An anti-wrinkle and anti-aging composition, its preparation method and use

Abstract

The application belongs to the field of skin care products, and particularly relates to an anti-wrinkle and anti-aging composition as well as a preparation method and application thereof. The anti-wrinkle and anti-aging composition comprises a neurotransmitter inhibitory peptide, a signal peptide, hydroxyl asperosaponin, myo-inositol and glycerol glucoside. The neurotransmitter inhibitory peptide is at least three of acetyl hexapeptide-8, arginine / lysine polypeptide, dipeptide diaminobutyroyl benzylamide diacetate and acetyl octapeptide-3, and the signal peptide is at least two of palmitoyl pentapeptide-4, decapeptide-4 and acetyl tetrapeptide-9. Compared with the prior art, the anti-wrinkle and anti-aging composition has the advantages that the components act on different anti-aging pathways, can cooperate with each other in terms of antioxidant, anti-inflammatory, moisturizing, enhanced cell vitality, reduced wrinkles and the like, can provide more comprehensive and better anti-aging effect, can comprehensively resist skin aging, and can make the skin appear more youthful, and the anti-wrinkle and anti-aging composition has small irritation and good stability.

Description

Technical Field

[0001] This invention relates to the field of skincare technology, and in particular to an anti-wrinkle and anti-aging composition, its preparation method, and its application. Background Technology

[0002] The "2025 Oral Anti-Aging Consumer Trend Insights" report reveals that skin problems are a fundamental anti-aging need for consumers, with 65% of surveyed consumers focusing on "loose skin / increased wrinkles." Furthermore, female consumers prioritize "beauty anti-aging," while male consumers place greater emphasis on "health anti-aging" that improves internal functions. This demonstrates that effectively delaying skin aging and improving the symptoms of aging skin is a pressing need.

[0003] Skin aging is a complex biological process influenced by a variety of internal and external factors. External factors mainly include ultraviolet radiation, oxidation, and unhealthy lifestyle habits. UVA rays, in particular, have strong penetrating power, reaching deep into the dermis and damaging collagen and elastin fibers, leading to sagging skin and increased wrinkles. Simultaneously, they cause a surge in free radicals, accelerating cell apoptosis. Many metabolic processes in the body produce peroxidized free radicals. When the body's free radical metabolism is unbalanced, excessive free radicals can cause damage, oxidizing unsaturated fatty acids into superoxide, forming lipofuscin. Excessive oxygen free radicals can also damage cell membranes and other important components, impairing protein and enzyme function. When the accumulated damage caused by free radicals overcomes the body's repair capabilities, it leads to changes or even loss of cell differentiation, thus causing or accelerating aging.

[0004] Wrinkles are the most obvious and primary sign of skin aging. They are a major factor affecting perceived age (i.e. how old one looks, directly influenced by signs of skin aging) and the most direct indicator for users to evaluate the efficacy of anti-aging products.

[0005] Currently, anti-aging products on the market primarily prevent free radical damage by combating and eliminating free radicals. Their main active ingredients include enzyme-based antioxidants such as SOD, and small-molecule antioxidants such as vitamin C and vitamin E. However, these ingredients have poor stability in skincare products, and enzyme-based antioxidants have large molecular weights, making them difficult for the skin to absorb. Furthermore, antioxidants can only prevent wrinkles from forming, not remove existing wrinkles, resulting in less than satisfactory effects in reducing the perceived age of the skin, which can easily lead users to doubt the product's effectiveness.

[0006] Peptides, as a class of small-molecule proteins with significant biological activity, possess various benefits such as delaying skin aging and improving wrinkles. Different peptide structures target different areas and have different effects. However, current anti-aging products related to peptides typically use only a single peptide, which is effective. Even when using peptide combinations, they merely stack similar active ingredients on repetitive targets or similar anti-aging mechanisms, easily reaching their efficacy limit and resulting in insignificant anti-aging effects. Furthermore, most peptides currently suffer from low transdermal efficiency and are easily degraded.

[0007] Therefore, there is an urgent need to develop a new anti-wrinkle and anti-aging composition that is highly stable, has good anti-wrinkle and anti-aging effects, and is less irritating. Summary of the Invention

[0008] Based on this, the purpose of the present invention is to overcome the defects or deficiencies of the prior art and provide an anti-wrinkle and anti-aging composition with immediate wrinkle removal, long-lasting anti-aging, anti-inflammatory and soothing, moisturizing and repairing effects.

[0009] An anti-wrinkle and anti-aging composition comprising neurotransmitter inhibitory peptides, signaling peptides, asiaticoside, inositol, and glyceryl glucoside; wherein the neurotransmitter inhibitory peptides are at least three of acetyl hexapeptide-8, arginine / lysine polypeptide, dipeptide diaminobutyryl benzylamide diacetate, and acetyl octapeptide-3, and the signaling peptides are at least two of palmitoyl pentapeptide-4, decapeptide-4, and acetyl tetrapeptide-9.

[0010] Compared with existing technologies, the anti-wrinkle and anti-aging composition of the present invention has components that act on different anti-aging pathways, and can work together in multiple aspects such as anti-oxidation, anti-inflammation, moisturizing, enhancing cell vitality, and reducing wrinkles to provide a more comprehensive and better anti-aging effect, comprehensively resist skin aging, and make the skin appear more youthful. In addition, the anti-wrinkle and anti-aging composition has low irritation and good stability, and is suitable for use in the preparation of anti-wrinkle and anti-aging skin care products.

[0011] In one embodiment, the neurotransmitter inhibitory peptide is acetyl hexapeptide-8, arginine / lysine polypeptide, and dipeptide diaminobutyryl benzylamide diacetate, and the signaling peptide is palmitoyl pentapeptide-4 and decapeptide-4.

[0012] In one embodiment, the volume fractions of acetyl hexapeptide-8, arginine / lysine polypeptide, dipeptide diaminobutyryl benzylamide diacetate, palmitoyl pentapeptide-4, and decapeptide-4 are 0.005-0.2 parts, 0.01-0.2 parts, 0.01-0.2 parts, 0.005-0.1 parts, and 0.005-0.1 parts, respectively.

[0013] In one embodiment, the volume fractions of asiaticoside, inositol, and glyceryl glucoside are 0.2-0.8 parts, 2-8 parts, and 0.1-2 parts, respectively.

[0014] In one embodiment, the anti-wrinkle and anti-aging composition further includes dipropylene glycol, 1,2-hexanediol, and water, in volume fractions of 20-30 parts, 2-4 parts, and 60-70 parts, respectively.

[0015] In addition, the present invention also provides an anti-wrinkle essence, which is made by mixing phase A, phase B, phase C, phase D and phase E;

[0016] Phase A includes water, EDTA-2Na, Carbomer 941, and betaine;

[0017] Phase B includes sodium hyaluronate and 1,3-butanediol;

[0018] Phase C includes triethanolamine;

[0019] Phase D includes p-hydroxyacetophenone and 1,3-butanediol;

[0020] Phase E includes the anti-wrinkle and anti-aging composition, preservatives, glyceryl glucoside, and bis-PEG-18 methyl ether dimethylsilane.

[0021] In one embodiment, by volume parts:

[0022] Phase A consists of 83-88 parts water, 0.01-0.05 parts EDTA-2Na, 0.1-0.3 parts Carbomer 941, and 1-2 parts betaine;

[0023] Phase B consists of 0.1-0.3 parts sodium hyaluronate and 2-4 parts 1,3-butanediol;

[0024] Phase C includes 0.1-0.4 parts of triethanolamine;

[0025] Phase D comprises 0.1-0.4 parts of p-hydroxyacetophenone and 1-3 parts of 1,3-butanediol;

[0026] Phase E includes 3-7 parts of an anti-wrinkle and anti-aging composition, 0.5-1.5 parts of a preservative, 1-2 parts of a glyceryl glucoside, and 0.1-0.5 parts of bis-PEG-18 methyl ether dimethylsilane.

[0027] This invention also provides a method for preparing the above-mentioned anti-wrinkle essence, comprising the following steps in sequence:

[0028] S1. Heat phase A to 80-85℃ and stir to dissolve;

[0029] S2. After phase A cools down to 50°C, add phase B to phase A and stir to dissolve.

[0030] S3. Add phase C to the mixture from step S2 and stir.

[0031] S4. After the mixture from step S3 has cooled to 45°C, add the dissolved D phase and stir until homogeneous.

[0032] S5. After the mixture from step S4 has cooled to 42°C, add each raw material of phase E in sequence and stir until homogeneous.

[0033] The present invention also provides the use of the aforementioned anti-wrinkle and anti-aging composition in the preparation of anti-wrinkle and anti-aging skin care products.

[0034] In one embodiment, the anti-wrinkle and anti-aging skincare product includes toner, skincare gel, skincare lotion, skincare cream, serum, mask, and spray.

[0035] To better understand and implement this invention, the following detailed description is provided in conjunction with the accompanying drawings. Attached Figure Description

[0036] Figure 1 The inhibition rate of composition 1-6 against matrix metalloproteinases is given.

[0037] Figure 2 The permeation-enhancing factor is the permeation-enhancing factor for different permeation-enhancing components.

[0038] Figure 3 Comparison of skin elasticity index R before and after using different anti-wrinkle serums.

[0039] Figure 4 A comparison of skin firmness before and after using different anti-wrinkle serums.

[0040] Figure 5 A comparison of wrinkle levels (crow's feet) before and after using different anti-wrinkle serums.

[0041] Figure 6 The improvement rates of various indicators before and after using different anti-wrinkle serums.

[0042] Figure 7 Example 1 illustrates how the anti-wrinkle essence in Example 1 improves fine lines around the eyes.

[0043] Figure 8 Example 2 shows how the anti-wrinkle essence in Example 1 improves fine lines around the eyes.

[0044] Figure 9 Example 3 shows how the anti-wrinkle essence in Example 1 improves fine lines around the eyes. Detailed Implementation

[0045] In view of the shortcomings of existing anti-aging products, such as single efficacy and insignificant anti-aging effects, this invention considers combining peptides and antioxidant ingredients with different wrinkle-reducing and anti-aging mechanisms to achieve multi-target anti-aging.

[0046] Skin wrinkles can be divided into dynamic wrinkles and static wrinkles. Dynamic wrinkles (also called expression lines) are muscle-related wrinkles, caused by muscle movement, such as forehead wrinkles, frown lines (lines between the eyebrows), and crow's feet (eye wrinkles). Static wrinkles refer to fine lines that appear even when the face is relaxed and natural. People with dry skin are more prone to static wrinkles. Static wrinkles are persistent and become more severe with age. The transition from dynamic to static wrinkles may be due to damage caused by frequent muscle contractions. For example, frequent exaggerated facial expressions (such as laughing or frowning) cause repeated muscle contractions, eventually forming dynamic wrinkles that are difficult to smooth out and gradually deepening into static wrinkles. The development of static wrinkles occurs with age. Therefore, wrinkle formation is a dual result of muscle contraction and tissue loss, and skin softness and moisture content play an important role in the formation and morphology of skin wrinkles.

[0047] Based on this, the present invention attempts to combine neurotransmitter inhibitory peptides (peptides are compounds of 2 to 16 amino acids linked by peptide bonds), signaling peptides, and antioxidants. Neurotransmitter inhibitory peptides can inhibit nerve excitation, relax muscles, reduce the formation of dynamic wrinkles, and provide an immediate wrinkle-reducing effect. Signaling peptides can stimulate collagen production, improve wrinkles and skin elasticity, and reduce the formation of dynamic wrinkles, providing an immediate wrinkle-reducing effect. Antioxidants can reduce damage caused by free radicals, thereby achieving the synergistic effect of multiple anti-aging pathways and compensating for the shortcomings of single ingredients.

[0048] First, this invention screens antioxidant components: peptide compositions are compounded with different antioxidant components, and their effects are studied. It was found that asiaticoside, when compounded with peptide compositions, significantly enhances the efficacy of the compositions. Acetonide is an active ingredient extracted from Centella asiatica and possesses various biological activities. In addition to its antioxidant activity, it can inhibit inflammation-related signaling pathways such as nuclear factor-κB (NF-κB), reduce the expression of inflammatory factors such as tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6), exerting an anti-inflammatory effect. It can also promote the expression of skin barrier-related proteins, enhance the skin's ability to resist external stimuli, improve impaired barrier function, stimulate fibroblast proliferation, promote collagen synthesis and arrangement, and accelerate tissue repair. Furthermore, asiaticoside has a moisturizing effect, prolonging the time for the skin to absorb the peptide composition, promoting skin hydration, and reducing the formation of static wrinkles caused by dry skin.

[0049] Then, this invention screened neurotransmitter inhibitory peptides and signaling peptides, and combined several peptides with good effects with antioxidant ingredients, and explored the anti-wrinkle effect of the combined composition. The components and contents of the composition are shown in Table 1. Dipropylene glycol, 1,2-hexanediol and water are used as solvents, humectants and preservatives in the composition, which have low irritation and can improve the stability of the complex.

[0050] The present invention then tested the inhibition rate of compositions 1-6 against matrix metalloproteinase-1 (MMP-1). For example... Figure 1 As shown, the inhibition rates of the six compositions against matrix metalloproteinase-1, from highest to lowest, are: Composition 6 > Composition 3 > Composition 5 > Composition 2 > Composition 4 > Composition 1. That is, Composition 6 exhibits the highest inhibition rate against matrix metalloproteinase-1, followed by Composition 3. This indicates that combinations containing both neurotransmitter inhibitory peptides and signal peptides have a higher inhibition rate against matrix metalloproteinase-1 than combinations containing only neurotransmitter inhibitory peptides or signal peptides alone, and combinations containing only signal peptides have a higher inhibition rate than combinations containing only neurotransmitter inhibitory peptides.

[0051] Table 1. Composition and content (volume ratio) of compositions 1-9

[0052]

[0053] By comparing the inhibition rates of matrix metalloproteinase-1 by compositions 4 and 1, it can be seen that acetyl hexapeptide-8 is more effective than acetyl octapeptide-3 in the composition. Similarly, by comparing the results of compositions 2 and 5, it is shown that decapeptide-4 is more effective than acetyl tetrapeptide-9. Therefore, composition 6 was selected for further research.

[0054] However, in application, it was found that the absorption efficiency of Composition 6 was limited, and the active ingredients had difficulty penetrating into the dermis, thus failing to effectively promote collagen production. Therefore, this invention screened penetration-enhancing ingredients and discovered that the signal peptide (decapeptide-4), in addition to activating collagen and elastin synthesis, can synergistically work with glyceroglucoside and inositol to significantly promote the absorption of other ingredients, thereby improving the overall anti-wrinkle and anti-aging effect of the composition.

[0055] In composition 6, decapeptide-4 not only functions as an active ingredient in the formula to exert anti-aging effects, but also enhances the overall penetration of the formula. However, the penetration of active ingredients in the skin is affected by various factors, and relying solely on the penetration-enhancing effect of decapeptide-4 is insufficient for the formula to achieve its intended efficacy.

[0056] In order to improve the penetration effect of the composition and enhance its anti-aging and moisturizing effects, this embodiment combines decapeptide-4 with different penetration-enhancing ingredients and compares their penetration effects through transdermal absorption experiments. Then, it is combined with composition 6 to obtain compositions 7-9 (as shown in Table 1).

[0057] Transdermal absorption assay method: Accurately weigh 2.00 g of vitamin C sample into a 10 mL volumetric flask, dissolve and dilute with pH 7.4 PBS buffer, and bring to volume to obtain the vitamin C stock solution. Accurately measure 2 mL of the vitamin C stock solution into a 15 mL test tube, and add equal amounts of four samples (decapeptide-4, decapeptide-4 + inositol, decapeptide-4 + glyceryl glucoside, and decapeptide-4 + inositol + glyceryl glucoside), mix thoroughly, and use as the test sample for the transdermal absorption experiment. The vitamin C stock solution is used as the vitamin C test sample for the transdermal absorption experiment.

[0058] The test skin was taken from the abdomen of a Bama miniature pig. The skin was placed between the receiving and supply tanks, with the outer epidermis facing the supply tank. The water temperature system was adjusted to 32℃, and the stirring speed was 600 rpm. Pre-warmed PBS solution (32℃) was added to the receiving tank, and all air bubbles were removed. The inner surface of the skin was brought into contact with the receiving solution, and 500 μL of the drug was quantitatively applied (the sample to be tested was the sample processed under the sample preparation section). The sample was injected into the supply tank, adhering tightly to the skin surface. The supply tank was sealed with sealing film to prevent drug evaporation. Four hours after sample release, 2.5 mL of the receiving solution was drawn using a syringe and used as the subcutaneous test solution. The experiment was set up in duplicate, with one blank skin group. The skin in the blank group did not come into contact with the sample, and all other procedures were the same as the experimental group. Samples were taken at the 4-hour time point, and the vitamin C content in the receiving tank and skin tissue was tested using high-performance liquid chromatography (HPLC).

[0059] The vitamin C content of the skin receiving fluid and the skin tissue homogenate after 4 hours was determined. The permeability was calculated as: (Vitamin C content in the receiving fluid of each group / Vitamin C stock solution content) × 100%. The permeation enhancement factor of the sample was calculated as: (Permeation amount of the experimental group / Permeation amount of the control group). The permeation enhancement factor is the ratio of the skin permeation amount of the target active ingredient (vitamin C) under the condition of adding the permeation enhancement component to the permeation amount without the permeation enhancement component (control group). The larger the permeation enhancement factor, the stronger the permeation enhancement effect of the permeation enhancement component.

[0060] See Figure 2The penetration enhancement ratios of decapeptide-4, decapeptide-4 + inositol, decapeptide-4 + glyceryl glucoside, and decapeptide-4 + inositol + glyceryl glucoside were 9.86, 13.74, 12.53, and 20.44, respectively. When decapeptide-4 was used alone as a penetration enhancer, its penetration enhancement ratio was the lowest. When decapeptide-4 was combined with inositol or glyceryl glucoside, the penetration enhancement ratio increased somewhat, but the effect was limited. When decapeptide-4 was combined with both inositol and glyceryl glucoside, the penetration enhancement ratio increased significantly, indicating that the combination of these three components can significantly improve the penetration effect of the formulation.

[0061] Based on the above research, the present invention provides an anti-wrinkle and anti-aging composition comprising neurotransmitter inhibitory peptides, signaling peptides, asiaticoside, glyceryl glucoside, and inositol, wherein the neurotransmitter inhibitory peptides are at least three of acetyl hexapeptide-8, arginine / lysine polypeptide, dipeptide diaminobutyryl benzylamide diacetate, and acetyl octapeptide-3, and the signaling peptides are at least two of palmitoyl pentapeptide-4, decapeptide-4, and acetyl tetrapeptide-9.

[0062] Preferably, the anti-wrinkle and anti-aging composition includes acetyl hexapeptide-8, arginine / lysine polypeptide, dipeptide diaminobutyryl benzylamide diacetate, palmitoyl pentapeptide-4, decapeptide-4, asiaticoside, glyceryl glucoside, and inositol. The present invention has surprisingly found that the above composition has a long-lasting anti-aging effect and a moisturizing and soothing effect, and has good stability.

[0063] Acetyl hexapeptide-8, also known as acetylrepinephrine, can bind to the SNAP-25 protein extracellularly, interfering with the formation of the SNARE complex. It can also competitively bind to nAChR, preventing the release of acetylcholine. The end result is a reduction in neurotransmitter release and signal intensity, thereby decreasing the amplitude of muscle contractions. This reduces dynamic wrinkles such as crow's feet and forehead wrinkles caused by repeated facial muscle contractions, improving skin elasticity and making the skin firmer. Acetyl hexapeptide-8 can also neutralize free radicals, reducing oxidative stress damage to the skin and delaying skin aging.

[0064] Dipeptide diaminobutyryl benzylamide diacetate is a synthetic tripeptide that mimics the activity of the snake venom venom Waglerin-1. It targets the muscle nicotinic acetylcholine receptor (nmAChR), blocking the binding of acetylcholine to the receptor, keeping sodium ion channels closed. Sodium ions cannot be absorbed, depolarized, and nerve impulse signals cannot be transmitted to the muscles, thereby inhibiting excessive muscle contraction, relaxing muscles, reducing wrinkles, making the skin appear smoother, and improving skin firmness and elasticity.

[0065] Arginine / lysine peptides are biomimetic synthetic peptides that inhibit nerve signal transmission and reduce excessive muscle contraction by blocking the activity of voltage-gated sodium ion channels (NaV1.4) and nicotinic acetylcholine receptors. This effectively reduces the appearance of dynamic wrinkles (such as expression lines and crow's feet), resulting in smoother skin. It also stimulates fibroblast activity, promotes the synthesis of collagen and elastin fibers, enhances the skin's self-repair ability, and improves the texture of damaged or aging skin. Furthermore, it replenishes lost elastin in the skin, helping to restore elasticity and firmness, reducing sagging, and making the skin fuller and younger.

[0066] Palmitoyl pentapeptide-4 is a synthetically produced small-molecule bioactive peptide composed of a five-amino acid peptide chain linked to palmitic acid via acylation. This structural design preserves the peptide's biological activity, enabling it to mimic natural signaling peptides and bind to skin cell receptors, promoting transdermal absorption and bioavailability. Simultaneously, the lipophilicity of palmitic acid significantly enhances the molecule's lipid solubility and skin permeability, increasing its transdermal efficiency and allowing it to more easily penetrate the stratum corneum to exert its effects. Palmitoyl pentapeptide-4 binds to specific receptors on fibroblast membranes, activating a series of signal transduction pathways, thereby stimulating fibroblasts to synthesize more collagen, including type I, III, and IV collagen, as well as extracellular matrix components such as fibronectin and glycosaminoglycans. By increasing collagen and elastin levels, palmitoyl pentapeptide-4 enhances skin elasticity, effectively reducing fine lines and wrinkles, resulting in firmer and smoother skin. It also strengthens skin cell connections, improving the integrity and stability of the skin barrier, leading to healthier and more elastic skin.

[0067] Decapeptide-4 is a biomimetic peptide of basic fibroblast growth factor (bFGF), mimicking its biological functions to promote skin cell proliferation and repair damage. It penetrates the dermis, activating collagen and elastin synthesis, thus reversing skin aging through inside-out reconstruction, improving skin elasticity, and reducing wrinkles and fine lines. Decapeptide-4 can also bind to epidermal keratinocytes, affecting the expression of ATP1B1 protein. ATP1B1 protein participates in cellular metabolism and delivers essential substances to cells, while also maintaining cell membrane potential and osmotic pressure balance by regulating ion transmembrane transport. By regulating ATP1B1 protein expression, decapeptide-4 reversibly opens skin channels, allowing biomolecules to penetrate deeper into the skin, significantly promoting the absorption of other active ingredients in the product.

[0068] Glyceryl glucoside is a natural glycoside compound composed of glycerol and glucose linked by a glycosidic bond. Its small molecular weight and hydrophilic structure allow it to penetrate the dermis transdermally, delivering moisture and bound active ingredients for deep hydration and ingredient delivery. Furthermore, it can enhance the skin cells' ability to absorb and retain moisture by promoting the expression of aquaporins (such as AQP3), improving dry skin and maintaining a hydrated state. Simultaneously, it promotes the regeneration of natural moisturizing factor (NMF) and filaggrin, strengthening the skin barrier function and enhancing the skin's resistance to external environmental factors.

[0069] Inositol is a small molecule compound capable of penetrating deep into the skin. Its hydrophilic properties attract moisture from the environment, helping the stratum corneum retain moisture and thus improving dryness and roughness. As a polyol penetration enhancer, inositol can increase the hydration level, solubility, and fluidity of the stratum corneum, facilitating the distribution and penetration of other active ingredients into the deeper layers of the skin. Inositol can also improve fibroblast metabolism, regulate intercellular signaling, resulting in healthier cell structure and indirectly promoting the transfer of nutrients and signaling molecules between cells.

[0070] Furthermore, the present invention investigated the content of each component in the anti-wrinkle and anti-aging composition, and found that the composition was more effective when the volume parts of acetyl hexapeptide-8, arginine / lysine polypeptide, dipeptide diaminobutyryl benzylamide diacetate, palmitoyl pentapeptide-4, decapeptide-4, asiaticoside, glyceryl glucoside, and inositol were 0.005-0.2 parts, 0.01-0.2 parts, 0.01-0.2 parts, 0.005-0.1 parts, 0.005-0.1 parts, 0.2-0.8 parts, 2-8 parts, and 0.1-2 parts, respectively. In addition, the anti-wrinkle and anti-aging composition also contains 20-30 parts of dipropylene glycol, 2-4 parts of 1,2-hexanediol, and 60-70 parts of water.

[0071] Based on the above-mentioned anti-wrinkle and anti-aging composition, the present invention provides an anti-wrinkle essence comprising: phase A, phase B, phase C, phase D, and phase E, in volume parts as follows:

[0072] Phase A consists of 83-88 parts deionized water, 0.01-0.05 parts EDTA-2Na, 0.1-0.3 parts Carbomer 941, and 1-2 parts betaine.

[0073] Phase B consists of 0.1-0.3 parts sodium hyaluronate and 2-4 parts 1,3-butanediol.

[0074] Phase C includes 0.1-0.4 parts of triethanolamine.

[0075] Phase D comprises 0.1-0.4 parts of p-hydroxyacetophenone and 1-3 parts of 1,3-butanediol.

[0076] Phase E includes 3-7 parts of an anti-wrinkle and anti-aging composition, 0.5-1 part of a preservative, 1-2 parts of glyceryl glucoside, and 0.1-0.5 parts of bis-PEG-18 methyl ether dimethylsilane.

[0077] The preparation method of the above-mentioned anti-wrinkle essence includes the following steps.

[0078] S1. Heat phase A to 80-85℃ and stir to dissolve.

[0079] S2. After phase A cools down to 50°C, add phase B to phase A and stir to dissolve.

[0080] S3. Add phase C to the mixture from step S2 and stir.

[0081] S4. After the mixture from step S3 has cooled to 45°C, add the dissolved D phase and stir until homogeneous.

[0082] S5. After the mixture from step S4 has cooled to 42°C, add each raw material of phase E in sequence and stir until homogeneous.

[0083] The anti-wrinkle and anti-aging composition of the present invention will be described in detail below with reference to specific embodiments and accompanying drawings.

[0084] Example 1

[0085] This embodiment provides an anti-wrinkle and anti-aging composition, the components and contents of which are shown in Table 2.

[0086] Table 2. Components and content (volume ratio) of the anti-wrinkle and anti-aging composition of Example 1

[0087]

[0088] Based on the above-mentioned anti-wrinkle and anti-aging composition, this embodiment also provides an anti-wrinkle essence, the formulation of which is shown in Table 3.

[0089] The preparation method of the anti-wrinkle essence includes the following steps.

[0090] S1. Clean and disinfect the instruments and equipment to be used. Heat phase A to 80-85℃ and stir to dissolve.

[0091] S2. Cool down to 50℃, add phase B to phase A, and stir to dissolve.

[0092] S3. Add phase C, stir, and cool.

[0093] S4. Cool down to 45℃, add the dissolved D phase, and stir until homogeneous.

[0094] S5. Cool down to 42°C, add each ingredient in phase E in sequence, and stir for 10 minutes.

[0095] The above-mentioned anti-wrinkle and anti-aging composition and anti-wrinkle serum were subjected to stability tests under three storage conditions: -10℃, 48℃, and alternating -10℃ / 48℃, for a duration of 30 days. The results showed that the anti-wrinkle and anti-aging composition and anti-wrinkle serum did not separate into layers or show any solid precipitation after 30 days of storage, demonstrating good stability.

[0096] Table 3. Ingredients and content (by volume) of anti-wrinkle serums

[0097]

[0098] Comparative Examples 1-3

[0099] Comparative Examples 1-3 provide an anti-wrinkle serum, the preparation method and ingredients of which are basically the same as the anti-wrinkle serum of Example 1, the difference being the different anti-wrinkle and anti-aging compositions. The components and contents of the anti-wrinkle and anti-aging compositions used in Comparative Examples 1-3 are shown in Table 4.

[0100] Table 4. Components and contents (volume ratio) of the anti-wrinkle and anti-aging compositions of Comparative Examples 1-3

[0101]

[0102] Test Example 1

[0103] 120 healthy Chinese men and women aged 30-60 years were selected, with no allergic diseases, no history of allergies to cosmetics or other topical preparations, no skin lesions or eczema, and no serious chronic wasting diseases (asthma, diabetes, etc.). Facial skin should be free of birthmarks, scratches, vitiligo, pigmented nevi, or other conditions that might affect the test. The 120 subjects were randomly divided into 4 groups of 30 each, using anti-wrinkle serums prepared from 4 different formulations of anti-wrinkle and anti-aging compositions (Tables 2 and 4). Instrumental testing was used to observe the subjects' skin data before and after product use, combined with self-evaluations and satisfaction surveys after use, to evaluate the skin improvement and safety of the products, providing evidence for claims of anti-wrinkle, firming, soothing, and gentle non-irritating effects of the cosmetics.

[0104] (1) Skin elasticity index

[0105] The Cutometer® MPA580 skin elasticity probe (2mm diameter) from Germany was used to collect skin elasticity parameters. The probe tests the vertical elasticity recovery displacement of the subject's skin per unit time. Before and after product use, the results were analyzed to determine if there was a significant improvement in the subject's skin elasticity.

[0106] The average skin elasticity index R of the subjects before the trial (D0) and after the trial (D28) is shown in Table 5. After 28 days of continuous use of the four anti-wrinkle serums, the subjects' skin elasticity index R increased to varying degrees compared with D0. Among them, the anti-wrinkle serum of Example 1 showed the greatest increase in the average skin elasticity index R, and the difference from the initial value was statistically significant (P<0.001). Figure 3 ).

[0107] Table 5. Average value of skin elasticity index R

[0108]

[0109] (2) Skin firmness

[0110] The skin elasticity probe test provides feedback on the subject's skin firmness. Before and after product use, the analysis shows a significant improvement in skin firmness (lower values ​​indicate better firmness).

[0111] The average skin firmness of the subjects before the trial (D0) and after the trial (D28) is shown in Table 6. After 28 days of continuous use of the four anti-wrinkle serums, the skin firmness values ​​of the subjects all decreased to varying degrees, indicating that these four anti-wrinkle serums can improve skin firmness. Among them, Example 1 showed the greatest decrease, and the difference from the initial value was statistically significant (P<0.001). Figure 4 ).

[0112] Table 6 Average Skin Firmness

[0113]

[0114] (3) Wrinkle (crow's feet) level assessment

[0115] Dermatologists analyzed the facial wrinkles of the subjects. Before and after product use, the wrinkle levels of the subjects' skin were compared to assess whether there was a significant decrease. Facial wrinkles were assessed using the following four levels: Human skin wrinkles are classified into four levels: mild, moderate, severe, and extreme. Level I is mild wrinkles, barely noticeable when the face is at rest, only faintly visible when the face is moving; Level II is moderate wrinkles, faintly visible when the face is at rest, but clearly visible when the face is moving; Level III is severe wrinkles, clearly visible even when the face is at rest, but significantly reduced when the wrinkles are stretched; Level IV is extreme wrinkles, clearly visible even when stretched.

[0116] The average wrinkle grade assessment (crow's feet) of the subjects before the trial (D0) and after the trial (D28) is shown in Table 7. After 28 days of continuous use of the four anti-wrinkle serums, the wrinkle grade (crow's feet) of the subjects all decreased, but the degree of decrease varied. The anti-wrinkle serum of Example 1 showed the greatest decrease, and the difference from the initial value was statistically significant (P<0.001). Figure 5 ).

[0117] Table 7. Wrinkle Level Assessment (Crow's Feet) Average Value

[0118]

[0119] (4) Improvement rate of various indicators

[0120] Calculation formula: Initial value D0: refers to the baseline value before using any product; Test value D28: the test data value after the subject uses the product for 28 days; Improvement value: the difference between the subject's D28 after using the product and the initial value D0; Improvement rate: refers to the ratio between the improvement value of D28 and the initial value D0.

[0121] After 28 days of use of the anti-wrinkle serum, the improvement rates of the subjects' skin elasticity index (R), skin firmness, and wrinkle grade (crow's feet) are shown in Table 9. Example 1 showed the highest improvement rates for all indicators, indicating that among the four anti-wrinkle serums, Example 1 had the best anti-aging and firming effects. Figure 6 ).

[0122] Table 8 Improvement Rate of Each Indicator / %

[0123]

[0124] (5) Record of adverse reactions of subjects

[0125] If any adverse reaction occurs on the subject's skin during the entire testing process, the test should be terminated and recorded. Adverse reactions are also one of the test indicators.

[0126] Table 9. Evaluation Criteria for Adverse Reactions

[0127]

[0128] Table 10 Adverse Reactions in Subjects

[0129]

[0130] No adverse reactions were observed in any of the 120 participants who used the four anti-wrinkle serums during the trial.

[0131] (6) Evaluation conclusions of the anti-wrinkle essence efficacy

[0132] This trial used human efficacy testing methods, along with subject self-reporting and satisfaction assessment methods, to test 120 subjects. No subjects withdrew. The results are as follows:

[0133] Anti-wrinkle efficacy results: After 28 days of use of four anti-wrinkle serums by 120 subjects, the wrinkle grade assessment (crow's feet) of the anti-wrinkle serums in Comparative Examples 1-3 and Example 1 improved by 17.54%, 21.63%, 25.00%, and 31.43%, respectively. The results indicate that the anti-wrinkle serum in Example 1 had the best anti-wrinkle efficacy.

[0134] Firming Efficacy Results: After 28 days of use of four anti-wrinkle serums by 120 subjects, the skin elasticity index R of the anti-wrinkle serums in Comparative Examples 1-3 and Example 1 improved by 11.15%, 14.60%, 21.51%, and 29.06%, respectively, and the skin firmness improved by 14.42%, 16.04%, 23.61%, and 26.31%, respectively. The results indicate that the anti-wrinkle serum in Example 1 had the best firming effect.

[0135] Additionally, see Figure 7-9 The anti-wrinkle essence in Example 1 significantly reduced fine lines around the eyes after 28 days of use.

[0136] In summary, the anti-wrinkle and anti-aging composition provided by this invention has the effects of immediate wrinkle removal, long-lasting anti-aging, anti-inflammatory and soothing, moisturizing and repairing. It is a very effective comprehensive anti-aging formula and can be added as an active ingredient to different types of anti-aging products, such as creams, lotions, serums, moisturizing waters and masks.

[0137] The anti-wrinkle and anti-aging composition of the present invention has components that act on different anti-aging pathways, and can work together in multiple ways, such as anti-oxidation, anti-inflammation, moisturizing, enhancing cell vitality, and reducing wrinkles, to provide a more comprehensive and better anti-aging effect, comprehensively resist skin aging, and make the skin appear more youthful.

[0138] Among them, three neurotransmitter-inhibiting peptides act on the entire signaling pathway leading to dynamic wrinkles, effectively reducing dynamic wrinkles (such as expression lines) by inhibiting muscle contraction, providing an immediate wrinkle-reducing effect: Acetyl hexapeptide-8 blocks the release of acetylcholine; dipeptide diaminobutyryl benzylamide diacetate prevents acetylcholine from binding to receptors; and arginine / lysine peptides block voltage-gated Na+ channels. These three neurotransmitter-inhibiting peptides reduce muscle contraction from different targets and mechanisms, with multi-target synergistic effects, more effectively reducing the formation of dynamic wrinkles and enhancing muscle relaxation and skin elasticity.

[0139] Two signaling peptides stimulate the synthesis of collagen (type I, type II, and type IV) and elastin, increasing the content of the extracellular matrix in skin cells, effectively improving skin elasticity and firmness, reducing wrinkle formation from the root, and having a long-lasting anti-aging effect.

[0140] Signaling peptides can synergistically work with neurotransmitter inhibitory peptides to enhance the inhibitory rate of matrix metalloproteinase-1 (MMP-1). Simultaneously, neurotransmitter inhibitory peptides reduce muscle contraction, providing a better skin environment for signaling peptides to stimulate collagen synthesis. The promotion of collagen synthesis by signaling peptides further enhances skin elasticity and reduces wrinkles. The two work together to achieve anti-wrinkle and anti-aging effects by inhibiting muscle contraction and promoting collagen synthesis.

[0141] The peptide composition exerts its anti-wrinkle and anti-aging effects by inhibiting muscle contraction and promoting collagen synthesis. Hydroxyacine has multiple benefits, including antioxidant, anti-inflammatory, skin barrier repair-promoting, collagen synthesis and arrangement-promoting, and moisturizing effects. The combination of the two allows hydroxyasiaticoside to reduce free radical and inflammatory damage to the skin, providing a favorable internal skin environment for the peptides to exert their effects. Simultaneously, its moisturizing effect prolongs the duration of action of the peptide composition on the skin, enhancing its anti-wrinkle and anti-aging effects.

[0142] Decapeptide-4, inositol, and glyceryl glucoside all possess penetration-enhancing effects. Decapeptide-4 regulates ATP1B1 protein expression, opening skin channels; inositol increases stratum corneum hydration; and glyceryl glucoside carries moisture and active ingredients into the dermis and promotes aquaporin expression. The combination of these three ingredients significantly improves the formula's penetration, allowing active ingredients such as neurotransmitter inhibitory peptides, signaling peptides, and asiaticoside to better penetrate deeper into the skin, fully exerting their respective effects and achieving more efficient anti-wrinkle, anti-aging, moisturizing, and soothing results.

[0143] Dipropylene glycol has strong hygroscopic properties, absorbing moisture from the air and penetrating the stratum corneum of the skin to form a moisture-locking barrier, effectively relieving dryness and peeling, and maintaining skin hydration. Its permeability is superior to glycerin, making it suitable for skincare products requiring deep hydration. Dipropylene glycol can neutralize free radicals, reducing oxidative stress damage to the skin. 1,2-Hexanediol forms a molecular film to lock in moisture, reducing skin moisture loss and relieving dryness and tightness; its lubricating properties improve the product's feel, making application smoother. In addition, dipropylene glycol and 1,2-Hexanediol also have antibacterial and preservative effects, and as alternatives to traditional preservatives (such as phenoxyethanol), they help extend the shelf life of the composition, reduce irritation, and maintain the stability and dispersibility of the components.

[0144] The embodiments described above are merely examples of several implementations of the present invention, and while the descriptions are relatively specific and detailed, they should not be construed as limiting the scope of the invention. It should be noted that those skilled in the art can make various modifications and improvements without departing from the concept of the present invention, and these modifications and improvements all fall within the scope of protection of the present invention.

Claims

1. An anti-wrinkle anti-aging composition characterized in that, The composition comprises neurotransmitter inhibitory peptide, signal peptide, hydroxyl asperosaponin, inositol and glycerol glucoside; the neurotransmitter inhibitory peptide is acetyl hexapeptide-8, arginine / lysine polypeptide and dipeptide diaminobutyroyl benzylamide diacetic acid salt, and the signal peptide is palmitoyl pentapeptide-4 and decapeptide-4, wherein the volume fractions of acetyl hexapeptide-8, arginine / lysine polypeptide, dipeptide diaminobutyroyl benzylamide diacetic acid salt, palmitoyl pentapeptide-4, decapeptide-4 and hydroxyl asperosaponin are 0.005-0.2 parts, 0.01-0.2 parts, 0.01-0.2 parts, 0.005-0.1 parts, 0.005-0.1 parts and 0.2-0.8 parts, respectively; the volume fractions of inositol and glycerol glucoside are 0.1-2 parts and 2-8 parts, respectively.

2. The anti-wrinkle anti-aging composition according to claim 1, characterized in that, It also comprises dipropylene glycol, 1,2-hexanediol and water, and the volume fractions are 20-30 parts, 2-4 parts and 60-70 parts, respectively.

3. An anti-wrinkle serum, characterized by, It is prepared by mixing A phase, B phase, C phase, D phase and E phase; The A phase comprises water, EDTA-2Na, Carbopol 941 and betaine; The B phase comprises sodium hyaluronate and 1,3-butanediol; The C phase comprises triethanolamine; The D phase comprises p-hydroxyacetophenone and 1,3-butanediol; The E phase comprises the anti-wrinkle and anti-aging composition according to any one of claims 1-2, preservative, glycerol glucoside and bis-PEG-18 methyl ether dimethyl silane.

4. The anti-wrinkle serum according to claim 3, characterized in that, In terms of volume fractions: The A phase comprises 83-88 parts of water, 0.01-0.05 parts of EDTA-2Na, 0.1-0.3 parts of Carbopol 941 and 1-2 parts of betaine; The B phase comprises 0.1-0.3 parts of sodium hyaluronate and 2-4 parts of 1,3-butanediol; The C phase comprises 0.1-0.4 parts of triethanolamine; The D phase comprises 0.1-0.4 parts of p-hydroxyacetophenone and 1-3 parts of 1,3-butanediol; The E phase comprises 3-7 parts of the anti-wrinkle and anti-aging composition, 0.5-1.5 parts of preservative, 1-2 parts of glycerol glucoside and 0.1-0.5 parts of bis-PEG-18 methyl ether dimethyl silane.

5. The method for preparing the anti-wrinkle essence according to claim 3 or 4, characterized in that: It comprises the following steps in sequence: S1, heat the A phase to 80-85℃ and stir to dissolve; S2, after the A phase is cooled to 50℃, add the B phase to the A phase and stir to dissolve; S3, add the C phase to the mixture of step S2 and stir; S4, after the mixture of step S3 is cooled to 45℃, add the dissolved D phase and stir uniformly; S5, after the mixture of step S4 is cooled to 42℃, add the raw materials of the E phase in sequence and stir uniformly.

6. Use of the anti-wrinkle and anti-aging composition according to any one of claims 1-2 in the preparation of anti-wrinkle and anti-aging skin care products.

7. Use according to claim 6, characterized in that, The anti-wrinkle and anti-aging skin care products comprise skin softener, skin jelly, skin emulsion, skin cream, essence, facial mask and spray.

Images