bond structure, the molecules of fullerene are extremely prone to electron rearrangement or oxidation reactions under ultraviolet or visible light, resulting in decomposition and failure. In this invention, by embedding it in microcapsules constructed from poly(lactic-co-glycolic acid) (PLGA), a closed biodegradable barrier is formed, effectively isolating the direct effects of oxygen and light in the environment. Experimental data shows that after 7 days in Example 1, fullerene still maintains a residual amount of nearly 80%, while in Comparative Example 1, the free fullerene degrades severely, leaving only 11.5%, verifying the substantial protective effect of this structural design.

[0133] This difference mainly stems from the "dual-barrier mechanism" provided by the microcapsules in skin products: Firstly, the PLGA structure can reduce the direct contact of water with fullerene, delaying its dissolution and degradation; Secondly, the nanoparticles stably dispersed in the emulsion system further form a multi-level structure for encapsulation, enhancing the light-shielding and heat-insulating properties. This microcarrier design with controlled release and anti-degradation not only improves the stability of fullerene but also lays a foundation for its subsequent skin penetration and slow release.

[0134] In addition, the particle size control range of the microcapsules also demonstrates its distribution advantage in the experiment. Smaller and more uniform particle sizes not only facilitate the stability of the system but also mean a relatively larger surface area of the capsules, making the release curve more controllable and avoiding the irritation problems caused by the instantaneous release of fullerene. Through this experiment, it can be confirmed that the fullerene microcapsule technology of this invention achieves significantly better stability performance than the conventional free addition method in both the physical structure and functional release dimensions, providing a remarkable improvement in the safety and efficacy sustainability in actual product development.

[0135] Experiment 2:

[0136] Experiment purpose:

[0137] Evaluate the changes in the particle size distribution, system uniformity, and physical stability of the emulsion under different emulsification systems and treatment conditions, and further verify the key role of octyl glucoside and high-shear emulsification in the structure construction of this invention.

[0138] Experiment materials and instruments:

[0139] Samples: Example 1, Comparative Example 2 (without octyl glucoside);

[0140] Instrument equipment:

[0141] Laser particle size analyzer (for testing the particle size of the emulsion);

[0142] Centrifuge (for accelerating the stability test);

[0143] Centrifuge tubes, transparent glass bottles, centrifuge tube scales;

[0144] Incubator (set temperature: 25°C);

[0145] Experimental procedures:

[0146] Particle size measurement: Dilute each sample by 10 times and measure the average particle size (Z-avg) and particle size distribution range (PDI) using a laser particle size analyzer.

[0147] Accelerated centrifugation stability test:

[0148] Take 10 mL of each sample and place it in a centrifuge tube.

[0149] Centrifuge at 4000 rpm for 30 minutes.

[0150] Observe and record the height of oil-water stratification (or flocculation sedimentation), and take photos for documentation.

[0151] Initial screening of natural stability (auxiliary observation):

[0152] Leave each sample static in an environment at 25 °C for 7 days.

[0153] Record whether there are physical changes such as sedimentation, oil separation, and phase separation in the emulsion every day (detailed data are shown in Table 2).

[0154] Table 2

[0155]

[0156] Experimental summary:

[0157] It can be observed from the emulsion particle size measurement that the average particle size of Example 1 is significantly smaller than that of Comparative Example 2, and the distribution is uniform, indicating that a stable microemulsion structure is formed under the synergistic action of high shear force and non-ionic emulsifier. Octyl glucoside was not added in Comparative Example 2. Although high-shear homogenization was used, the oil phase was not thoroughly dispersed in water, resulting in large oil droplets, leading to an increase in particle size and uneven distribution, indicating that the emulsifier plays a core role in interfacial tension regulation and structure stability.

[0158] The instability of the microstructure was finally amplified and verified in the centrifugation test. Example 1 showed almost no stratification at 4000 rpm, demonstrating excellent emulsification stability; while in Comparative Example 2, different degrees of oil separation or stratification occurred, and obvious accumulation of the oil phase at the top was also observed, indicating that the system lacking an emulsifier is prone to phase separation under external disturbance, which directly affects the consistency of the finished product during storage and use.

[0159] From the perspective of the preparation process, high-shear homogenization provides the necessary energy input in the structure construction, enabling the aqueous phase and the oil phase to form a well-mixed state and be rapidly sheared into small-sized particles. Octyl glucoside forms a gentle and stable emulsifying layer at the oil-water interface, preventing the re-aggregation and coalescence of the particles. The two work together to establish a continuous and stable network of the emulsion microstructure, which is an important basis for the present invention to stably carry a variety of plant extracts and fullerene microcapsules. If any one of the conditions is missing, the network will be disrupted, resulting in emulsion instability and a decline in the user experience, indicating that the present invention has a clear and verifiable technological breakthrough in dosage form design.

[0160] Experiment 3:

[0161] Experiment purpose:

[0162] To evaluate the inhibitory effects of Example 1 and Comparative Example 3 (without kojic acid) on melanogenesis at the cellular level, so as to verify the functional necessity of kojic acid as a tyrosinase inhibitor in the formula of the present invention.

[0163] Experiment materials and equipment:

[0164] Cell line: Mouse B16 melanoma cells

[0165] Drugs and reagents: α-MSH (inducer), L-DOPA (substrate), NaOH (to dissolve melanin), MTT reagent, DMSO;

[0166] Equipment: CO2 incubator, microplate reader, 96-well cell culture plate, centrifuge, microscope;

[0167] Experiment steps:

[0168] Cell culture and treatment:

[0169] Seed B16 cells in a 96-well plate (1×10 4 cells per well) and culture for 24 hours;

[0170] Before the treatment of each group, add α-MSH (100 ng / mL) to induce melanin synthesis;

[0171] Add the sample treatment solutions: the dilution of Example 1, the dilution of Comparative Example 3 (with the same concentrations of 1%, 0.5%, 0.25%), and set up a blank group and a positive control (kojic acid alone);

[0172] Continue to culture for 72 hours.

[0173] Determination of melanin content:

[0174] Wash the cells twice with cold PBS;

[0175] Add 1M NaOH (containing 10% DMSO) to lyse cells, and incubate in a water bath at 95°C for 1 hour to release melanin;

[0176] Measure the absorbance (OD value) in an enzyme-linked immunosorbent assay (ELISA) reader at a wavelength of 405 nm, and calculate the relative content of melanin (see Table 3 for detailed data).

[0177] Cell viability control:

[0178] Simultaneously set up an MTT assay to detect cell viability to ensure that melanin inhibition is not caused by cell death.

[0179] Table 3

[0180]

[0181]

[0182] Experiment summary:

[0183] From the experimental data, it can be seen that Example 1 showed significant melanin synthesis inhibitory ability at different concentrations. Especially at a concentration of 1%, the inhibition rate exceeded 54%, which was better than the pure kojic acid group. In contrast, in Comparative Example 3, due to the absence of kojic acid, the inhibitory ability decreased significantly, and only about 29% was inhibited at the highest concentration. This fully proves that kojic acid is not an isolated additive component in the entire compounding system, but acts as a core tyrosinase pathway intervention agent, forming a multi-pathway inhibition mechanism with fullerene and plant extracts.

[0184] From a mechanistic perspective, kojic acid can directly act on the active center of tyrosinase and block the process of L-DOPA oxidation to dopaquinone, which is the source of inhibiting melanin production. In this invention, kojic acid is synergistically constructed with fullerene (antioxidant, free radical scavenging), liquiritin (intervening in melanin transport), paeonol (promoting pigment metabolism), etc. to act on the melanin metabolism pathway simultaneously from three dimensions: "source blocking + mid-course intervention + downstream scavenging".

[0185] Especially noteworthy is that Example 1 can ensure the stable and uniform release of kojic acid into the melanocyte environment through the microemulsion structure and efficient penetration pathway, avoiding local irritation or component inactivation. Compared with Comparative Example 3, it is verified that without the participation of kojic acid, even if other components are present, it is difficult to achieve a systemic tyrosinase intervention effect, further strengthening the rationality and necessity of the "kojic acid-fullerene-extract ternary linkage mechanism" in this invention.

[0186] Experiment 4:

[0187] Experiment purpose:

[0188] Compare the percutaneous penetration ability of Fullerene in Example 1 and Comparative Example 4 (without high-shear treatment) under the same skin model conditions, so as to verify the effect of the synergistic structure of high-shear constructed microemulsion + microcapsule on skin penetration efficiency.

[0189] Experimental materials and equipment:

[0190] Samples: Example 1, Comparative Example 4;

[0191] Instruments and equipment: Franz diffusion device (diffusion area 1 cm 2 ), constant temperature water bath (maintaining temperature at 32 °C), analytical balance, HPLC system;

[0192] Simulated skin: excised pig ear skin (thickness about 500 μm);

[0193] Solvents: acetonitrile / water (80:20), carbon tetrachloride (for extracting Fullerene);

[0194] Experimental procedures:

[0195] Cut the treated pig ear skin into appropriate segments, place it in the Franz diffusion cell with the epidermal side facing up and the dermal side in contact with the receptor cell liquid.

[0196] Add 0.5 mL of the sample emulsion to the donor cell (set 3 parallels for each sample).

[0197] The receptor liquid is phosphate buffer solution (simulated body fluid) containing a small amount of ethanol, maintain a constant temperature (32 ± 0.5 °C), and stir magnetically.

[0198] Collect the receptor liquid every 4 hours (total time is 24 h), and detect the Fullerene concentration by HPLC.

[0199] Calculate the cumulative penetration amount per unit time / area (μg / cm 2 )(Details of the data are shown in Table 4).

[0200] Table 4

[0201]

[0202]

[0203] Experimental summary:

[0204] The results showed that during the entire test period, the percutaneous penetration amount of fullerene in Example 1 was significantly higher than that in Comparative Example 4. Especially in the first 8 hours, the release rate of the example was almost twice that of the comparative example. This significant improvement in release and absorption efficiency verified the "particle size drive + interfacial affinity" mechanism of the microemulsion system formed by high-shear homogenization, constructed a more delicate and dynamically stable transmission path, and made the active ingredient easier to adhere to and penetrate the stratum corneum.

[0205] In addition, fullerene was stably encapsulated in PLGA nanoparticles in the form of microcapsules, and its particle size was controlled within 200 - 300 nm, which not only enhanced the distribution uniformity in the emulsion structure, but also, by virtue of its slow-release characteristics, prevented fullerene from being rapidly consumed in a short time, forming a "controlled-release - continuous penetration" gradient concentration propulsion mechanism. In contrast, Comparative Example 4 lacked high-shear emulsification, resulting in uneven emulsion particle size distribution and loose structure, causing uneven distribution of fullerene and reduced transfer efficiency, which affected the depth and persistence of skin absorption.

[0206] At the mechanism level, the present invention achieved the stable crossing and functional delivery of poorly soluble active ingredients (such as fullerene) in the skin barrier structure through the three-way collaborative design of "physical particle size control + carrier structure optimization + interfacial modification". This not only improved the penetration efficiency of the product, but also, to a certain extent, alleviated the irritation problem caused by local aggregation of fullerene, which is an important innovative point different from traditional emulsification structures. The experimental data further corroborated the overall progressiveness and practical value of the present invention in the integration of formulation technology and penetration system.

[0207] Although the embodiments of the present invention have been shown and described, it will be understood by those of ordinary skill in the art that various changes, modifications, substitutions, and variations can be made to these embodiments without departing from the principles and spirit of the present invention, and the scope of the present invention is defined by the appended claims and their equivalents.

Claims

1. A composition with skin whitening and freckle lightening effects and its skin care product, characterized in that, Comprising the following component materials in parts by mass: Fullerene: 0.1 - 2 parts; Kojic acid: 0.1 - 1 part; Angelica dahurica extract: 1 - 2 parts; Licorice extract: 0.5 - 2 parts; Moutan cortex extract: 0.3 - 1 part; Pearl powder extract: 0.5 - 1 part; Octyl glucoside: 0.5 - 2 parts; Vegetable oil phase: 5 - 15 parts; Microcapsules: 0.1 - 2 parts.

2. The composition with the function of skin whitening and freckle reduction and its skin care product according to claim 1, characterized in that, The fullerene in the microcapsules exists in an embedded form, the particle size of the microcapsules is between 200 - 500 nanometers, and the microcapsule carrier is poly (lactic - co - glycolic acid).

3. A composition with skin whitening and freckle lightening effects and its skin care product according to claim 1, characterized in that, The Angelica dahurica extract includes angelicol, angelicoside, and volatile oil, and the mass ratio thereof is angelicol:angelicoside:volatile oil = 2 - 3:1 - 2:1 - 2; The licorice extract includes glycyrrhizic acid, liquiritin, and licorice flavonoids, and the mass ratio thereof is glycyrrhizic acid:liquiritin:licorice flavonoids = 3 - 4:2 - 3:1 - 2.

4. A composition with skin whitening and freckle lightening effects and its skin care product according to claim 1, characterized in that, The Moutan cortex extract includes paeonol, paeoniflorin, and polysaccharides, and the mass ratio thereof is paeonol:paeoniflorin:polysaccharides = 2 - 3:1 - 2:1 - 2; The pearl powder extract includes pearl amino acids, pearl polysaccharides, and calcium, and the mass ratio thereof is pearl amino acids:pearl polysaccharides:calcium = 2 - 3:1 - 2:1 - 2.

5. Use of a composition having a skin whitening and freckle - reducing effect according to any one of claims 1 - 4 in the preparation of skin care products.

6. A skin care product comprising a composition having a skin whitening and freckle - reducing effect according to any one of claims 1 - 4.

7. The skin care product according to claim 6, wherein The skin care product is a cream, lotion, essence, facial mask, aqueous solution or gel, preferably a lotion.

8. The preparation method of the skin care product according to claim 6 or 5, characterized in that Including the following steps: Prepare an oil phase containing vegetable oil and octyl glucoside, and an aqueous phase containing Angelica dahurica extract, licorice extract, Moutan cortex extract, and pearl powder extract; Use a high - shear homogenizer to mix the oil phase and the aqueous phase to form a microemulsion; Use the microcapsules as a carrier and adopt an embedding technology to prepare in combination with fullerene; Add the microcapsules to the microemulsion and stir evenly to ensure that the microcapsules are evenly dispersed in the emulsion.

9. The preparation method of the skin care product according to claim 8, characterized in that, The oil phase is heated to 50 - 60 °C, and after completely dissolving octyl glucoside in the vegetable oil, it is mixed with the aqueous phase to form an emulsion; After being treated by a high - shear homogenizer, the particle size of the microemulsion is 50 - 200 nm.

10. The preparation method of the skin care product according to claim 8, characterized in that, The preparation steps of the embedding technology include: Dissolve fullerene in a carbon tetrachloride solvent; Adopt the solvent evaporation method to embed fullerene together with the poly (lactic - co - glycolic acid) of the microcapsules; The embedding rate of fullerene in the microcapsules is 90% - 95%.

Images