Acne removal composition as well as preparation method and application thereof
Through the synergistic effect of colloidal sulfur and lipoic acid supramolecules, an acne-removing composition with a double-wrapped structure is formed, which solves the problems of existing acne-removing compositions such as treatment without prevention, slow onset, and high irritation, and achieves rapid and effective acne removal and long-term prevention. The components are simple and skin-friendly.
Patent Information
- Application Number
- CN202510902666.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-07-01
- Publication Date
- 2025-09-19
AI Technical Summary
Existing acne-removing compositions have the problems of treating but not preventing, slow onset of effect, short duration, high irritation, and heavy burden on the skin. They fail to effectively prevent the recurrence of acne and have complex components.
The acne-removing composition adopts the synergistic effect of colloidal sulfur and lipoic acid supramolecular, forms a double-wrapped structure through physical coating and chemical cross-linking, and combines microencapsulation technology and supramolecular technology to control oil secretion, unclog pores, inhibit the proliferation of Propionibacterium acnes and reduce skin inflammation, achieving a combined preventive and therapeutic acne-removing effect.
It combines prevention and treatment to prevent recurrence of acne. It has a fast onset and long duration of effect. Its components are simple, mild and non-irritating, which significantly improves the effect of acne removal.
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Abstract
Description
Technical Field
[0001] The present invention belongs to the field of cosmetics, and in particular relates to an anti-acne composition, a preparation method and an application thereof. Background Art
[0002] Acne is a common, chronic inflammatory skin disease that most commonly affects adolescents (aged 12-24, affecting approximately 85%) with active sebaceous glands. The incidence in adults, particularly women, can reach 20-40%, primarily on the face, back, and chest. Acne not only affects appearance, causing acne, papules, and pustules, but can also lead to hyperpigmentation and permanent scarring. Acne also significantly impacts patients' psychological well-being, often triggering negative emotions such as low self-esteem, anxiety, and depression, impacting social interaction and quality of life. In severe cases, recurrent infections can lead to skin damage, complicating treatment. Therefore, timely, standardized treatment and appropriate nursing care are crucial to minimizing the harm caused by acne.
[0003] Modern medical research shows that the main factors that cause acne include excessive sebum secretion, abnormal keratinization of hair follicles, infection with Propionibacterium acnes, inflammatory response, genetic and hormonal factors, and environmental and lifestyle factors. Correspondingly, the treatment of acne-prone skin also focuses on regulating sebum secretion, improving abnormal keratinization of hair follicles, antibacterial and anti-inflammatory, hormone regulation, and lifestyle intervention. Most of the existing acne-removing compositions have the following defects: 1. Treatment, not prevention: An analysis of acne-removing compositions reveals that their core principles focus on inhibiting oil secretion, unclogging hair follicles, and achieving antibacterial and anti-inflammatory effects. This is a conventional approach and solution, and there's nothing wrong with it. However, recurring acne outbreaks create additional annoyance and burden for consumers, requiring not only frequent use of acne-removing products but also physical and psychological stress. Unfortunately, acne-removing compositions rarely address the combined approach of acne prevention and treatment. This is partly due to the inherent difficulty of acne prevention, and partly because attention is focused on acne treatment, leaving less attention on acne prevention.
[0004] 2. Slow onset and short duration of effect: Current acne-removing compositions are often composed of various extracts, which combine their efficacy to achieve acne removal. While these ingredients can achieve acne-removing effects, the active ingredients often exhibit slow onset and are easily oxidized and inactivated in the natural environment. This results in a slow onset and short duration of acne-removing effects, resulting in ineffective acne removal.
[0005] 3. High irritation and heavy burden on the skin: To address clogged pores and abnormal keratinization of hair follicles, many acne-fighting compositions often use various acidic ingredients to exfoliate and address pore issues. However, acidic substances are highly irritating and burdensome to already damaged acne-prone skin. Furthermore, some acne-fighting compositions contain nearly ten or even more ingredients. This complex composition also increases the burden on the skin and hinders its recovery. Summary of the Invention
[0006] The technical problem to be solved by the present invention is to overcome the deficiencies and defects mentioned in the above background technology, and provide an acne-removing composition that combines prevention and treatment, prevents recurrent acne attacks, has significant efficacy, fast onset, long duration, streamlined components, and is mild and non-irritating, as well as its preparation method and application.
[0007] In order to solve the above technical problems, the technical solution proposed by the present invention is: An acne-removing composition comprises the following components in parts by weight: 5-20 parts of colloidal sulfur homogenate; 0.05-5 parts of lipoic acid supramolecular; the solid content of the colloidal sulfur in the colloidal sulfur homogenate is 50-60%.
[0008] The acne-removing composition of the present invention utilizes the synergistic effects of colloidal sulfur and lipoic acid supramolecules to prevent and treat recurrent acne. It exhibits significant efficacy, rapid onset, long-lasting effect, a streamlined composition, and a mild, non-irritating nature. However, the dosage of each functional component must be properly controlled. If the dosage of a functional component is too low, the functional component's effect is not significant. Excessive dosage of a functional component, possibly due to excessive use of lipoic acid supramolecules and colloidal sulfur, can lead to a loss of skin function, resulting in an increase in acne rather than a decrease. More preferably, the acne-removing composition of the present invention comprises the following components in the following weight percentages: 10-14% colloidal sulfur homogenate, 0.2-0.5% lipoic acid supramolecules, and the balance water.
[0009] In the above-mentioned acne-removing composition, preferably, the colloidal sulfur is in a coating structure, and the coating structure is a physical coating layer of gum arabic. The use of a single coating structure is conducive to the full dispersion of the colloidal sulfur and the effectiveness of its action.
[0010] In the aforementioned acne-removing composition, the colloidal sulfur preferably has a multi-layer coating structure, comprising a physical coating layer of gum arabic on the sulfur surface and a chemical coating layer formed by cross-linking the gum arabic with a polyol and lipoic acid. This dual coating of physical coating and chemical cross-linking avoids the instability of a single physical coating, significantly improving the stability of the colloidal sulfur and contributing to its long-lasting and stable effect.
[0011] In the above-mentioned acne-removing composition, preferably, the lipoic acid supramolecule comprises cyclodextrin and a lipoic acid-matrine complex included in the cyclodextrin. The lipoic acid supramolecule can be an existing conventional component.
[0012] As a general technical concept, the present invention also provides a method for preparing the above-mentioned acne-removing composition, comprising the following steps: stirring and mixing colloidal sulfur homogenate and lipoic acid supramolecules in solvent water until uniformly mixed.
[0013] In the above preparation method, preferably, the colloidal sulfur has a multi-layer coating structure, and its preparation process comprises the following steps: uniformly dispersing sulfur powder in a gum arabic solution and stirring to obtain a dispersion; ball milling and filtering the dispersion to obtain a single-layer coated colloidal sulfur; adding lipoic acid and a polyol to the single-layer coated colloidal sulfur, stirring for reaction, and freeze-drying and crushing the reaction product to obtain a double-layer coated colloidal sulfur.
[0014] In the above preparation method, preferably, the gum arabic solution is an aqueous solution containing 1-20% gum arabic by mass; the gum arabic comprises high-viscosity gum arabic and low-viscosity gum arabic, the viscosity of the high-viscosity gum arabic aqueous solution being 500-2000 mPa.s, and the viscosity of the low-viscosity gum arabic aqueous solution being no more than 100 mPa.s; and the mass ratio of the high-viscosity gum arabic to the low-viscosity gum arabic is 1:(3-5). The present invention utilizes a combination of high-viscosity and low-viscosity gum arabic primarily to improve the sulfur encapsulation efficiency, mechanical properties, and chemical properties. High-viscosity gum arabic has a high viscosity and relatively low solubility in water (no more than 10%), while low-viscosity gum arabic has a low viscosity and a high solubility (up to 50% or more). Therefore, using low-viscosity gum arabic to encapsulate sulfur allows for a greater amount of gum arabic to be encapsulated around the sulfur. Furthermore, low-viscosity gum arabic has shorter chains, making it easier to coat the sulfur. A higher usage level exposes more active groups, making subsequent secondary cross-linking and double coating more likely to occur. However, high-viscosity gum arabic has longer chains, which, after coating, provides better mechanical properties and enhances stability. By properly controlling the amounts of high-viscosity and low-viscosity gum arabic, the coating efficiency, mechanical properties, and chemical properties can be guaranteed, significantly improving the stability of the colloidal sulfur and ensuring its long-lasting, stable effect, ensuring acne-removing results.
[0015] In the above preparation method, the amount of lipoic acid added is preferably 0.1-2% of the mass of the first layer of coated colloidal sulfur; and the mass ratio of lipoic acid to polyol is 1:(5-10). In the present invention, the addition of lipoic acid and polyol can chemically react with the gum arabic of the first coating layer, and their combined use yields enhanced results. The simultaneous use of lipoic acid and polyol ensures a more effective crosslinking reaction, allowing for better crosslinking with both high-viscosity and low-viscosity gum arabic. However, the ratio of lipoic acid to polyol must be appropriately controlled, and the amount of lipoic acid added should not be too high to avoid residual lipoic acid and the generation of an unpleasant odor.
[0016] The present invention uses lipoic acid and polyols as cross-linking agents to prepare a double-coated colloidal sulfur. The double-coated colloidal sulfur forms a double-coated structure outside the sulfur, making its chemical properties more stable and its sustained release effect stronger. The present invention uses physical coating and chemical cross-linking to form the double coating. First, a physical coating is formed on the outside of the sulfur using gum arabic. Then, lipoic acid and polyols are chemically reacted with the gum arabic to form a double coating. The double coating of physical coating and chemical cross-linking avoids the instability of single physical coating, can significantly improve the stability of the colloidal sulfur, help the colloidal sulfur exert its long-term and stable effect, and can better cooperate with the lipoic acid supramolecule to work. In addition, the present invention uses gum arabic, lipoic acid, and polyols to achieve the coating. These raw materials are conventional cosmetic raw materials and have high affinity for skin, no irritation problems, and higher safety.
[0017] As a general technical concept, the present invention also provides a use of the above-mentioned acne-removing composition in acne-removing cosmetics.
[0018] As a general technical concept, the present invention also provides a use of the above-mentioned acne-removing composition in acne-removing skin care products.
[0019] The acne-removing composition of the present invention is intended to provide a combination of preventive and therapeutic effects, preventing recurrent acne attacks with significant efficacy, rapid onset of action, long duration of action, streamlined components, and a mild, non-irritating effect. In terms of mechanism of action, the combination of colloidal sulfur and lipoic acid supramolecules can control oil secretion, unclog pores, inhibit the proliferation of Propionibacterium acnes, and reduce skin inflammation. This four-in-one acne-removing effect is bound to have significant acne-removing efficacy. In terms of onset and duration of action, the sustained-release sulfur of colloidal sulfur has the characteristics of rapid onset of action and direct and rapid antibacterial and anti-inflammatory effects. The combination of colloidal sulfur and lipoic acid supramolecules, and the integration of microencapsulation technology with supramolecule technology, can also achieve a long-lasting sustained release of the active ingredients. Furthermore, with the support of supramolecule technology, it can promote the transdermal absorption and penetration of lipoic acid, allowing it to penetrate into the inner layers of the skin even in skin with an intact barrier, further reducing skin inflammation. The sustained release of sulfur can also inhibit the abnormal proliferation of Propionibacterium acnes in hair follicles. The combination of the two can reduce recurrent acne attacks, achieving a combined preventive and therapeutic effect. In addition, the present invention has only two effective ingredients and no acidic ingredients are added. It has the characteristics of streamlined components, mildness and non-irritation, and is definitely more suitable for people with acne.
[0020] The advantages of this invention are mainly: 1. Combining prevention and treatment to prevent recurring acne: Conventional acne treatments often focus on resolving acne issues, but rarely address recurring acne and its prevention. This results in many consumers experiencing recurring acne after using acne treatments for a period of time. This can be due to factors such as hormones and lifestyle, or it can also be due to incomplete suppression of Propionibacterium acnes deep within the skin and incomplete elimination of inflammation.
[0021] This invention organically combines acne removal and prevention, using colloidal sulfur and lipoic acid supramolecular compounds as active ingredients to achieve both prevention and treatment, preventing recurrent acne. The sustained release of colloidal sulfur and lipoic acid supramolecular compounds directly and rapidly inhibits oil secretion, unclogs pores, and provides antibacterial and anti-inflammatory benefits, achieving acne-removing efficacy. The lipoic acid supramolecular technology also promotes transdermal penetration of lipoic acid, ensuring it reaches the inner layers of the skin and eliminates any residual inflammation. The sustained release of colloidal sulfur also prevents the abnormal proliferation of Propionibacterium acnes deep within hair follicles. This organic combination reduces the frequency of acne, achieving the goal of both prevention and treatment.
[0022] 2. Fast onset and long-lasting effect: Conventional acne-removing compositions often focus on acne removal efficiency, but rarely address the speed of acne removal. This is primarily because acne-removing compositions often contain active ingredients, making it difficult to achieve both a fast onset and long-lasting effectiveness. In the present invention, colloidal sulfur and lipoic acid supramolecules are organically combined. The sulfur released by the colloidal sulfur, combined with the lipoic acid sustained-released by the lipoic acid supramolecule, rapidly achieve antibacterial, anti-inflammatory, oil-control, and pore-unclogging effects. Both are encapsulated or supramolecules, enabling continuous, long-lasting sustained release. This long-term sustained release further enhances acne prevention, further strengthening the goal of combining prevention and treatment. Therefore, this composition not only has an extremely fast onset of action but also achieves long-lasting, sustained bactericidal and acne-removing effects.
[0023] 3. Significant efficacy: Analyzing the mechanism of acne production, in addition to abnormal sebum secretion, clogged pores and abnormal proliferation of Propionibacterium acnes, the abnormal proliferation of Propionibacterium acnes will activate Toll receptors, causing the skin to produce multiple inflammatory factors and chemokines, causing skin inflammation, and inflammation will further aggravate the abnormal proliferation of Propionibacterium acnes. Therefore, in order to achieve efficient acne removal, the reduction of inflammatory factors is also a necessary pathway of action. The present invention combines the inhibition of oil secretion, exfoliation, unclogged pores, inhibition of Propionibacterium acnes and inhibition of skin inflammation, starting from the multiple dimensions of acne occurrence and development, and is bound to have a better acne removal effect.
[0024] 4. Component Streamlining: Many compositions require the use of multiple or even nearly ten functional ingredients to achieve the effects of inhibiting oil secretion, unclogging pores, and inhibiting bacterial proliferation. However, the increase in functional ingredients will inevitably increase the burden on the skin, especially acne skin, which is even more fragile and sensitive. The above composition may cause new skin problems. The present invention only has two components: colloidal sulfur and lipoic acid supramolecular. Sulfur is originally a classic ingredient for treating acne. After being wrapped in gum arabic, it is milder and easier to disperse. Lipoic acid itself is a mild raw material. After being treated with supramolecular technology, its stability is enhanced. The present invention organically combines the two functional ingredients, not only having an extremely streamlined functional composition, but also being able to achieve multi-dimensional acne treatment from four dimensions: inhibiting oil secretion, unclogging pores, inhibiting bacterial proliferation, and inhibiting skin inflammation. It is certain to have a wider range of application scenarios.
[0025] 5. Gentle and non-irritating: Many acne-removing compositions contain acidic substances such as fruit acid and salicylic acid to exfoliate. However, using acidic ingredients to exfoliate acne-prone skin, which already has a damaged barrier, can severely strain the skin barrier. The present invention contains no acidic, irritating ingredients. Both the colloidal sulfur and the lipoic acid supramolecular formulations utilize microencapsulation and supramolecular encapsulation technologies, respectively, improving the stability and applicability of the raw materials while further enhancing their mildness and preventing any additional burden on the skin. Therefore, the composition prepared by the present invention is gentle and non-irritating, making it widely applicable to acne-prone skin.
[0026] The acne-removing composition of the present invention comprises colloidal sulfur and lipoic acid supramolecules. The mechanism of action and target of each effective component are analyzed as follows: 1. Colloidal sulfur Colloidal sulfur is a microencapsulation of elemental sulfur. Its purpose is to increase sulfur's solubility in water, reduce its odor, and expand its application areas. With the advancement of science and technology, the preparation methods of colloidal sulfur have continued to improve. In the 1950s, researchers improved the dispersibility and stability of colloidal sulfur through chemical synthesis and physical methods (such as ultrasonic treatment). These improvements led to a wider application of colloidal sulfur in cosmetics, particularly in anti-acne and oil-control products. Entering the 21st century, with the increasing attention paid to skin care, the application areas of colloidal sulfur have continued to expand. In modern cosmetics, colloidal sulfur is not only used as an anti-acne ingredient, but is also added to anti-aging and whitening products. The development of colloidal sulfur reflects the progress of science and technology and the public's concern for skin health. From its initial physical and chemical research to its widespread application today, the contribution of colloidal sulfur to various fields cannot be ignored.
[0027] 2. Lipoic acid supramolecular Lipoic acid is a naturally occurring sulfur-containing organic compound with potent antioxidant properties. It is soluble in both water and lipids, exerting antioxidant effects both inside and outside cells. Its primary applications in cosmetics include: Lipoic acid scavenges various free radicals, reduces oxidative stress damage to skin cells, and delays skin aging, achieving antioxidant and anti-aging benefits. It also inhibits melanin production and promotes skin metabolism, helping to improve dull skin tone and achieve whitening and brightening effects. Furthermore, lipoic acid can reduce skin inflammation, promote skin barrier repair, and stimulate the regeneration of other antioxidants, making it a multi-functional skincare ingredient.
[0028] Lipoic acid supramoleculars combine lipoic acid with carriers such as cyclodextrins through supramolecular encapsulation and compounding techniques, creating a more stable and easily absorbed complex. This encapsulation effectively prevents oxidative decomposition of lipoic acid in formulations, extending product shelf life and improving lipoic acid stability. Furthermore, the supramolecular structure helps lipoic acid better penetrate the skin barrier, increasing the utilization rate of its active ingredients and enhancing permeability and bioavailability. Furthermore, encapsulation reduces the potential for skin irritation, making it suitable for use on sensitive skin. In summary, lipoic acid supramoleculars can effectively enhance stability and promote absorption, which has a positive impact on its application in cosmetics.
[0029] Compared with the prior art, the advantages of the present invention are: The preparation method and application of the acne-removing composition of the present invention provide a combination of prevention and treatment, preventing recurrent acne attacks, with significant efficacy, rapid onset of action, long duration, streamlined components, and a mild, non-irritating acne-removing composition. The present invention combines colloidal sulfur and lipoic acid supramolecules with synergistic effects to control oil secretion, unclog pores, inhibit the proliferation of Propionibacterium acnes, and reduce skin inflammation. This four-in-one acne-removing effect is bound to have significant acne-removing efficacy. The sustained-release sulfur of the colloidal sulfur has the characteristics of rapid onset of action and direct and rapid antibacterial and anti-inflammatory effects. The combination of colloidal sulfur and lipoic acid supramolecules, and the combination of microencapsulation technology and supramolecule technology, can also achieve a long-lasting sustained release of the active ingredients. In addition, with the support of supramolecule technology, the transdermal and absorption of lipoic acid can be promoted, even in skin with an intact barrier, it can penetrate into the inner layers of the skin and further reduce skin inflammation. The sustained-release sulfur can also inhibit the abnormal proliferation of Propionibacterium acnes in hair follicles. The combination of the two can reduce recurrent acne attacks, achieving a combination of prevention and treatment. In addition, the present invention has only two effective ingredients and no acidic ingredients are added. It has the characteristics of streamlined components, mildness and non-irritation, and is definitely more suitable for people with acne. DETAILED DESCRIPTION
[0030] In order to facilitate understanding of the present invention, the present invention will be described more comprehensively and meticulously below in conjunction with preferred embodiments, but the protection scope of the present invention is not limited to the following specific embodiments.
[0031] Unless otherwise defined, all technical terms used hereinafter have the same meanings as those generally understood by those skilled in the art. The technical terms used herein are only for the purpose of describing specific embodiments and are not intended to limit the scope of protection of the present invention.
[0032] Unless otherwise specified, various raw materials, reagents, instruments and equipment used in the present invention can be purchased from the market or prepared by existing methods.
[0033] Example 1: An anti-acne composition comprises the components in parts by weight as shown in Table 1. There are two methods for preparing colloidal sulfur, wherein the first method comprises the following steps: (1) Weigh 2 g of high-viscosity gum arabic (the viscosity of its aqueous solution is about 700-900 mPa.s, and there is a certain fluctuation during measurement), and then weigh 8 g of low-viscosity gum arabic (the viscosity of its aqueous solution is about less than 100 mPa.s, and there is a certain fluctuation during measurement), and prepare a 10% concentration aqueous solution. After dispersing into a transparent and uniform aqueous solution, add 100 g of sulfur and disperse it evenly to obtain a sulfur suspension.
[0034] (2) Adjust the ratio of the balls in the ball mill to a diameter (mm) ratio of 15:10:5:3 and a mass (g) ratio of 50:150:200:100. Place the sulfur suspension into the ball mill and adjust the speed to 500 rpm. After grinding for 12 h, separate the balls from the material using an 80-mesh filter to obtain colloidal sulfur.
[0035] (3) Accurately weigh 100 g of colloidal sulfur, then accurately weigh 0.2 g of lipoic acid and 1.2 g of butanediol, uniformly disperse the lipoic acid in the butanediol, then add the dispersion to the colloidal sulfur, and stir at 45°C for 2 h. The reaction product is freeze-dried and crushed to obtain colloidal sulfur. Water is added to the colloidal sulfur to a solid content of about 55%, to obtain a colloidal sulfur slurry, which is recorded as colloidal sulfur slurry I.
[0036] Preparation method 2 comprises the following steps: (1) Weigh 2 g of high-viscosity gum arabic (the viscosity of its aqueous solution is about 700-900 mPa.s, and there is a certain fluctuation during measurement), and then weigh 8 g of low-viscosity gum arabic (the viscosity of its aqueous solution is about less than 100 mPa.s, and there is a certain fluctuation during measurement), and prepare a 10% concentration aqueous solution. After dispersing into a transparent and uniform aqueous solution, add 100 g of sulfur and disperse it evenly to obtain a sulfur suspension.
[0037] (2) Adjust the ratio of the balls in the ball mill to a diameter (mm) ratio of 15:10:5:3 and a mass (g) ratio of 50:150:200:100. The sulfur suspension was placed in a ball mill at a speed of 500 rpm. After milling for 12 h, the balls were separated from the material using an 80-mesh filter. The reaction product was freeze-dried and crushed to obtain colloidal sulfur. Water was added to the colloidal sulfur to a solids content of approximately 55% to obtain a colloidal sulfur slurry, designated as colloidal sulfur slurry II.
[0038] The lipoic acid supramolecule was prepared by referring to the description in Example 1 of patent CN116350540B.
[0039] When preparing the anti-acne composition, the colloidal sulfur homogenate and the lipoic acid supramolecular are added with water and stirred and mixed uniformly.
[0040] Example 2-5: The main difference between Examples 2-5 and Example 1 is the different raw material compositions and ratios, as shown in Table 1 below.
[0041] Comparative Examples 1-3: The main difference between Comparative Examples 1-3 and Example 1 is the different raw material compositions and ratios, as shown in Table 1 below.
[0042] Table 1: Raw material composition and ratio of Examples and Comparative Examples (unit: g)
[0043] The performance tests of the anti-acne compositions in Examples 1-5 and Comparative Examples 1-3 were conducted as follows: 1. Instant antibacterial effect 1) Test Principle The P. acnes inhibition test is primarily used to evaluate the inhibitory effect of a substance on P. acnes. The basic principle is to co-incubate the test sample with P. acnes and observe bacterial growth to determine the sample's antibacterial effect. In this experiment, the test sample was co-incubated with P. acnes for 24 hours, then counted using the agar plate method, and the P. acnes inhibition rate was calculated.
[0044] 2) Test methods ① Co-culture of samples and strains: Prepare a liquid culture medium containing Propionibacterium acnes, dispense it into test tubes, add 1% of the sample to be tested (i.e., the anti-acne composition in Examples 1-5 and Comparative Examples 1-3), and sterilize it for later use. Add Propionibacterium acnes culture medium to the culture medium containing the sample to be tested so that the final bacterial concentration in the system is 10 5 -10 6 , placed in a 37℃ anaerobic incubator for 24h.
[0045] ②Count: The co-cultures were diluted and plated, incubated in an anaerobic incubator (37°C, 48 h) and counted.
[0046] 3) Test results Immediate antibacterial rate: I= (I1-I2) / I1*100%; Where: I is the long-term antibacterial rate, %; I1 is the number of colonies in the culture medium without antibacterial raw materials; I2 is the number of colonies in the culture medium with added antibacterial raw materials.
[0047] The experimental data are shown in Table 2 below: Table 2: Timely antibacterial rate
[0048] As can be seen from the above table, the antibacterial rates of colloidal sulfur and the composite samples at 24 hours are relatively high. The analysis data shows that the data is more than 99%. Only the antibacterial rate of lipoic acid supramolecular is relatively low. The above results show that the timely antibacterial rates of colloidal sulfur and lipoic acid are relatively high.
[0049] 2. Long-term antibacterial rate 1) Test Principle The P. acnes inhibition test is primarily used to evaluate the inhibitory effect of a substance on P. acnes. The basic principle is to co-incubate the test sample with P. acnes and observe bacterial growth to determine the sample's antibacterial effect. In this experiment, the test sample was co-incubated with P. acnes for 7 days, then counted using the agar plate method, and the P. acnes inhibition rate was calculated.
[0050] 2) Test methods ① Co-culture of samples and strains: Prepare a liquid culture medium containing Propionibacterium acnes, dispense it into test tubes, add 1% of the sample to be tested, and sterilize it for later use. Add Propionibacterium acnes bacterial solution to the culture medium containing the sample to be tested so that the final bacterial solution concentration in the system is 10 5 -10 6 , and cultured in a 37°C anaerobic incubator for 7 days.
[0051] ②Count: The co-cultures were diluted and plated, incubated in an anaerobic incubator (37°C, 48 h) and counted.
[0052] 3) Test results Long-term antibacterial rate: L= (L1-L2) / L1*100%; Where: L is the long-term antibacterial rate, %; L1 is the number of colonies in the culture medium without antibacterial raw materials; L2 is the number of colonies in the culture medium with added antibacterial raw materials.
[0053] The experimental data are shown in Table 3 below: Table 3: Long-term antibacterial rate
[0054] These results demonstrate that colloidal sulfur exhibits a robust, long-lasting antibacterial effect, exceeding 50%. However, Examples 3 and 4, which combine colloidal sulfur with lipoic acid supramolecules, exhibit significantly superior antibacterial effects compared to either material alone. The synergistic effect of the combination of colloidal sulfur and lipoic acid supramolecules is evident. In particular, colloidal sulfur I, obtained using Preparation Method 1, exhibits superior stability, a more uniform sustained release, and a longer duration, resulting in a more sustained, long-lasting antibacterial effect.
[0055] Combining the immediate and long-term inhibition rate data reveals that the sample exhibits excellent antibacterial efficacy initially, but the inhibition rate decreases significantly by the seventh day. This may be because when viable bacterial counts fall below the detection limit (e.g., <10 CFU / mL), they cannot be detected by conventional plate counts, but residual bacteria may proliferate to detectable levels during the incubation process. Furthermore, the amount of hydrogen sulfide released from the colloidal sulfur may decrease over the course of seven days, leading to a decrease in the antibacterial efficacy.
[0056] 3. Deep antibacterial rate 1) Test Principle Thoroughly mix the bacterial solution and agar medium. After the agar solidifies, add the antibacterial agent to the surface. The agent diffuses into the agar. Strong antibacterial agents or those with good permeability can achieve deep inhibition. Comparing the bacterial growth heights of different antibacterial agents can assess the differences in their antibacterial effectiveness. The deep inhibition rate is calculated by taking the difference in bacterial growth height before and after sample addition.
[0057] 2) Test methods Add Propionibacterium acnes bacterial solution to a 10mL sterile centrifuge tube, and add agar medium cooled to 45°C (0.8mL bacterial solution, add agar to the 8mL scale line to ensure that all samples are at the same height in the centrifuge tube). After it is completely solidified, add 200uL of antibacterial drug to the surface of the culture medium, with a sample concentration of 5%. After culturing for 48-72 hours, observe the growth of Propionibacterium acnes.
[0058] 3) Test results Deep antibacterial rate: D= (D1-D2) / D1*100%; Where: D is the long-term antibacterial rate, %; D1 is the bacterial growth height without adding test sample; D2 is the bacterial growth height after adding the test sample.
[0059] The experimental data are shown in Table 4 below: Table 4: Deep antibacterial rate
[0060] These results suggest that colloidal sulfur has a relatively modest deep-layer antibacterial effect, with an inhibition rate of no more than 10%. However, the deep-layer antibacterial rates achieved in Examples 3 and 4, where colloidal sulfur and lipoic acid supramolecules were combined, reached as high as over 20%, demonstrating a significant synergistic effect. Furthermore, these results demonstrate that the combination of colloidal sulfur and lipoic acid supramolecules facilitates the penetration of the antibacterial components, inhibiting bacterial growth and reproduction at deeper levels.
[0061] 4. Human clinical test - instant acne removal 1) Test Principle Antera 3D (Miravex Limited, Ireland) uses 24 LED lights of 7 different wavelengths for spatial and spectral analysis to reconstruct skin surface features and combines it with dedicated software to analyze skin surface features and color.
[0062] 2) Test methods On the day of the official trial, qualified participants arrived at the testing center, cleansed their faces with warm water, and sat quietly for 30 minutes in a constant temperature and humidity environment. A clinician selected a pimple as a target for a one-hour assessment, followed by the Antera3D test. Following the test, participants applied the test product as directed by a technician. After one hour, they washed the product off the pimple and repeated the Antera3D test. Three participants were assigned to each sample.
[0063] 3) Test results Acne volume improvement rate: M= (M1-M2) / M1*100%; Where: M is the volume improvement rate, %; M1 is the acne volume measurement before using the sample; M2 is the acne volume measurement value 1 hour after using the sample.
[0064] The experimental data are shown in Table 5 below: Table 5: Acne volume improvement rate
[0065] As shown in the table above, using either colloidal sulfur or lipoic acid supramolecular alone can improve acne volume to a certain extent, but the extent of improvement is limited. Combining the two significantly enhances the improvement rate.
[0066] 5. Human clinical testing - long-term acne removal 1) Test Principle Before using the acne treatment product, a professional dermatologist counted the number of facial acne spots, including papules, pustules, whiteheads, and blackheads. After seven days of regular use of the test sample, the clinician recounted the number of acne spots in the test area and statistically analyzed the overall change in the number of acne spots in the test area to determine the product's acne treatment efficacy.
[0067] 2) Test methods Qualified subjects will first undergo a 1-hour immediate efficacy test. After the follow-up visit on the 3rd day, each subject will receive the experimental product and usage diary, and go home to use the product for 7 consecutive days as required. A follow-up visit will be conducted after 7 days of use, and a professional doctor will evaluate various indicators.
[0068] 3) Test results Long-term acne removal rate: N= (N1-N2) / N1; Note: N is the long-term acne removal rate, %; N1: Total number of pimples in the test area before using the sample; N2 is the total number of pimples in the test area after using the sample for 7 days.
[0069] The experimental data are shown in Table 6 below: Table 6: Long-term acne removal rate
[0070] As shown in the table above, colloidal sulfur or lipoic acid supramolecules alone have some efficacy in reducing the number of acne breakouts, but the effect is relatively limited. However, combined use of both significantly increases the acne breakout inhibition rate. Comparing the data from Example 3 with those from Comparative Examples 1 and 3 demonstrates a significant synergistic effect.
[0071] 6. Human clinical trials - preventive effects 1) Test Principle Before using the acne treatment product, a professional dermatologist counted the number of facial acne spots, including papules, pustules, whiteheads, and blackheads. After using the test sample normally for 7 days and then stopping the product for 14 days, the subjects returned to the testing center for a recount of acne spots by a clinician. The overall change in acne count in the test area was statistically analyzed to determine the product's effectiveness in preventing acne recurrence.
[0072] 2) Test methods Qualified subjects were screened and first underwent a 1-hour immediate efficacy test. After the follow-up visit on the third day, each subject received the experimental product and a usage diary. They were required to go home and use the product for 7 consecutive days before stopping the use. A follow-up visit was conducted 14 days after stopping the use, and a professional doctor evaluated various indicators.
[0073] 3) Test results Acne prevention rate: Z=(Z1-Z2) / Z1; Where: Z is the acne prevention rate, %; Z1: Total number of acne in the test area before using the sample; Z2 is the total number of pimples in the test area 14 days after stopping the use of the sample.
[0074] The experimental data are shown in Table 7 below: Table 7: Acne prevention rate
[0075] As shown in the table above, when colloidal sulfur or lipoic acid supramoleculars were used alone for 7 days followed by a 14-day break, the total number of acne cases decreased, albeit to a limited extent. This suggests that these ingredients have some effectiveness in inhibiting and preventing acne growth. When both ingredients were used together for 7 days followed by a 14-day break, the acne prevention rate was significantly improved. Furthermore, the dosage of colloidal sulfur or lipoic acid supramoleculars should be neither too high nor too low. For example, if the dosage of colloidal sulfur or lipoic acid supramoleculars is too high (as in Example 5), the excessive use of lipoic acid and colloidal sulfur may lead to a loss of skin function, resulting in an increase in acne cases rather than a decrease.
Claims
1. An anti-acne composition, characterized in that: The invention comprises the following components in parts by weight: 5-20 parts of colloidal sulfur homogenate; 0.05-5 parts of lipoic acid supramolecular; and the solid content of the colloidal sulfur in the colloidal sulfur homogenate is 50-60%.
2. The anti-acne composition according to claim 1, characterized in that The colloidal sulfur is a coating structure, and the coating structure is a physical coating layer of gum arabic.
3. The anti-acne composition according to claim 1, characterized in that The colloidal sulfur is a multi-layer coating structure, comprising a gum arabic physical coating layer located on the sulfur surface and a chemical coating layer located on the surface of the gum arabic physical coating layer. The chemical coating layer is obtained by cross-linking reaction of polyol and lipoic acid with gum arabic.
4. The anti-acne composition according to claim 1, characterized in that The lipoic acid supramolecule comprises cyclodextrin and a lipoic acid-matrine complex included in the cyclodextrin.
5. A method for preparing the anti-acne composition according to any one of claims 1 to 4, characterized in that: The method comprises the following steps: stirring and mixing colloidal sulfur homogenate and lipoic acid supramolecules in solvent water to obtain the product.
6. The preparation method according to claim 5, characterized in that The colloidal sulfur has a multi-layer coating structure, and its preparation process includes the following steps: uniformly dispersing sulfur powder in a gum arabic solution and stirring to obtain a dispersion; ball milling and filtering the dispersion to obtain a single-layer coated colloidal sulfur; adding lipoic acid and a polyol to the single-layer coated colloidal sulfur, stirring for reaction, and freeze-drying and crushing the reaction product to obtain a double-layer coated colloidal sulfur.
7. The preparation method according to claim 6, characterized in that The gum arabic solution is an aqueous solution with a mass fraction of gum arabic of 1-20%. The gum arabic includes high-viscosity gum arabic and low-viscosity gum arabic. The viscosity of the high-viscosity gum arabic aqueous solution is 500-2000 mPa.s, and the viscosity of the low-viscosity gum arabic aqueous solution does not exceed 100 mPa.s. The mass ratio of the high-viscosity gum arabic to the low-viscosity gum arabic is 1:(3-5).
8. The preparation method according to claim 6, characterized in that The added amount of the lipoic acid is 0.1-2% of the mass of the one-layer coated colloidal sulfur; the mass ratio of the lipoic acid to the polyol is 1:(5-10).
9. Use of the anti-acne composition according to any one of claims 1 to 4 or the anti-acne composition prepared by the preparation method according to any one of claims 5 to 8 in anti-acne cosmetics.
10. Use of the anti-acne composition according to any one of claims 1 to 4 or the anti-acne composition prepared by the preparation method according to any one of claims 5 to 8 in an anti-acne skin care product.