A mild acne-removing composition and its preparation method and application

Abstract

The present invention belongs to the technical field of material chemistry, and in particular to a mild anti-acne composition and its preparation method and application. Its composition and weight ratio are: 0.5-5% of plant retinol, 0.1-3% of pomegranate peel extract, 10-50% of hydrogel, 0.01-1% of polypeptides, 0.1-2% of resorcinol and its derivatives, 0-20% of plant extract composition, and the rest is solvent; the polypeptide is one or more of palmitoyl pentapeptide-4, myristoyl hexapeptide-5, and palmitoyl tripeptide-8; the plant extract composition is one or more of saffron extract aqueous solution, olive leaf extract aqueous solution, sophora flavescens extract, and citrus fruit extract aqueous solution.

Description

Technical field:

[0001] The invention belongs to the technical field of material chemistry, and in particular relates to a mild acne-removing composition and a preparation method and application thereof. Background technology:

[0002] Phyto-retinol is extracted from plants and has the same efficacy as retinol. Compared with retinol, it is not photosensitive and is very mild, but its efficacy is slightly weaker than that of retinol. Silymarin is a flavonol lignan compound extracted from the fruit and seeds of the traditional Chinese herbal medicine milk thistle, which has high biological activity. As a type of plant retinol, it has strong retinoic acid (vitamin A) activity and can exert obvious retinoic acid-like effects when used on the skin: firming and removing wrinkles, whitening and lightening spots, removing acne and controlling oil, etc. Silymarin also has antioxidant, anti-glycation, anti-inflammatory, anti-allergic, anti-microbial, hair growth promotion, and red blood streak removal effects that VA does not have. It is also an ideal choice for preventing and treating skin diseases such as eczema, atopic dermatitis, and chloasma in children.

[0003] Bakuchiol is an extract from the leaves and seeds of the Babuchi plant, and this plant-derived compound has emerged as a new retinoid ingredient in skin care. Bakuchiol is currently offered as a gentler alternative to retinol, but with many of the same benefits. It can also act as an antioxidant and is used to boost skin health and promote healthy aging. This plant-based compound is used as an alternative to retinol for people with sensitive skin. While retinol can sometimes cause redness, burning, and stinging, studies show that bakuchiol is gaining attention for its ability to improve acne, melasma, photoaging, and hyperpigmentation without the side effects.

[0004] The olive leaf active ingredients in the extracts from soothing and anti-inflammatory sources have anti-inflammatory, repairing and soothing effects. They kill bacteria and phagocytize them in the early stages of inflammation, inhibit the release of histamine, and reduce the expression of inflammatory factors TNF-α and IL-1β, which have anti-inflammatory effects. This improves red blood streaks, inflammatory acne, and post-inflammatory pigmentation caused by inflammation; citrus fruits are rich in vitamin B, vitamin C, flavonoids, and carotenoids, which can be anti-inflammatory and antioxidant. Plant-derived soothing and anti-inflammatory substances are safer and less irritating, and can weaken the irritation and inflammatory response caused by the acne removal effect in the composition. Summary of the invention:

[0005] The present invention aims at the above problems and provides a mild acne-removing composition and a preparation method and application thereof.

[0006] In order to achieve the above-mentioned purpose, the present invention adopts the following technical scheme, the composition and weight ratio of which are: 0.5-5% of plant retinol, 0.1-3% of pomegranate peel extract, 10-50% of hydrogel, 0.01-1% of polypeptides, 0.1-2% of resorcinol and its derivatives, 0-20% of plant extract composition, and the rest is solvent;

[0007] The polypeptides are one or more of palmitoyl pentapeptide-4, myristoyl hexapeptide-5, and palmitoyl tripeptide-8;

[0008] The plant extract composition is one or more of saffron extract aqueous solution, olive leaf extract aqueous solution, sophora flavescens extract, and citrus fruit extract aqueous solution.

[0009] The plant retinol is one or more of silymarin, bakuchiol, salicylic acid phytosphingosine, Bidens pilosa extract, and Helichrysum exigua extract.

[0010] The hydrogel comprises a solvent, a thickener and lecithin, wherein the solvent is one or more of deionized water, floral water and fermented water, and the thickener is one or more of ammonium acryloyldimethyltaurate / behenyl ether-25 methacrylate cross-linked polymer and acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer.

[0011] The floral water can be Egyptian blue water lily (NYMPHAEA CAERULEA) floral water, white lily (LILIUM CANDIDUM) floral water, white chamomile (ANTHEMIS NOBILIS) floral water, North American witch hazel (HAMAMELIS VIRGINIANA) floral water, safflower (CARTHAMUS TINCTORIUS) floral water, golden chamomile (CHRYSANTHELLUM INDICUM) floral water, bitter orange (CITRUSAURANTIUM AMARA) floral water, broad-leaved linden (TILIA PLATYPHYLLOS) floral water, lotus (NELUMBIUM SPECIOSUM) floral water, lotus (NELUMBO NUCIFERA) floral water, verbena (VERBENA OFFICINALIS) floral water, rose (ROSA RUGOSA) floral water, plum (PRUNUS MUME) floral water, Moroccan chamomile (ORMENIS Mixta flower water, Jasmine flower water, Chamomile flower water, Peony flower water, Lippia flower water, Tilia flower water, Horse chestnut flower water, Centaurea cynanchum flower water, Jasminum officinale flower water, Prunus persica flower water, Citrus aurantium flower water, Rose flower water, Elderberry flower water, Melissa officinalis flower water, Pelargonium flower water One or more of the following: GRAVEOLENS floral water, LAVANDULA ANGUSTIFOLIA floral water, ROSA CENTIFOLIA floral water, HELICHRYSUM ITALICUM floral water, OLEAEUROPAEA floral water, and LAVANDULA HYBRIDA floral water.

[0012] The fermentation water can be a filtrate of Pichia pastoris fermentation lysate, a filtrate of ozonated yeast fermentation lysate, a budding Aureobasidium fermentation product, a rice fermentation product filtrate, a bifid yeast fermentation product filtrate, a bifid yeast fermentation product lysate, a bifid yeast fermentation product extract, a fermentation product extract of Zymomonas fermentation product, a galactosaccharomyces fermentation product filtrate, a Monascus (MONACS) / rice fermentation product, a Pseudoalteromonas fermentation product extract, a Candida / Cambogia (GARCINIA CAMBOGIA) fermentation product, a Candida albicans / glucose / rapeseed oleic acid methyl ester fermentation product, an Alteromonas fermentation product extract, a yeast fermentation product extract, a yeast / coix lacryma-jobi (COIX LACRYMA-JOBI) YUEN) Seed Ferment Filtrate, Saccharomyces / Soy Protein Ferment, Saccharomyces / Barley Seed Ferment Filtrate, Saccharomyces / Rice Ferment Filtrate, Saccharomyces / Tourmaline Ferment, Saccharomyces / Calcium Ferment, Saccharomyces / Silicon Ferment, Saccharomyces / Potassium Ferment, Saccharomyces / Malachite Ferment, Saccharomyces / Laminaria Ferment, Saccharomyces / Potato Extract Ferment Filtrate, Saccharomyces / Magnesium Ferment, Saccharomyces / Manganese Ferment, Saccharomyces / Rice Bran Ferment, Saccharomyces / Glucose GRAPE FERMENT EXTRACT, SACCHARIDES / IRON FERMENT, SACCHARIDES / COPPER FERMENT, SACCHARIDES / ZINC FERMENT, SACCHARIDES / MOTHER OF PEARL FERMENT LYSATE FILTRANTE, SACCHARIDES FERMENT, SACCHARIDES FERMENT FILTRANTE, SACCHARIDES FERMENT LYSATE FILTRANTE, SACCHARIDES / ACETOBACTER XYLIUM / BLACK TEA FERMENT, RANNELLIA / SOY PROTEIN FERMENT, SCHIZOSACCHAROMYCES MYCELIUM FERMENT FILTRANTE, EUROLEA / OLIC ACID FERMENT, LEUNCONSTRUCT / RAPHANUS SATIVUS ROOT FERMENT FILTRANTE, ENDOMYCES FERMENT FILTRANTE, VITISVINIFERA FERMENT EXTRACT, SPHINGOMONAS FERMENT EXTRACT, ASPERGILLUS FERMENT, ASPERGILLUS / GLUCOSE / SOYBEAN / STARCH FERMENT FILTRANTE.Lactobacillus / ERIODICTYON CALIFORNICUM Ferment Extract, Lactobacillus / Soybean Ferment Extract, Lactobacillus / Soybean Extract Ferment Filtrate, Lactobacillus / Rice Ferment, Lactobacillus / Soy Milk Ferment Filtrate, Lactobacillus / Water Hyacinth Ferment, Lactobacillus / Black Mustard Seed Ferment Extract, Lactobacillus / Rye Powder Ferment, Lactobacillus / Pear Juice Ferment Filtrate, Lactobacillus / Mung Bean (PHASEOLUS RADIATUS) Seed Extract / Monosodium Glutamate Ferment Filtrate, Lactobacillus / Hibiscus Sabdariffa Flower Ferment Filtrate, Lactobacillus / Cucurbita Pepo Ferment Extract, Lactobacillus / Milk / Ferment Filtrate, Lactobacillus / Milk / Magnesium / Zinc Ferment Lysate, Lactobacillus / Ginseng Root Ferment Filtrate, Lactobacillus / WASABIA JAPONICA ROOT FERMENT EXTRACT, LACTOBACILLUS / PUNICA GRANATUM FRUIT FERMENT EXTRACT, LACTOBACILLUS / CITRUS MEDICA LIMONUM PEEL FERMENT EXTRACT, LACTOBACILLUS / ALGAE EXTRACT FERMENT, LACTOBACILLUS / ACERA CHERRY FERMENT, LACTOBACILLUS FERMENT, LACTOBACILLUS FERMENT LYSATE, LACTOBACILLUS / PHASEOLUS RADIATUS SEED EXTRACT FERMENT FILTRANS, LACTOBACILLUS / MILF FERMENT LYSATE, LACTOBACILLUS FERMENT, LACTOBACILLUS FERMENT LYSATE, LACTOBACILLUS FERMENT EXTRACT, STREPTOCOCCUS THERMOPHILUS FERMENT, THERMUS THERMOPHILLUS FERMENT, ACIDOPHILS / GRAPEFERMENT, VITRASCILLUS FERMENT, CHLORELLA VULGARIS / LUPINUS One or more of ALBUS) protein fermentation product, Chlorella fermentation product, Bacillus / soybean fermentation product extract, Bacillus / glutamic acid fermentation product filtrate, Bacillus / rice bran extract / soybean extract fermentation product filtrate, Bacillus fermentation product, Porphyridium / zinc fermentation product.

[0013] The resorcinol and its derivatives are one or more of 2-methylresorcinol, 4-butylresorcinol, phenethylresorcinol, hexylresorcinol and resorcinol.

[0014] The solvent is one or more of deionized water, floral water, and fermented water.

[0015] The specific preparation steps are:

[0016] 1. The plant retinol and lecithin (phosphatidylcholine content is not less than 95%, and liposome accounts for 60%) are circulated for 3-5 times under the high-pressure microfluidization pressure of 120-180 MPa to obtain liposome plant retinol for standby use. The liposome encapsulation mainly solves the problems of water solubility and stability of plant retinol.

[0017] 2. Add thickener powder and the liposomal plant retinol prepared in step 1 into the solvent at the same time and homogenize for 30 to 60 minutes to obtain the hydrogel-encapsulated active substance.

[0018] 3. Add the remaining active ingredients, including pomegranate peel extract, peptides, resorcinol and its derivatives, and plant extract composition, to the complex of step 2 in sequence, and stir at 500-1500 rpm for 10-30 min until evenly dispersed without color bands.

[0019] The composition can be applied to the field of cosmetics as an important component of acne-removing products.

[0020] Beneficial effects of the present invention:

[0021] 1. The acne removal method of the present invention is effective quickly, and the effect can be seen with the naked eye within 24 hours or 7 days.

[0022] 2. Compared with products with the same efficacy on the market, the present invention is mild and soothing, with low irritation, and meets consumers' further demand for acne-removing products.

[0023] 3. The present invention adopts the form of hydrogel-coated active ingredients to achieve the effects of sustained release of efficacy and mild product. It is innovative and novel in the cosmetics market and has strong product competitiveness. Description of the drawings:

[0024] Figure 1 This is the inhibition zone MIC diagram of Example 1.

[0025] Figure 2 This is the chicken embryo experiment diagram of Example 1.

[0026] Figure 3 These are facial images of some volunteers in the acne removal test of Example 1. Specific implementation method:

[0027] Example 1

[0028] The composition and weight ratio of the composition are: 1% bakuchiol, 0.5% silymarin, 23% hydrogel encapsulation, 0.05% myristoyl hexapeptide-5, 1% hexylresorcinol, 0.2% sodium heparin, 0.1% pomegranate peel extract, 2% saffron extract, 4% olive leaf extract, 1% sophora flavescens extract, 3% citrus fruit extract, and the rest is deionized water.

[0029] Among them, the thickener in the 23% hydrogel is 0.5%, 20% is deionized water, and lecithin is 2.5%. The thickener is specifically 0.25% of ammonium acryloyldimethyltaurate / behenyl alcohol polyether-25 methacrylate crosslinked polymer and 0.25% of acrylic acid (ester) / C10-30 alkyl acrylate crosslinked polymer.

[0030] Example 2

[0031] Not coated with hydrogel, not subjected to coating process.

[0032] Example 3

[0033] The difference from Example 1 is that no plant extract composition was added.

[0034] Example 4

[0035] The composition and weight ratio of the composition are: 2% bakuchiol, 1.0% silymarin, 23% hydrogel encapsulation, 0.05% myristoyl hexapeptide-5, 1% hexylresorcinol, 0.2% sodium heparin, 0.1% pomegranate peel extract, 2% saffron extract aqueous solution, 4% olive leaf extract aqueous solution, 1% sophora flavescens extract, 3% citrus fruit extract aqueous solution, and the rest is solvent.

[0036] Among them, the thickener in the 23% hydrogel is 0.5%, 20% is deionized water, and lecithin is 2.5%. The thickener is specifically 0.25% of ammonium acryloyldimethyltaurate / behenyl alcohol polyether-25 methacrylate crosslinked polymer and 0.25% of acrylic acid (ester) / C10-30 alkyl acrylate crosslinked polymer.

[0037] Example 5

[0038] The composition and weight ratio of the composition are: 0.5% of bakuchiol, 0.1% of silymarin, 0.05% of myristoyl hexapeptide-5, 1% of hexylresorcinol, 0.2% of sodium heparin, 0.1% of pomegranate peel extract, 2% of saffron extract aqueous solution, 4% of olive leaf extract aqueous solution, 1% of sophora flavescens extract, 3% of citrus fruit extract aqueous solution, and the rest are solvents.

[0039] The hydrogel contains 0.5% thickener, 20% water and 2.5% lecithin.

[0040] Example 6 Performance Test

[0041] A certain acne removal product which is among the top three in the market in terms of sales volume, mainly containing picolinamide and acid components, was selected as comparative example 1, and deionized water was selected as comparative example 2 for comparative evaluation with embodiments 1-5.

[0042] 1. Antibacterial test (inhibition zone: MIC)

[0043] Test strain: Propionibacterium acnes

[0044] Test method: Propionibacterium acnes is a pathogen that causes acne. In the present invention, the microbial inhibition zone (MIC) test of Propionibacterium acnes was performed on the examples and comparative examples.

[0045] The preserved Propionibacterium acnes (ATCC 6919) was inoculated into BHI liquid medium under sterile conditions, cultured in an anaerobic incubator at 37°C for 48 h, and then centrifuged and resuspended. The concentration of Propionibacterium acnes was adjusted to 1×10 6 CFU / ml, for standby use. Take a sterile culture dish with a diameter of 90 mm in a sterile environment, introduce 20 mL of BHI melted culture medium into each culture dish and cool and fix it, evenly apply 100 μl of the resuspended Propionibacterium acnes solution on the culture medium, take a circular filter paper with a diameter of 7 mm and dip the test drug, dilute the samples in the comparative example and the embodiment to a concentration of 0.5%, and after the blank control group and the positive control group are prepared, the filter paper dipped in the test drug is evenly placed on the above-mentioned BHI solid culture medium coated with Propionibacterium acnes, and 3 parallels are performed respectively. The culture dish is sealed with a sealing film, horizontally inverted in an anaerobic incubator at 37°C and cultured for 20 hours, the diameter of the antibacterial ring is measured, and the average diameter of the antibacterial ring of each test drug is calculated.

[0046] The blank control group was PBS solution;

[0047] The positive control group was 0.1% trichlorohydroxydiphenyl ether, and the test results are shown in Table 1.

[0048] Table 1 Propionibacterium acnes inhibition zone results

[0049]

[0050] In Table 1, sterile PBS treatment showed no antibacterial zone, the antibacterial zone diameter of the positive control group with 0.1% concentration of tri-hydroxydiphenyl ether was 40.3 mm, Examples 1, 3, 4 and Comparative Example 1 all had obvious antibacterial effects, while Examples 2 and 5 were weaker. This shows that the coating process has a certain influence on the antibacterial effect, and the content of plant retinol cannot be too low, otherwise the antibacterial ability will decrease. However, when the content of plant retinol increases, the antibacterial effect does not increase much.

[0051] 2. Acne removal efficacy test

[0052] Test objective: Test the acne removal effect on the human body for 24 hours and 7 days.

[0053] Directions for use: Apply topically to acne. Do not use with acid / vitamin A products.

[0054] Frequency of use: once in the morning and evening after cleansing, reapply every 3-4 hours.

[0055] Reference method: T / TDCA 004-2021 Test method for anti-acne efficacy of cosmetics.

[0056] T. / CNMA 0012-2020 Clinical evaluation standards for anti-acne functional skin care products.

[0057] Cosmetic Safety Technical Specifications (2015 Edition).

[0058] Testing process:

[0059] D0: Subject registration, laboratory technicians screened qualified subjects with oily skin and no less than 5 acne, and completed the selection. The subjects cleaned their faces with the designated cleansing sample and sat in the laboratory at 21±1℃ and 50±10%RH for 30 minutes; the basic value of the subject's skin was tested: Primos-CR took photos and analyzed the volume of acne.

[0060] T24h: The test subjects' skin values ​​were measured 24 hours after using the samples. Primos-CR took photos and analyzed the acne volume.

[0061] D7: The skin values ​​of the test subjects were measured 7 days after using the samples. Primos-CR took photos and analyzed the acne volume.

[0062] Instrument Description: Primos-CR is a digital optical 3D image analysis instrument developed based on a digital microscopic fringe projector. By testing the position change of fringe light and the grayscale value of all image points, a digital 3D image of the entire test skin surface or test object can be obtained. The smaller the measured value, the smaller the acne volume. The results are shown in Tables 2 and 3.

[0063] Table 2 24h acne removal test results of various examples / comparative examples

[0064]

[0065] Table 3 7d acne removal test results of various examples / comparative examples

[0066]

[0067] As shown in Table 2 and Table 3, Examples 1, 3, 4 and Comparative Example 1 have better acne volume improvement rates, while Comparative Example 2 has a lower acne improvement rate after basically regulating its own immunity, and Examples 2 and 5 have lower acne improvements than other Examples.

[0068] 3. Irritation test: Chicken embryo experiment

[0069] Test item: Chicken chorioallantoic membrane test for cosmetic eye irritation / corrosion

[0070] Test basis: SN / T2329-2009 "Chicken embryo chorioallantoic membrane test for cosmetic eye irritation / corrosion"

[0071] 3.1 Irritation score method: The following formula is used to calculate the irritation score (IS), and the result is rounded to two decimal places:

[0072]

[0073] Where: Sec H, Sec L, and Sec C represent the average time to the onset of bleeding, vascular lysis, and coagulation observed on the CAM membrane, respectively, in seconds (s);

[0074] Table 4 Evaluation of stimulation scoring method results

[0075] Stimulus score Irritation classification IS<1 Non-irritating 1≤IS<5 Mild irritation 5≤IS<9 Moderate irritation IS ≥ 10 Strong irritant / corrosive

[0076] 3.2 Endpoint scoring method: The score of each chicken embryo = the sum of bleeding, coagulation and vascular lysis observed in each chicken embryo; the endpoint evaluation (ES) = the sum of the scores of 6 chicken embryos.

[0077] Table 5 End point scoring method results evaluation

[0078] Stimulus score Irritation classification ES≤12 No / mild irritation 12<ES<16 Moderate irritation ES≥16 Strong irritant / corrosive

[0079] Test Acceptability Criteria:

[0080]

[0081]

[0082] The test results of the embodiments and comparative examples are shown in Table 6 (since the samples are non-transparent, the blood vessels on the surface will be covered when added, which will affect the judgment of the blood vessels, so the ES scoring method is used instead of the IS).

[0083] Table 6 Irritation test results

[0084] sample ES score Comparative Example 1 11 Example 2 13 Example 3 14 Example 4 12 Example 5 9 Comparative Example 1 15 Comparative Example 2 0

[0085] The results show that Examples 1, 5 and Comparative Example 2 have no / mild irritation (ES is not greater than 12), while the remaining Examples and Comparative Example 1 are moderately irritating. It can be seen that the hydrogel coating and the intervention of soothing plant extracts have a soothing effect on irritation, and too high a content of plant retinol will also affect the irritation of chicken embryos.

[0086] The above are only embodiments of the present invention, and are not intended to limit the patent scope of the present invention. Any equivalent transformations made using the contents of the present invention specification, or directly or indirectly applied in related technical fields, are also included in the patent protection scope of the present invention.

Claims

1. A mild acne-removing composition, It is characterized in that Its composition and weight ratio are: 0.5-5% of plant retinol, 0.1-3% of pomegranate peel extract, 23% of hydrogel, 0.01-1% of polypeptides, 0.1-2% of resorcinol and its derivatives, 0-20% of plant extract composition, and the rest is solvent; The polypeptides are one or more of palmitoyl pentapeptide-4, myristoyl hexapeptide-5, and palmitoyl tripeptide-8; The plant extract composition is one or more of saffron extract aqueous solution, olive leaf extract aqueous solution, sophora flavescens extract, and citrus fruit extract aqueous solution; The plant retinol is one or more of silymarin and bakuchiol; The hydrogel comprises a solvent, a thickener and lecithin, wherein the solvent is one or more of deionized water, floral water and fermented water, and the thickener is one or more of ammonium acryloyldimethyltaurate / beheneth-25 methacrylate cross-linked polymer and acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer; The resorcinol and its derivatives are one or more of 2-methylresorcinol, 4-butylresorcinol, phenethylresorcinol, hexylresorcinol, and resorcinol; The specific preparation steps are: (1) circulating plant retinol and lecithin for 3-5 times under high pressure microfluidization pressure of 120-180 MPa to obtain liposomal plant retinol for standby use; (2) Adding thickener powder and the liposomal plant retinol obtained in step 1) into a solvent simultaneously and homogenizing for 30 to 60 minutes to obtain a hydrogel-encapsulated active substance; (3) The remaining active ingredients, including pomegranate peel extract, peptides, resorcinol and its derivatives, and plant extract composition, are added to the complex of step 2) in sequence, and stirred at 500-1500 rpm for 10-30 min until they are evenly dispersed without color bands.

2. The mild anti-acne composition according to claim 1, It is characterized in that The solvent is one or more of deionized water, floral water, and fermented water.

3. A method for preparing the mild anti-acne composition according to claim 1, It is characterized in that The specific preparation steps are: (1) circulating plant retinol and lecithin for 3-5 times under high pressure microfluidization pressure of 120-180 MPa to obtain liposomal plant retinol for standby use; (2) Adding thickener powder and the liposomal plant retinol obtained in step 1) into a solvent simultaneously and homogenizing for 30 to 60 minutes to obtain a hydrogel-encapsulated active substance; (3) The remaining active ingredients, including pomegranate peel extract, peptides, resorcinol and its derivatives, and plant extract composition, are added to the complex of step 2) in sequence, and stirred at 500-1500 rpm for 10-30 min until they are evenly dispersed without color bands.

Images