阅读说明：本技术 一种具有改善皮肤屏障的纳米乳液组合物及其应用 (Nanoemulsion composition capable of improving skin barrier and application thereof ) 是由 何健 容宝珊 许显 何廷刚 冯有好 刘思欣 徐碧茜 张兴宏 余育玲 李艳媚 郑晓 于 2020-06-15 设计创作，主要内容包括：本发明公开了一种具有改善皮肤屏障的纳米乳液组合物及其应用,包含如下组分：(A)乳化剂0.005-2.5%；(B)高级醇0.01-5%；(C)油脂0.02-60%；(D)多元醇或多糖3-30%；其中,所述组分(C)的含量≥组分(A)+组分(B)的含量之和。本发明通过选用低含量以及特定种类的乳化剂,与特定含量的高级醇、油脂以及多元醇或多糖进行复配,控制油脂含量≥乳化剂和乳化剂的复配重量之和,制备得到平均粒径≤200nm的纳米乳液组合物,该纳米乳液组合物具有低的粘度,从而具有便捷的使用感；具有不受不同种类油脂的影响和良好的稳定性；具有良好的透明感和如膏霜般柔软、滋润等肤感,可以增加肌肤保湿度、滋润度、光滑度和提升柔软性；由于乳化剂用量降低,可增加肌肤耐受性。(The invention discloses a nano-emulsion composition capable of improving skin barrier and application thereof, wherein the nano-emulsion composition comprises the following components: (A) 0.005-2.5% of emulsifier; (B) 0.01-5% of higher alcohol; (C) 0.02-60% of grease; (D) 3-30% of polyol or polysaccharide; wherein the content of the component (C) is more than or equal to the sum of the content of the component (A) and the content of the component (B). According to the invention, the low-content and specific-type emulsifier is selected and compounded with the specific-content higher alcohol, the specific-content grease and the specific-content polyol or polysaccharide, the grease content is controlled to be more than or equal to the sum of the compounded weights of the emulsifier and the emulsifier, and the nano-emulsion composition with the average particle size of less than or equal to 200nm is prepared and has low viscosity, so that the nano-emulsion composition has convenient use feeling; the grease is not influenced by different types of grease and has good stability; the skin care cream has good transparent feeling and soft and moist skin feeling like cream, and can increase the moisture retention, the moistening degree and the smoothness of the skin and improve the softness; the dosage of the emulsifier is reduced, so that the skin tolerance can be improved.)

1. A nanoemulsion composition for improving skin barrier, which is characterized by comprising the following components in percentage by weight:

(A) 0.005-2.5% of emulsifier;

(B) 0.01-5% of higher alcohol;

(C) 0.02-60% of grease;

(D) 3-30% of polyol or polysaccharide;

wherein the content of the component (C) is more than or equal to the sum of the contents of the component (A) and the component (B).

2. The nanoemulsion composition of claim 1, comprising the following components in weight percent:

(A) 0.01 to 1.5 percent of emulsifier;

(B) 0.02-3% of higher alcohol;

(C) 0.5-40% of grease;

(D) 6-25% of polyol or polysaccharide;

wherein the content of the component (C) is more than or equal to the sum of the contents of the component (A) and the component (B).

3. The nanoemulsion composition of any of claims 1-2, comprising the following components, in weight percent:

(A) 0.03-1.2% of emulsifier;

(B) 0.06-2% of higher alcohol;

(C) 2-20% of grease;

(D) 10-20% of polyhydric alcohol or polysaccharide;

wherein the content of the component (C) is more than or equal to the sum of the contents of the component (A) and the component (B).

4. The nanoemulsion composition of any of claims 1-3, wherein component (A) is selected from one or more of alkyl glycoside emulsifiers, polyglycerol emulsifiers, amino acid based gemini surfactants, lecithins and modified emulsifiers thereof.

5. The nanoemulsion composition of claim 4, wherein the alkyl group of the alkyl glycoside emulsifier is selected from one or more of lauryl, coco, myristyl, cetyl, stearyl; the polyglycerol emulsifier is selected from glycerol with the polymerization degree of 6-10, and the alkyl is selected from one or more of lauryl, coco, myristyl, cetyl and stearyl; the amino acid based gemini surfactant has at least two hydrophobic hydrocarbon chains, two polar head groups and a linking group selected from the group consisting of: one or more of arginine-based gemini surfactant, lysine-based gemini surfactant, cystine-based gemini surfactant and serine-based gemini surfactant; the lecithin and the modified emulsifier thereof are selected from one or more of soybean lecithin, hydroxylated lecithin, hydrogenated lysolecithin and lysolecithin.

6. A nanoemulsion composition according to any one of claims 1-3, characterised in that the sum of the contents of component (a) + component (B) is ≥ 0.015%, preferably ≥ 0.1%.

7. The nanoemulsion composition of any one of claims 1-3, wherein the ratio of component (A): the compound weight ratio of the component (B) is more than or equal to 1: 0.3, preferably ≥ 1: 0.6.

8. the nanoemulsion composition according to any one of claims 1 to 3, characterized in that the component higher alcohol (B) is selected from one or more of octanol, decanol, lauryl alcohol, myristyl alcohol, stearyl alcohol, isostearyl alcohol, cetyl alcohol, oleyl alcohol, linoleyl alcohol, behenyl alcohol, octanol, undecanol, tridecyl alcohol, pentadecanol, heptadecanol, nonadecanol, heneicosanol; the component (C) is one or more selected from silicone oil, silica gel and modified substances thereof, fat, oil, wax, hydrophobic plant extract, olefin, lipoid, ester, liquid alcohol, vitamin, sun-screening agent, essential oil and phospholipid; the component (D) is one or more selected from glycerol, sorbitol, propylene glycol, butanediol, pentanediol, isoprene glycol, hexanediol, glucose, maltose, maltitol, sucrose, fructose, xylitol, pentaerythritol and starch degrading sugar.

9. The nanoemulsion composition of any one of claims 1-8, wherein the nanoemulsion composition has an average particle size of 200nm or less, and can be used in one or more of high-pressure homogenization, microfluidization, and ultrasound in high-energy emulsification.

10. Use of a nanoemulsion composition with skin barrier improving properties as claimed in any one of claims 1 to 9, in cosmetics or pharmaceuticals for the skin, scalp and hair, characterized in that: the product can be used alone or mixed with other cosmetic or pharmaceutical raw materials to prepare into spray, gel, lotion, ointment, and cream.

Technical Field

The invention relates to the technical field of cosmetics or medicines, in particular to a nano-emulsion composition capable of improving skin barrier and application thereof.

Background

Various emulsified compositions have been widely used in the field of cosmetics or medicines, but most of the emulsified compositions are cream-like or white turbid emulsions, and the viscosity of the emulsified compositions is high; in order to improve the appearance and reduce the viscosity, part of cosmetics achieve the milky appearance of the body by adding the traditional opacifier (such as styrene/acrylic acid (ester) copolymer), but the substances belong to plastic particles, are not easy to degrade, have adverse effects on the environment and biological enrichment, and do not have the moistening and moisturizing effects of an emulsion formula; in addition, some methods for reducing the emulsified particle size are commonly adopted as D-phase emulsification, agglutination or PIT emulsification, and have certain requirements on the selection of an emulsifier in a formula, the dosage of the emulsifier, the type and content of oil and fat and a process; increased emulsifier content, which may lead to increased formulation irritation; due to stability, the oil content of the oil-water emulsion cannot be too high, so that the moistening degree is insufficient; the types of the grease are limited, and the skin feeling requirements required by the emulsification formula cannot be met; these characteristics limit their use in cosmetics or pharmaceuticals for application to the skin, scalp and hair.

Disclosure of Invention

In view of this, the present invention aims to overcome the disadvantages of the prior art and to provide a nanoemulsion composition (average particle size ≦ 200nm) with improved skin barrier, which has low viscosity and good stability; therefore, the skin cream has good transparent feeling and soft and moist skin feeling like cream; and can increase skin moisture and improve skin softness; the dosage of the emulsifier is reduced to 1/214 of the dosage of the grease, so that the irritation caused by the emulsifier can be obviously reduced, and the tolerance of the skin is improved; aiming at the characteristic that different oils and fats need different HLB (hydrophile-lipophile balance) emulsification systems are not considered in the formula of the traditional emulsification system, the invention can directly use different oils and fats without changing the type and the dosage of an emulsifier in the formula, thereby greatly widening the adaptability of the formula and simplifying the formula development; aiming at the characteristics of the nano emulsion, the nano emulsion is expected to be used in cosmetics and medicines to increase the transdermal absorption of active substances and improve the utilization rate of functional components and the product efficacy.

The invention relates to a nano-emulsion composition for improving skin barrier, which comprises the following components in percentage by weight:

wherein the content of the component (C) is more than or equal to the sum of the contents of the component (A) and the component (B).

Preferably, the nano emulsion composition comprises the following components in percentage by weight:

wherein the content of the component (C) is more than or equal to the sum of the contents of the component (A) and the component (B).

More preferably, the nano emulsion composition comprises the following components in percentage by weight:

wherein the content of the component (C) is more than or equal to the sum of the contents of the component (A) and the component (B).

Wherein the component (A) is selected from one or more of alkyl glycoside emulsifier, polyglycerol emulsifier, amino acid group gemini surfactant, lecithin and modified emulsifier thereof.

As the alkyl glycoside emulsifier of the component (A) of the present invention, saturated and unsaturated alkyl groups having 8 to 22 carbons can be used. They may be used alone or in admixture of two or more of the foregoing. In view of the raw material source, one or more of lauryl, cocoyl, myristyl, cetyl and stearyl groups are particularly preferable.

The polymerization degree of glucose in the alkyl glycoside as the component (A) is not particularly limited, and the average polymerization degree of the glycoside is particularly preferably 1 to 5 in consideration of the origin of the raw material.

As the polyglycerin emulsifier of the component (A) of the present invention, saturated and unsaturated alkyl groups of 8 to 22 carbons can be used. They may be used alone or in admixture of two or more of the foregoing. In view of the raw material source, one or more of lauryl, cocoyl, myristyl, cetyl and stearyl groups are particularly preferable.

The polymerization degree of the polyglycerin emulsifier of the component (A) glycerin is selected to be 6 to 10 in consideration of the source of the raw material.

The amino acid group gemini surfactant of the component (A) has at least two hydrophobic hydrocarbon chains, two polar head groups and a connecting group, and is specifically selected from one or more of arginine group gemini surfactant, lysine group gemini surfactant, cystine group gemini surfactant and serine group gemini surfactant; more preferably sodium bis (lauramidoglutamine) lysine.

The lecithin and modified emulsifier of the component (A) are selected from one or more of soybean lecithin, hydroxylated lecithin, hydrogenated lysolecithin and lysolecithin.

Wherein the sum of the contents of the component (A) and the component (B) is more than or equal to 0.015 percent, and the moisture is partially volatilized during coating, so that cream-like use feeling can be obtained under the dosage; the sum of the contents of the component (A) and the component (B) is preferably more than or equal to 0.1 percent; when the sum of the contents of the component (A) and the component (B) is less than 0.015%, gelation does not occur, and a cream-like feeling of use does not occur.

Preferably, the component (a): the compound weight ratio of the component (B) is more than or equal to 1: 0.3, preferably 1: 0.6. a component (A): component (B) < 1: at 0.3, the viscosity increases during formulation stability and the low viscosity requirements of the present invention are not met.

The higher alcohol of the component (B) may include one or more of octanol, decanol, lauryl alcohol, myristyl alcohol, stearyl alcohol, isostearyl alcohol, cetyl alcohol, oleyl alcohol, linoleyl alcohol, behenyl alcohol, octanol, undecyl alcohol, tridecyl alcohol, pentadecyl alcohol, heptadecyl alcohol, nonadecyl alcohol, and heneicosyl alcohol. They may be used alone or in admixture of two or more of the foregoing, with stearyl alcohol and cetyl alcohol being particularly preferred.

The component (C) is selected from one or more of silicone oil, silica gel and modified substances thereof, fat, oil, wax, hydrophobic plant extract, olefin, lipoid, ester, liquid alcohol, vitamin, sun-screening agent, essential oil and phospholipid. The silicone oil, the silica gel and modified substances thereof, such as linear or cyclic polydimethylsiloxane, amino, alkyl, phenyl silicone oil and the like; the fats and oils include natural fats and oils such as shea butter, jojoba seed oil, avocado oil, rice bran oil, olive oil, grape seed oil, sunflower seed oil, soybean oil, almond oil, coconut oil, beef tallow, lard, etc.; saturated oil obtained by hydrogenating the oil; and synthetic mono-, di-or triglycerides; among them, waxes such as lanolin and the like and their corresponding derivatives; the hydrophobic plant extract such as phytosterol, resveratrol, etc.; olefins such as liquid paraffin, mineral esters, squalene, squalane, mineral oil, and the like; such lipids as cholesterol, ceramide, sucrose esters, and ceramides; esters such as isopropyl myristate, isopropyl palmitate, and the like; the liquid alcohol such as octyldodecanol, etc.; the vitamins, such as vitamins A, D and E, and vitamin alkyl esters, including vitamin C alkyl esters; the sunscreen agent, such as octyl methoxy cinnamate, butyl methoxy benzoyl methane, etc.; the essential oil, such as oleum Menthae Dementholatum, oleum Jasmini sambac, lemon oil, oleum Eucalypti, tea tree oil, and oleum Lavandula Angustifolia; they may be used alone or in admixture of two or more of the foregoing.

The component (D) is one or more selected from glycerol, sorbitol, propylene glycol, butanediol, pentanediol, isoprene glycol, hexanediol, glucose, maltose, maltitol, sucrose, fructose, xylitol, pentaerythritol and starch degrading sugar.

Wherein the average particle size of the nano emulsion composition is less than or equal to 200nm, and the application process can be one or more of high-pressure homogenization, microjet or ultrasonic in high-energy emulsification. If the average particle diameter exceeds 200nm, demulsification or viscosity increase may occur at a low viscosity. The average particle diameter used here was measured by a dynamic scattering method, specifically, particle diameter measurement was performed using a malvern mastersizer 3000.

The nanoemulsion composition having the effect of improving the skin barrier of the present invention may appropriately contain various suitable components used in general cosmetics, special cosmetics, pharmaceuticals, etc., in addition to the above-described main components, without reducing the effect of the present invention. More specifically, water, essence, ultraviolet absorber, moisturizer, physiologically active ingredient, antioxidant, anti-inflammatory agent, antibacterial agent, antiperspirant, chelating agent (e.g., disodium EDTA), thickener, neutralizer, pH adjuster (e.g., citric acid), etc. may be included, and the above components may be included in an amount conventionally added to cosmetics or pharmaceuticals, depending on the particular use and form.

After the thickening agent such as carbomer is added, the moisturizing effect of the cream emulsion is achieved, the effect of wiping water is achieved, and the use feeling of the cream emulsion has good use feeling which cannot be achieved by the existing cream emulsion formula.

The nanoemulsion composition having an improved skin barrier according to the present invention is suitable for use in cosmetics or pharmaceuticals for skin, scalp and hair.

Compared with the prior art, the invention has the following beneficial effects:

according to the invention, the low-content and specific-type emulsifier is selected and compounded with the emulsifier, the grease and the polyol or the polysaccharide with specific content, the grease content is controlled to be more than or equal to the sum of the compounded weight of the emulsifier and the emulsifier, and the nano-emulsion composition with the average particle size of less than or equal to 200nm is prepared, and has low viscosity (the physical property of aqueous solution can be improved when the nano-emulsion composition is filled or taken out), so that the nano-emulsion composition has convenient use feeling; the stability is good; has good transparent feeling and soft and moist skin feeling like cream; compared with the daily emulsifying system formula, the emulsifier content in the composition can be as low as 1/214 of the oil content, which is far lower than the emulsifier content in the daily emulsifying system formula, so that the irritation caused by the emulsifier in the composition can be obviously reduced; aiming at the characteristics of the nano emulsion, the nano emulsion can be used for increasing the transdermal absorption of active substances in cosmetics and medicines and improving the utilization rate of functional components and the product efficacy. After the thickening agent such as carbomer is added, the moisturizing effect of the cream emulsion can be achieved, the effect of wiping water can be achieved, and the use feeling of the cream emulsion has good use feeling which cannot be achieved by the existing cream emulsion formula.

Detailed Description

The present invention is further illustrated by the following specific examples, which are, however, not intended to limit the scope of the invention.

The raw materials used in the examples of the present invention are all commercially available.

The test method of each performance index is as follows:

stability test method of nanoemulsion composition: the samples were placed in an oven at room temperature and 50 ℃ for 4 weeks, respectively, and tested for appearance, particle size, viscosity, feel and moisture retention.

Method for testing the appearance of the nanoemulsion composition: and (4) carrying out visual observation at room temperature under direct sunlight.

Method for testing average particle size of nanoemulsion composition: particle size measurements were performed using a malvern mastersizer3000, using D50 as the particle size measurement.

Method for testing viscosity of nanoemulsion composition:

viscosity range 0-50 mPas: brookfiltered DV-C digital viscometer, No. 61 rotor, rotating speed 60rpm, material body temperature: 25 ℃, reading time: readings were taken 1 minute after start-up.

Viscosity range 51-300 mPas: brookfiltered DV-C digital viscometer, No. 62 rotor, rotating speed 60rpm, material body temperature: 25 ℃, reading time: readings were taken 1 minute after start-up.

Viscosity range 301-: brookfiltered DV-C digital viscometer, No. 63 rotor, rotating speed 60rpm, material body temperature: 25 ℃, reading time: readings were taken 1 minute after start-up.

Viscosity range 1200-6000 mPas: brookfiltered DV-C digital viscometer, No. 64 rotor, rotating speed of 60rpm, material body temperature: 25 ℃, reading time: readings were taken 1 minute after start-up.

Method for testing the feeling of use of the nanoemulsion composition: assessing whether the cream-like use feeling is achieved when the cream-like use feeling is applied, and scoring: the user can feel the use feeling like cream and slightly feel the use feeling like cream; the user feels little sensation like cream, and the user feels no sensation like cream.

Skin moisturization, elasticity and smoothness improvement evaluation

The test population: the subject is 18-35 years old, healthy Chinese male and female.

Skin type: dry skin.

Number of human subjects: 30 persons

The product using method comprises the following steps: the use method comprises the following steps: the inner side of the arm is positioned in a subarea mode, a drop of product is dripped to the corresponding area, and the product is uniformly coated on the area by one finger. The dosage is as follows: 1 drop at a time. Frequency: twice a day, in the morning and at night.

And (3) testing period: visits were made each at 4 weeks, week 0, week 1, weeks two and 4 weeks, for a total of 4 visits.

The use time is as follows: 4W

Testing time points: four time points: t0, T1w, T2w, T4 w.

Evaluation method of moisturizing property of nanoemulsion composition:

and (3) testing environment: temperature: 21. + -. 1 ℃ humidity: 40-60 percent;

the evaluation method comprises the following steps: the TEWL values of the same arm site were counted and averaged before and after the test sample was used for 1 week, 2 weeks, and 4 weeks, and the TEWL improvement rate was calculated by comparing the initial values (low TEWL means improvement).

And (3) testing items: trans-epidermal water loss rate (g/m2 h): a transepidermal water loss rate tester TewameterTM300(Courage & Khazaka, Germany) was used;

evaluation method of skin elasticity improvement degree of nanoemulsion composition:

and (3) testing environment: temperature: 21. + -. 1 ℃ humidity: 40-60 percent;

the evaluation method comprises the following steps: the elastic values of the same arm part before and after the test sample is used for the subject for 1 week, 2 weeks and 4 weeks are counted and averaged, and the elastic improvement rate (high elastic value means improvement) is calculated by comparing the initial values.

And (3) testing items: r2(a.u.) skin elasticity tester CutomermerMPA 580(Courage & Khazaka, Germany)

Evaluation method of skin smoothness improvement of nanoemulsion composition:

and (3) testing environment: temperature: 21. + -. 1 ℃ humidity: 40-60 percent;

the evaluation method comprises the following steps: the friction force of the same arm part of the subject before and after the test sample is used for 1 week, 2 weeks and 4 weeks is counted and averaged, and the friction force improvement rate (low friction force means improvement) is calculated by comparing the initial values.

Testing indexes are as follows: friction force (a.u.), skin friction force test probe FR700(Courage & Khazaka, Germany)