CN116370342A - Mild acne-removing composition, and preparation method and application thereof - Google Patents

Abstract

The invention belongs to the technical field of material chemistry, and particularly relates to a mild acne-removing composition, and a preparation method and application thereof. The composition and weight proportion are, plant retinol 0.5-5%, pomegranate rind extract 0.1-3%, hydrogel 10-50%, polypeptide 0.01-1%, resorcinol and its derivative 0.1-2%, plant extract composition 0-20%, 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 crocus sativus extract aqueous solution, olive leaf extract aqueous solution, radix Sophorae Flavescentis extract, and citrus fruit extract aqueous solution.

Description

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

Technical field:

The invention belongs to the technical field of material chemistry, and in particular relates to a mild acne-removing composition and its preparation method and application.

Background technique:

Plant retinol is extracted from plants and has the same efficacy as A-alcohol (retinol). Compared with A-alcohol (retinol), it has no photosensitivity and is very mild, but its efficacy is slightly weaker than A-alcohol. Silymarin is a flavonoid lignan compound extracted from the traditional Chinese herbal medicine milk thistle fruit and seeds, which has high biological activity. As a type of plant retinol, it has strong retinoid (retinoic acid) activity, and it can exert obvious retinoic acid effects when used on the skin: firming and anti-wrinkle, whitening and lightening, acne and oil control, etc. Silymarin also has anti-oxidation, anti-glycation, anti-inflammatory, anti-allergic, anti-microbial, hair growth-promoting, red blood removal effects that VA does not have. Ideal for skin disorders.

Bakuchiol, an extract derived from the leaves and seeds of the baboch plant, is a plant-derived compound that has emerged as a new retinoid ingredient in skin care. Currently, bakuchiol is a milder alternative to retinol but offers many of the same benefits. It also acts as an antioxidant for promoting skin health and promoting 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, research has shown that bakuchiol has gained attention for its ability to improve acne, melasma, photoaging, and hyperpigmentation without side effects.

Soothing and anti-inflammatory source extracts have anti-inflammatory, repairing and soothing olive leaf actives that kill and phagocytize bacteria in the early stage of inflammation, inhibit the release of histamine, and reduce the expression of inflammatory factors TNF-α and IL-1β. Has anti-inflammatory properties. Thereby improving red blood streaks, inflammatory acne, and post-inflammatory hyperpigmentation caused by inflammation; citrus is rich in vitamin B, vitamin C, flavonoids, and carotenoids, which can resist inflammation and oxidation. The soothing and anti-inflammatory substances derived from plants are relatively safe and less irritating, and in the composition can weaken the irritation and inflammatory response caused by the acne-removing effect.

Invention content:

The present invention just aims at the above problems, and provides a mild acne-removing composition and its preparation method and application.

In order to achieve the above object, the present invention adopts the following technical scheme, its composition and weight ratio are: plant retinol 0.5-5%, pomegranate peel extract 0.1-3%, hydrogel 10-50%, polypeptide 0.01- 1%, resorcinol and its derivatives 0.1-2%, plant extract composition 0-20%, 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, bakuchiol, phytosphingosine salicylate, ghost needle grass extract, and southern French helichrysum extract.

The hydrogel includes a solvent, a thickener and lecithin, the solvent is one or more of deionized water, floral water, and fermented water, and the thickener is ammonium acryloyldimethyltaurate/behenyl One or more of alcohol polyether-25 methacrylate crosspolymer, acrylic acid (ester)/C10-30 alkanol acrylate crosspolymer.

Flower water can be Egyptian blue water lily (NYMPHAEA CAERULEA), white lily (LILIUM CANDIDUM) flower water, white flower chamomile (ANTHEMIS NOBILIS) flower water, North American witch hazel (HAMAMELIS VIRGINIANA) flower water, safflower (CARTHAMUS TINCTORIUS) Flower water, golden chamomile (CHRYSANTHELLUM INDICUM) flower water, bitter orange (CITRUSAURANTIUM AMARA) flower water, broadleaf linden (TILIA PLATYPHYLLOS) flower water, lotus (NELUMBIUM SPECIOSUM) flower water, lotus (NELUMBO NUCIFERA) flower water, verbena ( VERBENA OFFICINALIS) flower water, rose (ROSA RUGOSA) flower water, plum (PRUNUS MUME) flower water, Moroccan chamomile (ORMENIS MIXTA) flower water, jasmine (JASMINUMSAMBAC) flower water, chamomile (CHAMOMILLA RECUTITA) flower water, peony ( PAEONIA SUFFRUTICOSA) flower water, lemon vine (LIPPIA CITRIODORA) flower water, European linden (TILIA CORDATA) flower water, European horse chestnut (AESCULUSHIPPOCASTANUM) flower water, cornflower (CENTAUREA CYANUS) flower water, Sufang flower ( JASMINUM OFFICINALE) flower water, peach (PRUNUS PERSICA) flower water, lime (CITRUS AURANTIUM DULCIS) flower water, Turkic rose (ROSADAMASCENA) flower water, western elderberry (SAMBUCUS NIGRA) flower water, lemon balm (MELISSA OFFICINALIS) flower Water, geranium (PELARGONIUM GRAVEOLENS) flower water, lavender (LAVANDULA ANGUSTIFOLIA) flower water, rose (ROSA CENTIFOLIA) flower water, Italian chrysanthemum (HELICHRYSUM ITALICUM) flower water, olive (OLEAEUROPAEA) flower water, miscellaneous lavender (LAVANDULA) One or more of HYBRIDA) flower water.

The fermented water can be Pichia pastoris fermentation lysate filtrate, ozonated yeast fermentation lysate filtrate, Aureobasidium pullulans fermentation product, rice fermentation product filtrate, Bifida yeast fermentation product filtrate, Bifida yeast fermentation product Lysate, Bifida ferment extract, Zymomonas ferment extract, Galactosaccharomyces ferment filtrate, Monascus (MONASCUS)/rice ferment, Pseudoalteromonas ferment extract, Candida/Garcinia Cambogia (GARCINIA CAMBOGIA) Ferment, Candida alpipes/Glucose/Rapeseed Methyl Oleate Ferment, Alteromonas Ferment Extract, Yeast Ferment Extract, Saccharomyces/Kawagu (COIX LACRYMA-JOBI MA-YUEN) Seed Ferment Filtrate, Yeast/Soybean Protein Ferment, Yeast/Barley Seed Ferment Filtrate, Yeast/Rice Ferment Filtrate, Yeast/Tourmaline Ferment, Yeast/ Calcium Ferment, Yeast/Silicon Ferment, Yeast/Potassium Ferment, Yeast/Malachite Ferment, Yeast/Laminarose Ferment, Yeast/Potato Extract Ferment Filtrate, Yeast/Magnesium Ferment Product, Yeast/Manganese Ferment, Yeast/Rice Bran Ferment, Yeast/Grape Ferment Extract, Yeast/Iron Ferment, Yeast/Copper Ferment, Yeast/Zinc Ferment, Yeast/Pearl Mother Ferment Lysate Filtrate, Yeast Ferment, Yeast Ferment Filtrate, Yeast Ferment Lysate Filtrate, Saccharomyces/Acetobacter xylinum/Black Tea Ferment, Lahnella/Soybean Protein Ferment, Schizosaccharomyces (SCHIZOSACCHAROMYCES) mycelium fermentation filtrate, euglena/oleic acid fermentation product, Leuconostococcus/radish (RAPHANUS SATIVUS) root fermentation product filtrate, endomyces (ENDOMYCES) fermentation product filtrate, grape (VITISVINIFERA) fermentation extract, Sphingomonas (SPHINGOMONAS) Ferment Extract, Aspergillus Ferment, Aspergillus/Glucose/Soybean/Starch Ferment Filtrate. Lactobacillus/North American Holy Grass (ERIODICTYON CALIFORNICUM) Ferment Extract, Lactobacillus/Soybean Ferment Extract, Lactobacillus/Soybean Extract Ferment Filtrate, Lactobacillus/Rice Ferment, Lactobacillus/Soymilk Ferment Filtrate, Lactic Acid Bacillus/water hyacinth ferment product, Lactobacillus/black mustard (BRASSICA NIGRA) seed fermentation product extract, Lactobacillus/rye fine powder fermentation product, Lactobacillus/pear juice fermentation product filtrate, Lactobacillus/mung bean (PHASEOLUS RADIATUS) Seed Extract/Sodium Glutamate Ferment Filtrate, Lactobacillus/Roselle (HIBISCUS SABDARIFFA) Flower Ferment Filtrate, Lactobacillus/Zucchini Ferment Extract, Lactobacillus/Milk/Ferment Filtrate, Lactobacillus/Milk/Magnesium / Zinc Ferment Lysate, Lactobacillus / Ginseng Root Ferment Filtrate, Lactobacillus / WASABIA JAPONICA Root Ferment Extract, Lactobacillus / Pomegranate (PUNICA GRANATUM) Fruit Ferment Extract, Lactobacillus / Aroma Citron (CITRUS MEDICA LIMONUM) peel fermentation product extract, Lactobacillus/algae extract fermentation product, Lactobacillus/acerola cherry fermentation product, Lactobacillus fermentation product, Lactobacillus fermentation lysate, Lactobacillus/mung bean (PHASEOLUS RADIATUS) seed Extract Ferment Filtrate, Lactic Acid Bacteria/Milk Ferment Lysate, Lactic Acid Bacteria Ferment, Lactic Acid Bacteria Ferment Lysate, Lactic Acid Bacteria Ferment Extract, Streptococcus Thermophilus Ferment, THERMUS THERMOPHILLUS Ferment, Acidophilus Bacteria/Grape Ferment, Vitiligo Ferment, Chlorella Vulgaris/Lupinus ALBUS Protein Ferment, Chlorella Ferment, Bacillus/Soybean Ferment Extract, Bacillus/Grain One or more of acid fermentation product filtrate, Bacillus/rice bran extract/soybean extract fermentation product filtrate, Bacillus fermentation product, Porphyrococcus/zinc fermentation product.

Described resorcinol and derivatives thereof are in 2-methylresorcinol, 4-butylresorcinol, phenylethylresorcinol, hexylresorcinol, resorcinol One or more.

The solvent is one or more of deionized water, flower water and fermented water.

The specific preparation steps are,

1. The plant retinol and lecithin (the content of phosphatidylcholine is not less than 95%, and the proportion of liposome is 60%) are circulated for 3-5 times under the action of high-pressure micro-jet pressure of 120-180MPa to obtain lipid Body phytoretinol ready for use. The liposome encapsulation mainly solves the problems of water solubility and stability of plant retinol.

2. Add the thickener powder and the liposomal phytoretinol prepared in step 1 into the solvent at the same time and homogenize for 30-60 minutes to obtain the hydrogel-coated active substance.

3. Add the remaining active substances, including pomegranate peel extract, polypeptides, resorcinol and its derivatives, and plant extract composition to the compound in step 2 in sequence, and stir at 500-1500rpm for 10-30min , until uniformly dispersed without color bands.

The above-mentioned composition can be applied in the field of cosmetics as an important component of acne-removing products.

Beneficial effects of the present invention:

1. The anti-acne of the present invention has quick effect, and the effect can be seen by naked eyes within 24 hours and 7 days.

2. Compared with products with the same efficacy on the market, the present invention is mild and soothing, and less irritating, which meets the further needs of consumers for acne-removing products.

3. The present invention adopts the form of hydrogel-coated active substances to achieve the effect of sustained release of efficacy and mild product, which is innovative and novel in the cosmetics market, and has strong product competitiveness.

Description of drawings:

Fig. 1 is the MIC figure of the inhibition zone of embodiment 1.

Fig. 2 is the chicken embryo experiment figure of embodiment 1.

Fig. 3 is the face image of some volunteers in the acne removal test of embodiment 1.

Detailed ways:

Example 1

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

Among them, the thickener in 23% hydrogel is 0.5%, 20% is deionized water, lecithin is 2.5%, and the thickener is specifically ammonium acryloyldimethyl taurate/beheneth- 25 Methacrylate Crosspolymer 0.25%, Acrylates/C10-30 Alkyl Acrylate Crosspolymer 0.25%.

Example 2

Not covered by hydrogel, not covered by the coating process.

Example 3

The difference from Example 1 is that no plant extract composition is added.

Example 4

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

Among them, the thickener in 23% hydrogel is 0.5%, 20% is deionized water, lecithin is 2.5%, and the thickener is specifically ammonium acryloyldimethyl taurate/beheneth- 25 Methacrylate Crosspolymer 0.25%, Acrylates/C10-30 Alkyl Acrylate Crosspolymer 0.25%.

Example 5

The composition and weight proportion of the composition are: 0.5% of bakuchiol, 0.1% of silymarin, 0.05% of myristoyl hexapeptide-5, 1% of hexyl resorcinol, 0.2% of heparan sodium, pomegranate peel extract 0.1%, 2% aqueous solution of saffron extract, 4% aqueous solution of olive leaf extract, 1% aqueous solution of Sophora flavescens extract, 3% aqueous solution of citrus fruit extract, and the rest are solvents.

Wherein, the thickener content in the hydrogel is 0.5%, the water content is 20%, and the lecithin content is 2.5%.

Embodiment 6 performance test

Select the top three acne-removing products on the market, mainly containing Piaoning and acid components, as Comparative Example 1, and deionized water as Comparative Example 2, for comparative evaluation with Examples 1-5.

1. Antibacterial test (inhibition zone: MIC)

Test strain: Propionibacterium acnes

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

Under sterile conditions, inoculate the preserved Propionibacterium acnes (ATCC 6919) in BHI liquid medium, culture in an anaerobic incubator at 37°C for 48 hours, then centrifuge and resuspend, and adjust the concentration of Propionibacterium acnes to 1×10 ⁶ CFU/ml ,spare. Take a sterile petri dish with a diameter of 90 mm in a sterile environment, introduce 20 mL of BHI melted medium into each petri dish, cool and fix it, spread 100 μl of the resuspended Propionibacterium acnes solution evenly on the culture medium, and take A circular filter paper with a diameter of 7mm is dipped in the test drug, and the samples in the comparative example and the embodiment are diluted to 0.5% concentration respectively. After the blank control group and the positive control group are prepared respectively, the filter paper dipped in the test drug is evenly placed on On the above-mentioned BHI solid medium covered with Propionibacterium acnes, perform three parallel experiments, seal the petri dishes with parafilm, and place them horizontally upside down in an anaerobic incubator at 37°C for 20 hours, measure the diameter of the antibacterial ring, and calculate the The average diameter of the bacteriostatic ring.

The blank control group was PBS solution;

The positive control group is 0.1% triclosan, and the test results are shown in Table 1.

Table 1 Propionibacterium acnes inhibition zone results

In table 1, aseptic PBS treatment does not show antibacterial zone, the antibacterial zone diameter of positive control group 0.1% concentration trifilter hydroxydiphenyl ether is 40.3mm, embodiment 1,3,4 and comparative example 1 all have obvious Bacteriostasis effect, and embodiment 2 and 5 are weaker, thus it can be seen that coating process has certain influence to bacteriostasis, and the content of phytoretinol can not be too low, bacteriostasis ability can decline, but phytoretinol When the content increased, the antibacterial effect increased little.

2. Anti-acne efficacy test

Test objective: To test the 24h and 7d anti-acne effect on human body.

How to use: Apply locally on acne, do not stack with acid/vitamin A products.

Frequency of use: Once in the morning and evening after cleansing, reapply every 3-4 hours.

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

T./CNMA 0012-2020 Clinical Evaluation Criteria for Effective Skin Care Products for Acne Treatment.

Cosmetics safety technical specification (2015 edition).

Test process:

D0: Subject registration, laboratory technicians screen qualified subjects with oily skin and no less than 5 acnes, and complete the selection. The subject washes the face with the specified cleansing sample, and sits quietly for 30 minutes in a laboratory with a temperature of 21±1°C and 50±10% RH; test the basic value of the subject’s skin: take pictures with Primos-CR and analyze the volume of acne.

T24h: The test subject's skin value after 24 hours of using the sample, Primos-CR takes pictures and analyzes the acne volume.

D7: The test subject's skin value after 7 days of using the sample, Primos-CR took pictures and analyzed the acne volume.

Instrument description: Among them, Primos-CR is a digital optical three-dimensional image analysis instrument developed on the basis of a digital micro-stripe projector. By testing the position changes of the striped light and the gray value of all image points, the entire test can be obtained. A digital 3D image of the skin surface or test object. The smaller the measurement, the smaller the acne volume. The results are shown in Table 2 and Table 3.

The 24h anti-acne test result of table 2 various embodiment/comparative example sample

The 7d acne-removing test result of table 3 various embodiment/comparative example sample

As can be seen from Table 2 and Table 3, the improvement rate of acne volume in Embodiment 1, 3, 4 and Comparative Example 1 is better, and after comparative example 2 is basically adjusted by autoimmunity, the improvement rate of acne is lower. 5. Acne improvement is lower than other examples.

3. Irritation test: chicken embryo experiment

Test item: chicken embryo chorioallantoic membrane test for eye irritation/corrosion of cosmetics

Test basis: SN/T2329-2009 "Cosmetic Eye Irritation/Corrosivity Test for Chicken Embryo Chorioallantoic Membrane"

3.1 Stimulus score method: apply the following formula to calculate the stimulus score (IS), and keep the result to two decimal places:

In the formula: Sec H, Sec L, and Sec C respectively represent the average time of hemorrhage, angiolysis and coagulation observed on the CAM membrane, in seconds (s);

Table 4 Stimulus scoring method result evaluation

stimulus score Irritant classification IS<1 non-irritating 1≤IS＜5 Mild irritation 5≤IS＜9 Moderate irritation IS≥10 Strong irritant / corrosive

3.2 End point scoring method: score of each chicken embryo = the sum of hemorrhage, coagulation and angiolysis observed in each chicken embryo; end point evaluation (ES) = the sum of the scores of 6 chicken embryos.

Table 5 Evaluation of the results of the endpoint scoring method

stimulus score Irritant classification ES≤12 No/mild irritation 12<ES<16 Moderate irritation ES≥16 Strong irritant / corrosive

Test Acceptance Criteria:

The test results of Examples and Comparative Examples are shown in Table 6 (because the sample is non-transparent, adding it will cover the blood vessels on the surface, which will affect the judgment of blood vessels, so the ES scoring method is used instead of IS).

Table 6 Irritation Test Results

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

The results showed that Examples 1, 5 and Comparative Example 2 had no/slight irritation (ES not greater than 12), while the remaining Examples and Comparative Example 1 were 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.

The above is only an embodiment of the present invention, and does not limit the scope of the patent of the present invention. Any equivalent transformation made by the content of the description of the present invention, or directly or indirectly used in the relevant technical field, is equally included in the scope of patent protection of the present invention. Inside.

Claims (7)

1. The mild acne-removing composition is characterized by comprising, by weight, 0.5-5% of plant retinol, 0.1-3% of pericarpium Granati extract, 10-50% of hydrogel, 0.01-1% of polypeptides, 0.1-2% of resorcinol and derivatives thereof, 0-20% of plant extract composition and the balance of 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 crocus sativus extract aqueous solution, olive leaf extract aqueous solution, radix Sophorae Flavescentis extract, and citrus fruit extract aqueous solution.

2. The mild acne-removing composition according to claim 1, wherein said phytoretinol is one or more of silymarin, bakuchiol, phytosphingosine salicylate, bidens pilosa extract, and helichrysum extract.

3. The mild acne-removing composition according to claim 1, wherein said 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 acryloyldimethyl taurate/behenate-25 methacrylate cross-linked polymer and acrylic acid (esters) type/C10-30 alkanol acrylate cross-linked polymer.

4. The mild acne-removing composition according to claim 1, wherein said resorcinol and its derivatives are one or more of 2-methyl resorcinol, 4-butyl resorcinol, phenethyl resorcinol, hexyl resorcinol, resorcinol.

5. The mild acne-removing composition according to claim 1, wherein said solvent is one or more of deionized water, floral water, and fermented water.

6. A method for preparing the mild acne-removing composition according to claim 1, wherein the specific preparation steps are as follows,

(1) The phytoretinol and lecithin are circulated for 3 to 5 times under the action of high-pressure microjet pressure of 120 to 180MPa, and the liposome phytoretinol is obtained for standby. The liposome coating mainly solves the problem of water solubility and stability of the plant retinol.

(2) And (2) adding the thickener powder and the liposome plant retinol prepared in the step (1) into a solvent at the same time, and homogenizing for 30-60 min to obtain the hydrogel-coated active substance.

(3) Sequentially adding the rest active substances including pericarpium Granati extract, polypeptides, resorcinol and its derivatives, and plant extract composition into the compound of step 2), stirring at 500-1500 rpm for 10-30 min until the color bands are uniformly dispersed.

7. Use of a mild acne-removing composition according to claim 1, characterized in that it is applicable in the cosmetic field as an important ingredient of an acne-removing product.

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