A pimple-repeating-preventing and acne-removing composition for regulating skin micro-ecology and its use

Abstract

The present application relates to the technical field of skin external agents, in particular to a kind of acne-removing composition for regulating skin microecology and preventing acne recurrence and application thereof, the composition is composed of Piancailu, white willow bark extract and hydrolyzed pearl;The mass ratio of Piancailu, white willow bark extract and hydrolyzed pearl is (1-9):(93-107):(2-8). The present application combines Piancailu, white willow bark extract and hydrolyzed pearl in a specific ratio, realizes the synergistic effect among the components, shows outstanding oil control and soothing effect, and also shows better effect in regulating skin metabolism expression, realizing the regulation of Staphylococcus epidermidis, which is beneficial to skin, and Propionibacterium acnes, which is harmful to skin, effectively removes acne and inhibits acne recurrence, solves the problem that existing acne-removing products can quickly eliminate red and swollen acne but acne often recurs after use is stopped, and meets the urgent consumer demand for preventing acne recurrence and maintaining stability.

Description

Technical Field

[0001] This invention relates to the field of topical skin agents, specifically to an acne-removing composition that regulates the skin's microecology and prevents recurring acne, and its application. Background Technology

[0002] Acne is a core pain point throughout the consumer lifecycle and a major driver of growth in the functional skincare market. Acne is a multifactorial, chain-like pathological process based on excessive sebum production, clogged hair follicles, and microecological imbalance dominated by Propionibacterium acnes. Ultimately, the innate immune system releases inflammatory factors, resulting in clinical symptoms. Facial acne not only causes immediate pain and itching, but can also leave persistent acne scars and pits, causing lifelong cosmetic damage. It severely impacts the self-confidence and self-esteem of those with acne, easily triggering anxiety, depression, and other emotional disorders, affecting close relationships and normal interpersonal interactions.

[0003] Most acne treatment products currently on the market focus on immediate, superficial effects in their research and marketing. They claim to quickly eliminate red, swollen pimples through strong oil control, rapid exfoliation, and powerful antibacterial properties, satisfying consumers' urgent need to extinguish the fire. However, this "treat the symptom, not the cause" strategy often ignores the complex root causes of acne. While using strong remedies, they easily damage the skin barrier, leading to oily skin on the outside but dry underneath, sensitivity, and redness, creating a vicious cycle where the more acne is treated, the more fragile the skin becomes. More importantly, these solutions lack long-term management for stabilizing acne-prone skin and preventing recurrence, failing to break the vicious cycle of "breakout-treatment-improvement-breakout." Summary of the Invention

[0004] The purpose of this invention is to provide an acne-removing composition and its application that, in addition to oil control and soothing effects, regulates skin metabolic expression, promotes the growth of Staphylococcus epidermidis, inhibits the growth of Propionibacterium acnes, and exerts a dual regulatory effect on the skin microecology.

[0005] To achieve the above objectives, the present invention provides the following technical solution: An acne-removing composition that regulates the skin's microecology and prevents recurring acne, the composition comprising Pien Tze Huang, white willow bark extract, and hydrolyzed pearl; wherein the mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is (1-9):(93-107):(2-8).

[0006] Furthermore, the mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 5:100:5.

[0007] Furthermore, the content of salicylic acid in the white willow bark extract is 53-65%.

[0008] The present invention also includes the use of any of the acne-removing compositions described herein in the preparation of acne-removing products that regulate the skin microecology and prevent recurring acne.

[0009] Pien Tze Huang is a precious traditional Chinese medicine with good anti-inflammatory, soothing, heat-clearing, detoxifying, blood-cooling, blood-stasis-removing, swelling-reducing, and pain-relieving effects. White willow bark extract, often called "natural aspirin," has excellent anti-inflammatory and soothing effects, and also regulates skin oil and directly inhibits specific bacteria. Hydrolyzed pearl has good soothing, antioxidant, and tyrosinase-inhibiting effects. Compared with existing technologies, this invention combines Pien Tze Huang, white willow bark extract, and hydrolyzed pearl in a specific ratio to achieve synergistic effects among the components, exhibiting outstanding oil-controlling and soothing effects. It also shows better effects in regulating skin metabolic expression and regulating beneficial bacteria like Staphylococcus epidermidis and harmful bacteria like Propionibacterium acnes. While effectively removing acne, it also effectively inhibits acne recurrence, solving the problem that existing acne products, while quickly eliminating red and swollen pimples, often recur after discontinuation, and meeting the current consumer demand for preventing acne recurrence and maintaining stable skin. Attached Figure Description

[0010] Figure 1 Examples of papule volume changes in group 1 subjects before use, after 28 days of continuous use, and 28 days after discontinuation, were captured using Antera 3D imaging.

[0011] Figure 2 Examples of papule volume changes in group 2 subjects before use, after 28 days of continuous use, and 28 days after discontinuation, were captured using Antera 3D imaging.

[0012] Figure 3 Examples of papule volume changes in group 3 subjects before use, after 28 days of continuous use, and 28 days after discontinuation, were captured using Antera 3D imaging. Detailed Implementation

[0013] The technical solution of the present invention will be further described below with reference to specific embodiments. It should be understood that the following embodiments are merely illustrative and explanatory of the present invention and should not be construed as limiting the scope of protection of the present invention. All technologies implemented based on the above content of the present invention are covered within the scope of protection intended by the present invention.

[0014] All raw materials used in this invention are commercially available cosmetic raw materials. Among them, the Pien Tze Huang used in the following examples and comparative examples is a traditional Chinese medicine with the trade name Pien Tze Huang and is manufactured by Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd.; the white willow bark extract used requires a salicylic acid content of 53-65% and is manufactured by Active Concepts LLC; the hydrolyzed pearl is a mixture of pearls processed by crushing, hydrolysis, filtration, concentration and other processes, with a total protein content greater than 1.5% and is manufactured by Shanghai LanHai Biotechnology Co., Ltd.

[0015] Example 1 Example composition 1 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 1:107:2.

[0016] Example 2 Example composition 2 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 5:100:5.

[0017] Example 3 Example composition 3 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 9:93:8.

[0018] Comparative Example 1 Comparative composition 1 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 110:0:0.

[0019] Comparative Example 2 Comparative composition 2 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 0:110:0.

[0020] Comparative Example 3 Comparative composition 3 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 0:0:110.

[0021] Comparative Example 4 Comparative composition 4 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 0:105:5.

[0022] Comparative Example 5 Comparative composition 5 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 0:100:10.

[0023] Comparative Example 6 Comparative composition 6 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 105:0:5.

[0024] Comparative Example 7 Comparative composition 7 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 5:0:105.

[0025] Comparative Example 8 Comparative composition 8 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 10:100:0.

[0026] Comparative Example 9 Comparative composition 9 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 5:105:0.

[0027] Comparative Example 10 Comparative composition 10 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 0.5:109:0.5.

[0028] Comparative Example 11 Comparative composition 11 is composed of the following proportions: The mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is 45:40:15.

[0029] Example 1: Evaluation of the skin microecological regulation effect based on the co-culture model of human immortalized keratinocytes with Propionibacterium acnes and Staphylococcus epidermidis. Evaluation Method: Staphylococcus epidermidis is a common resident bacterium on the skin, capable of occupying the skin surface and forming a biofilm to effectively resist the invasion of pathogens. It belongs to the Gram-positive cocci, most of which are non-pathogenic, playing a major role in ecological balance and skin self-cleaning. Staphylococcus epidermidis can inhibit the biofilm formation of harmful bacteria such as Propionibacterium acnes by producing a hydrolytic protease (Esp). Simultaneously, Esp can enhance the antibacterial effect of the β-antimicrobial peptide hBD2, thereby maintaining the balance of the skin's microecology. Excessive proliferation of Propionibacterium acnes on facial skin can easily cause follicular blockage and inflammatory reactions, leading to skin problems such as acne and papules. It is a common opportunistic pathogen that can decompose sebum and induce local immune responses. When Propionibacterium acnes over-colonizes the skin, it disrupts the balance of the skin's microecology, affecting skin health. At this time, measures need to be taken to regulate its growth and restore the balance of the skin's microecology.

[0030] Therefore, this experiment used keratinocytes, the main cells of human epidermal skin, as a skin model. The cells were cultured for 24 hours with the same mass concentration (0.0011 wt%) of the sample. After the culture treatment, the cells were washed, and Staphylococcus epidermidis labeled with green fluorescence (Dio) and Propionibacterium acnes labeled with red fluorescence (Dil) were mixed 1:1 and co-incubated with the washed cells for 30 min. The growth of Staphylococcus epidermidis and Propionibacterium acnes on the surface was observed by fluorescence microscopy to reflect the regulatory effect of the test substance on the skin microecological balance.

[0031] Upregulation rate of beneficial bacteria (%) = |Number of beneficial bacteria in the sample group / Number of beneficial bacteria in the blank group - 1| × 100% Inhibition rate of harmful bacteria (%) = |1 - (Number of harmful bacteria in the sample group / Number of harmful bacteria in the blank group)| × 100% Test evaluation results: The results are shown in Table 1 Table 1. Effects of each group of compositions on Staphylococcus epidermidis and Propionibacterium acnes Example 1 / Increased by 25.15% Inhibit 70.33% Example 2 / Upward adjustment of 28.63% Inhibition of 72.74% Example 3 / Upward adjustment of 27.32% Inhibition of 65.44% Comparative Example 1 Based on Examples 1-3, the white willow bark extract and hydrolyzed pearl components were removed, and only the single component of Pien Tze Huang was added. Upward adjustment of 11.86% Inhibit 9.04% Comparative Example 2 Based on Examples 1-3, the Pien Tze Huang and hydrolyzed pearl components were removed, and only the single component of white willow bark extract was added. No upward adjustment Inhibit 10.35% Comparative Example 3 Based on Examples 1-3, the components of Pien Tze Huang and white willow bark extract were removed, and only hydrolyzed pearl single component was added. Increased by 6.30% No inhibition Comparative Example 4 Based on Example 2, the Pien Tze Huang component was removed, and its original proportion was increased to the white willow bark extract component, while the proportion of the hydrolyzed pearl component remained unchanged. Upward adjustment of 4.97% Inhibit 16.12% Comparative Example 5 Based on Example 2, the Pien Tze Huang component was removed, and its original proportion was increased to the hydrolyzed pearl component, while the proportion of the white willow bark extract component remained unchanged. Up 2.33% Inhibition of 15.77% Comparative Example 6 Based on Example 2, the white willow bark extract component was removed, and its original proportion was increased accordingly in the Pien Tze Huang component, while the proportion of hydrolyzed pearl component remained unchanged. Up 10.11% Inhibit 8.34% Comparative Example 7 Based on Example 2, the white willow bark extract component was removed, and its original proportion was increased to the hydrolyzed pearl component, while the proportion of Pien Tze Huang component remained unchanged. Increased by 5.01% Inhibit 5.15% Comparative Example 8 Based on Example 2, the hydrolyzed pearl component was removed, and its original proportion was increased accordingly to the Pien Tze Huang component, while the proportion of the white willow bark extract component remained unchanged. Up 7.15% Inhibition of 17.89% Comparative Example 9 Based on Example 2, the hydrolyzed pearl component was removed, and its original proportion was correspondingly increased in the white willow bark extract component, while the proportion of the Pien Tze Huang component remained unchanged. Upward adjustment of 8.39% Inhibit 10.11% Comparative Example 10 Based on Example 1, the proportion of Pien Tze Huang and hydrolyzed pearl components was reduced, and the reduced proportion was increased in the white willow bark extract component. Up 14.50% Inhibition of 42.74% Comparative Example 11 Based on Example 3, the proportion of white willow bark extract was reduced, and the reduced proportion was increased in the Pien Tze Huang and hydrolyzed pearl components. Upward adjustment of 16.62% Inhibition of 50.79% The effects on Staphylococcus epidermidis and Propionibacterium acnes are shown in Table 1. At the same mass concentration, the compositions of this invention in Examples 1-3, after treatment of cells, showed a good promoting effect on Staphylococcus epidermidis growth and a good inhibitory effect on Propionibacterium acnes growth. Their effects were significantly better than those of the single-component sample groups 1-3, the sample groups lacking any component 4-9, and the sample groups with component ratios outside the scope of this invention 10-11. This confirms that within the proportion range of the compositions of this invention, the components synergistically regulate skin metabolic expression, achieving an unexpected dual regulatory effect on the skin microecology.

[0032] Experimental Example 2: Evaluation of Oil Control Efficacy Based on 5α-Reductase Inhibition Experiment Evaluation Method: 5α-reductase is a membrane protease dependent on reduced coenzyme I (NADPH) and an important androgen-metabolizing enzyme in the skin, irreversibly converting testosterone (T) to dihydrotestosterone (DHT). DHT is the most potent androgen, capable of inducing excessive sebum secretion from the sebaceous glands. Inhibiting 5α-reductase activity to reduce DHT levels can effectively alleviate excessive sebum secretion. Therefore, the in vitro oil-controlling efficacy of each sample was evaluated by detecting its ability to inhibit 5α-reductase at the same mass concentration (0.0011 wt%).

[0033] Test evaluation results: The results are shown in Table 2 Table 2 Results of 5α-reductase inhibition rate of each group of compositions Example 1 / 16.24% Example 2 / 22.58% Example 3 / 20.35% Comparative Example 1 Based on Examples 1-3, the white willow bark extract and hydrolyzed pearl components were removed, and only the single component of Pien Tze Huang was added. 6.71% Comparative Example 2 Based on Examples 1-3, the Pien Tze Huang and hydrolyzed pearl components were removed, and only the single component of white willow bark extract was added. 4.70% Comparative Example 3 Based on Examples 1-3, the components of Pien Tze Huang and white willow bark extract were removed, and only hydrolyzed pearl single component was added. 5.37% Comparative Example 4 Based on Example 2, the Pien Tze Huang component was removed, and its original proportion was increased to the white willow bark extract component, while the proportion of the hydrolyzed pearl component remained unchanged. 4.98% Comparative Example 5 Based on Example 2, the Pien Tze Huang component was removed, and its original proportion was increased to the hydrolyzed pearl component, while the proportion of the white willow bark extract component remained unchanged. 6.24% Comparative Example 6 Based on Example 2, the white willow bark extract component was removed, and its original proportion was increased accordingly in the Pien Tze Huang component, while the proportion of hydrolyzed pearl component remained unchanged. 7.88% Comparative Example 7 Based on Example 2, the white willow bark extract component was removed, and its original proportion was increased to the hydrolyzed pearl component, while the proportion of Pien Tze Huang component remained unchanged. 6.01% Comparative Example 8 Based on Example 2, the hydrolyzed pearl component was removed, and its original proportion was increased accordingly to the Pien Tze Huang component, while the proportion of the white willow bark extract component remained unchanged. 8.35% Comparative Example 9 Based on Example 2, the hydrolyzed pearl component was removed, and its original proportion was correspondingly increased in the white willow bark extract component, while the proportion of the Pien Tze Huang component remained unchanged. 5.77% Comparative Example 10 Based on Example 1, the proportion of Pien Tze Huang and hydrolyzed pearl components was reduced, and the reduced proportion was increased in the white willow bark extract component. 7.46% Comparative Example 11 Based on Example 3, the proportion of white willow bark extract was reduced, and the reduced proportion was increased in the Pien Tze Huang and hydrolyzed pearl components. 9.27% The results of the 5α-reductase inhibition rate are shown in Table 2. At the same mass concentration, the inhibition rate of 5α-reductase in sample groups 1-3 of the present invention is significantly better than that in sample groups 1-3 (single component), sample groups 4-9 (lacking any component), and sample groups 10-11 (component ratios outside the scope of the present invention). This confirms that within the proportion range of the present invention, the components synergistically achieve an unexpected oil-controlling effect.

[0034] Example 3: Evaluation of the soothing efficacy of a human acute monocytic leukemia (THP-1) cell model induced by bacterial lipopolysaccharide (LPS). Evaluation Method: Bacterial lipopolysaccharide binds to the surface antigen recognition receptor of human acute monocytic leukemia (AML) cells, inducing AML cells to secrete pro-inflammatory cytokines, such as interleukin-6 (IL-6), triggering a cascade reaction that leads to tissue damage and skin irritation. Therefore, inhibiting IL-6 can improve skin irritation and achieve a soothing effect. This test used LPS-induced THP-1 as the detection system, with three replicates per group. The soothing effect of each sample was analyzed by detecting the change in IL-6 content after treatment with the same mass concentration (0.0011 wt%) of the sample.

[0035] Test evaluation results: The results are shown in Table 3. Table 3. Inhibition results of IL-6 by the compositions in each group Example 1 / 13.22% Example 2 / 15.45% Example 3 / 14.35% Comparative Example 1 Based on Examples 1-3, the white willow bark extract and hydrolyzed pearl components were removed, and only the single component of Pien Tze Huang was added. 6.95% Comparative Example 2 Based on Examples 1-3, the Pien Tze Huang and hydrolyzed pearl components were removed, and only the single component of white willow bark extract was added. 3.43% Comparative Example 3 Based on Examples 1-3, the components of Pien Tze Huang and white willow bark extract were removed, and only hydrolyzed pearl single component was added. 3.57% Comparative Example 4 Based on Example 2, the Pien Tze Huang component was removed, and its original proportion was increased to the white willow bark extract component, while the proportion of the hydrolyzed pearl component remained unchanged. 4.24% Comparative Example 5 Based on Example 2, the Pien Tze Huang component was removed, and its original proportion was increased to the hydrolyzed pearl component, while the proportion of the white willow bark extract component remained unchanged. 4.64% Comparative Example 6 Based on Example 2, the white willow bark extract component was removed, and its original proportion was increased accordingly in the Pien Tze Huang component, while the proportion of hydrolyzed pearl component remained unchanged. 8.08% Comparative Example 7 Based on Example 2, the white willow bark extract component was removed, and its original proportion was increased to the hydrolyzed pearl component, while the proportion of Pien Tze Huang component remained unchanged. 7.61% Comparative Example 8 Based on Example 2, the hydrolyzed pearl component was removed, and its original proportion was increased accordingly to the Pien Tze Huang component, while the proportion of the white willow bark extract component remained unchanged. 8.05% Comparative Example 9 Based on Example 2, the hydrolyzed pearl component was removed, and its original proportion was correspondingly increased in the white willow bark extract component, while the proportion of the Pien Tze Huang component remained unchanged. 4.72% Comparative Example 10 Based on Example 3, the proportion of white willow bark extract was reduced, and the reduced proportion was increased in the Pien Tze Huang and hydrolyzed pearl components. 4.60% Comparative Example 11 Based on Example 3, the proportion of white willow bark extract was reduced, and the reduced proportion was increased in the Pien Tze Huang and hydrolyzed pearl components. 8.25% The IL-6 inhibition results are shown in Table 3. At the same mass concentration, the inhibition rate of IL-6 by the composition samples of the present invention in Examples 1-3 was significantly better than that of the single-component sample groups 1-3, the sample groups lacking any component 4-9, and the sample groups with component ratios outside the scope of the present invention 10-11. This confirms that within the proportion range of the composition of the present invention, the components synergistically achieve an unexpected soothing effect.

[0036] Example 4: Evaluation of the effects of clinical trials on acne treatment and prevention of acne recurrence. Evaluation Methods: The trial recruited 30 healthy Asian (Chinese) subjects with facial acne and papules in three groups. The three groups used test samples of the acne-clearing lotion containing 0 wt%, 0.0011 wt%, and 4.2 wt% of Example Composition 2, respectively. Skin parameters were compared before and after 28 days of continuous use and 28 days after discontinuation of the test sample, assessing its acne-clearing efficacy and its ability to prevent acne recurrence. Subjective evaluations were used, with "strongly agree" or "somewhat agree" indicating effectiveness; otherwise, it was considered ineffective. A higher percentage of agreement (over 50%) was considered effective.

[0037] Test evaluation results: The results are shown in Table 4 and Figure 1-3 .

[0038] Table 4. Clinical and self-assessment results of the acne-clearing efficacy and prevention of acne recurrence in the test samples of each group of acne-clearing solution with added compositions. 1 0wt% Example Composition 2 The size of papules and the number of comedones did not decrease significantly compared with before use. 36.67% of users reported a reduction in the number of pimples on their face after using the product. 43.33% reported that red and swollen pimples subsided more quickly after using the product. 0.00% of respondents felt that their facial acne did not recur after discontinuing use. 2 0.0011wt% Example Composition 2 The number of acne papules was significantly reduced compared to before use. 83.33% of users reported a reduction in the number of pimples on their face after using the product. 90.00% reported that red and swollen pimples subsided more quickly after using the product. 90.00% of users reported that their facial acne did not recur after discontinuing use. 3 4.2wt% Example Composition 2 The size of papules and the number of comedones were significantly reduced compared to before use. 93.33% of users reported a reduction in the number of pimples on their face after using the product. 93.33% of users reported that red and swollen pimples subsided more quickly after using the product. 100.00% of users reported that their facial acne did not recur after discontinuing use. From Table 4 and Figure 1-3 The clinical and self-assessment results show that the acne-clearing water test sample without Example Composition 2 (Group 1) showed no significant acne-clearing effect in either clinical or subject self-assessment after 28 days of use, and the effect of preventing acne recurrence was not significant in either case after 28 days of discontinuation. However, the skincare test samples with 0.0011 wt% and 4.2 wt% Example Composition 2 showed good acne-clearing effects in both clinical and subject self-assessment after 28 days of use, and the effect of preventing acne recurrence was also shown in the subject self-assessment after 28 days of discontinuation. This indicates that the composition of the present invention has significant acne-clearing efficacy and an unexpected effect in preventing acne recurrence.

[0039] While specific embodiments of the present invention have been described above, those skilled in the art should understand that the specific embodiments described are merely illustrative and not intended to limit the scope of the present invention. Equivalent modifications and variations made by those skilled in the art in accordance with the spirit of the present invention should be covered within the scope of protection of the claims of the present invention.

Claims

1. An acne-removing composition that regulates the skin's microecology and prevents recurring acne, characterized in that: The composition comprises Pien Tze Huang, white willow bark extract, and hydrolyzed pearl; the mass ratio of Pien Tze Huang: white willow bark extract: hydrolyzed pearl is (1-9):(93-107):(2-8).

2. The acne-removing composition according to claim 1, which regulates the skin microecology and prevents recurring acne, is characterized in that: The mass ratio of Pien Tze Huang, white willow bark extract, and hydrolyzed pearl is 5:100:

5.

3. The acne-removing composition according to claim 1, which regulates the skin microecology and prevents recurring acne, is characterized in that: The content of salicylic acid in the white willow bark extract is 53-65%.

4. The application of an acne-removing composition as described in any one of claims 1-3, characterized in that: Application in the preparation of acne-removing products that regulate the skin's microecology and prevent recurring acne.

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