Composition acting on skin and application thereof

By using compositions of seboresoid liposomes, urea tubular inclusions and dendrobium fermentation products, the problem of existing skin care products damaging the skin barrier when promoting the absorption of high-concentration polypeptides, retinol and other ingredients is solved, and efficient penetration, long-term soothing and moisturizing effects are achieved, reducing product costs.

CN119679665APending Publication Date: 2025-03-25GUANGZHOU XUJOHN BIO-TECH CO LTD
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Patent Information

Application Number
CN202411791744.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-06
Publication Date
2025-03-25

AI Technical Summary

Technical Problem

When existing skin care products promote the absorption of high-concentration polypeptides, retinol and other ingredients, they can easily damage the skin barrier, leading to irritation, redness and swelling, and the long-term soothing effect is difficult to achieve, resulting in increased product costs but poor results.

Method used

Compositions of seboresoid liposomes, urea tubular inclusions and dendrobium fermentation products are used to promote the penetration and absorption of target functional ingredients through their unique structure and composition, reduce the irritation to the skin, and achieve long-term soothing effect.

Benefits of technology

It improves the permeability and absorption effect of the target effective ingredients, reduces the irritation to the skin, achieves long-term soothing and moisturizing effects, and reduces product costs.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention relates to the field of skin care compositions, and discloses a composition acting on skin and application of the composition. The composition acting on the skin, provided by the invention, is prepared from the following components in parts by weight: 0.1 to 5 parts of sebum-like lipidosome, 0.01 to 3 parts of urea tubular clathrate compound and a dendrobium nobile fermentation product, the sebum-like liposome is prepared from the following components in parts by weight: 5 to 15 parts of prinsepia utilis royle oil, 5 to 10 parts of caprylic / capric triglyceride, 5 to 10 parts of simmondsia chinensis seed oil, 5 to 10 parts of squalane, 0.1 to 2 parts of sterol substances, 0.1 to 5 parts of ceramide AP and 0.1 to 5 parts of ceramide NP. The urea tubular clathrate compound comprises the following components in parts by weight: a fermented active matter, glycerol and urea, the fermented active matter is a product obtained by fermenting pumpkin seeds, bamboo shoots, melons and fruits inoculated with bacillus subtilis. The composition has the effects of relieving and promoting penetration of functional substances.
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Description

Technical Field

[0001] The present invention relates to the technical field of skin care compositions, in particular to a composition acting on the skin and application thereof. Background Art

[0002] Adding chemical penetration enhancers is the most commonly used penetration enhancement method so far. Water-soluble chemical penetration enhancers are usually used: dimethyl sulfoxide, pentanediol, dipropylene glycol, ethoxydiglycol, bis-diethoxydiglycol cyclohexane 1,4-dicarboxylate, etc. to promote the absorption of water-soluble active ingredients, or lauroyl pyrazolone, cyclodextrins, essential oils, or changing the physical properties of the functional ingredients to promote the absorption of lipophilic active ingredients through liposomes and nanoemulsions that encapsulate the target functional components. However, water-based polyols have poor transdermal effects, alcohol ethers are irritating and have a bad odor when added in large amounts, and liposomes that encapsulate the target functional substances face the disadvantages of high cost and low wide applicability.

[0003] Adding plant extracts is the most common soothing method; usually used are ginger root extract, dipotassium glycyrrhizinate, kava leaf / root / stem extract, aloe extract, rosemary leaf extract, chamomile extract, olive leaf extract, oat extract, etc. In addition, there are also methods of adding bisabolol, hydroxyphenylpropylamide benzoic acid, and 4-tert-butyl cyclohexanol to inhibit the stress response manifested by the skin, but these cannot achieve the effect of long-term, continuous release of soothing factors.

[0004] Due to the rapid development of the beauty industry in recent years, high-concentration and fast-acting cosmetics such as peptides, phospholipids, salicylic acid, retinol, and niacinamide have been popular among a large number of consumers. However, in order for these products to work on the market, they basically adopt the method of "breaking first and then building", that is, first impacting the skin barrier function, then re-establishing the barrier protection of the skin, stimulating collagen regeneration, etc. Some still require more professional techniques to achieve the effect. For example: high-concentration peptides, due to their difficult permeability, generally use the method of adding chemical permeants or microneedle introduction, while slightly milder chemical permeants (pentylene glycol, dipropylene glycol, ethoxydiglycol) have a general penetration effect, and microneedle introduction will inevitably cause skin breakage, bleeding, redness, swelling, and peeling. Another example is retinol and its derivatives. Although the transdermal absorption rate of different derivatives is different, their use will impact the skin barrier protection function, causing skin redness and burning sensation, as well as photosensitivity, dryness, and peeling. At present, in order to solve these problems with retinol, people basically build up tolerance gradually, or add a large amount of plant extracts, synthetic anti-allergic agents, or use it with other skin care products to achieve moisturizing and soothing effects. However, this is bound to increase the cost of the product, and in the end it may not have a good moisturizing and soothing effect.

[0005] In view of this, the present invention is proposed. Summary of the invention

[0006] The object of the present invention is to provide a composition for acting on the skin and its use.

[0007] The present invention is achieved in that:

[0008] In a first aspect, the present invention provides a composition for acting on the skin, comprising 0.1 to 5 parts of a dermoid liposome, 0.1 to 3 parts of a urea tubular inclusion compound, and a dendrobium fermentation product, wherein the amount of the dendrobium active substance therein is 0.03 to 0.6 parts;

[0009] The epidermosome comprises, by weight: 5-15 parts of prickle oil, 5-10 parts of caprylic / capric triglyceride, 5-10 parts of jojoba seed oil, 5-10 parts of squalane, 0.1-2 parts of sterols, 0.1-5 parts of ceramide AP and 0.1-5 parts of ceramide NP;

[0010] The urea tubular inclusion compound comprises, by weight: 15.5 to 32.5 parts of the fermented active substance, including the active ingredient, 30 to 50 parts of glycerol and 8 to 20 parts of urea, wherein the glycerol and the urea form a tubular structure to include the fermented active substance therein; the fermented active substance is a mixture of a first fermentation product and a second fermentation product, the first fermentation product is a product obtained by fully fermenting a culture medium containing pumpkin seeds by inoculating Bacillus subtilis, and the second fermentation product is a product obtained by fully fermenting a culture medium containing squash and fruits by inoculating Bacillus subtilis;

[0011] Alternatively, the fermented active substance is the product of fully fermenting the culture medium containing pumpkin seeds and winter squash fruits after inoculating Bacillus subtilis into the medium;

[0012] The components in the active matter after fermentation are calculated based on the winter squash and pumpkin seeds used for fermentation, and the mass ratio of the two is 1-10:5-35.

[0013] In an optional embodiment, the sebaceous liposomes include, by weight: 9-11 parts of prickle oil, 7-9 parts of caprylic / capric triglyceride, 7-9 parts of jojoba seed oil, 7-9 parts of squalane, 0.8-1.2 parts of sterols, 4-5 parts of ceramide AP, and 4-5 parts of ceramide NP;

[0014] Optionally, the sterol substance is selected from at least one of cholesterol, phytosterols, dihydrocholesterol, soybean sterols, rape sterols and avocado sterols.

[0015] In an optional embodiment, the urea tubular inclusion compound comprises, by weight: 15.5-32.5 parts of the active matter after fermentation, calculated as the active ingredient therein, 45-50 parts of glycerol and 13-17 parts of urea, wherein the components in the active matter after fermentation are calculated based on the winter melons and pumpkin seeds used for fermentation, and the mass ratio of the two is 4-6:20.

[0016] In an alternative embodiment, the method for preparing the transdermal liposome comprises:

[0017] Heat and mix prickle oil, caprylic / capric triglyceride, jojoba seed oil, squalane, sterols, ceramide AP and ceramide NP until there are no particles, to obtain a first mixture;

[0018] mixing the first mixture with the first solvent so that the first mixture is fully dissolved in the first solvent to obtain a second mixture;

[0019] Under vacuum conditions, removing the first solvent in the second mixture by rotary evaporation to obtain a lipid film;

[0020] The lipid film was mixed with a PBS phosphate buffer solution having a concentration of 0.04 to 0.06 mol / L at a solid-liquid ratio of 0.08 to 0.12 g:1 mL to obtain a third mixture, and the mixture was rotated at normal pressure for 45 min to obtain a third mixture;

[0021] The third mixture is treated 3 to 5 times by a dynamic high-pressure microfluidizer at a pressure of 130 to 170 MPa to obtain epidermal liposomes.

[0022] In an optional embodiment, the prickle oil, caprylic / capric triglyceride, jojoba seed oil, squalane, sterols, ceramide AP and ceramide NP are heated in a constant temperature water bath at a temperature of 55 to 65° C. for 18 to 20 minutes, and then ultrasonically assisted dissolution is performed for 10 to 20 minutes.

[0023] In an optional embodiment, the first solvent is anhydrous ethanol;

[0024] Optionally, the first mixture is mixed with anhydrous ethanol at a solid-liquid ratio of 18-22 mg:1 mL;

[0025] Optionally, the temperature of the rotary evaporation under vacuum conditions is 35-45°C.

[0026] In an optional embodiment, the method for preparing the post-fermentation active substance comprises:

[0027] In parts by weight, according to 25 parts of pumpkin seeds and winter squash fruits in total and 5 to 7 parts of glucose, crushed pumpkin seeds, crushed winter squash fruits, glucose and water are mixed, and sterilized to obtain a mixed culture medium;

[0028] Inoculating the bacterial liquid containing Bacillus subtilis into the mixed culture medium, fermenting at 35-40°C and 150-170R / min for 4-6 days, and filtering after fermentation to obtain the fermentation active substance;

[0029] The concentration of Bacillus subtilis in the bacterial solution is 5 to 10 cfu / mL, and the ratio of the inoculum volume of the bacterial solution to the volume of the culture medium is 7 to 9:100;

[0030] Optionally, the amount of water added is 55 to 65 parts;

[0031] Optionally, the sterilization method is 121°C for 15 min;

[0032] Optionally, the pH of the mixed culture medium is 6-7.

[0033] In an optional embodiment, the method for preparing the tubular inclusion compound comprises:

[0034] The urea and glycerol are mixed evenly to fully dissolve the urea to obtain a fourth mixture, the fermented active substance is mixed with the fourth mixture, and stirred at a temperature of 18 to 22° C. and a rotation speed of 700 to 800 r / min for 10 to 14 hours to obtain a viscous tubular inclusion compound.

[0035] In an optional embodiment, the combination comprises 0.8-1.2 parts of epidermosomes, 0.4-0.6 parts of urea tubular inclusion complexes, and 0.03-0.6 parts of the dendrobium fermentation product in which the amount of the dendrobium active ingredient is 0.03-0.6 parts.

[0036] In a second aspect, the present invention provides use of the composition according to any one of the aforementioned embodiments in ointments, cosmetics, skin care products or toiletries;

[0037] The target functional substance is contained in ointments, cosmetics, skin care products or toiletries;

[0038] The target efficacy substance includes at least one of an oily efficacy substance and a water-based efficacy substance;

[0039] The oily functional substance is selected from at least one of retinol palmitate, retinol, retinal, retinol acetate, retinol propionate, retinol palmitate, hydroxypinacolone retinoic acid ester, ascorbyl palmitate, ascorbyl tetraisopalmitate, ascorbyl tocopheryl maleate, tetrahexyldecyl ascorbate, ascorbyl stearate, salicylic acid, capryloyl salicylic acid, bakuchiol, pyridoxine tri-hexyldecanoate, artemisia annua oil, turmeric oil and carotene;

[0040] The aqueous functional ingredient is selected from at least one of acetyl hexapeptide-8, palmitoyl tripeptide-5, dipeptide diaminobutyroyl benzylamide diacetate, myristoyl hexapeptide-5, biotin, palmitoyl tripeptide-8, hydroxypropyl tetrahydropyrantriol, tetrahydromethylpyrimidine carboxylic acid, ergothioneine, oligopeptide-1, ascorbic acid (vitamin C), magnesium ascorbate, ascorbyl glucoside, niacinamide and 3-o-ethyl ascorbic acid.

[0041] The present invention has the following beneficial effects:

[0042] Prinus prickle oil, caprylic / capric triglyceride, jojoba seed oil, squalane, sterols, ceramide AP and ceramide NP are similar to the components of human biological membrane structure. Prinus prickle oil, jojoba seed oil, squalane, ceramide AP and ceramide NP have the effects of soothing and reducing inflammation. They are made into epidermal liposomes with a phospholipid bimolecular structure. By utilizing their tissue compatibility, low toxicity, amphiphilicity and good sustained-release effect, they are compounded to expand other functional substances, which can open the absorption channel of the skin, promote the functional substances to be more easily absorbed by the skin, have higher permeability, reduce the irritation of the functional substances to the skin, and have a long-lasting soothing effect. Therefore, epidermal liposomes have the effect of promoting the penetration of water-based or oily target functional ingredients; urea is one of the natural moisturizing factors in the skin, has strong water absorption, helps skin cells to renew and regenerate, reduces the amount of water loss in the epidermis or the outermost layer, and has a small molecular weight. When used with other ingredients, it can improve the penetration of other ingredients. Both zucchini seeds and winter squash are rich in tryptophan, which is a biochemical precursor of vitamin B3 and can be biosynthesized into vitamin B3 in the human body. Compared with the water extraction method, the tryptophan content of zucchini seeds and winter squash fermented with Bacillus subtilis has been greatly improved. Since urea has a very perfect planar triangular geometric configuration, urea and glycerol are made into the main body of a tubular inclusion complex. Through hydrogen bonding, the B3 precursor substances in the fermented pumpkin seeds and winter squash are chelated as objects. The main body surrounds the objects, and the B3 precursor substances are retained in the tubular structure and continuously released, which can achieve immediate and long-lasting moisturizing and soothing effects. Because urea has a small molecular weight, it can carry some effective substances (especially water-soluble substances) into the skin, playing a role in promoting penetration; the combination of epidermal liposomes and urea tubular inclusion complexes can achieve the effect of promoting the absorption of effective substances from different angles; the fermentation product of Dendrobium officinale is a fermentation liquid obtained by co-fermentation of two bacteria, Saccharomyces cerevisiae and Pichia pastoris. After double-bacteria fermentation, the molecular weight of Dendrobium polysaccharide is converted from a super large molecular weight to a polysaccharide with a "large-medium-small" multidimensional molecular weight distribution, and the molecular weight less than 15K accounts for 95% of the total polysaccharide content. Because of its small molecular weight, it can increase the retention of some effective substances in the epidermis and dermis of the skin, and at the same time, slow-release penetration. Therefore, combining an appropriate amount of Dendrobium officinale fermentation product with epidermal liposomes and tubular inclusion complexes can further promote the penetration of effective substances.

[0043] Therefore, the composition provided by the present invention, the epidermosome, the urea tubular inclusion compound and the fermented product of Dendrobium, play a synergistic role from different angles, so that the composition has a better effect of promoting the penetration and absorption of the functional substance. In addition, the combination of the above three substances can not only achieve the effect of promoting the penetration of the functional substance, but also synergistically achieve a soothing effect. DETAILED DESCRIPTION

[0044] In order to make the purpose, technical scheme and advantages of the embodiments of the present invention clearer, the technical scheme in the embodiments of the present invention will be described clearly and completely below. If the specific conditions are not specified in the embodiments, they are carried out according to conventional conditions or conditions recommended by the manufacturer. If the manufacturer of the reagents or instruments used is not specified, they are all conventional products that can be purchased commercially.

[0045] The features and performance of the present invention are further described in detail below in conjunction with the embodiments.

[0046] The composition for acting on the skin and its application provided by the embodiments of the present invention are described in detail below.

[0047] The composition for acting on the skin provided by the embodiment of the present invention comprises, by weight, 0.1 to 5 parts of skin-like liposomes, 0.01 to 3 parts of urea tubular inclusion compounds, and 0.03 to 0.6 parts of the dendrobium fermentation product in which the amount of the dendrobium active substance is calculated;

[0048] The epidermosome comprises, by weight: 5-15 parts of prickle oil, 5-10 parts of caprylic / capric triglyceride, 5-10 parts of jojoba seed oil, 5-10 parts of squalane, 0.1-2 parts of sterols, 0.1-5 parts of ceramide AP and 0.1-5 parts of ceramide NP;

[0049] The urea tubular inclusion compound comprises, by weight:

[0050] The urea tubular inclusion compound comprises, by weight: 15.5 to 32.5 parts of the fermented active substance, including the active ingredient, 30 to 50 parts of glycerol and 8 to 20 parts of urea, wherein the glycerol and the urea form a tubular structure to include the fermented active substance therein; the fermented active substance is a mixture of a first fermentation product and a second fermentation product, the first fermentation product is a product obtained by fully fermenting a culture medium containing pumpkin seeds by inoculating Bacillus subtilis, and the second fermentation product is a product obtained by fully fermenting a culture medium containing squash and fruits by inoculating Bacillus subtilis;

[0051] Alternatively, the fermented active substance is the product of fully fermenting the culture medium containing pumpkin seeds and winter squash fruits after inoculating Bacillus subtilis into the medium;

[0052] The components in the active matter after fermentation are calculated based on the winter squash and pumpkin seeds used for fermentation, and the mass ratio of the two is 1-10:5-35.

[0053] Since prickle oil is rich in unsaturated fatty acids and its composition is similar to human sebum, it has skin regeneration and moisturizing effects; it also has strong skin penetration ability and can play a similar role to azone. Jojoba oil has a very significant beauty effect on the skin, can unclog pores, regulate the oil secretion of oily or mixed skin, and improve inflamed skin, eczema, psoriasis, acne, etc. It has considerable therapeutic effect and soothing effect on allergic skin, and can restore vitality and luster to dry hair and dry wrinkled skin. Caprylic / capric triglyceride helps protect the skin barrier function, enhances the skin's resistance to external stimuli, and promotes collagen production; it is often used as a solvent, emollient, and penetration enhancer to improve product ductility, make the skin soft and have a lubricating effect; squalane has the function of strengthening the repair of the epidermis and damaged cells, opening the skin pores, promoting blood microcirculation, enhancing cell metabolism, helping to repair damaged cells, and has anti-inflammatory and sedative properties. By inhibiting the production and release of inflammatory factors, it can reduce skin sensitivity, redness, irritation and other discomfort symptoms. Phytosterol is a W / O type emulsifier with good and stable emulsification properties. It is a commonly used emulsifier for preparing vesicles with a phospholipid bilayer structure; in addition, phytosterol has a strong anti-inflammatory effect on the human body, has a good repair effect, has a high permeability to the skin, can reduce lipoprotein, enhance lipase activity, prevent erythema, inhibit skin inflammation, maintain skin surface moisture, prevent skin aging, etc., and can be used as a skin nutrient in many cosmetics.

[0054] Ceramide AP and ceramide NP help repair the skin barrier, maintain the normal barrier function of the skin's stratum corneum, and achieve the effect of hydrating and moisturizing. They have anti-inflammatory effects, help reduce skin inflammation, enhance the skin's protective barrier function, prevent water loss, and reduce skin dryness.

[0055] Prinus prickle oil, caprylic / capric triglyceride, jojoba seed oil, squalane, sterols, ceramide AP and ceramide NP are similar to the components of human biological membrane structure. Prinus prickle oil, jojoba seed oil, squalane, ceramide AP and ceramide NP have the effects of soothing and reducing inflammation. They are made into epidermal liposomes with a phospholipid bimolecular structure. By utilizing their tissue compatibility, low toxicity, amphiphilicity and good sustained-release effect, they are compounded to expand other functional substances, which can open the absorption channel of the skin, promote the functional substances to be more easily absorbed by the skin, have higher permeability, reduce the irritation of the functional substances to the skin, and have a long-lasting soothing effect. Therefore, epidermal liposomes have the effect of promoting the penetration of water-based or oily target functional ingredients; urea is one of the natural moisturizing factors in the skin, has strong water absorption, helps skin cells to renew and regenerate, reduces the amount of water loss in the epidermis or the outermost layer, and has a small molecular weight. When used with other ingredients, it can improve the penetration of other ingredients. Both zucchini seeds and winter squash are rich in tryptophan, which is a biochemical precursor of vitamin B3 and can be biosynthesized into vitamin B3 in the human body. Compared with the water extraction method, the tryptophan content of zucchini seeds and winter squash fermented with Bacillus subtilis has been greatly improved. Since urea has a very perfect planar triangular geometric configuration, urea and glycerol are made into the main body of a tubular inclusion complex. Through hydrogen bonding, the B3 precursor substances in the fermented pumpkin seeds and winter squash are chelated as objects. The main body surrounds the objects, and the B3 precursor substances are retained in the tubular structure and continuously released, which can achieve immediate and long-lasting moisturizing and soothing effects. Because urea has a small molecular weight, it has a strong effect of softening the stratum corneum and hydrating the skin, and can increase the moisture content of the stratum corneum, because it can carry some effective substances (especially water-soluble substances) into the skin, which plays a role in promoting penetration; the combination of epidermal liposomes and urea tubular inclusion complexes can achieve the effect of promoting the absorption of effective substances from different angles; the fermentation product of Dendrobium officinale is a fermentation liquid obtained by co-fermentation of two bacteria, Saccharomyces cerevisiae and Pichia pastoris. After double fermentation, the molecular weight of Dendrobium polysaccharide is converted from a super large molecular weight to a polysaccharide with a "large-medium-small" multidimensional molecular weight distribution, and the molecular weight less than 15K accounts for 95% of the total polysaccharide content. Because of its small molecular weight, it can increase the retention of some effective substances in the epidermis and dermis of the skin, and at the same time, it can be sustained-released and penetrated. Therefore, combining an appropriate amount of Dendrobium officinale fermentation product with epidermal liposomes and tubular inclusion complexes can further promote the penetration of effective substances.

[0056] Therefore, the composition provided by the present invention, the epidermosome, the urea tubular inclusion compound and the fermented product of Dendrobium officinale, play a synergistic role from different angles, so that the composition has a better effect of promoting the penetration of the functional substance. In addition, the combination of the above three substances can not only achieve the effect of promoting the penetration of the functional substance, but also synergistically achieve a soothing effect.

[0057] Preferably, the composition comprises, by weight, 0.8 to 1.2 parts of epidermosomes, 0.4 to 0.6 parts of urea tubular inclusion complexes, and 0.03 to 0.6 parts of the dendrobium fermentation product in which the amount of the dendrobium active substance is calculated;

[0058] Preferably, the fermentation product of Dendrobium officinale is the fermentation product disclosed in Patent No.: ZL 202410102750.3. The application of this fermentation product of Dendrobium officinale to the present application has a better effect.

[0059] Preferably, the sebaceous liposome comprises, by weight: 9-11 parts of prickle oil, 7-9 parts of caprylic / capric triglyceride, 7-9 parts of jojoba seed oil, 7-9 parts of squalane, 0.8-1.2 parts of sterols, 4-5 parts of ceramide AP and 4-5 parts of ceramide NP.

[0060] Specifically, the preparation method of the transdermal liposome comprises:

[0061] S1. Mix prickle oil, caprylic / capric triglyceride, jojoba seed oil, squalane, sterols, ceramide AP and ceramide NP in a constant temperature water bath at a temperature of 55 to 65° C. (e.g., 55° C., 60° C. or 65° C.) with stirring for 18 to 22 min, and then dissolve with ultrasound for 10 to 20 min to obtain a first mixture.

[0062] Optionally, the sterol substance is selected from at least one of cholesterol, phytosterols, dihydrocholesterol, soybean sterols, rape sterols and avocado sterols.

[0063] S2. Mixing the first mixture with the first solvent, so that the first mixture is fully dissolved in the first solvent to obtain a second mixture.

[0064] Optionally, the first solvent is anhydrous ethanol.

[0065] Optionally, the first mixture is mixed with anhydrous ethanol at a solid-liquid ratio of 18 to 22 mg:1 mL (eg, 18 mg:1 mL, 20 mg:1 mL, or 22 mg:1 mL).

[0066] S3. Under vacuum conditions at 35-45° C. (eg, 35° C., 40° C. or 45° C.), remove the first solvent in the second mixture by rotary evaporation to obtain a lipid film.

[0067] S4. Mix the lipid film with PBS phosphate buffer having a pH of 6 to 7 and a concentration of 0.04 to 0.06 mol / L (e.g., 0.04 mol / L, 0.05 mol / L or 0.06 mol / L) at a solid-liquid ratio of 0.08 to 0.12 g:1 mL (e.g., 0.08 g:1 mL, 0.1 g:1 mL or 0.12 g:1 mL) to obtain a third mixture, and rotate at normal pressure for 45 min to obtain the third mixture.

[0068] S5. The third mixture is treated 3 to 5 times by a dynamic high-pressure microfluidizer at a pressure of 130 to 170 MPa to obtain viscous epidermal liposomes.

[0069] Preferably, the urea tubular inclusion compound comprises, by weight: 0.5 to 2.5 parts of the fermented active matter, including the active ingredient therein, 45 to 50 parts of glycerol and 13 to 17 parts of urea.

[0070] Specifically, the method for preparing the post-fermentation active substance includes:

[0071] S1. Shell the pumpkin seeds, soak them in water at 35-45°C for 6-10 hours, then take them out, dry them with a paper towel, and crush them with a wall-breaking machine for 3-7 minutes to obtain coarsely processed pumpkin seeds.

[0072] S2. Wash the melon and cut it into dices, and crush it with a wall-breaking machine for 3 to 7 minutes to obtain roughly processed melon.

[0073] S3. Mix the crudely processed pumpkin seeds obtained in step S1, the crudely processed winter melons obtained in step S2, glucose and water according to 25 parts of pumpkin seeds and winter melons, 5-7 parts of glucose and 55-65 parts of water in parts by weight, and sterilize at 121°C for 15 minutes to obtain a mixed culture medium with a pH value of 6-7.

[0074] Optionally, in a total of 25 portions of pumpkin seeds and winter squash, the ratio of winter squash to pumpkin seeds is 1-10:5-35; preferably 4-6:20 (eg, 4:20, 5:20 or 6:20).

[0075] S4, after cooling the culture medium obtained in S3, inoculating the bacterial liquid containing Bacillus subtilis into the mixed culture medium, fermenting at 35-40° C. (e.g., 35° C., 38° C., or 40° C.) and 150-170 R / min (e.g., 150 R / min, 160 R / min, or 170 R / min) for 4-6 days, and filtering after fermentation to obtain liquid fermentation active substances;

[0076] The concentration of Bacillus subtilis in the bacterial solution is 5 to 10 cfu / mL (eg, 5 cfu / mL, 8 cfu / mL or 10 cfu / mL), and the ratio of the inoculum volume of the bacterial solution to the culture medium volume is 7 to 9:100 (eg, 7:100, 8:100 or 9:100).

[0077] Optionally, the Bacillus subtilis used in the examples of the present application is a conventional Bacillus subtilis, strain collection number: CCTCC AB 130003, which is deposited in China Center for Type Culture Collection.

[0078] Among the fermented active substances prepared in this step, the active ingredients are pumpkin seed fermentation product lysate, zucchini fruit fermentation product lysate and Bacillus fermentation product, which are 10-20 parts, 5-10 parts and 0.5-2.5 parts by weight respectively.

[0079] Specifically, the preparation method of the tubular inclusion compound comprises:

[0080] The urea and glycerol are mixed evenly to fully dissolve the urea to obtain a fourth mixture, the fermented active substance is mixed with the fourth mixture, and stirred for 10 to 14 hours (for example, 10 hours, 12 hours or 14 hours) at a temperature of 18 to 22° C. (for example, 18° C., 20° C. or 22° C.) and a rotation speed of 700 to 800 r / min (for example, 700 r / min, 750 r / min or 800 r / min) to obtain a tubular inclusion compound.

[0081] Optionally, the amount of urea is 8 to 20 parts, the amount of glycerol is 30 to 50 parts, and the active matter after fermentation is 15.5 to 32.5 parts of the active ingredients therein; preferably, the amount of urea is 13 to 17 parts, the amount of glycerol is 45 to 50 parts, and the active matter after fermentation is 15.5 to 32.5 parts of the active ingredients therein;

[0082] Optionally, the fourth mixture and the fermented active substance are mixed in a mass ratio of 1:0.8 to 1.2, for example, 1:1.

[0083] Application of the above composition provided by the embodiment of the present invention in ointments, cosmetics, skin care products or toiletries;

[0084] The target functional substance is contained in ointments, cosmetics, skin care products or toiletries;

[0085] The target efficacy substance includes at least one of an oily efficacy substance and a water-based efficacy substance;

[0086] The oily functional substance is selected from at least one of retinol palmitate, retinol, retinal, retinol acetate, retinol propionate, retinol palmitate, hydroxypinacolone retinoic acid ester, ascorbyl palmitate, ascorbyl tetraisopalmitate, ascorbyl tocopheryl maleate, tetrahexyldecyl ascorbate, ascorbyl stearate, salicylic acid, capryloyl salicylic acid, bakuchiol, pyridoxine tri-hexyldecanoate, artemisia annua oil, turmeric oil, and carotene;

[0087] The aqueous functional ingredient is selected from at least one of acetyl hexapeptide-8, palmitoyl tripeptide-5, dipeptide diaminobutyroyl benzylamide diacetate, myristoyl hexapeptide-5, biotin, palmitoyl tripeptide-8, hydroxypropyl tetrahydropyrantriol, tetrahydromethylpyrimidine carboxylic acid, ergothioneine, oligopeptide-1, ascorbic acid (vitamin C), magnesium ascorbate, ascorbyl glucoside, niacinamide and 3-o-ethyl ascorbic acid.

[0088] A number of embodiments and comparative examples are provided below to further illustrate the present invention.

[0089] Examples 1, 2 and Comparative Examples 8 to 9

[0090] The preparation methods and specific selections of the epidermosomes, tubular inclusion compounds and dendrobium fermentation products involved in Examples 1, 2 and Comparative Examples 8 to 9 are as follows:

[0091] The preparation method of epidermosomes is as follows:

[0092] By weight, 10 parts of prickle oil, 8 parts of caprylic / capric triglyceride, 8 parts of jojoba seed oil, 8 parts of squalane, 1 part of phytosterols, 5 parts of ceramide AP and 5 parts of ceramide NP were stirred and mixed in a water bath at a temperature of 60° C. for 15 minutes until there were no particles, to obtain a first mixture;

[0093] The first mixture was mixed with anhydrous ethanol at a solid-liquid ratio of 20 mg:1 mL, and the temperature was raised to 40° C. and stirred until completely dissolved to obtain a second mixture;

[0094] The ethanol in the second mixture is evaporated by rotary evaporation under vacuum to obtain a dry lipid film;

[0095] The lipid film was mixed with PBS phosphate buffer solution having a concentration of 0.05 mol / L and a pH of 6.5 at a solid-liquid ratio of 0.1 g:1 mL to obtain a third mixture, and the mixture was rotated at normal pressure for 45 min to obtain a third mixture;

[0096] The third mixture was treated four times using a dynamic high-pressure microfluidizer at a pressure of 150 MPa to obtain viscous epidermal liposomes.

[0097] The preparation method of the active substance after fermentation is as follows:

[0098] Take 20 parts of pumpkin seeds by weight, remove the shells, soak them in 35°C water for 8 hours, then take them out, dry them with paper towels, and crush them with a wall-breaking machine for 5 minutes to obtain coarse pumpkin seeds;

[0099] Take 5 portions of winter melon, wash them, cut them into dices, and crush them with a wall-breaking machine for 5 minutes to obtain roughly processed winter melon;

[0100] The crudely processed pumpkin seeds, crudely processed winter melons, 6 parts of glucose and 61 parts of water were mixed, sterilized at 121° C. for 15 minutes, and then cooled to obtain a mixed culture medium, wherein the pH of the culture medium was 6-7;

[0101] A bacterial solution containing Bacillus subtilis (wherein the concentration of Bacillus subtilis is about 8 cfu / mL) is inoculated into a mixed culture medium and fermented at 37°C and 160R / min for 5 days. After fermentation, the filtrate is filtered and collected to obtain the fermentation active substance. The ratio of the inoculation amount of the bacterial solution to the culture medium volume is 8:100.

[0102] The preparation method of tubular embedding is as follows:

[0103] In parts by weight, 15 parts of urea and 45 parts of glycerol are evenly mixed to fully dissolve the urea to obtain a fourth mixture, and the fermented active matter (active ingredient content is about 40%wt, including about 25%wt of pumpkin seed fermentation product lysate, 12.4%wt of zucchini fermentation product lysate and 2.6%wt of Bacillus fermentation product) is mixed with the fourth mixture in a mass ratio of 1:1, and stirred at a temperature of 20°C and a rotation speed of 700-800r / min for 12h to obtain a tubular inclusion compound.

[0104] The Dendrobium fermentation product is a fermentation product obtained by the fermentation method disclosed in Example 1 of Patent ZL 202410102750.3, wherein the content of Dendrobium active matter is about 6%, namely, the Asahi Makeup Dendrobium in Tables 1 to 6.

[0105] Examples 1, 2 and Comparative Examples 8-9 respectively provide an emulsion, and the formulas thereof are shown in Tables 1 to 5.

[0106] Table 1 Ingredient ratio of Example 1

[0107]

[0108]

[0109] Table 2 Ingredient ratio of Example 2

[0110]

[0111] Table 3 Ingredient ratio of comparative examples 1 to 3

[0112]

[0113]

[0114] Table 4 Ingredient ratio of comparative examples 4 to 7

[0115]

[0116] Table 5 Ingredient ratio of comparative examples 8 and 9

[0117]

[0118] Examples 3, 4 and Comparative Examples 10, 11

[0119] Examples 3, 4 and Comparative Examples 10, 11 are substantially the same as Example 1, except that their composition ratios are shown in Table 6:

[0120] Table 6 Ingredient ratios of Examples 3, 4 and Comparative Examples 10, 11

[0121]

[0122]

[0123] Experimental Example 1

[0124] Penetration-promoting effect test:

[0125] The Franz diffusion cell transdermal absorption test was conducted in accordance with the national standard GB / T 27818-2011 “In vitro test method for skin absorption of cosmetics”.

[0126] In vitro permeation was performed using Bama miniature pig skin and a modified Franz diffusion cell, and then the permeability of retinol palmitate was determined by HPLC-UV. The emulsions and creams of Examples 1-4 and Comparative Examples 1-7 and Comparative Examples 10-11 were tested using a diffusion cell test.

[0127] The specific steps are: take the skin of a one-month-old suckling pig (the thickness of the separated skin is 0.4-0.8mm), remove the subcutaneous tissue, cut it into circles with a diameter of about 1cm, wash it with saline, and absorb the moisture with filter paper for later use.

[0128] According to the standard of transdermal absorption, the pig skin was fixed between the upper and lower chambers of a vertical Franz diffusion cell, with the stratum corneum facing upwards. The effective area of ​​the diffusion cell was 3.14 cm 2, using 30% methanol aqueous solution as receiving solution, weigh about 0.5g of the cream of Examples 1-4 and Comparative Examples 1-7, 10, and 11, evenly apply it on the surface of pig skin, and seal it with a sealing film, so that the dermis of the skin is in close contact with the receiving solution (no bubbles are allowed). Place the diffusion cell in a constant temperature water bath (37±0.5)℃ of a transdermal diffusion tester, start electromagnetic stirring, and the speed is 250r / min; start timing 10min after adding the sample, collect 1mL of the solution in the receiving solution after 2, 4, 6, and 8h, and immediately replenish an equal amount of receiving solution, use a high performance liquid chromatograph to test the content of retinol palmitate and acetyl hexapeptide-8 and calculate the permeability. The chromatographic column used was EC-C18 (250 mm×4.6 mm, 5 μm) column, the column temperature was 30° C., the volume fraction ratio of the mobile phase was acetonitrile and tetrahydrofuran = 98:2, the flow rate was 1.0 mL / min, the detection wavelength was 325 nm, and the injection volume was 10 μL.

[0129] Table 7 Permeability (%) test results

[0130]

[0131] From the permeability of retinol palmitate in Table 7, it can be concluded that the permeability of Examples 1 to 2 is significantly higher than that of Comparative Examples 1-7. Comparing Example 1 with Example 2, since Example 2 is a thin milk, the texture is lighter, the film-forming agent and oil are less, and retinol palmitate is easier to penetrate, so Example 2 is slightly higher than Example 1; and the permeability of Comparative Examples 1-7 compared with Example 1 shows that the permeability of Example 1 is better than that of a single component or a pair of two, and is better than Comparative Example 7 without adding the patented composition. Even when used alone, a single component increases the dosage, and can only achieve an effect close to two-thirds at most. However, in actual product development, the cost-effectiveness issue must also be considered, so there are certain disadvantages. It can be seen that the composition provided by the present invention can improve the permeability of the target efficacy substance-retinol palmitate due to the coordination of the three components of the skin-like liposome, the urea tubular inclusion compound and the fermentation product of Dendrobium. From the permeability of acetyl hexapeptide-8 in Table 8, the permeability of Examples 3-4 is higher than that of Comparative Examples 10-11. Since the molecular weight of acetyl hexapeptide-8 is not high and it is a water-soluble functional substance, it is easier to absorb and penetrate on the skin. When the composition provided by the present application is added, the small molecule dendrobium polysaccharide increases the water content of the stratum corneum of the skin, so that the cells of this layer (especially the cells of the basal stratum corneum) swell, and the active substance forms a reservoir in this layer, thereby maintaining a certain release and action time of the active substance, and promoting the acetyl hexapeptide-8 to penetrate and absorb through the aqueous channel; there are also tubular inclusion compounds that can increase the moisture content of the stratum corneum, and it can be continuously released as a carrier, and the water-soluble substance can be better locked in the brick structure of the skin and slowly released. And the skin-like liposome can be known in many experiments that its bilayer structure is similar to the phospholipids of the skin, which can make the functional substance enter the dermis of the skin together to achieve a penetration-promoting effect.

[0132] Experimental Example 2

[0133] Soothing effect test:

[0134] According to QTC-C-LAB-TOP-055 "In vitro test method for soothing effect of cosmetics (hyaluronidase inhibition method)", the soothing effect is characterized by evaluating the inhibition rate of hyaluronidase activity of the test sample. It is suitable for evaluating cosmetics that achieve soothing effect by inhibiting hyaluronidase activity.

[0135] Hyaluronic acid is an important component of the extracellular matrix of the skin and plays an important role in maintaining the volume of the extracellular matrix and the normal physiological function of the skin. Hyaluronidase is an enzyme that can hydrolyze hyaluronic acid and is associated with most IgE-mediated type I and T-cell-mediated type IV allergic reactions. In addition, the hydrolysis products of hyaluronic acid promote skin inflammatory reactions. Inhibiting the activity of hyaluronidase can ensure the normal content and function of hyaluronic acid in the skin. This test method is an in vitro method, which mainly characterizes the soothing effect by evaluating the inhibition rate of the test sample on the activity of hyaluronidase.

[0136] Example 1 and Comparative Examples 1 to 9 were diluted with deionized water to 10 mg / mL; 0 mg / mL was used as a negative control, and 3.0 mg / mL of dipotassium glycyrrhizinate was used as a positive control; then 0.5 mL of hyaluronidase and 0.1 mL of CaCl2 were added to the reaction tube, and the mixture was incubated at 37°C for 20 min. 0.5 mL of sample diluent was added, and the mixture was incubated at 37°C for 20 min. 0.5 mL of sodium hyaluronate solution was added, and the mixture was incubated at 37°C for 30 min, and then placed at room temperature for 5 min. 0.1 mL of sodium carbonate solution was added and heated in boiling water for 10 min, and then immediately cooled with ice water. 1 mL of p-dimethylaminobenzaldehyde color developer was added, and finally the volume was adjusted to 5 mL with glacial acetic acid, and the mixture was placed for 45 min for color development. Each reaction solution was placed in a 1 cm colorimetric dish, and the absorbance was measured at 583 nm using a UV spectrophotometer. The hyaluronidase inhibition rate was calculated based on the absorbance, and the results were recorded in Table 8.

[0137] Hyaluronidase inhibition rate (%) = [1-(AB) / (CD)] × 100%;

[0138] Where: A is the absorbance of the experimental group;

[0139] B is the absorbance of the experimental blank group;

[0140] C is the absorbance of the control group;

[0141] D is the absorbance of the blank group.

[0142] Table 8 Hyaluronidase inhibition rate test results

[0143]

[0144] It can be concluded from the results of Table 8 that when the sample test concentration is 10 mg / mL, there are significant differences between Example 1 and Comparative Examples 1-8 and the negative control. The results of Example 1 and Comparative Example 8 show that when the target efficacy substance retinol palmitate is not added, the hyaluronidase inhibition rate of Comparative Example 8 is the highest. The inhibition rate of Example 1 after adding retinol palmitate is lower than that of Comparative Example 8, indicating that retinol palmitate is indeed irritating, but after adding the composition provided by the present application, it still has an excellent soothing effect, and the hyaluronidase inhibition rate is well characterized. It can be concluded from the results of Comparative Examples 1 to 6 that each component in the present application combination shows a good hyaluronidase inhibition rate, but the lack of one or two of them significantly reduces the effect. When the composition of the present application is not added, the inhibition rate of Comparative Example 9 is worse than that of Comparative Example 7, indicating that the increase of the target efficacy substance will increase irritation. Although the enzyme inhibition rate is higher than that of the negative control, the performance of the enzyme inhibition rate can only rely on the soothing effect of moisturizers and oils to protect the skin barrier. It can be seen that the composition provided by the invention has excellent soothing performance.

[0145] Example 3

[0146] Human skin patch test

[0147] The human skin patch test is to detect the potential adverse reactions of cosmetic products to human skin. The patch tester is applied to the intact part of the flexor side of the subject's forearm, and lightly pressed with fingers. After 24 hours of application, it is removed. After removing the patch tester, the results are interpreted according to the recommended standards of the International Contact Dermatitis Research Group (ICDRG). All negative reactions are judged as mild.

[0148] Test Area: Subject's face

[0149] Number of testers: 330

[0150] Subject screening: healthy, without skin and immune diseases, excluding pregnant, lactating women or women who are preparing to become pregnant within six months, volunteers aged 18 to 60 years old, both men and women, the test site has not received skin treatment, beauty and other tests that may affect the results; those who have not used hormonal drugs and immunosuppressants in the past month; those whose test site has not participated in other clinical trials now or in the past three months.

[0151] Test method: 0.02 mL of test sample (Examples 1, 2; Comparative Examples 1-9, 30 subjects in each group) was injected into each spot tester chamber, and no substance was placed as a blank control (30 subjects).

[0152] The judgment criteria are shown in Table 9, and the test results are shown in Table 11.

[0153] Table 9 Skin occlusive patch test skin reaction grading standard

[0154]

[0155]

[0156] Table 10 Skin occlusion patch test skin reaction test results

[0157]

[0158] According to the skin reactions of the subjects in Table 10, ① all the subjects in Example 1, Example 2, Comparative Example 8 and the blank control group showed negative reactions; ② When only the target efficacy substance (i.e., retinol palmitate) was added to Comparative Examples 7 and 9, and the composition provided by the present application was not added, different degrees of irritation reactions occurred, and the retinol palmitate in Comparative Example 9 was higher, and the number of irritation allergic reactions was more; ③ When the target efficacy substance was not added to Comparative Example 8, and the composition provided by the present application was added, there was no irritation allergic reaction; ④ After adding retinol palmitate and the composition provided by the present application, the subjects could No redness, sensitivity, itching and other reactions were shown after adding retinol palmitate; ⑤ When retinol palmitate was added and one or two of the compositions provided by the present application were removed, different degrees of irritation reactions also occurred, but not as serious as those in Comparative Examples 7 and 9; In summary, the composition provided by the present application can reduce the intolerance reaction after the use of retinol palmitate, play a soothing role, and enhance the skin barrier. Reducing one or two of them or not adding them will reduce the soothing effect; the composition provided by the present application can also achieve the same effect as a high dose at a low dose, making the overall product more cost-effective and gentler.

[0159] Example 4

[0160] Visia Skin Detector: Evaluation of Skin Brightening and Wrinkle Removal Effects

[0161] Professionals used the image analysis instrument VISIA (an instrument from German CK company) to compare the facial images of the users before and after the trial. VISIA obtains 8 indicators of the skin by taking photos, and numerically displays the real condition of the epidermis and subcutaneous layer of the skin, and analyzes it through three major analytical data.

[0162] Test subjects: 150 volunteers aged 18 to 60 years old with healthy skin and no skin or immune diseases were selected. Pregnant, lactating women or women who are preparing to get pregnant within six months were excluded. Both men and women were accepted. The test parts had not received skin treatment, beauty treatment or other tests that may affect the results; those who had not used hormone drugs and immunosuppressants in the past month; those whose test parts had not participated in other clinical trials now or in the past three months. They were divided into 15 test groups, with 10 volunteers in each group.

[0163] Test method: After cleaning the skin every morning and evening, the right face of the test subject is used as the experimental group. Each group of test subjects is evenly smeared with 0.5g of Examples 1 to 4 and Comparative Examples 1 to 11, and the left face of the test subject is used as the control group. 0.5g of pure water is evenly applied once a day at night for 4 consecutive weeks. No other cosmetics are used during the experiment. Use VISIA-CR to evaluate the skin color L*A*B* value of the test subject before use, 14d and 28d after use, and the image area of ​​the wrinkles around the eyes. The skin color is calculated by the L*A*B* value to calculate the average ITA° value of each group. The larger the ITA° value, the whiter the skin color. The average increase rate of facial ITA° value = [ITA° (after use by the experimental group) - ITA° (before use by the experimental group)] - [ITA° (after use by the control group) - ITA° (before use by the control group)] × 100% / ITA° (before use by the experimental group); The wrinkle removal effect was evaluated by using VISIA-CR to collect and analyze the image area of ​​the periocular skin wrinkles of the test subjects before use, 14d and 28d after use. The average reduction rate of periocular skin wrinkles in each test group = - (average area of ​​periocular skin wrinkles in each test group during the test - average area of ​​periocular skin wrinkles on the left face) × 100% / average area of ​​periocular skin wrinkles before use in each test group. The test results are shown in Tables 11 and 12:

[0164] Table 11 Average improvement rate of facial ITA° value

[0165]

[0166] From the statistical data in Table 11, it can be seen that ① the brightening rates of Comparative Example 8 without adding the target efficacy substance (i.e., retinol palmitate) and Comparative Example 7 with the target efficacy substance but without adding the composition provided by the present invention are relatively close, indicating that the target efficacy substance and the composition provided by the present invention have an effect on skin brightening; ② In Example 1, when both the target efficacy substance and the patented composition are added, the combined effect of the two is greatly improved in terms of skin brightening effect, and is much higher than the effect of single use. Combined with the results of the penetration promotion experiment of Test 1, it can be inferred that the composition provided by the present invention promotes the penetration of the target efficacy composition while brightening, so the improvement rate of Example 1 is greater than the sum of the improvement rates of Comparative Example 7 and Comparative Example 8; ③ From the improvement rates of Example 1 and Comparative Examples 1 to 6, it can be concluded that, under the premise of adding the same target efficacy substance and the total amount being similar, any one of the compositions provided by the present invention can assist the efficacy performance of the target efficacy substance. However, the lack of one or both of them will reduce the effect; ④ Summarizing the results of all the embodiments and comparative examples together, it can be seen that when the target efficacy substance is added, the average improvement rate of the facial ITA° value of comparative example 9 is close to the results of comparative examples 3 and 4, and the effect of adding comparative examples 8 and 9 is still weaker than that of embodiment 1; In summary, it can be concluded that the composition provided by the present invention is effective in brightening the skin, can synergize with the target efficacy substance, and can achieve the same efficacy as a high dose at a low dose, so that the overall product has a higher cost performance and better effect.

[0167] Comparing Examples 3 and 4 with Comparative Examples 10 and 11, respectively, the average increase rate of the ITA° value of Examples 3 and 4 is greater, indicating that the target efficacy substance (acetyl hexapeptide-8) combined with the composition provided by the present invention improves skin wrinkles, and thus has a better brightening effect.

[0168] Table 12 Average reduction rate of wrinkles around the eyes

[0169]

[0170] From the statistical data in Table 12, it can be seen that ① the wrinkle reduction rate of Comparative Example 8 without adding the target efficacy substance (i.e., retinol palmitate) and Comparative Example 7 with the target efficacy substance but without adding the composition provided by the present invention are relatively close, indicating that the target efficacy substance and the patent composition both have an improvement effect on periocular skin wrinkles; ② Comparison between Comparative Example 7 and Comparative Example 9 shows only a difference in the dosage of retinol palmitate. From the data, it can be seen that Comparative Example 9 has a better anti-wrinkle effect under the high dosage addition; ③ From the average area reduction rate of periocular skin wrinkles of Example 1 and Comparative Examples 1 to 7, it can be concluded that, under the premise of adding the same target efficacy substance, any one of the compositions provided by the present invention can assist the efficacy performance of the target efficacy substance. However, the lack of one or both of them will significantly reduce the effect; ④ In the case of adding both the target efficacy substance and the patented composition in Example 1, the combined effect of the two greatly improves the skin brightening effect, and is much higher than the effect of using them alone. Combined with the results of the penetration promotion experiment of Experimental Example 1, it can be inferred that the patented composition promotes the penetration of the target efficacy composition while anti-wrinkle. Therefore, the improvement rate of Example 1 is greater than the sum of the improvement rates of Comparative Example 7 and Comparative Example 8, and greater than the high-dose effect of Comparative Example 9. ⑤ For Comparative Example 9, the testers reported that they would have a red and itchy reaction after use, and they would continue to use it only after the red and itchy stopped. Therefore, when using it at a high dose, some testers need to build tolerance and then continue to use it, which is equivalent to the skin needing to repair itself, which reduces the number of uses, so its 28-day effect is not good.

[0171] Comparing Examples 3 and 4 with Comparative Examples 10 and 11, respectively, Examples 3 and 4 have significantly higher reduction rates on the area of ​​periocular wrinkles, indicating that the target efficacy substance (acetyl hexapeptide-8) combined with the composition provided by the present invention has a better improvement effect on periocular wrinkles.

[0172] In summary, the composition acting on the skin provided by the embodiment of the present invention has the function of promoting penetration and achieving a soothing effect. By combining the target efficacy component with the composition, the target efficacy group can be added in a low amount but has the same efficacy as a high amount, making the overall product more cost-effective and milder, and can also reduce the appearance of various other side effects of skin problems. The target efficacy component that can be matched with water-soluble or oil-soluble has no limitations, avoiding the disadvantages of the liposome that encapsulates the target efficacy substance, which is high in cost and not widely applicable.

[0173] The above are only preferred embodiments of the present invention and are not intended to limit the present invention. For those skilled in the art, the present invention may have various modifications and variations. Any modification, equivalent replacement, improvement, etc. made within the spirit and principle of the present invention shall be included in the protection scope of the present invention.

Claims

1. A composition for acting on the skin, characterized in that: The composition comprises, by weight, 0.1 to 5 parts of epidermal liposomes, 0.1 to 3 parts of urea tubular inclusion compounds, and 0.03 to 0.6 parts of the dendrobium fermentation product in which the amount of the dendrobium active substance is calculated; The epidermosome comprises, by weight: 5-15 parts of prickle oil, 5-10 parts of caprylic / capric triglyceride, 5-10 parts of jojoba seed oil, 5-10 parts of squalane, 0.1-2 parts of sterols, 0.1-5 parts of ceramide AP and 0.1-5 parts of ceramide NP; The urea tubular inclusion compound comprises, by weight: 15.5 to 32.5 parts of the fermented active substance, including active ingredients therein, 30 to 50 parts of glycerol, and 8 to 20 parts of urea, wherein the glycerol and the urea form a tubular structure to include the fermented active substance therein; the fermented active substance is a mixture of a first fermentation product and a second fermentation product, wherein the first fermentation product is a product obtained by fully fermenting a culture medium containing pumpkin seeds by inoculating Bacillus subtilis, and the second fermentation product is a product obtained by fully fermenting a culture medium containing squash and fruits by inoculating Bacillus subtilis; Alternatively, the fermented active substance is the product of fully fermenting the culture medium containing pumpkin seeds and winter squash fruits after inoculating Bacillus subtilis into the medium; The components in the active substances after fermentation are calculated based on the winter squash fruits and pumpkin seeds used for fermentation, and the mass ratio of the two is 1-10:5-35.

2. The composition according to claim 1, characterized in that The epidermosome comprises, by weight: 9-11 parts of prickle oil, 7-9 parts of caprylic / capric triglyceride, 7-9 parts of jojoba seed oil, 7-9 parts of squalane, 0.8-1.2 parts of sterols, 4-5 parts of ceramide AP and 4-5 parts of ceramide NP; Optionally, the sterol substance is selected from at least one of cholesterol, phytosterols, dihydrocholesterol, soybean sterols, rape sterols and avocado sterols.

3. The composition according to claim 1, characterized in that The urea tubular inclusion compound comprises, by weight: 15.5 to 32.5 parts of the fermented active matter, in which the active ingredients are calculated, 45 to 50 parts of glycerol, and 13 to 17 parts of urea, wherein the components of the fermented active matter are calculated based on the winter melons and pumpkin seeds used for fermentation, and the mass ratio of the two is 4 to 6:

20.

4. The composition according to claim 1 or 2, characterized in that The preparation method of the transdermal liposome comprises: Heat and mix prickle oil, caprylic / capric triglyceride, jojoba seed oil, squalane, sterols, ceramide AP and ceramide NP until there are no particles, to obtain a first mixture; mixing the first mixture with a first solvent so that the first mixture is fully dissolved in the first solvent to obtain a second mixture; Under vacuum conditions, removing the first solvent in the second mixture by rotary evaporation to obtain a lipid film; The lipid film is mixed with a PBS phosphate buffer solution having a concentration of 0.04 to 0.06 mol / L at a solid-liquid ratio of 0.08 to 0.12 g:1 mL to obtain a third mixture, and the mixture is rotated at normal pressure for 45 min to obtain a third mixture; The third mixture is treated 3 to 5 times by a dynamic high-pressure microfluidizer at a pressure of 130 to 170 MPa to obtain epidermal liposomes.

5. The composition according to claim 4, characterized in that Prinus prickle oil, caprylic / capric triglyceride, jojoba seed oil, squalane, sterols, ceramide AP and ceramide NP were heated in a constant temperature water bath at 55-65°C for 18-20 minutes, followed by ultrasound-assisted dissolution for 10-20 minutes.

6. The composition according to claim 4, characterized in that The first solvent is anhydrous ethanol; Optionally, the first mixture is mixed with the anhydrous ethanol at a solid-liquid ratio of 18 to 22 mg:1 mL; Optionally, the temperature of the rotary evaporation under vacuum conditions is 35-45°C.

7. The composition according to claim 1 or 3, characterized in that The method for preparing the fermented active substance comprises: In parts by weight, according to 25 parts of pumpkin seeds and winter squash fruits in total and 5 to 7 parts of glucose, crushed pumpkin seeds, crushed winter squash fruits, glucose and water are mixed, and sterilized to obtain a mixed culture medium; Inoculating the bacterial liquid containing Bacillus subtilis into the mixed culture medium, fermenting at 35-40° C. and 150-170 R / min for 4-6 days, and filtering after fermentation to obtain the fermentation active substance; The concentration of Bacillus subtilis in the bacterial solution is 5 to 10 cfu / mL, and the ratio of the inoculation volume of the bacterial solution to the volume of the culture medium is 7 to 9:100; Optionally, the amount of water added is 55 to 65 parts; Optionally, the sterilization method is 121°C for 15 min; Optionally, the pH of the mixed culture medium is 6-7.

8. The composition according to claim 1 or 3, characterized in that The preparation method of the tubular inclusion compound comprises: The urea and glycerol are mixed evenly to fully dissolve the urea to obtain a fourth mixture, the fermented active substance is mixed with the fourth mixture, and stirred at a temperature of 18 to 22° C. and a rotation speed of 700 to 800 r / min for 10 to 14 hours to obtain the viscous tubular inclusion compound.

9. The composition according to claim 1, characterized in that The composition comprises 0.8-1.2 parts of epidermosome, 0.4-0.6 parts of urea tubular inclusion compound and 0.03-0.6 parts of dendrobium fermentation product in which the amount of dendrobium active substance is 0.03-0.6 parts.

10. Use of the composition according to any one of claims 1 to 9 in ointments, cosmetics, skin care products or toiletries; The ointment, the cosmetic, the skin care product or the toiletries contain the target functional substance; The target efficacy substance includes at least one of an oily efficacy substance and a water-based efficacy substance; The oily functional substance is selected from at least one of retinol palmitate, retinol, retinal, retinol acetate, retinol propionate, retinol palmitate, hydroxypinacolone retinoic acid ester, ascorbyl palmitate, ascorbyl tetraisopalmitate, ascorbyl tocopheryl maleate, tetrahexyldecyl ascorbate, ascorbyl stearate, salicylic acid, capryloyl salicylic acid, bakuchiol, pyridoxine tri-hexyldecanoate, artemisia annua oil, turmeric oil and carotene; The aqueous functional ingredient is selected from at least one of acetyl hexapeptide-8, palmitoyl tripeptide-5, dipeptide diaminobutyryl benzylamide diacetate, myristoyl hexapeptide-5, biotin, palmitoyl tripeptide-8, hydroxypropyl tetrahydropyrantriol, tetrahydromethylpyrimidine carboxylic acid, ergothioneine, oligopeptide-1, ascorbic acid, magnesium ascorbate, ascorbyl glucoside, niacinamide and 3-o-ethyl ascorbic acid.

Citation Information

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