Oil control composition, use and skin care

Abstract

This invention belongs to the field of skin care technology and discloses an oil-controlling composition, its uses, and skin care products. The oil-controlling composition, by weight, comprises 0.5-1 parts of zinc PCA, 4-9 parts of niacinamide, 0.5-2 parts of pink passionflower extract, and 0.3-0.7 parts of acetyl tetrapeptide-5. The oil-controlling composition of this invention not only inhibits 5α-reductase activity but also promotes autophagy in sebaceous gland cells, thereby enhancing the oil-controlling efficacy of the composition.

Description

Technical Field

[0001] This invention relates to the field of skin care technology, specifically to an oil-controlling composition, its uses, and skin care products. Background Technology

[0002] The skin contains numerous sebaceous glands, which secrete oil that travels through the hair follicle sebaceous gland duct to the skin's surface, moisturizing it and helping to maintain a slightly acidic environment. Under normal circumstances, the sebum secreted by the sebaceous glands maintains the skin's moisture and integrity. However, with increasing environmental pollution, work and life stress, unhealthy habits such as staying up late, and puberty, sebum secretion increases abnormally. Excessive oil not only makes the skin look greasy but also easily leads to clogged pores, causing skin problems such as acne, blackheads, and pimples.

[0003] Most skincare products currently address excessive oil production by inhibiting 5α-reductase. For example, prior art 1: Chinese patent application 202110915319.7 discloses a balancing oil composition and its oil-controlling gel that inhibits 5α-reductase activity. This composition includes a solvent, thickener, moisturizer, preservative, esterifying agent, pH adjuster, and balancing oil composition. The preparation method of this formulation includes the following steps: S1: Accurately weigh each component in the formula and clean the production equipment; S2: Add the solvent, moisturizer, and thickener to an emulsifying pot, stir and heat to 85-90℃, homogenize for 3-5 minutes until completely dissolved, and sterilize at a constant temperature for 10 minutes; S3: Stir and cool to 70-75℃, add the preservative, stir for 3 minutes, and vacuum at a constant temperature to completely defoam; S4: Stir and cool to 40-45℃, add the pH adjuster, esterifying agent, and acne-prone skin conditioning composition sequentially, stir evenly, and the preparation is complete.

[0004] This patent application regulates excessive sebum secretion from sebaceous glands by inhibiting 5α-reductase activity, thereby achieving a water-oil balance.

[0005] 5α-reductase is a membrane protease that depends on reduced coenzyme II (NADPH). It is an important androgen metabolic enzyme in the skin and can irreversibly convert testosterone into dihydrotestosterone (DHT). DHT can induce excessive sebum secretion from the sebaceous glands. By inhibiting the activity of 5α-reductase to reduce DHT levels, excessive sebum secretion from the sebaceous glands can be effectively relieved.

[0006] Currently, many existing technologies achieve oil control by inhibiting 5α-reductase, and rarely address the problem of excessive sebum secretion from sebaceous glands through other means. Achieving excellent oil control in one direction requires high concentrations of active ingredients, which is costly and can easily lead to skin safety issues. Summary of the Invention

[0007] One of the objectives of this invention is to provide an oil-controlling composition that regulates sebum secretion from sebaceous glands by inhibiting 5α-reductase activity and promoting autophagy in sebaceous gland cells, thereby effectively improving the oil-controlling effect of the composition and effectively avoiding the cost and skin safety issues caused by achieving oil control efficacy in a single direction.

[0008] Another objective of this invention is to provide a use for an oil-controlling composition, which, when used in the preparation of skincare products, can effectively prevent excessive sebum secretion from the sebaceous glands, thereby reducing clogged pores and skin problems such as acne, blackheads, and pimples.

[0009] Another objective of this invention is to provide a skincare product containing the oil-controlling composition of this invention, which can control oil in multiple directions, bringing more oil-controlling options to the market.

[0010] To achieve the above objectives, the present invention provides an oil-controlling composition comprising, by weight, 0.5-1 parts of zinc PCA, 4-9 parts of nicotinamide, 0.5-2 parts of pink passionflower extract and 0.3-0.7 parts of acetyl tetrapeptide-5.

[0011] PCA zinc not only has the antibacterial, sebum-inhibiting, and anti-inflammatory effects of zinc, but also helps the stratum corneum retain moisture and maintain a healthy barrier.

[0012] Niacinamide is a derivative of vitamin B3. It can accelerate metabolism, promote the shedding of melanin-containing keratinocytes, promote the synthesis of epidermal proteins, and improve skin texture. It can also reduce the production of fatty acids and triglycerides in sebum, thereby minimizing pores and reducing the severity of acne.

[0013] Pink passionflower extract mainly contains flavonoids, alkaloids and other substances, which have antioxidant, anti-inflammatory and nerve-relieving effects;

[0014] Acetyl tetrapeptide-5 primarily reduces sebum secretion by targeting and regulating the MC5R receptor on sebaceous cells, thereby modulating sebaceous gland cell differentiation.

[0015] This invention combines four components—PCA zinc, nicotinamide, pink passionflower extract, and acetyl tetrapeptide-5—to not only effectively inhibit 5α-reductase activity but also promote autophagy in sebaceous gland cells. These two components work synergistically to regulate sebum secretion, achieving excellent oil control.

[0016] This invention provides the use of oil-controlling compositions in the preparation of skin care products.

[0017] Meanwhile, the present invention provides a skin care product containing 1-3 wt% of the above-mentioned oil-control composition.

[0018] Furthermore, the skincare products include lotions, creams, serums, and masks.

[0019] Beneficial effects

[0020] Compared with the prior art, the present invention has at least the following advantages:

[0021] (1) This invention discloses an oil-controlling composition, which produces a significant effect of inhibiting 5α-reductase activity by combining four components: zinc PCA, nicotinamide, pink passionflower extract and acetyl tetrapeptide-5.

[0022] (2) The oil-controlling composition of the present invention can not only inhibit 5α-reductase activity, but also promote the autophagy of sebaceous gland cells, thereby enhancing the oil-controlling effect of the composition. Attached Figure Description

[0023] The present invention will be further described below with reference to the accompanying drawings and embodiments;

[0024] Figure 1 This is a test diagram of the chorioallantoic membrane vascular test of chicken embryos, which is an application example of this application. Detailed Implementation

[0025] The present invention will be further described below with reference to embodiments, but this does not constitute any limitation on the present invention. Any limited modifications made within the scope of the claims of the present invention are still within the scope of the claims of the present invention.

[0026] To illustrate the technical content of the present invention in detail, the following description is provided in conjunction with the embodiments.

[0027] In the following examples and comparative examples, the zinc PCA was purchased from Guangzhou Aoxue Chemical Co., Ltd.; the nicotinamide was purchased from Guangzhou Hemiao Biotechnology Co., Ltd.; the pink passionflower extract was purchased from Guangzhou Miyanxiu Biotechnology Co., Ltd.; and the acetyl tetrapeptide-5 was purchased from Guangzhou Best Chemical Co., Ltd.

[0028] It should be noted that the technical solution of the present invention is not limited to the above-mentioned raw materials; all the same raw materials that are available on the market can achieve the technical solution of the present invention.

[0029] Unless otherwise specified, in the following examples and comparative examples, the parts and percentages refer to parts by weight and weight percentages, respectively; in the following examples and comparative examples, deionized water is used as a solvent, which does not affect the efficacy of the composition.

[0030] Example 1

[0031] An oil-controlling composition is prepared by mixing 1 part zinc PCA, 4 parts nicotinamide, 1.2 parts pink passionflower extract, 0.5 parts acetyl tetrapeptide-5 and 93.3 parts deionized water.

[0032] Example 2

[0033] An oil-controlling composition is prepared by mixing 0.5 parts of zinc PCA, 6 parts of nicotinamide, 2 parts of pink passionflower extract, 0.3 parts of acetyl tetrapeptide-5 and 91.2 parts of deionized water.

[0034] Example 3

[0035] An oil-controlling composition comprising 0.8 parts of zinc PCA, 9 parts of nicotinamide, 0.5 parts of pink passionflower extract, 0.7 parts of acetyl tetrapeptide-5 and 89 parts of deionized water.

[0036] Comparative Example 1

[0037] An oil-controlling composition is prepared by mixing 6.3 parts nicotinamide, 2.1 parts pink passionflower extract, 0.4 parts acetyl tetrapeptide-5 and 91.2 parts deionized water.

[0038] Comparative Example 2

[0039] An oil-controlling composition is prepared by mixing 1.5 parts of zinc PCA, 6.3 parts of pink passionflower extract, 1 part of acetyl tetrapeptide-5 and 91.2 parts of deionized water.

[0040] Comparative Example 3

[0041] An oil-controlling composition is prepared by mixing 0.6 parts of zinc PCA, 7.8 parts of nicotinamide, 0.4 parts of acetyl tetrapeptide-5 and 91.2 parts of deionized water.

[0042] Comparative Example 4

[0043] An oil-controlling composition is prepared by mixing 0.5 parts of zinc PCA, 6.2 parts of nicotinamide, 2.1 parts of pink passionflower extract, and 91.2 parts of deionized water.

[0044] Comparative Example 5

[0045] An oil-controlling composition is obtained by mixing 8.8 parts of zinc PCA and 91.2 parts of deionized water.

[0046] Comparative Example 6

[0047] An oil-controlling composition is obtained by mixing 8.8 parts of nicotinamide and 91.2 parts of deionized water.

[0048] Comparative Example 7

[0049] An oil-controlling composition is obtained by mixing 8.8 parts of pink passionflower extract and 91.2 parts of deionized water.

[0050] Comparative Example 8

[0051] An oil-controlling composition is obtained by mixing 8.8 parts of acetyl tetrapeptide-5 and 91.2 parts of deionized water.

[0052] Efficacy test

[0053] I. 5α-reductase activity inhibition rate

[0054] 5α-Reductase is a key enzyme that catalyzes the conversion of testosterone to dihydrotestosterone (DHT), which in turn stimulates excessive sebum secretion from the sebaceous glands. The 5α-reductase inhibition rate test indirectly assesses the oil-controlling ability of a analyte by detecting its inhibitory effect on enzyme activity. During the experiment, 5α-reductase metabolizes testosterone into DHT, which then continues to react under the action of the enzyme. The product generated during this reaction exhibits a specific peak at a wavelength of 405 nm. By detecting the change in absorbance of this product at 405 nm, the amount of DHT produced is reflected, ultimately indicating the change in 5α-reductase activity, thus evaluating the inhibitory effect of the sample.

[0055] Inhibition rate = (Control group - Sample group) / (Control group - Blank group) * 100%;

[0056] The control group consisted of a base material without the composition.

[0057] The blank group contains no composition or base material;

[0058] The sample groups are Examples 1-3 and Comparative Examples 1-4.

[0059] The inhibitory effects of Examples 1-3 and Comparative Examples 1-4 are shown in Table 1;

[0060] Table 1. Results of 5α-reductase activity inhibition rate of the compositions in Examples 1-3 and Comparative Examples 1-4

[0061] absorbance Inhibition rate control group 0.996 - Blank group 0.051 - Example 1 0.251 78.84% Example 2 0.317 71.85% Example 3 0.386 64.55% Comparative Example 1 0.796 21.16% Comparative Example 2 0.489 53.65% Comparative Example 3 0.556 46.56% Comparative Example 4 0.678 33.65%

[0062] According to the results in Table 1:

[0063] According to the data results of Examples 1-3, the technical solution of this application, which combines PCA zinc, nicotinamide, pink passionflower extract and acetyl tetrapeptide-5, has an extremely high 5α reductase activity inhibition rate.

[0064] Based on the data comparison between Example 2 and Comparative Example 1, it can be seen that when PCA zinc is missing and the amounts of other components are increased accordingly, the 5α reductase activity inhibition rate of the composition decreases significantly. The reason for this is speculated to be:

[0065] (1) Zinc PCA itself has an extremely high 5α reductase activity inhibition rate, while other components themselves have a low 5α reductase activity inhibition rate;

[0066] (2) The combination of zinc PCA, nicotinamide, pink passionflower extract and acetyl tetrapeptide-5 produced a synergistic effect. The lack of zinc PCA led to the disappearance or weakening of the synergistic inhibition of 5α reductase activity.

[0067] However, a comparison of the data from Examples 2 and 3 shows that while the content of zinc PCA in Example 3 is higher than that in Example 2, the 5α-reductase activity inhibition rate is lower than that in Example 2. This indicates that zinc PCA itself does not possess the 5α-reductase activity inhibition efficacy that would cause a 50.69% decrease in the 5α-reductase activity inhibition rate of Comparative Example 1 compared to Example 2. Therefore, the reason for the significant decrease in the 5α-reductase activity inhibition rate of Comparative Example 1 should be that the combination of zinc PCA, nicotinamide, pink passionflower extract, and acetyl tetrapeptide-5 produced a synergistic effect, and the lack of zinc PCA caused the synergistic inhibition of 5α-reductase activity to disappear or be greatly weakened.

[0068] Similarly, a comparison of the data from Example 2 and Comparative Examples 2-4 shows that the absence of any one of nicotinamide, pink passion fruit extract, and acetyl tetrapeptide-5 also leads to a significant decrease in the 5α-reductase activity inhibition rate of the composition, further confirming that the combination of zinc PCA, nicotinamide, pink passion fruit extract, and acetyl tetrapeptide-5 produces a synergistic effect in enhancing the 5α-reductase activity inhibition rate.

[0069] II. Verification of autophagy in sebaceous gland cells

[0070] Autophagy is a ubiquitous self-protective mechanism in eukaryotic cells. Cells contain aging and damaged organelles, incorrectly synthesized proteins, invading bacteria, and macromolecules. Autophagy forms autophagosomes to encapsulate these harmful substances and combines with lysosomes to form autolysosomes, thus breaking down and clearing them, maintaining cellular homeostasis and the recycling of intracellular substances. Enhancing the autophagy capacity of sebaceous gland cells can increase the sebaceous glands' ability to metabolize sebum and reduce sebum secretion.

[0071] Autophagy levels were assessed by detecting the expression levels of autophagy-related proteins LC3-II and p62 in sebaceous gland cells using Western blotting. Upregulation of LC3-II / β-actin and downregulation of p62 / β-actin indicated increased autophagy levels.

[0072] LC3-II change rate = (sample group - blank group) / blank group * 100%;

[0073] p62 change rate = (sample group - blank group) / blank group * 100%;

[0074] The sample groups consist of Examples 1-3 and Comparative Examples 1-8;

[0075] The blank group consists of the base material without the addition of the composition.

[0076] The effects of sebaceous gland autophagy on Examples 1-3 and Comparative Examples 1-8 are shown in Table 2;

[0077] Table 2. Sebaceous gland autophagy effects of the compositions in Examples 1-3 and Comparative Examples 1-8

[0078] LC3-II / β-actin ratio LC3-II rate of change p62 / β-actin ratio p62 rate of change Blank group 0.553 - 1.253 - Example 1 1.235 123.33% 0.635 -49.32% Example 2 0.989 78.84% 0.716 -42.86% Example 3 1.014 83.36% 0.683 -45.49% Comparative Example 1 0.627 13.38% 1.153 -7.98% Comparative Example 2 0.735 32.91% 0.983 -21.55% Comparative Example 3 0.639 15.55% 1.013 -19.15% Comparative Example 4 0.743 34.36% 0.939 -25.06% Comparative Example 5 0.697 26.04% 0.882 -29.61% Comparative Example 6 0.652 17.90% 1.113 -11.17% Comparative Example 7 0.686 24.05% 0.852 -32.00% Comparative Example 8 0.579 4.70% 1.208 -3.59%

[0079] According to the data comparison in Table 2:

[0080] According to the data from Examples 1-3 of this application, the technical solution of this application has extremely high levels of LC3-II protein expression enhancement and p62 expression inhibition. Furthermore, comparing the data in Table 1, unlike Table 1, Example 3 shows higher LC3-II expression enhancement and lower p62 expression inhibition than Example 2, but lower than Example 1. The difference in LC3-II change rate between Example 1 and Example 3 is much greater than the difference between Example 3 and Example 2, and the difference in p62 change rate between Example 1 and Example 3 is also greater than the difference between Example 3 and Example 2. It is speculated that the reason might be that while zinc PCA plays an important role in enhancing LC3-II and inhibiting p62 expression, it is not the only important factor; the ratio of other components also plays a crucial role. Considering the content of each component in Examples 1-3, it is very likely that the combination of zinc PCA, nicotinamide, pink passionflower extract, and acetyl tetrapeptide-5 synergistically enhances LC3-II protein expression and inhibits p62 expression.

[0081] According to the data from Comparative Examples 5-8, the effect of individual components in regulating the expression levels of LC3-II and p62 is: PCA zinc > pink passionflower extract > nicotinamide > acetyl tetrapeptide-5. At the same dosage, PCA zinc and pink passionflower extract have similar effects in promoting LC3-II expression and inhibiting p62 expression, while the regulatory effect of acetyl tetrapeptide-5 on the expression levels of LC3-II and p62 is not significant.

[0082] Based on the data from Comparative Examples 5-8, theoretically, Example 2 should have a better effect on regulating the expression levels of LC3-II and p62 than Example 1. However, in reality, the effect of Example 1 was significantly higher than that of Example 2. It is speculated that the reason for the discrepancy between the actual effect and the expected effect is:

[0083] (1) In the synergistic effect of this composition, zinc PCA plays the main role in regulating the expression levels of LC3-II and p62, and the amount of PCA used has a significant impact on the efficacy of the composition.

[0084] (2) Although acetyl tetrapeptide-5 itself does not have a significant regulatory effect on the expression levels of LC3-II and p62, it plays an important synergistic promoting role in the composition of this application, and thus the increase of its dosage seriously affects the efficacy of the composition.

[0085] However, based on the data comparison of Examples 1 and 3, the above two speculations have not been proven. Therefore, it can be inferred that in the technical solution of this application, the combined dosage of PCA zinc, nicotinamide, pink passionflower extract and acetyl tetrapeptide-5 is particularly important for promoting LC3-II expression and inhibiting p62 expression. Under specific ratios, the regulatory effect of the composition on LC3-II and p62 expression can be significantly enhanced.

[0086] Application examples

[0087] Configure the product according to Table 3. The specific configuration method is as follows:

[0088] 1) Mix glycerol, carbomer, butylene glycol, macromolecular HA and water until homogeneous, then heat to 85°C and keep warm for 15 minutes to obtain mixture A;

[0089] 2) Mix Olivem 1000, 1618 alcohol, jojoba oil and squalane evenly, heat to 85°C, and keep warm for 15 minutes to obtain mixture B;

[0090] 3) While mixing mixture A, add mixture B and mix until homogeneous and evenly mixed;

[0091] 4) Cool to 40±2℃; add a small amount of water to dissolve the arginine and ketone, then add hexanediol, the composition, and the flavoring, and stir well.

[0092] Table 3 Product Formula Table

[0093] Components source Dosage % water - To 100 Kapo Guangzhou Zhaoheng Trade Development Co., Ltd. 0.2 glycerin Guangzhou Bino Biotechnology Co., Ltd. 5 Butylene glycol Guangzhou Hengtao Trading Co., Ltd. 2 macromolecular HA Guangzhou Hemiao Biotechnology Co., Ltd. 0.01 Olivem 1000 Guangzhou Bino Biotechnology Co., Ltd. 0.8 1618 alcohol Guangzhou Chichen Trading Co., Ltd. 0.3 Jojoba oil Guangzhou Baihaobo Co., Ltd. 2 squalane Guangzhou Hengtao Trading Co., Ltd. 1 Arginine Guangzhou Hemiao Biotechnology Co., Ltd. 0.2 Composition Example 1 2 Fresh Ketone Guangzhou Hemiao Biotechnology Co., Ltd. 0.4 Hexanediol Guangzhou Hemiao Biotechnology Co., Ltd. 0.5 essence Guangzhou Fangya Biotechnology Co., Ltd. 0.05

[0094] Application Example Test

[0095] III. Human Experimentation Verification

[0096] Test Method: Referring to T / CAB 0152—2022 "Test Methods for Seven Efficacy Items of Cosmetics: Anti-wrinkle, Firming, Moisturizing, Oil Control, Repairing, Nourishing, and Soothing", 10 subjects were recruited to apply the product to both sides of their face. One side used a lotion without added ingredients, and the other side used a lotion with added ingredients. Sebum secretion was tested before and 14 days after use. On the day of the test, subjects first cleansed the test area with an alkaline soap-based cleanser. After cleansing, sebum secretion was measured at least 4 hours later. The test results are shown in Table 4.

[0097] Table 4. Results of skin sebum secretion measurement

[0098]

[0099] Data shows that after using the emulsion with the added composition, sebum secretion was significantly reduced after 4 hours (p<0.05), with a reduction rate of 22.15%. This indicates that the composition has an oil-controlling effect.

[0100] IV. Mildness Test

[0101] Test method: Following T / GDCA 036-2024 "Cosmetic Eye Irritation - Chicken Embryo Choronal Allantoic Membrane Vascular Test Method", the mildness of the test application example was assessed, with a score of 1.33 (stressful stimulation). Test screenshots are shown below. Figure 1 :

[0102] Figure 1 In the study, 1-1, 1-2, and 1-3 represent three different chicken embryo chorioallantoic membrane vascular experiments.

[0103] The embodiments presented herein are merely selected implementations based on combinations of all possible embodiments. The appended claims should not be limited to the embodiments described herein. Some numerical ranges used in the claims include sub-ranges within them, and variations within these ranges should also be covered by the appended claims.

Claims

1. An oil-controlling composition, characterized in that, By weight, it consists of the following active ingredients: 1 part zinc PCA, 4 parts niacinamide, 1.2 parts pink passionflower extract and 0.5 parts acetyl tetrapeptide-5.

2. Use of the oil-control composition as described in claim 1 in the preparation of skin care products.

3. A skincare product, characterized in that, Contains 1-3 wt% of the oil-controlling composition as described in claim 1.

4. The skincare product according to claim 3, characterized in that, The skincare products include lotions, creams, serums, and masks.

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