A composition for treating acne and a method of preparing the same

Abstract

The present application belongs to the technical field of skin care products, and particularly relates to a composition for treating acne and a preparation method thereof. The composition comprises the following components: 1-2% of a lactic acid bacillus fermentation product, and 5-8% of a plant extraction component; the plant extraction component is composed of a Pinus Nigra Leaf Extract, a Osmorhiza Aristata Root Extract, and a Echinacea Purpurea Extract. The mass ratio of the Pinus Nigra Leaf Extract, the Osmorhiza Aristata Root Extract, and the Echinacea Purpurea Extract is 1:(1-3):(5-10). The Osmorhiza Aristata Root Extract, the Pinus Nigra Leaf Extract, and the Echinacea Purpurea Extract have a certain synergistic effect in the composition formula, and therefore, the acne treatment composition provided by the present application can effectively inhibit the growth of Propionibacterium acnes, reduce the occurrence of skin inflammation, effectively treat acne, and has a good market application prospect.

Description

Technical Field

[0001] This invention belongs to the field of skin care technology, specifically relating to a composition for treating acne and its preparation method. Background Technology

[0002] Acne, a chronic inflammatory skin disease affecting the pilosebaceous unit, is prevalent among adolescents and young adults. Its pathological mechanism involves the synergistic effects of multiple factors, including abnormal keratinization of the pilosebaceous duct, excessive sebum secretion, and microbial colonization. Clinically, it manifests as diverse skin lesions such as comedones, papules, and cysts in areas rich in sebaceous glands, such as the face, chest, and back. Prolonged disease progression can lead to scarring and psychological distress, severely impacting patients' quality of life.

[0003] Microbiome dysbiosis is a core component of acne pathogenesis, with the Gram-positive anaerobic bacterium *Propionibacterium acnes* widely recognized as a key pathogen. This bacterium catalyzes the breakdown of sebum triglycerides into keratinizing free fatty acids by secreting extracellular enzymes such as lipases, proteases, and hyaluronidase. Simultaneously, it induces the release of pro-inflammatory factors (such as IL-1β and TNF-α), exacerbating excessive keratinization of the follicular epithelium and local inflammatory responses. Furthermore, the symbiotic relationship between *Staphylococcus* and *Malassezia furfur* may also synergistically worsen the condition.

[0004] Currently, topical acne treatments are widely used as a non-invasive prevention and treatment method. However, existing product formulations mostly rely on chemically synthesized bactericides (such as benzoyl peroxide and triclosan) and keratolytic agents (such as salicylic acid). Although these can inhibit the proliferation of pathogens and unclog hair follicles in the short term, long-term use can easily lead to irritation reactions such as impaired skin barrier function, erythema, and desquamation. In addition, the overuse of antibiotic ingredients may lead to the spread of drug-resistant Propionibacterium acnes strains.

[0005] Therefore, developing products containing naturally derived acne-fighting active ingredients that combine highly effective antibacterial activity with low skin irritation has become a pressing technical challenge in the fields of dermatology and cosmetics. Summary of the Invention

[0006] To overcome the shortcomings of the prior art, the present invention aims to provide a composition containing plant extracts and probiotic metabolites with natural and bio-derived active ingredients, which can replace traditional chemically synthesized bactericides, reduce the risk of damage to the skin barrier, reduce adverse reactions such as erythema and desquamation, and the composition can effectively inhibit the growth of Propionibacterium acnes, soothe inflammation, and has a significant therapeutic effect on acne.

[0007] To achieve the above objectives, the present invention discloses the following technical solutions:

[0008] In a first aspect, the present invention provides a composition for treating acne, wherein the composition comprises, by weight percentage:

[0009] Lactobacillus fermentation products 1-2%;

[0010] Plant extract components 5-8%;

[0011] The plant extracts consist of European red pine leaf extract, celery root extract, and aster extract.

[0012] Preferably, the mass ratio of the European red pine leaf extract, the celery root extract and the aster extract is 1:(1-3):(5-10).

[0013] Preferably, the composition further comprises the following components:

[0014] Base oils, salicylic acid, emulsifiers, chelating agents, humectants, preservatives, and solvents.

[0015] More preferably, the amount of base oil added to the composition is 1-2 wt%;

[0016] The base oil is selected from at least one of isononyl isononanoate, caprylic / capric triglyceride, and coconut oil alcohol-caprylate / capric ester.

[0017] More preferably, the amount of salicylic acid added in the composition is 0.1-0.2 wt%.

[0018] More preferably, the amount of emulsifier added to the composition is 0.1-0.3 wt%;

[0019] The emulsifier is selected from at least one of cocoyl glucoside, polyglycerol-6 behenate, and PEG-100 glyceryl stearate.

[0020] More preferably, the amount of chelating agent added to the composition is 0.01-0.02 wt%;

[0021] The chelating agent is selected from disodium EDTA.

[0022] More preferably, the amount of humectant added to the composition is 1-5 wt%;

[0023] The amount of preservative added in the composition is 0.1-0.5 wt%.

[0024] The moisturizer is selected from at least one of glycerin, 1,3-propanediol, and butylene glycol;

[0025] The preservative is selected from at least one of p-hydroxyacetophenone, capryloyl hydroxamic acid, and ethylhexylglycerin.

[0026] More preferably, the solvent in the composition is deionized water.

[0027] In a second aspect, the present invention provides a method for preparing the acne treatment composition described in the first aspect, comprising the following steps:

[0028] Step 1. Stir the emulsifier and base oil at 80-90℃ and 300-500r / min until homogeneous to obtain solution A;

[0029] Step 2. Stir the preservative, chelating agent, humectant and deionized water at 80-90℃ and 300-500r / min until homogeneous to obtain solution B;

[0030] Step 3. At 80-90℃, add solution A to solution B, first homogenize and disperse at 10000-15000 r / min for 10-15 min, then stir at 200-300 r / min for 40-50 min to obtain mixture C;

[0031] Step 4. After cooling mixture C to 45-50℃, add lactobacillus fermentation product, plant extract, and salicylic acid in sequence, and stir at 200-300r / min for 13-20min to obtain the composition for treating acne.

[0032] In this invention:

[0033] European red pine leaf extract inhibits the proliferation of Propionibacterium acnes through terpenoids (such as α-pinene) and polyphenols, reducing key pathogens that cause acne. Flavonoids (such as quercetin) and pinoresinin can regulate inflammatory signaling pathways (such as NF-κB), reduce the release of pro-inflammatory factors (IL-6, TNF-α), and alleviate redness and inflammation. Simultaneously, antioxidants such as proanthocyanidins neutralize free radicals, reduce oxidative stress damage, and promote skin repair to reduce acne scars. Furthermore, its potential astringent and trace element properties may help regulate sebum secretion and improve clogged pores.

[0034] Celery root extract is rich in flavonoids (such as apigenin), which can inhibit the release of inflammatory factors such as IL-6 and TNF-α, and reduce skin inflammation by regulating signaling pathways such as NF-κB. This helps to relieve symptoms such as redness and pain caused by acne. The flavonoids in celery root extract also have significant antioxidant capacity, which can scavenge free radicals, reduce oxidative stress damage to the skin, promote skin metabolism and repair the skin barrier, and accelerate the fading of acne scars.

[0035] Aster extract mainly contains flavonoids, triterpenoids, steroids, and other compounds. It has antioxidant properties, which can scavenge free radicals, reduce damage to skin cells, and delay aging; it has anti-inflammatory properties, which can reduce skin inflammation and relieve redness, swelling, and itching; it has moisturizing properties, which help the skin retain moisture and improve dryness and peeling; it has antibacterial properties, which can inhibit the growth of harmful bacteria on the skin surface and prevent acne and skin infections; as a skin protectant, it can isolate the skin from external environmental damage and enhance the skin's barrier function.

[0036] The beneficial effects of this invention are:

[0037] 1. The celery root extract, red pine leaf extract, and aster extract in the composition of the present invention can produce a synergistic effect in the treatment of acne; thus, the provided acne treatment composition can effectively inhibit the growth of Propionibacterium acnes, reduce the occurrence of skin inflammation, and thereby effectively treat acne.

[0038] 2. The acne treatment composition provided by the present invention can promote the metabolism of the stratum corneum of the skin, improve facial luster, and repair acne-damaged skin, and has significant effects in removing acne, inhibiting acne, inhibiting bacteria, and reducing inflammation. Detailed Implementation

[0039] To better illustrate the objectives, technical solutions, and advantages of this invention, the invention will be further described below with reference to specific embodiments. Those skilled in the art should understand that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention.

[0040] Unless otherwise specified, the test methods used in the examples and comparative examples are conventional methods; the materials and reagents used are commercially available unless otherwise specified; and the percentages mentioned in the examples and comparative examples are mass percentages unless otherwise specified.

[0041] In this invention:

[0042] Lactobacillus fermentation products: purchased from Guangzhou Huayang Biotechnology Co., Ltd.;

[0043] European red pine leaf extract: purchased from Shenzhen Ruijite Biotechnology Co., Ltd.;

[0044] Celery root extract: purchased from New Horizon Biotechnology Co., Ltd.;

[0045] Aster extract: purchased from Xinyanghe Biotechnology Co., Ltd.

[0046] Preparation of acne treatment composition:

[0047] Weigh the raw materials precisely according to the mass percentage in Table 2;

[0048] Step 1. Stir the emulsifier and base oil at 80-90℃ and 300-500r / min until homogeneous to obtain solution A;

[0049] Step 2. Stir the preservative, chelating agent, humectant and deionized water at 80-90℃ and 300-500r / min until homogeneous to obtain solution B;

[0050] Step 3. At 80-90℃, add solution A to solution B, first homogenize and disperse at 10000-15000 r / min for 10-15 min, then stir at 200-300 r / min for 40-50 min to obtain mixture C;

[0051] Step 4. After cooling mixture C to 45-50℃, add lactobacillus fermentation product, plant extract, and salicylic acid in sequence, and stir at 200-300r / min for 13-20min to obtain the composition for treating acne.

[0052] The plant extract components are compounded according to the mass ratios in Table 1:

[0053] Table 1. Mass ratio of raw materials for plant extract components

[0054]

[0055] Note: " / " in the table indicates no addition.

[0056] Table 2. Raw material components and their mass percentage in the composition for treating acne.

[0057]

[0058] Note: " / " in the table indicates no addition.

[0059] To verify the impact of key ingredients in the examples on the overall acne-removing and acne-suppressing performance of the formula, adjustments were made to the ingredients or their proportions based on the formula of Example 3, as follows:

[0060] Table 3. Comparative Example Compositions and Their Mass Percentages

[0061]

[0062]

[0063] Performance testing

[0064] 1. Sample stability test:

[0065] 1. Heat resistance test: The constant temperature incubator was adjusted to 40℃. The four examples and five comparative examples prepared above were used as nine test samples. Three samples of each test sample were placed in a transparent glass bottle with a sample volume of 20ml / bottle. After sealing, the bottle was placed in the constant temperature incubator. After three months, the bottle was taken out, allowed to return to room temperature, and the appearance changes were observed.

[0066] 2. Cold resistance test: The constant temperature incubator was adjusted to -10℃. The four examples and five comparative examples prepared above were used as nine test samples. Three samples of each test sample were placed in a transparent glass bottle with a sample volume of 20ml / bottle. After sealing, the bottles were placed in the constant temperature incubator. After three months, the bottles were taken out, allowed to return to room temperature, and the appearance changes were observed.

[0067] 3. Room temperature test: The four examples and five comparative examples prepared above were used as nine test samples. Three samples of each test sample were placed in a transparent glass bottle with a sample volume of 20 ml / bottle. After sealing, the bottles were placed at room temperature for 6 months, and the appearance changes of the samples were observed.

[0068] No precipitation or sedimentation was observed in the heat resistance test, cold resistance test, or room temperature test, and the original appearance was maintained.

[0069] 2. Human skin patch test:

[0070] Human skin occlusive patch testing was conducted in accordance with the human skin patch test requirements specified in the "Cosmetic Safety Technical Specifications".

[0071] 2.1 Test objective: To detect the potential for the test substance to cause adverse skin reactions in humans.

[0072] 2.2 Test Design: A patch containing the test substance was applied to the skin on the back of the subject for 24 hours. The skin was scored according to the skin reaction grading standard for closed patch tests at 30 minutes (after the indentation disappeared), 24 hours, and 48 hours after the patch was removed.

[0073] 2.3 Test substances: Compositions prepared in Examples 1-4 and Comparative Examples 1-5.

[0074] 2.4 Test Method:

[0075] Volunteer requirements: Select volunteers aged 18-60 who meet the trial requirements as subjects, and randomly assign them to groups of 30 people each;

[0076] Test procedure: Select an area not exceeding 50mm² 2 A qualified spot test kit with a depth of approximately 1 mm. Place the test substance into the small chamber of the spot test kit, using approximately 0.02 mL to 0.025 mL. Apply the spot test kit containing the test substance to the back of the subject using low-sensitivity adhesive tape, and gently press it with the palm of your hand to ensure even adhesion to the skin, leaving it on for 24 hours.

[0077] Skin reactions were observed according to the standards in Table 4 at 30 min (after the indentation disappeared), 24 h and 48 h after the removal of the test sample applicator, and the results were recorded. The results are shown in Table 5.

[0078] Table 4. Grading Criteria for Skin Reactions in Closed Patch Tests

[0079]

[0080] Table 5 Results of Human Safety Tests

[0081]

[0082]

[0083] In vitro inhibition test of samples against Propionibacterium acnes:

[0084] Test samples: Examples 1-4 and Comparative Examples 1-5.

[0085] The third generation of Propionibacterium acnes (ATCC6919) was selected as the test strain, and the antibacterial test was carried out according to "5.1.2 Quantitative antibacterial test by carrier immersion" in WS / T 650—2019 "Evaluation method for antibacterial and antimicrobial effects".

[0086] Take 10 μL of bacterial suspension (5.0 × 10⁻⁶) 6 ~5.0×10 7 CFU / mL) was placed on a sterile carrier and air-dried at room temperature for later use. 5g / tablet of test sample was weighed into a sterile Petri dish and placed in a 20℃ water bath for 5 min. The infected carrier was completely immersed in the sample, and the time was immediately started. After 15 min and 30 min of treatment, each infected carrier was added to 5.0 mL of PBS buffer and shaken to wash off the test bacteria. 1.0 mL of sample solution was taken from each dish, and the number of surviving bacteria was determined according to the viable bacteria culture counting method. Two Petri dishes were inoculated from each sample solution. All the Petri dishes were placed at 37℃ and anaerobically cultured for 72 h to observe the results. A positive control group was set up for each test sample (the positive controls for each group were those for Examples 1-4 and Comparative Examples 1-5, respectively, which lacked Lactobacillus fermentation products and plant extracts). The experiment was repeated 3 times, and the inhibition rate (X) was calculated according to formula (1). The results are shown in Table 6.

[0087]

[0088] In the formula:

[0089] G0: Average total bacterial count in the positive control group, CFU / plate;

[0090] G1: Average total bacterial count of the sample group, CFU / slab.

[0091] Table 6 Antibacterial Results

[0092]

[0093] Anti-inflammatory performance test

[0094] Test substances: compositions prepared in Examples 1-4 and Comparative Examples 1-5, and dexamethasone.

[0095] LPS-stimulated macrophages are a classic cell model for studying inflammatory pathways. The level of inflammation suppression by the test substance was evaluated by comparing the levels of pro-inflammatory factors TNF-α and IL-1β secreted by macrophages in the negative control group and the sample group.

[0096] Before testing, the cell viability was ≥90% was selected as the safe range for the test substance by cytotoxicity assay (MTT method), and the safe dosing concentration of the test substance was determined as the working concentration (the unified working concentration for the examples and comparative examples was 3 mg / mL, and for dexamethasone it was 100 μg / mL).

[0097] Resuscitated mouse macrophages were seeded into 6-well plates and cultured in an incubator (37°C, 5 v / v% CO2) for 24 h. The old cell culture medium in the wells was then aspirated.

[0098] Sample group: Add 2 mL of cell culture medium containing the working concentration of the compositions prepared in Examples 1-4 and Comparative Examples 1-5 to each well;

[0099] Negative control group: Add 2 mL of cell culture medium without any test substance to each well;

[0100] Positive control group: 2 mL of cell culture medium containing a safe dosage concentration of dexamethasone was added to each well;

[0101] After administration, the 6-well plates of the different groups were placed in an incubator and incubated for 2 hours. Then, 200 μL of working solution containing 1 μg / mL lipopolysaccharide (LPS) was added to each well of each group and the plates were incubated for another 22 hours.

[0102] After incubation, the cell culture medium was collected and the contents of IL-1β and TNF-α were detected according to the ELISA kit instructions. Each group of experiments was repeated 3 times and the average value was taken. The inhibition rate of IL-1β and TNF-α was calculated according to formula (2). The results are shown in Table 7.

[0103]

[0104] In the formula:

[0105] S: IL-1β / TNF-α inhibition rate;

[0106] T0: Average IL-1β / TNF-α ratio in the negative control group;

[0107] T1: Average IL-1β / TNF-α content in the drug-treated (sample or positive control) group.

[0108] Table 7 Anti-inflammatory performance test

[0109]

[0110]

[0111] Conclusion Analysis:

[0112] According to the data in Table 7, the positive control group showed the best results, indicating the effectiveness of the experimental method. The inhibition rates of IL-1β and TNF-α in Example 3 were higher than those in other examples and comparative examples, indicating that the formulation of Example 3 performed best in anti-inflammatory effects. Comparative Examples 1-3 lacked celery root extract, red pine leaf extract, and aster extract, respectively. The results showed that the antibacterial and anti-inflammatory effects of Comparative Examples 1-3 were significantly weaker, and Comparative Example 2 had the lowest inhibition rate of inflammatory factors, indicating that celery root extract, red pine leaf extract, and aster extract produced a synergistic effect in the overall formulation.

[0113] The mass ratios of celery root extract, red pine leaf extract, and aster extract in Comparative Examples 4 and 5 are not within the preferred mass ratio range of this invention. The results show that the inflammatory factor inhibition rates of Comparative Examples 4 and 5 are lower than those of Examples 1-4, but higher than those of Comparative Examples 1-3. This reflects that although the proportions of the three plant extract components have been adjusted, the effect of the combination with all three components is still better than the effect without the components. However, their IL-1β and TNF-α inhibition rates are significantly lower than those of the examples, indicating that the mass ratios of celery root extract, red pine leaf extract, and aster extract also play an important role in the overall formulation.

[0114] Human efficacy test

[0115] Subjects: Fifty-four male volunteers aged 20-35 years were recruited, consisting of six people in each group, who had obvious bilateral facial acne in the nascent or inflammatory stage and whose facial skin was prone to acne. Subjects were excluded from using immunosuppressants or antihistamines, using other facial acne treatment products within the past month, having serious systemic diseases, currently using systemic medications, or being sensitive to drug allergies.

[0116] Test samples: Compositions prepared in Examples 1-4 and Comparative Examples 1-5.

[0117] Testing Procedure: Discontinue use of similar products 5 days prior to the start of the test. After the test begins, cleanse your face morning and evening, apply toner, and then use 5ml of the sample, applying it evenly to your face. Continue this treatment for 28 consecutive days.

[0118] 1. Facial microbial activity

[0119] Porphyrins are substances secreted by Propionibacterium acnes, and the amount of porphyrin fluorescence can indirectly reflect the quantity of Propionibacterium acnes. Images of the subjects' faces were acquired using VISIA, and the porphyrin values ​​on the faces were analyzed using image analysis software. The values ​​were recorded on day 1 and day 28.

[0120] Formula for calculating ΔT: ΔT = T 28 -T1

[0121] T 28 Average porphyrin levels in each group on day 28;

[0122] T1: Average porphyrin value for each group on day 1.

[0123] 2. Skin hemoglobin content

[0124] The E value in the skin represents the heme content in the skin. The higher the E value in the acne area, the more severe the inflammation at the acne site, and vice versa. The face of the test subject was measured using the MX18 probe from the German company CK with heme testing, and the values ​​were recorded on day 1 and day 28.

[0125] Formula for calculating ΔE: ΔE = E 28 -E1

[0126] E 28 Average E value for each group on day 28;

[0127] E1: Average E value for each group on day 1.

[0128] The results of the human efficacy test are shown in Table 8.

[0129] Table 8 Results of Human Efficacy Test

[0130]

[0131] Test Result Analysis:

[0132] As can be seen from Table 8, Examples 1-4 showed significantly better inhibitory effects on Propionibacterium acnes than Comparative Examples 1-5, indicating that the composition for treating acne provided by the present invention has excellent ability to inhibit Propionibacterium acnes. Compared with Comparative Examples 1-5, Example 3 showed significantly better antibacterial effects, indicating that the addition of European red pine leaf extract, celery root extract, and aster extract in the composition for treating acne, as well as their specific mass ratio, has a synergistic effect in antibacterial and anti-inflammatory aspects.

[0133] According to the results of human efficacy tests, the acne treatment composition provided by this invention can effectively inhibit the growth of bacteria on the skin surface and reduce the occurrence of skin inflammation. Satisfaction surveys were conducted on subjects using the products of Examples 1-4. Subjects reported no facial discomfort after 28 days of product use, significant improvement in facial itching, enhanced skin radiance, lighter acne scars, and significant reduction in acne inflammation. These results demonstrate that the acne treatment composition provided by this invention can promote the metabolism of the stratum corneum, improve facial radiance, repair acne-damaged skin, and has significant acne-removing, anti-acne, antibacterial, and anti-inflammatory effects.

[0134] Finally, it should be noted that the above descriptions are merely preferred embodiments of the present invention and are not intended to limit the present invention. Although the present invention has been described in detail with reference to the foregoing embodiments, those skilled in the art can still modify the technical solutions described in the foregoing embodiments or make equivalent substitutions for some of the technical features. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the protection scope of the present invention.

Claims

1. A composition for treating acne, characterized in that, The composition comprises the following components by weight percentage: Lactobacillus fermentation products 1-2%; Plant extract components 5-8%; The plant extract components consist of European red pine leaf extract, celery root extract and aster extract; The mass ratio of the European red pine leaf extract, the celery root extract and the aster extract is 1:(1-3):(5-10).

2. The composition for treating acne according to claim 1, characterized in that, The composition also contains the following components: Base oils, salicylic acid, emulsifiers, chelating agents, humectants, preservatives, and solvents.

3. The composition for treating acne according to claim 2, characterized in that, The amount of base oil added in the composition is 1-2 wt%; The base oil is selected from at least one of isononyl isononanoate, caprylic / capric triglyceride, and coconut oil alcohol-caprylate / capric ester.

4. The composition for treating acne according to claim 2, characterized in that, The amount of salicylic acid added in the composition is 0.1-0.2 wt%.

5. The composition for treating acne according to claim 2, characterized in that, The amount of emulsifier added in the composition is 0.1-0.3 wt%; The emulsifier is selected from at least one of cocoyl glucoside, polyglycerol-6 behenate, and PEG-100 glyceryl stearate.

6. The composition for treating acne according to claim 2, characterized in that, The amount of chelating agent added in the composition is 0.01-0.02 wt%; The chelating agent is selected from disodium EDTA.

7. The composition for treating acne according to claim 2, characterized in that, The amount of moisturizer added in the composition is 1-5 wt%; The amount of preservative added in the composition is 0.1-0.5 wt%; The moisturizer is selected from at least one of glycerin, 1,3-propanediol, and butylene glycol; The preservative is selected from at least one of p-hydroxyacetophenone, capryloyl hydroxamic acid, and ethylhexylglycerin.

8. The composition for treating acne according to claim 2, characterized in that, The solvent in the composition is deionized water.

9. A method for preparing the composition for treating acne according to claim 8, characterized in that, Includes the following steps: Step 1. Stir the emulsifier and base oil at 80-90℃ and 300-500r / min until homogeneous to obtain solution A; Step 2. Stir the preservative, chelating agent, humectant and deionized water at 80-90℃ and 300-500r / min until homogeneous to obtain solution B; Step 3. At 80-90℃, add solution A to solution B, first homogenize and disperse at 10000-15000 r / min for 10-15 min, then stir at 200-300 r / min for 40-50 min to obtain mixture C; Step 4. After cooling mixture C to 45-50℃, add lactobacillus fermentation product, plant extract, and salicylic acid in sequence, and stir at 200-300r / min for 13-20min to obtain the composition for treating acne.

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