A skin cell energy-based anti-wrinkle firming soothing efficacy ingredient combination and application

Abstract

The application discloses an anti-wrinkle firming soothing efficacy component combination based on skin cell energy and application, and belongs to the technical field of cosmetics. The composition comprises EPHMER mitochondrial marine protective factors, adenosine silanol, DPHP ligament repair factors and AQUXYL five-dimensional barrier repair factors in specific proportions. The application takes mitochondrial energy metabolism as the core, constructs a "protection-energy supply-repair-barrier" multi-pathway synergistic system, and breaks through the single target limitation of traditional anti-aging components. The composition can specifically target mitochondria, significantly increase the ATP content of cells, efficiently promote collagen synthesis, strengthen the skin barrier and reduce irritation, and is especially suitable for sensitive skin anti-aging. Through cell, 3D skin model and human body test verification, the composition shows significant and mild effects in terms of anti-wrinkle, firming and soothing. The composition provided by the application can be widely applied to cosmetics such as essence and cream.

Description

Technical Field

[0001] This invention relates to the field of cosmetic technology, and more specifically, to a combination of anti-wrinkle, firming, and soothing ingredients based on skin cell energy and their application. Background Technology

[0002] The core underlying mechanism of skin aging is cellular energy metabolism disorder. Mitochondria, as the cell's "energy factory," are responsible for synthesizing over 90% of the cell's direct energy currency—adenosine triphosphate (ATP). Research shows that skin aging is closely related to mitochondrial functional decline, insufficient ATP production, and excessive accumulation of mitochondrial reactive oxygen species (mtROS), forming a vicious cycle of "energy deficiency - oxidative damage - functional decline." This leads to a decrease in the ability of fibroblasts to synthesize collagen and elastin, loss of extracellular matrix (ECM), and upregulation of matrix metalloproteinases (MMPs) activity, accelerating collagen degradation, ultimately manifesting as wrinkles and sagging. Energy deficiency also weakens the epidermal cell renewal and barrier repair capabilities, leading to dry and sensitive skin. Therefore, targeting and enhancing mitochondrial function at the root of cellular energy metabolism has become a cutting-edge direction in the anti-aging field.

[0003] Current anti-aging cosmetic ingredients mostly focus on a single pathway or downstream process. For example, while retinol and its derivatives can promote collagen synthesis, they are highly irritating and unsuitable for sensitive skin; high-concentration fruit acids improve skin texture by promoting keratinocyte renewal, but can damage the skin barrier; and most peptide ingredients mainly inhibit MMPs or replenish collagen fragments, failing to address the root cause of aging—insufficient cellular energy. Furthermore, many potent ingredients struggle to balance effective anti-aging with gentle soothing, often requiring trade-offs between efficacy and safety.

[0004] In recent years, with the release of industry standards such as the "Guidelines for the Research and Development of Mitochondrial Energy Skincare Products (T / CAPS 055-2025)," the concept of "energy skincare" targeting mitochondria has gradually become a research hotspot. These guidelines clarify that the research and development of mitochondrial energy skincare products should adhere to principles of scientific rigor, safety, and effectiveness, and propose technical requirements such as multi-pathway synergy and multi-model validation. However, currently, there is still a gap in the development of anti-aging compositions that strictly adhere to the framework of these guidelines, simultaneously achieving multi-dimensional synergy of "energy replenishment - mitochondrial protection - structural repair - barrier strengthening," and are suitable for sensitive skin. In particular, how to screen ingredients with complementary functions, achieve a synergistic effect of "1+1>2" through precise formulation, and comprehensively verify its comprehensive effects in mitochondrial targeting, energy enhancement, collagen synthesis, and gentleness using modern detection methods (such as Seahorse cell energy metabolism analysis and confocal fluorescence imaging) remains a challenge in current technological research and development.

[0005] Therefore, developing a combination of effective ingredients that can target and enhance skin cell energy, synergistically combat aging through multiple pathways, possess both high efficacy and gentleness, and comply with the latest industry R&D standards has significant market value and technological importance. Summary of the Invention

[0006] The purpose of this invention is to overcome the shortcomings of existing technologies and provide a combination and application of anti-wrinkle, firming, and soothing active ingredients based on skin cell energy. This composition targets mitochondrial energy metabolism and, through the synergistic effect of four complementary core ingredients, constructs a closed-loop system of "protection-energy supply-repair-barrier," fundamentally improving skin aging and sensitivity problems caused by insufficient cellular energy.

[0007] To achieve the above objectives, the present invention adopts the following technical solution: In a first aspect, the present invention provides a combination of anti-wrinkle, firming, and soothing active ingredients based on skin cell energy, comprising the following components by weight percentage: EPHMER mitochondrial marine protection factor 0.05%-0.2%; Adenosylsilane alcohol 0.1%-1%; DPHP ligament repair agent 0.5%-2%; AQUXYL Five-Dimensional Barrier Repair Factor 2%-5%; And the acceptable amount of excipients in cosmetics.

[0008] The EPHMER mitochondrial marine protection factor, whose INCI name is Undaria pinnatifida extract, functions to protect mitochondria, clear mtROS, and upregulate PGC-1α and SIRT-1 expression.

[0009] The adenosylsilaneol, whose INCI name is adenosylsilanetriol, functions to directly supply ATP precursors, activate the AMPK pathway, and optimize mitochondrial respiratory chain function.

[0010] The DPHP ligament repair factor, whose INCI name is dipalmitoyl hydroxyproline, functions to inhibit MMPs activity, promote type I collagen synthesis, and repair the extracellular matrix.

[0011] The AQUXYL five-dimensional barrier repair factor, whose INCI name is xylitol glucoside, dehydrated xylitol, and xylitol, functions to promote the synthesis of barrier proteins such as ceramide and tight junction protein ZO-1, and regulate epidermal Ca2+ homeostasis.

[0012] Preferably, the weight ratio of EPHMER mitochondrial marine protection factor, adenosylsilane alcohol, DPHP ligament repair factor, and AQUXYL five-dimensional barrier repair factor is 1:5:10:30. This specific ratio is the optimal synergistic ratio selected through 23 sets of orthogonal experiments, which maximizes the synergistic effect of each component.

[0013] Secondly, this invention provides a method for preparing the above-mentioned combination of active ingredients, comprising the following steps: dissolving AQUXYL five-dimensional barrier repair factor and DPHP ligament repair factor in deionized water at 35-45℃; cooling to 25-30℃, adding EPHMER mitochondrial marine protection factor and adenosylsilanol, and stirring evenly; finally adding the remaining cosmetic excipients, adjusting the pH to 5.5-6.5, and filtering to obtain the final product. This segmented temperature control process can maximize the preservation of the bioactivity of each core ingredient.

[0014] Thirdly, this invention provides the application of the above-mentioned combination of active ingredients in the preparation of cosmetics for anti-wrinkle, firming, and soothing skin. The cosmetics include, but are not limited to, dosage forms such as serums, eye creams, face creams, and lotions.

[0015] Compared with the prior art, the present invention has at least the following beneficial effects: 1. Mechanism Innovation, Root Cause Anti-aging: This invention's composition breaks through the limitations of traditional anti-aging ingredients that focus on a single downstream target. With mitochondrial energy metabolism as its core, it constructs a multi-pathway synergistic closed-loop system of "energy-driven (adenosylsilanol) - mitochondrial protection (EPHMER) - structural repair (DPHP) - barrier strengthening (AQUXYL)". This system activates cellular function from the root of cellular bioenergetics, realizing a causal chain of "sufficient energy to functional activation to improvement of aging phenotypes," aligning with the cutting-edge direction of "multi-pathway synergistic improvement of mitochondrial function".

[0016] 2. Synergistic Effect and Significant Efficacy: The optimal ratio of the four components (1:5:10:30) was selected, achieving a synergistic effect of "1+1+1+1>4". Experimental data show that this combination can increase the ATP content of fibroblasts by 81.16% and the synthesis of type I collagen by 547%, far exceeding the simple sum of the effects of using each component alone.

[0017] 3. Gentle and Effective, Suitable for Sensitive Skin: This invention achieves highly effective anti-aging while significantly reducing the potential irritation of the formula through the synergistic effect of its ingredients. In a trial involving 30 people with sensitive skin (including rosacea patients), the product showed extremely low irritation scores. Specifically, AQUXYL's barrier repair function and adenosine silanol's energy supply jointly enhance the tolerance of sensitive skin cells, filling a market gap for highly effective yet gentle anti-aging products. Attached Figure Description

[0018] Figure 1 The graph shows the results of relative ATP content (%). Note: Ctrl, E1, E2, E3, P1, P2, P3, P4, P5, and P6 correspond to the blank control group, Example 1, Example 2, Example 3, Comparative Example 1, Comparative Example 2, Comparative Example 3, Comparative Example 4, Comparative Example 5, and Comparative Example 6, respectively.

[0019] Figure 2 The graph shows the results of type I collagen content. Note: Ctrl, E1, E2, E3, P1, P2, P3, P4, P5, and P6 correspond to the blank control group, Example 1, Example 2, Example 3, Comparative Example 1, Comparative Example 2, Comparative Example 3, Comparative Example 4, Comparative Example 5, and Comparative Example 6, respectively.

[0020] Figure 3 The graph shows the relative expression levels of ZO-1 mRNA.

[0021] Figure 4 The graph shows the relative expression levels of AQP3 mRNA. Detailed Implementation

[0022] To make the objectives, technical solutions, and advantages of this invention clearer, the invention will be further described in detail below with reference to embodiments. It should be understood that the specific embodiments described herein are only for explaining the invention and are not intended to limit the invention. Experimental methods in the following embodiments that do not specify specific conditions are generally performed under conventional conditions or as recommended by the manufacturer. Unless otherwise specified, all raw materials used in all embodiments are commercially available.

[0023] Example 1: Preparation of the active ingredient composition This embodiment provides an optimally proportioned composition of active ingredients, the components and their weight percentages of which are as follows: EPHMER Mitochondrial Marine Protection Factor (INCI: Undaria Pinnatifida Extract) 0.1%; (purchased from Solabia Group, EPHEMER™); Adenosylsilane 0.5% (purchased from Aimei); DPHP Ligament Repair Agent (INCI: Dipalmitoyl Hydroxyproline) 1%; (purchased from Seppic, SEPILIFT™ DPHP); AQUXYL Five-Dimensional Barrier Repair Factor (xylitol glucoside, etc.) 3%; (purchased from Seppic, AQUAXYL™). Glycerin (humectant) 5%; Phenoxyethanol (preservative) 0.5%; Citric acid (pH adjuster), appropriate amount; Add deionized water to a concentration of 100%.

[0024] Preparation method: (1) Add 80% of the calculated amount of deionized water to the reactor, heat to 40°C, and add AQUXYL five-dimensional barrier repair factor and DPHP ligament repair factor in sequence while stirring at 300 rpm. Maintain the temperature and stir for 25 minutes until completely dissolved.

[0025] (2) Cool the system to 28°C, and slowly add EPHMER mitochondrial marine protection factor and adenosylsilanol while stirring continuously for 20 minutes.

[0026] (3) Add glycerol, phenoxyethanol and the remaining deionized water, and stir well. Adjust the pH of the system to 6.0 with citric acid aqueous solution.

[0027] (4) The resulting mixture is filtered through a 200-mesh filter and bottled to obtain the active ingredient composition (in the form of an essence).

[0028] Example 2: Compositions emphasizing energy and barrier This embodiment provides an efficacy composition focusing on energy supply and barrier repair, the components and weight percentages of which are as follows: EPHMER mitochondrial marine protection factor 0.05%; adenosylsilane alcohol 1.0%; DPHP ligament repair factor 2.0%; AQUXYL five-dimensional barrier repair factor 5.0%; glycerol 5%; phenoxyethanol 0.5%; citric acid as needed; deionized water added to 100%. The preparation method is the same as in Example 1.

[0029] Example 3: Compositions emphasizing protection and gentleness This embodiment provides a composition with efficacy focusing on mitochondrial protection and gentle anti-aging. Its components and weight percentages are as follows: EPHMER mitochondrial marine protection factor 0.2%; adenosylsilane alcohol 0.1%; DPHP ligament repair factor 0.5%; AQUXYL five-dimensional barrier repair factor 2.0%; glycerol 5%; phenoxyethanol 0.5%; citric acid as needed; deionized water to 100%. The preparation method is the same as in Example 1.

[0030] Comparative Example 1: Composition lacking EPHMER mitochondrial marine protective factor The composition of this comparative example is basically the same as that of Example 1, but without the addition of EPHMER mitochondrial marine protection factor, and its weight percentage is made up by deionized water.

[0031] Comparative Example 2: Compositions lacking adenosine silanol The composition of this comparative example is basically the same as that of Example 1, but adenosine silanol is not added, and its weight percentage is made up by deionized water.

[0032] Comparative Example 3: Composition lacking DPHP ligament repair factor The composition of this comparative example is basically the same as that of Example 1, but without the addition of DPHP ligament repair factor, and its weight percentage is made up by deionized water.

[0033] Comparative Example 4: Composition lacking AQUXYL five-dimensional barrier repair factor The composition of this comparative example is basically the same as that of Example 1, but without the addition of AQUXYL five-dimensional barrier repair factor, and its weight percentage is made up by deionized water.

[0034] Comparative Example 5: Compositions lacking EPHMER and adenosine silanol The composition of this comparative example is basically the same as that of Example 1, but without the addition of EPHMER mitochondrial marine protection factor and adenosine silanol, and its weight percentage is made up by deionized water.

[0035] Comparison Example 6: Commercially available common anti-aging serums This comparative example uses a commercially available anti-aging serum with palmitoyl tripeptide-5 (3%) and other signal peptides as the main active ingredients, as a reference for common technical solutions on the market.

[0036] Experiment Example 4: Test for Increased ATP Content at the Cellular Level Materials and Methods: Normal human dermal fibroblasts (NHDF) were seeded into 96-well plates. After cell adhesion, the medium was replaced with maintenance medium containing 1% fetal bovine serum, and samples from Examples 1-3 and Comparative Examples 1-6 were added (diluted with maintenance medium to a total core component concentration of 0.1%). A blank control group (maintenance medium only) was set up. Each group had 6 replicates. After 24 hours of treatment, cells were lysed and ATP concentration was measured using an ATP assay kit (Beyotime, S0026). Total protein concentration was standardized using the BCA method. Data are expressed as mean ± standard deviation. One-way ANOVA was used for intergroup comparisons, and p < 0.05 was considered statistically significant.

[0037] The results are as follows Figure 1As shown: The ATP content of cells in the treatment group of Example 1 was (181.16 ± 8.37)%, significantly higher than that of the blank control group (set as 100%) (p<0.001). The ATP enhancement rates of Examples 2 and 3 were (165.42 ± 7.89)% and (142.33 ± 6.54)%, respectively, also showing significant effects. The ATP content of Comparative Examples 1 (deficient in EPHMER) and 2 (deficient in adenosylsilane) were (118.22 ± 5.41)% and (105.67 ± 4.82)%, respectively, significantly lower than that of Example 1 (p<0.01), indicating that the absence of any energy-related core component led to a significant decrease in energy supply. The ATP content of Comparative Example 6 (commercially available extract) was (102.15 ± 5.11)%, with no difference from the blank group. Conclusion: The complete composition of the present invention can significantly enhance cellular ATP levels, and the effect is superior to any formulation lacking a single component.

[0038] Experimental Example 5: Type I Collagen Synthesis Promotion Assay (ELISA Method) Materials and Methods: Human dermal fibroblasts were used, and the experimental groups were the same as in Experiment 1. After 72 hours of cell treatment, the cell culture supernatant was collected, and the content of secreted type I collagen in the supernatant was detected using a human type I collagen ELISA kit (Cloud-Clone, SEA571Hu) strictly following the instructions. Six replicates were set for each group. Data are expressed as mean ± standard deviation. One-way ANOVA was used for inter-group comparisons, and p < 0.05 was considered statistically significant.

[0039] The results are as follows Figure 2 As shown, ELISA analysis revealed that the type I collagen content in the cell culture supernatant of Example 1 group was (647.35 ± 25.18) ng / mL, approximately 5.5 times that of the control group (118.22 ± 9.76) ng / mL, with a highly significant difference (p<0.001). The collagen content in Comparative Example 3 (deficient in DPHP) was (265.47 ± 18.44) ng / mL, higher than the control but significantly lower than that in Example 1 (p<0.01), demonstrating that DPHP plays a crucial role in collagen synthesis. Notably, the collagen content in Comparative Example 2 (deficient in adenosylsilanol) was also significantly lower than that in Example 1 (152.33 ± 12.67) ng / mL (p<0.01), confirming the synergistic mechanism that "energy supply is the driving basis for collagen synthesis." Conclusion: The composition of the present invention achieves highly efficient promotion of collagen synthesis through the synergistic effect of "energy supply (adenosylsilanol) + repair (DPHP)".

[0040] Example 6: Combination Index (CI) Measurement Experiment Experimental objective: To evaluate the synergistic effect of the four core components (EPHMER, adenosylsilane, DPHP, and AQUXYL) in the active ingredient composition of this invention on promoting type I collagen synthesis.

[0041] Materials and Methods: Cells and samples: Normal human dermal fibroblasts (NHDF) were used. The four core raw materials were prepared into single-component stock solutions, and a combined drug group stock solution was prepared in a fixed proportion according to the weight ratio (1:5:10:30) of Example 1 of this invention.

[0042] Experimental design: The Chou-Talalay combined index analysis method was used. Multiple single-component treatment groups with different concentrations, combined treatment groups with mixtures in fixed proportions, and a blank control group were set up. Each concentration had 6 replicates.

[0043] Detection indicators: After 72 hours of cell treatment, the supernatant was collected, and the type I collagen content was detected using a human type I collagen ELISA kit. The amount of collagen synthesized was used as the effect indicator (Fa), and dose-response curves were calculated for each component alone and for the four components in combination.

[0044] Data Analysis: Using CompuSyn software, the combination index (CI) was calculated for each effect score (Fa) based on the median effect principle. CI < 1 indicates a synergistic effect, CI = 1 indicates an additive effect, and CI > 1 indicates an antagonistic effect.

[0045] Results: Regarding the key efficacy indicator of promoting type I collagen synthesis, the combined application of the four core components of this invention (EPHMER: adenosylsilaneol: DPHP: AQUXYL = 1:5:10:30) achieved an effect score (Fa) of 0.5 (i.e., ED). 50 ), 0.75 (ED) 75 ), 0.9 (ED) 90 ) and 0.95 (ED) 95 When the calculated combination index (CI) values ​​were 0.62, 0.71, 0.85 and 0.92, respectively, all of which were less than 1.

[0046] Conclusion: The experimental data demonstrate that, under the specific ratio described in this invention, the four core components exhibit a clear synergistic effect (CI<1) in promoting collagen synthesis. Their combined effect is significantly better than the simple sum of the effects of each component used alone, achieving a synergistic effect of "1+1+1+1>4", providing direct evidence for the inventiveness of the composition of this invention.

[0047] Experiment Example 7: Assay for the expression level of barrier-related protein mRNA (qPCR method) Materials and Methods: Immortalized human keratinocytes (HaCaT cells) were used. Cells were seeded in 6-well plates, and when the confluence reached 60-70%, the medium was replaced with a medium containing the samples from Example 1, Comparative Example 4 (lacking AQUXYL), and a blank control (total concentration 0.1%) for 48 hours. After treatment, total RNA was extracted from the cells using TRIzol reagent and reverse transcribed into cDNA. Using GAPDH as an internal reference gene, real-time quantitative PCR (qPCR) was performed using the SYBR Green dye method to detect the relative mRNA expression levels of tight junction protein 1 (ZO-1) and aquaporin 3 (AQP3). Primer sequences were synthesized by Sangon Biotech (Shanghai) Co., Ltd. Each group had 3 biological replicates, and each replicate had 3 technical replicates. Data were analyzed using 2... -ΔΔ The relative expression level was calculated using the Ct method, expressed as mean ± standard deviation, and statistical analysis was performed.

[0048] Results: qPCR results showed that after treatment with the composition of Example 1, the relative expression levels of ZO-1 and AQP3 mRNA in HaCaT cells were (2.42 ± 0.15) times and (1.76 ± 0.08) times that of the control group, respectively, both significantly upregulated (p<0.01). In contrast, under the control group (AQUXYL deficiency) treatment, the expression levels of ZO-1 and AQP3 showed no significant difference. Conclusion: The AQUXYL component in the composition of this invention is key to upregulating the expression of barrier-related protein genes, confirming its function in strengthening the skin barrier.

[0049] Experiment Example 8: Human Trial (Stimulation Assessment) Materials and Methods: Thirty volunteers aged 25-55 with sensitive skin (including 10 patients with stable rosacea) were recruited for product safety evaluation. The serum prepared in Example 1 was applied to the entire face morning and evening for 28 consecutive days. Visual evaluations were conducted by a professional dermatologist before the trial (D0), on day 7 (D7), and day 28 (D28), recording indicators such as erythema, scaling, burning, and stinging (scored on a scale of 0-4). Simultaneously, transepidermal water loss (TEWL) and facial redness index (a* value) were measured using a skin analyzer.

[0050] Results: Throughout the trial period, no volunteers experienced moderate or severe irritation. The average irritation scores on D0, D7, and D28 were 0.10 ± 0.31, 0.13 ± 0.35, and 0.07 ± 0.26, respectively, consistently remaining at extremely low levels (<0.5). Compared to D0, the average TEWL value of volunteers decreased by 18.5% (p<0.05) and the cheek a value decreased by 15.2% (p<0.05) on D28, indicating enhanced skin barrier function and improved redness. Conclusion: The active ingredient of this invention has high safety in sensitive skin populations and can effectively repair the skin barrier and reduce redness.

[0051] The above experiments fully demonstrate that the functional ingredient composition provided by this invention, through the precise ratio and synergistic effect of four core components, can target mitochondria, significantly enhance skin cell energy, efficiently promote collagen synthesis, and strengthen the skin barrier. It also exhibits excellent gentleness, achieving multiple effects of anti-wrinkle, firming, and soothing. Furthermore, its technical solution is fully industrially feasible and has broad application prospects. The above description represents a preferred embodiment of this invention. It should be noted that those skilled in the art can make various improvements and modifications without departing from the principles described in this invention, and these improvements and modifications should also be considered within the scope of protection of this invention.

Claims

1. A skin cell energy-based anti-wrinkle firming soothing efficacy ingredient combination, characterized in that, By weight percentage, it contains the following components: EPHMER mitochondrial marine protection factor 0.05%-0.2%; Adenosylsilane alcohol 0.1%-1%; DPHP ligament repair agent 0.5%-2%; AQUXYL Five-Dimensional Barrier Repair Factor 2%-5%; And the acceptable amount of excipients in cosmetics.

2. The combination of claim 1, wherein, The INCI name of the EPHMER mitochondrial marine protection factor is Undaria pinnatifida extract; the INCI name of the adenosine silanol is adenosine, silanetriol; the INCI name of the DPHP ligament repair factor is dipalmitoyl hydroxyproline; and the INCI name of the AQUXYL five-dimensional barrier repair factor is xylitol glucoside, dehydrated xylitol, xylitol.

3. The combination according to claim 1 or 2, characterized in that, The weight ratio of EPHMER mitochondrial marine protection factor, adenosylsilanol, DPHP ligament repair factor, and AQUXYL five-dimensional barrier repair factor is 1:5:10:

30.

4. Process for the preparation of a combination according to any one of claims 1-3, characterized in that, Includes the following steps: (1) Dissolve AQUXYL five-dimensional barrier repair factor and DPHP ligament repair factor in solvent at 35-45℃; (2) Cool the system obtained in step (1) to 25-30℃, add EPHMER mitochondrial marine protection factor and adenosylsilanol, and stir until homogeneous; (3) Add the remaining cosmetically acceptable excipients, adjust the pH to 5.5-6.5, filter, and the product is obtained.

5. A cosmetic product, characterized by, It contains a combination of anti-wrinkle, firming, and soothing ingredients based on skin cell energy as described in any one of claims 1-3.

6. The cosmetic product according to claim 5, characterized in that, The cosmetic product is a serum, eye cream, face cream, or lotion.

7. The use of the combination of anti-wrinkle, firming, and soothing active ingredients based on skin cell energy as described in any one of claims 1-3 in the preparation of cosmetics for anti-aging.

8. Use according to claim 7, wherein the compound is ###0002### The anti-aging measures include anti-wrinkle and / or skin firming.

9. The use of the combination of anti-wrinkle, firming, and soothing active ingredients based on skin cell energy as described in any one of claims 1-3 in the preparation of cosmetics for soothing the skin and repairing the skin barrier.

10. A non-therapeutic method of skin care, characterized in that, A cosmetic comprising any one of the combinations described in claims 1-3 is applied to the skin to improve one or more of the following conditions: wrinkles, sagging, dryness, or sensitivity.

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