Extended-spectrum multi-effect composite sunscreen carrier containing DHHB, IMC and DHBT as well as preparation and application of extended-spectrum multi-effect composite sunscreen carrier

Abstract

The invention discloses an extended-spectrum multi-effect composite sunscreen carrier containing DHHB, IMC and DHBT as well as preparation and application of the extended-spectrum multi-effect composite sunscreen carrier, and belongs to the field of cosmetics. The extended-spectrum multi-effect composite sunscreen carrier disclosed by the invention is prepared from DHHB (diethylaminohydroxybenzoyl hexyl benzoate), IMC (isoamyl p-methoxycinnamate), DHBT (diethylhexyl butyramido triazinone), pomegranate seed oil, a bergenia crassifolia extract and nano-carrier raw materials such as an emulsifier, a co-emulsifier, grease, polyhydric alcohol and water. According to the invention, the specific sun-screening agent and the sun-screening synergistic active component are combined, matched and loaded in the nano-structure lipid carrier, so that the irritation possibly occurring in the use process of the sun-screening agent can be effectively reduced, the damage of ultraviolet rays to the skin is relieved, and the overall sun-screening performance of the sun-screening carrier is improved. The sunscreen carrier disclosed by the invention can form a compact protective film on the surface of skin, so that the percutaneous moisture loss of the skin is effectively reduced, the safety of a product is enhanced, and meanwhile, the sunscreen can play an optimal role.

Description

Technical Field

[0001] The present invention belongs to the field of cosmetics, relates to sunscreen cosmetics, and particularly relates to an ultra-broad-spectrum multi-effect composite sunscreen carrier containing DHHB, IMC and DHBT, and its preparation and application. Background Art

[0002] The aging of human skin is mainly divided into natural aging and photoaging. Natural aging belongs to endogenous aging. As people age, the subcutaneous tissue begins to shrink, collagen is lost, the skin becomes thinner, elasticity decreases, and wrinkles gradually appear. This process is inevitable. Photoaging belongs to exogenous aging, which refers to skin aging caused by sunlight (ultraviolet rays). Studies have shown that 75% of the factors causing skin aging are caused by ultraviolet rays. Among them, long-wavelength UVA (320 - 400 nm) has weak energy but can penetrate to the lower part of the dermis, directly causing skin tanning. Medium-wavelength UVB (290 - 320 nm) has higher energy and can penetrate into the basal layer of the epidermis or the upper part of the dermis to damage DNA, resulting in skin sunburn, and then indirectly causing skin tanning. At the same time, there is also a risk of skin cancer. At present, with the continuous development of environmental biology and medicine, people's cognitive level has also been continuously improved, and the understanding and demand for sunscreen have also been continuously deepened and increased. This has prompted more and more cosmetics companies to focus on the research and development of sunscreen-related products and raw materials, making the cosmetics sunscreen market grow rapidly. In particular, high-sun protection index products are becoming more and more popular in the market, which is also the future development trend of sunscreen products.

[0003] The sun protection factor SPF value represents the protection against UVB, which refers to the ability to immediately prevent the skin from sunburn. The erythema dose is a clinical evaluation index. The higher the protection ability, the larger the SPF value. Currently, the highest SPF value marked in China is up to SPF50+. The sun protection factor PA value represents the protection against UVA, which refers to the ability to immediately prevent the skin from tanning. The melanization value is a clinical evaluation index. The highest PA value marked is up to PA++++. The sun protection ability of sun protection cosmetics mainly depends on the addition and use of sunscreens. According to different sun protection mechanisms, sunscreens are divided into organic sunscreens and inorganic sunscreens. Organic sunscreens achieve the protection effect by absorbing ultraviolet rays, and inorganic sunscreens achieve the protection effect by reflecting and scattering light. Both have their own advantages and disadvantages. Sunscreen products belong to characteristic products in China, and at the same time, the use of sunscreens is also limited. The higher the sun protection index requirement, the more the addition amount of sunscreens often needs to be increased, which not only increases the problems of product safety and skin feel, but also leads to an increase in cost. The key to solving these problems lies in the compound combination and optimization of sunscreens. Through special processes, different sunscreens are compounded to optimize their ratios and structures, and at the same time, active substances with sun protection enhancement and anti-inflammatory and soothing effects are added. On the one hand, it enables them to exert the best UVB / UVA protection effect, and on the other hand, it effectively reduces the possible irritation and inflammation during product use. By killing two birds with one stone, it can not only effectively reduce the use amount of sunscreens, but also optimize the skin feel and cost of the product to achieve the best cost performance.

[0004] Nanostructured Lipid Carriers (NLC) is a new generation of lipid nanodrug delivery system developed in recent years based on Solid lipid nanoparticles (SLN). It is a lipid nanoparticle prepared using a mixture of liquid lipids (such as medium-chain triglycerides, IPM, IPP, liquid paraffin, etc.) and solid lipids as the matrix material. Compared with the overly perfect solid lipid crystal structure of SLN, NLC mixes solid lipids with liquid lipids with significantly different physical properties to prepare a drug-loaded carrier, which can obtain a higher encapsulation rate and at the same time can adjust the drug release behavior of SLN and improve stability. Applying the nanostructured lipid carrier technology to sun protection cosmetics, different functional chemical sunscreens are encapsulated through the carrier technology. On the one hand, it solves problems such as the difficulty in applying some chemical sunscreens and easy crystallization and precipitation, and on the other hand, through scientific combination, each component can synergistically enhance the effect and optimize the cost and process.

[0005] DHHB: Diethylamino hydroxyphenyl benzoyl hexyl ester is an efficient UVA organic sunscreen agent. It is soluble in oil and alcohol, has high light stability and safety, as well as excellent solubility and formulation compatibility. However, DHHB has strong coloring ability and a relatively sticky skin feel. When added in high content, there is a risk of staining and coloring. How to alleviate the yellowing and coloring of the emulsion and the greasiness during application, in addition to optimizing the emulsification system, is to optimize the sunscreen system, effectively reduce the usage amount of the sunscreen agent, and make the use of the sunscreen agent achieve the best cost performance.

[0006] IMC: Isoamyl p-methoxycinnamate is a natural substance in the roots of kaempferia galanga. It is also the only naturally occurring and widely used UVB absorber, with an absorption peak at 307 nm. It is a polar oil-based UVB sunscreen agent, having high medium-wave ultraviolet absorption performance and special extinction performance. It is suitable as the main additive for sunscreens with spectral long-wave and medium-wave ultraviolet protection functions, and can also be used as an excellent solvent for solid organic sunscreen agents. The synthesized IMC belongs to natural equivalents and is commonly used in sunscreen products in European Union countries. In addition, isoamyl p-methoxycinnamate also has certain antioxidant and anti-inflammatory effects and can be used in skin care products to delay skin aging and improve skin quality. Although isoamyl p-methoxycinnamate is widely used in cosmetics and personal care products, its safety issues have also attracted much attention. Some studies have shown that isoamyl p-methoxycinnamate has good skin compatibility and strong skin permeability, and may cause skin irritation and allergic reactions. Therefore, safety is a key consideration in the application process of IMC.

[0007] DHBT: Diethylhexyl butamido triazone (abbreviation: HEB), with an off-white to light brown powder appearance, is an efficient new type of ultraviolet UVB sunscreen agent, having a relatively high absorption rate. Only a small concentration can achieve a relatively high SPF value; and it has extremely strong light stability. It is an alcohol-soluble and oil-soluble ultraviolet absorber, with an absorption wavelength range of 280 - 320 nm and a maximum absorption wavelength value of 311 nm. It has a synergistic effect when used together with other UVA ultraviolet absorbers and achieves broad-spectrum protection across the entire ultraviolet band. However, DHBT has a relatively large molecular weight, which will bring a sticky and heavy skin feel to the product. How to improve its skin feel is an issue that needs to be considered during application.

[0008] When DHHB, IMC and DHBT are used in combination, they can provide more comprehensive UV protection, covering the two main UV bands of UVA and UVB. However, most traditional sunscreen compositions only consider the synergistic effect between sunscreens, while ignoring the safety risks of the sunscreens themselves. First of all, all chemical sunscreens are risky substances and have certain safety risks to the human body and the environment, so the laws and regulations of various countries require limited addition of chemical sunscreens; secondly, chemical sunscreens have certain penetration risks, especially for sensitive skin, which may cause irritation and allergies; finally, ultraviolet radiation will directly cause skin redness, sunburn, and inflammation, and the light instability problem of some chemical sunscreens themselves will aggravate the skin's inflammatory response. Summary of the invention

[0009] The purpose of the present invention is to overcome the shortcomings and deficiencies of the prior art and to provide a hyperspectral (full-band ultraviolet absorption) multi-effect composite sunscreen carrier containing DHHB, IMC and DHBT, and its preparation and application.

[0010] In view of the physicochemical properties of the core sunscreens DHHB, IMC and DHBT, the present invention adopts nanostructured lipid carriers (NLC) to co-load chemical sunscreens and anti-inflammatory and soothing plant active ingredients, thereby improving the solubility of DHHB and DHBT. At the same time, by optimizing the sunscreen ratio and the combination of plant active ingredients, a synergistic effect is produced, which effectively reduces the irritation that may occur during the use of the sunscreen, alleviates the damage of ultraviolet rays to the skin, and further improves the overall sunscreen performance of the sunscreen carrier. In addition, the sunscreen carrier particle size is controlled between 100-1000nm (preferably 300-800nm), and the particle size distribution PDI (polydispersity index) is less than 0.300, ensuring that the particle size distribution is uniform, while reducing skin penetration, the sunscreen can also be attached to the skin more evenly, forming a dense protective film on the skin surface, effectively reducing skin transepidermal water loss, and while enhancing product safety, the sunscreen also allows the sunscreen to play the best effect.

[0011] The purpose of the present invention is achieved through the following technical solutions:

[0012] In the first aspect, the present invention provides an ultra-broad spectrum (full-band UV absorption) multi-effect composite sunscreen carrier, which is a nanostructured lipid carrier that co-loads sunscreens and sunscreen synergistic active ingredients, and the raw materials include sunscreens, sunscreen synergistic active ingredients, and nanocarrier raw materials. Among them, the sunscreens are DHHB (diethylaminohydroxybenzoyl hexyl benzoate), IMC (isoamyl p-methoxycinnamate), and DHBT (diethylhexyl butyramido triazone); the sunscreen synergistic active ingredients are pomegranate seed oil and thick-leaved Bergenia extract; the nanocarrier raw materials include emulsifiers, co-emulsifiers, oils, polyols, and water.

[0013] In some preferred embodiments, the ultra-broad-spectrum multi-effect composite sunscreen carrier comprises the following components by mass: 5-20 parts of DHHB (diethylamino hydroxybenzoyl hexyl benzoate), 5-20 parts of IMC (isopentyl p-methoxycinnamate), 5-20 parts of DHBT (diethylhexyl butamido triazone), 0.1-10 parts of pomegranate seed oil, 0.1-5 parts of Bergenia crassifolia extract, 5-40 parts of emulsifier, 0.1-10 parts of co-emulsifier, 0.1-20 parts of oil, 5-40 parts of polyol, and 10-40 parts of water.

[0014] The Bergenia crassifolia extract is preferably the root extract of Bergenia crassifolia.

[0015] The emulsifier preferably includes one or a combination of more than one of fatty alcohol polyoxyethylene ethers, polyethylene glycol fatty acid esters, polyol polyoxyethylene ethers, glycerol esters, polyglycerol fatty acid esters, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, glucosides, sucrose esters, silicone oils, phosphate esters, fatty acid salts, amino acids, phospholipids, etc.

[0016] The co-emulsifier preferably includes one or a combination of more than one of fatty alcohols, fatty acids, jojoba esters, rice bran wax, carnauba wax, beeswax, paraffin wax, etc.

[0017] The oil preferably includes one or a combination of more than one of triglyceride caprylate / caprate, isononyl isononanoate, dicaprylyl carbonate, cetyl ethylhexanoate, C12-15 alcohol benzoate, isopropyl myristate, neopentyl glycol diheptanoate, butyl octyl salicylate, dibutyl adipate, diethylhexyl malate, diethylhexyl maleate, diisopropyl adipate, diisopropyl sebacate, hexyl laurate, PPG-2 isodeceth-7 carboxylic acid isopropyl ester, phenethyl benzoate, butanediol dicaprylate / dicaprate, C12-15-alkanol polyether-9 carboxylic acid isopropyl ester, tridecyl salicylate, etc.

[0018] The polyol preferably includes one or a combination of more than one of glycerol, propylene glycol, 1,3-butanediol, 1,3-propanediol, 1,2-pentanediol, ethoxydiglycol, 1,2-hexanediol, dipropylene glycol, isopropyl alcohol, polyethylene glycol, PPG-10 sorbitol, octyldodecanol, hexyl decanol, 2,3-propanediol, decyl tetradecanol, hexanediol, methyl propylene glycol, octyldecanol, isopentylene glycol, octyldecanol, etc.

[0019] In some preferred embodiments, the particle size of the ultra-broad-spectrum multi-effect composite sunscreen carrier is 100-1000 nm. For the numerical ranges in the present invention, it includes each intermediate value between the upper and lower limits of the range, and also includes each smaller range within the range. For example, the particle size of the ultra-broad-spectrum multi-effect composite sunscreen carrier can be 100, 101, 102... 998, 999 or 1000 nm, or it can be the range between any two of these values. Further preferably, the particle size of the ultra-broad-spectrum multi-effect composite sunscreen carrier is 300-800 nm. Within this range, the sunscreen carrier of the present invention can better balance safety, stability, moisturizing effect and sunscreen effect.

[0020] In a second aspect, the present invention also provides a method for preparing the above-mentioned ultra-broad-spectrum multi-effect composite nano sunscreen carrier, which includes the following steps:

[0021] (1) Mix DHHB, IMC, DHBT, emulsifier, co-emulsifier, pomegranate seed oil, oil, and polyol to obtain mixture 1.

[0022] (2) Mix the extract of Bergenia crassifolia, polyol, and water to obtain mixture 2.

[0023] (3) Pour mixture 1 into mixture 2 and mix evenly to obtain mixture 3.

[0024] (4) Nanometerize mixture 3 to obtain the above-mentioned ultra-broad-spectrum multi-effect composite nano sunscreen carrier.

[0025] In the above steps (1), (2), and (3), the mixing is preferably carried out under heating and stirring conditions. The conditions are not limited, and it is only necessary to achieve uniform mixing and dissolution under the condition of not affecting the activity of the components. Further preferably, the mixing is carried out with stirring at 70-80 °C.

[0026] In step (4), the method of nanometerization includes methods such as high-pressure homogenization, high-speed microfluidics, or high-speed shearing. The high-pressure homogenization method is preferably used, and the homogenization pressure is preferably 100-1500 bar, and further preferably 500-1200 bar.

[0027] In a third aspect, the present invention also provides the application of the above-mentioned ultra-broad-spectrum multi-effect composite sunscreen carrier in the preparation of sunscreen cosmetics.

[0028] In a fourth aspect, the present invention also provides a sunscreen cosmetic, which contains the above-mentioned ultra-broad-spectrum multi-effect composite sunscreen carrier.

[0029] The dosage form of the sunscreen cosmetic is not limited, and it includes sunscreen lotion, sunscreen cream, sunscreen spray, etc.

[0030] The present invention has the following advantages and beneficial effects:

[0031] In the present invention, considering the sunscreen mechanism comprehensively, DHHB, IMC and DHBT are selected for compounding to achieve a broad-spectrum sunscreen effect. At the same time, the sunscreen synergistic active ingredients pomegranate seed oil and Bergenia crassifolia root extract are added, which synergistically enhance the effect with DHHB, IMC and DHBT. Pomegranate seed oil is the only plant-derived polyunsaturated conjugated linoleic acid, and its main component is punicic acid, with a content of up to 70-80%. Secondly, there are also active substances such as linolenic acid, linoleic acid, oleic acid, palmitic acid, stearic acid, as well as fat accompanying substances and bioflavonoids. Because the structure of punicic acid is closest to conjugated linoleic acid (CLA), it is called "super conjugated linoleic acid", and it is also called omega-5, which is a highly unsaturated fatty acid of the ω-3 type. Punicic acid has extremely strong antioxidant ability, can effectively resist human inflammation and the destructive effect of oxygen free radicals. At the same time, the bioflavonoids in pomegranate seed oil can directly help the skin resist the damage of ultraviolet rays. It is very suitable for use in sunscreen products. While strengthening the sunscreen function, it will not bring burden to the skin, and it is an excellent sunscreen synergist. Bergenia crassifolia root extract is rich in unique active substances such as condensed tannins, arbutin, and bergenin. Tannin has anti-inflammatory and astringent effects, and arbutin has anti-inflammatory and antioxidant effects, which can enhance the protection against ultraviolet rays, improve the antioxidant ability of the body, reduce inflammatory reactions, promote the differentiation of keratinocytes, and improve the skin's damage repair ability; while bergenin can inhibit the expression of tyrosinase and tyrosinase-related protein 2, reduce the catalytic oxidation of tyrosine based on tyrosinase (TYR), effectively reduce the skin damage caused by UVB, inhibit the production of melanin, and has significant whitening and anti-photoaging effects, preventing post-sun inflammatory reactions and pigmentation. When the two are used in combination with chemical sunscreens, they synergistically enhance the effect. On the one hand, it prevents excessive oxygen free radicals generated by chemical sunscreens due to ultraviolet irradiation, has anti-inflammatory and soothing effects, and can also slow down the skin irritation and inflammation that may occur during the penetration of the sunscreen, reducing the risks that may be brought during the penetration of the sunscreen; on the other hand, it increases the sun protection index and helps prevent skin sunburn and tanning.

[0032] In the present invention, according to the physical and chemical properties of DHHB, IMC and DHBT, a combination of active ingredients is co-loaded with pomegranate seed oil and Bergenia crassifolia root extract. By optimizing the emulsifier combination and the formulation process, while solving the solubility problems of DHHB and DHBT, the ratio of sunscreens is optimized, so that each component synergistically enhances the effect, reduces the possible irritation during the use of sunscreens, alleviates the damage of ultraviolet rays to the skin, optimizes the skin feel and improves the overall sunscreen performance of the sunscreen carrier.

[0033] Through the formulation process, the particle size of the sunscreen carrier of the present invention can be controlled between 100 - 1000 nm (preferably 300 - 800 nm), and the particle size distribution PDI (polydispersity index) is less than 0.300, ensuring a uniform and controllable particle size distribution. The nanostructured lipid carrier (NLC) with such particle size and particle size distribution can reduce skin penetration while enabling the sunscreen agent to adhere to the skin more evenly, forming a dense protective film on the skin surface, enhancing the safety of the product, and enabling the sunscreen agent to exert its best efficacy.

[0034] The superspectral multi-effect composite sunscreen carrier prepared by the present invention has good water dispersibility. When applied in the finished product formulation, it can be directly added to the water phase (W / O) or added at the end of the formulation (O / W), and then stirred evenly. There is no dosage form limitation, and it can be used in sunscreen lotions, creams, and sprays. It is very convenient to use, and compared with free components, it has a better sunscreen effect. Brief Description of the Drawings

[0035] Figure 1 It is the TEM electron micrograph of the sunscreen carrier of Example 1.

[0036] Figure 2 It is the bar graph of the skin retention amount of the sunscreen carrier of Example 1 and the free sunscreen agent.

[0037] Figure 3 It is the bar graph of the skin retention amount of the sunscreen carrier of Example 6 and the free sunscreen agent.

[0038] Figure 4 It is the diffusion of the RhoB sunscreen nanocarrier in the skin observed by a laser confocal microscope. Note: Compared with free RhoB, ** P < 0.01.

[0039] Figure 5 It is the calculated value of the sun protection index by the BASF sunscreen calculator. Detailed Description of the Invention

[0040] The present invention will be further described in detail below through specific examples. It should be understood that these examples are only a part of the examples of the present invention, rather than all of the examples, and the protection scope of the present invention is not limited to the following examples.

[0041] The materials, reagents, etc. used in the following examples can all be obtained commercially. For example, the extract of Bergenia crassifolia roots can be purchased from Kunming Qiancao Biotechnology Co., Ltd.

[0042] Example 1

[0043] A superspectrum multi-effect composite sunscreen carrier is prepared as follows:

[0044] (1) Mix 10 parts of DHHB, 10 parts of DHBT, 10 parts of IMC, 8 parts of Tween - 80, 5 parts of polyglyceryl - 10 laurate, 7 parts of PEG - 40 hydrogenated castor oil, 4 parts of polyglyceryl - 3 methylglucose distearate, 1 part of cetyl alcohol, 5 parts of ethoxydiglycol, 5 parts of butyl octyl salicylate, and 4 parts of pomegranate seed oil at 70 - 80 °C to form a homogeneous and clear liquid 1. All parts mentioned in the present invention are parts by mass.

[0045] (2) Mix 2 parts of Bergenia crassifolia root extract, 12 parts of propylene glycol, and 17 parts of water at 70 - 80 °C to form a homogeneous and clear liquid 2.

[0046] (3) Pour liquid 1 into liquid 2 and mix, then stir at 70 - 80 °C to form a homogeneous liquid 3.

[0047] (4) After homogenizing liquid 3 at 500 bar in a high - pressure homogenizer, a super - broad - spectrum multi - effect composite sunscreen carrier is obtained, with an average particle size of 702.2 nm and a PDI of 0.214. The TEM electron micrograph is shown in Figure 1 .

[0048] Example 2

[0049] A super - broad - spectrum multi - effect composite sunscreen carrier is prepared as follows:

[0050] (1) Mix 5 parts of DHHB, 5 parts of DHBT, 10 parts of IMC, 6 parts of polyglyceryl - 3 methylglucose distearate, 6 parts of polyglyceryl - 6 distearate, 5 parts of PEG - 40 hydrogenated castor oil, 5 parts of methyl glucose sesquistearate, 5 parts of Tween - 80, 1 part of cetyl alcohol, 5 parts of octyldodecanol, 5 parts of phenethyl benzoate, 5 parts of butyl octyl salicylate, and 0.5 parts of pomegranate seed oil at 70 - 80 °C to form a homogeneous and clear liquid 1.

[0051] (2) Mix 0.2 parts of Bergenia crassifolia root extract, 15 parts of propylene glycol, and 20 parts of water at 70 - 80 °C to form a homogeneous and clear liquid 2.

[0052] (3) Pour liquid 1 into liquid 2 and mix, then stir at 70 - 80 °C to form a homogeneous liquid 3.

[0053] (4) After homogenizing liquid 3 at 700 bar in a high - pressure homogenizer, a super - broad - spectrum multi - effect composite sunscreen carrier is obtained, with an average particle size of 655.7 nm and a PDI of 0.226.

[0054] Example 3

[0055] A super - broad - spectrum multi - effect composite sunscreen carrier is prepared as follows:

[0056] (1) Mix 8 parts of DHHB, 8 parts of DHBT, 15 parts of IMC, 10 parts of Tween - 80, 8 parts of cetearyl olivate, 10 parts of PEG - 40 hydrogenated castor oil, 2 parts of methyl gluceth sesquistearate, 1 part of cetyl alcohol, 5 parts of ethoxydiglycol, 3 parts of butyl octyl salicylate, and 0.5 part of pomegranate seed oil at 70 - 80 °C to form a homogeneous and clear liquid 1.

[0057] (2) Mix 0.1 part of Bergenia crassifolia root extract, 10 parts of propylene glycol, and 25 parts of water at 70 - 80 °C to form a homogeneous and clear liquid 2.

[0058] (3) Pour liquid 1 into liquid 2 and mix, then stir at 70 - 80 °C to form a homogeneous liquid 3.

[0059] (4) Homogenize liquid 3 at 900 bar in a high - pressure homogenizer to obtain an ultra - broad - spectrum multi - effect composite sunscreen carrier with an average particle size of 579.8 nm and a PDI of 0.204.

[0060] Example 4

[0061] An ultra - broad - spectrum multi - effect composite sunscreen carrier is prepared as follows:

[0062] (1) Mix 10 parts of DHHB, 10 parts of DHBT, 10 parts of IMC, 10 parts of Tween - 80, 5 parts of polyglyceryl - 10 laurate, 5 parts of PEG - 40 hydrogenated castor oil, 4 parts of sorbitan olivate, 4 parts of olive oil PEG - 7 esters, 1 part of cetyl alcohol, 5 parts of ethoxydiglycol, 5 parts of butyl octyl salicylate, and 4 parts of pomegranate seed oil at 70 - 80 °C to form a homogeneous and clear liquid 1.

[0063] (2) Mix 2 parts of Bergenia crassifolia root extract, 15 parts of butanediol, and 10 parts of water at 70 - 80 °C to form a homogeneous and clear liquid 2.

[0064] (3) Pour liquid 1 into liquid 2 and mix, then stir at 70 - 80 °C to form a homogeneous liquid 3.

[0065] (4) Homogenize liquid 3 at 300 bar in a high - pressure homogenizer to obtain an ultra - broad - spectrum multi - effect composite sunscreen carrier with an average particle size of 931.3 nm and a PDI of 0.277.

[0066] Example 5

[0067] An ultra - broad - spectrum multi - effect composite sunscreen carrier is prepared as follows:

[0068] (1) Mix 10 parts of DHHB, 10 parts of DHBT, 10 parts of IMC, 8 parts of Tween - 80, 2 parts of glyceryl stearate, 7 parts of PEG - 40 hydrogenated castor oil, 3 parts of polyglyceryl - 10 laurate, 4 parts of polyglyceryl - 3 methylglucose distearate, 2 parts of PEG - 100 stearate, 1 part of cetyl alcohol, 2 parts of hexyldecanol, 3 parts of phenethyl benzoate, 5 parts of butyl octyl salicylate, and 0.5 part of pomegranate seed oil at 70 - 80 °C to form a homogeneous and clear liquid 1.

[0069] (2) Mix 0.5 part of Bergenia crassifolia root extract, 10 parts of glycerol, and 23 parts of water at 70 - 80 °C to form a homogeneous and clear liquid 2.

[0070] (3) Pour liquid 1 into liquid 2 and mix, then stir at 70 - 80 °C to form a homogeneous liquid 3.

[0071] (4) Homogenize liquid 3 at 1100 bar in a high - pressure homogenizer to obtain an ultra - broad - spectrum multi - effect composite sunscreen carrier with an average particle size of 489.5 nm and a PDI of 0.226.

[0072] Example 6

[0073] An ultra - broad - spectrum multi - effect composite sunscreen carrier is prepared as follows:

[0074] (1) Mix 5 parts of DHHB, 5 parts of DHBT, 10 parts of IMC, 10 parts of Tween - 80, 5 parts of polyglyceryl - 10 laurate, 10 parts of PEG - 15 glyceryl isostearate, 5 parts of polyglyceryl - 2 diisostearate, 1 part of behenyl alcohol, 4 parts of phenethyl benzoate, 5 parts of butyl octyl salicylate, 5 parts of hexyldecanol, and 1 part of pomegranate seed oil at 70 - 80 °C to form a homogeneous and clear liquid 1.

[0075] (2) Mix 0.2 part of Bergenia crassifolia root extract, 22 parts of butanediol, and 12 parts of water at 70 - 80 °C to form a homogeneous and clear liquid 2.

[0076] (3) Pour liquid 1 into liquid 2 and mix, then stir at 70 - 80 °C to form a homogeneous liquid 3.

[0077] (4) Homogenize liquid 3 at 1300 bar in a high - pressure homogenizer to obtain an ultra - broad - spectrum multi - effect composite sunscreen carrier with an average particle size of 187.4 nm and a PDI of 0.219.

[0078] For Comparative Examples 1 - 13, taking Example 1 as a control, adjust the sunscreen agents and sunscreen synergistic components, and use the same method to prepare sunscreen carriers containing different active ingredients.

[0079] Comparative Example 1

[0080] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHHB and 10 parts of IMC, and the other components and preparation method are the same as those in Example 1.

[0081] Comparative Example 2

[0082] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHBT, and the other components and preparation method are the same as those in Example 1.

[0083] Comparative Example 3

[0084] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHHB, 10 parts of IMC, and 10 parts of DHBT, and the other components and preparation method are the same as those in Example 1.

[0085] Comparative Example 4

[0086] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHHB, 10 parts of IMC, and 4 parts of sunscreen-enhancing ingredient pomegranate seed oil, and the other components and preparation method are the same as those in Example 1.

[0087] Comparative Example 5

[0088] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHBT and 4 parts of sunscreen-enhancing ingredient pomegranate seed oil, and the other components and preparation method are the same as those in Example 1.

[0089] Comparative Example 6

[0090] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHHB, 10 parts of IMC, and 2 parts of sunscreen-enhancing ingredient Bergenia crassifolia root extract, and the other components and preparation method are the same as those in Example 1.

[0091] Comparative Example 7

[0092] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHBT and 2 parts of sunscreen-enhancing ingredient Bergenia crassifolia root extract, and the other components and preparation method are the same as those in Example 1.

[0093] Comparative Example 8

[0094] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHHB, 10 parts of IMC, 4 parts of sunscreen-enhancing ingredient pomegranate seed oil, and 2 parts of Bergenia crassifolia root extract, and the other components and preparation method are the same as those in Example 1.

[0095] Comparative Example 9

[0096] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHBT, 4 parts of sunscreen synergistic ingredient pomegranate seed oil, and 2 parts of Bergenia crassifolia root extract, and other components and the preparation method are the same as those in Example 1.

[0097] Comparative Example 10

[0098] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHHB, 10 parts of IMC, and 10 parts of DHBT, and 4 parts of sunscreen synergistic ingredient pomegranate seed oil, and other components and the preparation method are the same as those in Example 1.

[0099] Comparative Example 11

[0100] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 10 parts of sunscreen agent DHHB, 10 parts of IMC, and 10 parts of DHBT, and 2 parts of sunscreen synergistic ingredient Bergenia crassifolia root extract, and other components and the preparation method are the same as those in Example 1.

[0101] Comparative Example 12

[0102] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 4 parts of sunscreen synergistic ingredient pomegranate seed oil, and other components and the preparation method are the same as those in Example 1.

[0103] Comparative Example 13

[0104] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: It only contains 2 parts of sunscreen synergistic ingredient Bergenia crassifolia root extract, and other components and the preparation method are the same as those in Example 1.

[0105] Comparative Example 14

[0106] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: A certain amount of DHHB, DHBT, IMC, pomegranate seed oil, and Bergenia crassifolia root extract are added to ethoxydiglycol and mixed evenly to obtain a sunscreen free composition with the same contents of sunscreen agent and sunscreen synergistic ingredient as the sunscreen carrier in Example 1.

[0107] The average particle size of the sunscreen carriers obtained in the above Examples 1-6 and Comparative Examples 1-13 is within 100 nm - 1000 nm, and the PDI is 0.1 - 0.3. Each obtained sunscreen carrier is placed in a sealed container at -20°C, room temperature, 4°C, and 45°C for 3 months respectively, and no layering or precipitation phenomenon occurs, and the particle size also does not change significantly, indicating that the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention has good stability.

[0108] Test Example 1 Evaluation of Chicken Embryo Chorioallantoic Membrane Irritation

[0109] The sunscreen carriers of Examples 1-6 and the free composition of Comparative Example 14 were each diluted 5-fold with water, mixed evenly, and then 0.2 mL of the sample was respectively taken and dropped on the surface of the chorioallantoic membrane. The changes in CAM blood vessels were observed within 5 min, and the initial times when congestion, bleeding, and blood coagulation occurred in the CAM blood vessels were recorded, and the irritation score IS was calculated. The irritation score (IS) was calculated according to the following formula:

[0110] IS = [(301 - secH)×5 + (301 - secL)×7 + (301 - secC)×9] / 300

[0111] In the above formula, secH represents the initial time of congestion (s); secL represents the initial time of bleeding (s); secC represents the initial time of blood coagulation (s).

[0112] The results of Examples 1-6 were similar. When the sunscreen carrier after being diluted 5-fold contacted the chorioallantoic membrane of the chicken embryo for 300 s, there was no bleeding, no blood vessel lysis, and no blood coagulation in the capillaries, and the reaction score was 0.07, indicating that the sunscreen carrier of the present invention has good safety and no irritation. After the free composition (Comparative Example 14) after being diluted 5-fold contacted the chorioallantoic membrane of the chicken embryo for 300 s, there was bleeding in the capillaries, and the reaction score was 4.72, showing irritation. This shows that the sunscreen carrier of the present invention can reduce the irritation of the sunscreen itself.

[0113] Test Example 2 Patch test

[0114] The sunscreen carriers of Examples 1-6 were respectively added to a blank cream matrix (the main components are water, polyol, carbomer, and caprylic / capric triglyceride) to prepare samples with a sunscreen carrier content of 30 wt% as the experimental groups. 30 subjects were selected, and each experimental group and the blank control were applied to the flexor side of the forearm of the subjects for 24 h. After removing the patch tester, after an interval of 30 min, the skin reaction was observed after the indentation disappeared. The skin reaction was observed again 24 h and 48 h after removing the patch tester.

[0115] The results showed that none of the 30 subjects showed faint erythema, erythema, edematous erythema, significant swelling, infiltration or papules, and papules or blisters, indicating that the sunscreen carrier of the present invention has no irritation to human skin.

[0116] Test Example 3 In vitro skin penetration experiment

[0117] The transdermal experiment of ex vivo porcine skin was carried out by the vertical Franz diffusion cell method. DHHB, IMC, and DHBT were dissolved in ethoxydiglycol to prepare free component 1 and free component 6 with the same sunscreen content as in the sunscreen carrier of Example 1 or Example 6. The sunscreen carrier and the free component were respectively added to the blank cream (the main components are water, polyol, carbomer, and triglyceride of caprylic acid / capric acid) and stirred evenly to prepare test samples containing 40 wt% of the sunscreen carrier or the free component. The skin was fixed between the receiving chamber and the supply chamber, 1.0 g each in the supply chamber, and PBS (pH 7.4) was used as the receiving solution, and diffusion was carried out with stirring at 32 °C. At 4, 8, 12, and 24 h, 0.5 mL of the receiving solution was taken, and an equal amount of fresh receiving solution at a constant temperature was immediately replenished. After 24 h, the skin was removed, washed, cut into pieces, ground into a homogenate with an appropriate amount of solvent, centrifuged, and the supernatant was analyzed by HPLC to calculate the skin retention amount per unit area of DHHB (diethylamino hydroxyphenyl benzoyl benzoic acid hexyl ester), IMC (isopentyl p-methoxycinnamate), and DHBT (diethylhexyl butamido triazone).

[0118] The results are shown in Figure 2 and Figure 3 , the skin retention amounts per unit area of DHHB in free component 1 and sunscreen carrier 1 (Example 1) at 24 h were 6.27 μg / cm 2 and 1.02 μg / cm 2 . Compared with free component 1, the skin retention amount per unit area of DHHB in sunscreen carrier 1 (Example 1) decreased by 83.73%. The skin retention amounts per unit area of IMC in free component 1 and sunscreen carrier 1 (Example 1) at 24 h were 12.48 μg / cm 2 and 2.15 μg / cm 2 . Compared with free component 1, the skin retention amount per unit area of IMC in sunscreen carrier 1 (Example 1) decreased by 82.88%. The skin retention amounts per unit area of DHBT in free component 1 and sunscreen carrier 1 (Example 1) at 24 h were 5.86 μg / cm 2 and 0.79 μg / cm 2 . Compared with free component 1, the skin retention amount per unit area of DHBT in sunscreen carrier 1 (Example 1) decreased by 86.52%. The skin retention amounts per unit area of DHHB in free component 6 and sunscreen carrier 6 (Example 6) at 24 h were 3.58 μg / cm 2 and 2.54 μg / cm 2 . Compared with free component 6, the skin retention amount per unit area of DHHB in sunscreen carrier 6 (Example 6) only decreased by 27.93%. The skin retention amounts per unit area of IMC in free component 6 and sunscreen carrier 6 (Example 6) at 24 h were 12.27 μg / cm 2 and 8.74 μg / cm2 。Compared with the free component 6, the skin retention amount per unit area of IMC in the sunscreen carrier 6 (Example 6) only decreased by 28.77%. The skin retention amounts per unit area of DHBT at 24 h for the free component 6 and the sunscreen carrier 6 (Example 6) were 2.57 μg / cm 2 and 1.69 μg / cm 2 respectively. Compared with the free component 6, the skin retention amount per unit area of DHBT in the sunscreen carrier 6 (Example 6) only decreased by 34.24%. It shows that the sunscreen carrier 1 (with an average particle size of 702.2 nm) prepared by encapsulating the sunscreen agent can significantly reduce the retention of the sunscreen agent in the skin, while the difference in the retention of the sunscreen carrier 6 (with an average particle size of 187.4 nm) in the skin compared with the free component is not obvious. It indicates that the larger the particle size of the sunscreen carrier, the safer it is as a sunscreen agent, and the particle size of the sunscreen carrier is preferably greater than 300 nm.

[0119] Test Example 4 Observation of Skin Penetration by Laser Confocal Microscopy

[0120] Preparation of RhoB nanocarrier and free RhoB: Rhodamine B (RhoB) was added to the aqueous phase as a fluorescent label, and the rhodamine B sunscreen nanocarrier (RhoB nanocarrier) was prepared according to the method in Example 1, and an isoconcentration free rhodamine B solution (i.e., adding rhodamine B to the composition of Comparative Example 14) was prepared as a control sample (free RhoB). 20 g of free RhoB and 20 g of RhoB sunscreen nanocarrier were respectively added to 80 g of blank essence matrix (the main components are water, polyol, carbomer), and stirred evenly to obtain the corresponding free RhoB compounded essence and RhoB sunscreen nanocarrier compounded essence.

[0121] The skin penetration experiment of ex vivo porcine skin was carried out by the vertical Franz diffusion cell method. The skin was fixed between the receiving chamber and the supply chamber. 0.5 g of free RhoB labeled with RhoB and 0.5 g of RhoB sunscreen carrier compounded essence labeled with RhoB were taken in the supply chamber, and PBS was used as the receiving solution, and stirred and diffused at 37°C. Two parallels were set up in each group. After 4 h and 8 h, the residual samples on the skin were gently wiped off, the skin in the target area was removed, the skin was rinsed again, and the residual moisture was dried after thorough cleaning. The samples were cryosectioned, observed by laser confocal microscopy, and representative areas were selected for photographing.

[0122] The results are shown in Figure 4, the RhoB sunscreen carrier concentrated in the stratum corneum within 4 h and failed to penetrate the stratum corneum barrier, while free RhoB had penetrated the stratum corneum barrier and entered the deep skin tissues within 4 h. With the extension of time, at 8 h, the fluorescence penetration depth of free RhoB in the skin further increased, reaching a skin depth of 327 μm, while the RhoB sunscreen carrier still mostly concentrated in the stratum corneum at 8 h and failed to penetrate the stratum corneum barrier. The experimental results showed that within the same time, the fluorescence intensity and the penetration depth into the skin of free RhoB were significantly higher than those of the RhoB sunscreen carrier, revealing that the sunscreen carrier prepared by encapsulating the sunscreen agent could significantly reduce the retention of the sunscreen agent in the skin and was safer to be used as a sunscreen agent.

[0123] Test Example 5 Skin Moisture Content Test (Skin Film-Forming Effect)

[0124] Five volunteers aged 20 - 50 years were selected according to the principle of voluntariness. On the inner sides of the left and right arms of the subjects, a blank cream group, a free composition group (20 wt% of Comparative Example 14 + blank cream matrix), and a sunscreen carrier (Example 1) group (20 wt% of Example 1 + blank cream matrix) were set respectively according to the random principle. The main components of the above blank cream matrix were water, polyol, carbomer, and triglyceride caprylate / caprate. Another control site without applying any sample was set. Tests were carried out before use (0 h), 0.5 h after use, 1 h after use, 2 h after use, 4 h after use, and 8 h after use respectively. Before the test, the subjects washed the test sites with clean water, dried them, and then exposed the test sites. They needed to sit still for 20 min in an environment with constant temperature and humidity ((22 ± 2) °C, relative humidity 50% ± 10%).

[0125] Trans-epidermal water loss test: The level of the trans-epidermal water loss (TEWL) value is an important indicator for evaluating the strength of the skin barrier function, which can reflect the water retention ability of the stratum corneum of the skin and is one of the important indicators for evaluating the efficacy of moisturizing cosmetics. The Tewameter TM300 trans-epidermal water loss tester was used to measure the trans-epidermal water loss (TEWL) values of the inner sides of the subjects' arms before using the samples and at different times after use. The test results are shown in Table 1 below.

[0126] Table 1: Trans-epidermal water loss (TEWL) values of the skin at different times before and after using the samples

[0127]

[0128]

[0129] As can be seen from the results in the above table, for the same volunteer control group (without applying any products), the transdermal water loss value remained at a relatively high level over time and the fluctuation over time was not particularly obvious. This indicates that normal skin has a certain self-regulating ability without intervention, so the transdermal water loss value does not fluctuate greatly over time but remains relatively stable at a relatively high level. The blank group, free group, and carrier group can all reduce the transdermal water loss value of the skin, indicating a positive effect on both the skin and moisturization (the NLC carrier technology can form a dense protective film on the skin surface for related components such as sunscreen agents). The difference in the transdermal water loss values between the blank group and the free group is not significant, but both are significantly higher than the carrier group. This shows that the film-forming effect (moisturizing effect) of the free group and the blank group on the skin is not obvious, while the sunscreen carrier has a better moisturizing effect compared to the free components (i.e., reduced transdermal water loss of the skin). This indicates that when the NLC technology is applied to the sunscreen carrier, by controlling the particle size and structure of the carrier, the carrier components can be better spread on the skin surface during application to form a dense protective film, thereby reducing the water loss from the skin epidermis.

[0130] Test Example 6 Inflammatory Factor Inhibition Test

[0131] The Kunming mice were randomly divided into 6 groups (10 mice in each group): control group (blank matrix, referring to a blank cream without anti-inflammatory active ingredients), ultraviolet light (UV) group (blank matrix), free group 1 (20 wt% of Comparative Example 14 + blank matrix), sunscreen carrier group (20 wt% of Example 1 + blank matrix), comparative carrier group 1 (20 wt% of Comparative Example 3 + blank matrix), comparative carrier group 2 (20 wt% of Comparative Example 10 + blank matrix), and comparative carrier group 3 (20 wt% of Comparative Example 11 + blank matrix). The main components of the above blank matrix were water, polyol, carbomer, and triglyceride of caprylic / capric acid. The mice were depilated to expose 1.0 cm × 1.0 cm hairless skin. The mice in the control group had their bare skin not irradiated with ultraviolet light and were only coated with the blank matrix. The mice in the UV group and the sample groups were placed in special rectangular experimental boxes of 3.0 cm × 6.0 cm respectively. Their bare skin was coated with 0.1 mL of the corresponding sample, and the coating thickness was 0.1 cm, and they were pretreated for 15 min; then they were successively irradiated with long-wave ultraviolet light (UVA, 1.55 J / cm 2 , 18 min) and medium-wave ultraviolet light (UVB, 0.95 J / cm 2 , 11 min) to make a skin model with ultraviolet irradiation damage. Once a day for 7 consecutive days, after the irradiation, the skin tissues of the mice were taken and processed, and then the contents of biochemical indexes IL-1β, IL-6, and TNF-α were detected according to the instructions of the corresponding ELISA kit. The measurement results are shown in Table 2 below.

[0132] Table 2: Detection values of IL-1β, IL-6 and TNF-α contents in different test groups

[0133] Grouping IL-1β (pg / mL) IL-6 (pg / mL) TNF-α (pg / mL) Control group 59.78±4.47 78.25±3.38 69.54±4.73 UV group <![CDATA[185.59±8.23 ## > <![CDATA[221.32±6.74 ## > <![CDATA[201.32±8.37 ## > Free group <![CDATA[99.34±2.74 **bb > <![CDATA[105.87±3.36 **bb > <![CDATA[102.34±2.59 **bb > Sun protection carrier group <![CDATA[68.45±2.57 **aa > <![CDATA[89.76±2.39 **aa > <![CDATA[81.38±2.71 **aa > Comparison carrier group 1 <![CDATA[114.34±2.74 **bb > <![CDATA[122.87±3.36 **bb > <![CDATA[118.34±2.59 **bb > Comparison carrier group 2 <![CDATA[98.83±3.66 **bb > <![CDATA[110.38±2.39 **bb > <![CDATA[103.43±2.58 **bb > Comparison carrier group 3 <![CDATA[105.67±2.69 **bb > <![CDATA[101.33±2.41 **bb > <![CDATA[111.72±2.14 **bb >

[0134] Note: Compared with the control group, ##p < 0.01; compared with the UV group, **p < 0.01; compared with the free group, aap < 0.01, compared with the sunscreen carrier group, bbp < 0.01.

[0135] The experimental results in Table 2 showed that compared with the blank control group, the secretion levels of IL-1β, IL-6 and TNF-α in the UV group increased significantly after ultraviolet irradiation (p < 0.01); compared with the UV group, the free group, the sunscreen carrier group, comparison carrier group 1, comparison carrier group 2 and comparison carrier group 3 could all significantly reduce the secretion levels of IL-1β, IL-6 and TNF-α induced by UV irradiation (p < 0.01). Compared with the free group, the sunscreen carrier group had a more significant effect on reducing IL-1β, IL-6 and TNF-α after UV irradiation (p < 0.01), indicating that the nano-carrier could inhibit the inflammation induced by UV irradiation more effectively than the free component and was more conducive to the efficacy of the sunscreen active composition. Comparison carrier group 1, comparison carrier group 2 and comparison carrier group 3 all had a certain inhibitory effect on the increase of IL-1β, IL-6 and TNF-α after UV irradiation, and the inhibitory effects of comparison carrier group 2 and comparison carrier group 3 were better than that of comparison carrier group 1, but the difference was not significant; compared with the sunscreen carrier group and the comparison carrier groups (comparison carrier group 1, comparison carrier group 2, comparison carrier group 3), the inhibitory effect of the sunscreen carrier group on IL-1β, IL-6 and TNF-α after UV irradiation was very obvious and was significantly better than that of the comparison carrier groups, indicating that Adansonia digitata oil and Bergenia crassifolia root extract both had certain anti-inflammatory effects when applied to the sunscreen carrier, could help inhibit the production of erythema after UV irradiation, and the combination of the two had a significant synergistic effect, which was very beneficial for improving the sun protection index.

[0136] Test Example 7 Sun Protection Index Test

[0137] The test instrument used was UV2000S. Test method: The test sample was applied on the rough PMMA plate by weight (the rough side was on the top), and the application amount was 1.3 mg / cm 2(Actual application amount). When applying, it is evenly applied in the form of small droplets with approximately equal volumes. The sheet is weighed immediately before and after application and the evaporation of the product is controlled. The applied sheet is equilibrated in the dark at ambient temperature for at least 15 minutes to help form a standard and stable product film. A reference sample with 100% transmittance is prepared by applying a few microliters of glycerol or other suitable UV-transparent substance to the rough surface of the substrate, and the transmittance of the UV radiation through the reference plate is determined. Each sample to be tested is applied to at least three PMMA plates, and each plate should be measured at multiple different positions, and the single-point area should exceed 0.5 cm 2 , and ensure that the total measured area is at least 2 cm 2 . The incident irradiance is measured in the plane of the surface of the treated plate for UV irradiation, and the transmittance measurement after UV irradiation is carried out at the same plate position as exactly as possible as the previous measurement. The final SPF and UVA-PF values are equal to the average of the values derived from individual plates.

[0138] The sunscreen carriers of Example 1 and Comparative Examples 1-13 were diluted 4 times with a blank cream matrix (main components are water, polyol, carbomer, triglyceride caprylate / caprate) respectively, and then the SPF and UVA-PF values were measured. The measurement results are shown in Table 3 below.

[0139] Table 3: Measurement results of sunscreen indices after diluting the sunscreen carriers of Example 1 and Comparative Examples by 4 times

[0140] Measurement object SPF UVA-PF Example 1 18.38 12.12 Comparative example 1 5.64 6.31 Comparative example 2 7.18 1.26 Comparative example 3 14.27 8.85 Comparative example 4 6.93 7.02 Comparative example 5 8.37 1.91 Comparative example 6 6.86 6.95 Comparative example 7 8.28 2.11 Comparative example 8 7.43 7.72 Comparative example 9 9.57 2.82 Comparative example 10 15.67 10.07 Comparative example 11 15.15 9.79 Comparative example 12 0.46 0.39 Comparative example 13 0.32 0.27

[0141] From the machine test results of Comparative Examples 12 and 13, when pomegranate seed oil and Bergenia crassifolia root extract were added alone, both had certain sun protection index values, but the numbers were small. Excluding possible experimental errors, the sun protection efficacy of pomegranate seed oil and Bergenia crassifolia root extract used alone could not be determined. Comparing Comparative Example 1 with Comparative Examples 4, 6, and 8, and Comparative Example 2 with Comparative Examples 5, 7, and 9, the SPF values and UVA-PF values of the DHHB, IMC combination (Comparative Examples 1, 4, 6, 8) and DHBT (Comparative Examples 2, 5, 7, 9) used alone were not very ideal. When a single sunscreen was added with pomegranate seed oil or Bergenia crassifolia root extract alone, it had a certain promoting effect on the sun protection index, but the promoting effect was not obvious; when a single sunscreen was added with both pomegranate seed oil and Bergenia crassifolia root extract, the promoting effect on the sun protection index was greater than the sum of adding a single component alone, indicating that adding pomegranate seed oil and Bergenia crassifolia root extract simultaneously had a certain synergistic effect on a single sunscreen, but the effect was not significant. Comparing Example 1 with Comparative Examples 3, 10, and 11, there was an obvious synergistic effect after the compounding of DHHB, IMC, and DHBT. The SPF value of Example 1 increased by about 1.35 times compared with the sum of each single component (the sum of Comparative Examples 1, 2, 12, and 13), and the UVA-PF value increased by about 1.47 times; the SPF value of Comparative Example 3 increased by about 1.11 times compared with the sum of each single component (the sum of Comparative Examples 1 and 2), and the UVA-PF value increased by about 1.17 times; the SPF value of Comparative Example 10 increased by about 1.18 times compared with the sum of each single component (the sum of Comparative Examples 1, 2, and 12), and the UVA-PF value increased by about 1.27 times; the SPF value of Comparative Example 11 increased by about 1.15 times compared with the sum of each single component (the sum of Comparative Examples 1, 2, and 13), and the UVA-PF value increased by about 1.25 times; and Example 1 increased by about 1.28 times compared with Comparative Example 3, and the UVA-PF value increased by about 1.32 times; Comparative Example 10 increased by about 1.10 times in SPF value compared with Comparative Example 3, and the UVA-PF value increased by about 1.14 times; Comparative Example 11 increased by about 1.06 times in SPF value compared with Comparative Example 3, and the UVA-PF value increased by about 1.11 times. The above results indicate that adding pomegranate seed oil or Bergenia crassifolia root extract alone had a certain synergistic effect on the DHHB, IMC composition, and DHBT composite sunscreen system, but the effect was not obvious. Using pomegranate seed oil and Bergenia crassifolia root extract simultaneously had a more obvious promoting effect on the sun protection index of the DHHB, IMC, and DHBT composite sunscreen system, indicating that using pomegranate seed oil and Bergenia crassifolia root extract simultaneously had an obvious synergistic effect. The anti-inflammatory and soothing effects of pomegranate seed oil and Bergenia crassifolia root extract could not be demonstrated in this test, but these effects could play a better role in actual applications or human tests.

[0142] Test Example 8 Comparative Test of Sun Protection Index in the Practical Application of the Sun Protection Carriers of Example 1 and Example 4

[0143] Taking the sun protection carriers of Example 1 and Example 4 as references, their direct application to emulsifying creams of O / W and W / O dosage forms is taken as the application example; a free sun protection composition with the same content of sun protection agents and active substances as those in the sun protection carriers of Example 1 and Example 4 (for the preparation of the free sun protection composition, see Comparative Example 14) is added to the same-dosage-form formulations of the application example as the comparative application example.

[0144] Applied to the traditional O / W or W / O emulsifying system, Application Example 1A is 30 wt% of the sun protection carrier of Example 1 + 2 wt% of BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) + O / W or W / O blank cream matrix formulation, and Comparative Application Example 1A is 30 wt% of the free composition with the same content of sun protection agents and active substances as those in the sun protection carrier of Example 1 + 2 wt% of BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) + O / W or W / O blank cream matrix formulation. Application Example 4A is 30 wt% of the sun protection carrier of Example 4 + 2 wt% of BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) + O / W or W / O blank cream matrix formulation, and Comparative Application Example 4A is 30 wt% of the free composition with the same content of sun protection agents and active substances as those in the sun protection carrier of Example 4 + 2 wt% of BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) + O / W or W / O blank cream matrix formulation.

[0145] Applied to the traditional O / W or W / O emulsifying system, Application Example 1B is 30 wt% of the sun protection carrier of Example 1 + 2 wt% of BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) + 2 wt% of PBSA (phenylbenzimidazole sulfonic acid) + O / W or W / O blank cream matrix formulation, and Comparative Application Example 1B is 30 wt% of the free composition with the same content of sun protection agents and active substances as those in the sun protection carrier of Example 1 + 2 wt% of BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) + 2 wt% of PBSA (phenylbenzimidazole sulfonic acid) + O / W or W / O blank cream matrix formulation. Application Example 4B is 30 wt% of the sun protection carrier of Example 4 + 2 wt% of BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) + 2 wt% of PBSA (phenylbenzimidazole sulfonic acid) + O / W or W / O blank cream matrix formulation, and Comparative Application Example 4B is 30 wt% of the free composition with the same content of sun protection agents and active substances as those in the sun protection carrier of Example 4 + 2 wt% of BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) + 2 wt% of PBSA (phenylbenzimidazole sulfonic acid) + O / W or W / O blank cream matrix formulation.

[0146] The main components of the above O / W blank cream matrix formula are water, polyols, acryloyldimethyltaurine ammonium / VP copolymer, behenyl alcohol, polydimethylsiloxane, acrylic acid (ester) / C10-30 alkyl acrylate cross-linked polymer, polymethyl methacrylate and tromethamine. The main components of the W / O blank cream matrix formula are water, polyols, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, lauryl PEG-8 polydimethylsiloxane, polydimethylsiloxane, polydimethylsiloxane / polydimethylsiloxane cross-linked polymer, polyglyceryl-3 polyricinoleate, polyglyceryl-3 ricinoleate, dimethyldistearylammonium lithium montmorillonite, polymethylsilsesquioxane, polymethyl methacrylate and sodium chloride.

[0147] Then, the sun protection factor was determined according to the method described in Test Example 7, and the test results are shown in Table 4 below.

[0148] Table 4: Measurement results of sun protection factor in the actual application of the sun protection carriers in Example 1 and Example 4

[0149]

[0150]

[0151] Figure 5 are the SPF value and UVA-PF value calculated by BASF computer simulation under the same sunscreen content. From Table 4 and Figure 5 the results, it can be seen that the machine-measured results of the SPF of the comparative application example are closer to the simulation calculation results of the BASF sunscreen calculator, while the machine-measured results of Application Example 1A and Application Example 1B are much higher than the simulation calculation results, indicating that the composite sunscreen nanocarrier (Application Example 1) has an obvious promoting effect on the improvement of the sun protection factor. The machine-measured results of Application Example 4A and Application Example 4B have no obvious difference from the comparative application example and the calculator simulation value, indicating that the composite sunscreen nanocarrier (Application Example 4) has no obvious promoting effect on the improvement of the sun protection factor. It shows that for the same type and content of sunscreen agents, the same plant sunscreen synergistic active components and carrier types, the promoting effect of the sunscreen composite nanocarrier on the sun protection factor is related to the carrier particle size. The larger the carrier particle size, the less obvious the promoting effect on the sun protection factor. This is because the larger the carrier particle size, on the one hand, the worse the carrier stability and the more uneven the particle size distribution, and long-term placement will cause the aggregation of sunscreen particles, thus affecting the sunscreen effect; on the other hand, the larger the carrier particle size, the more uneven the distribution of the carrier particles on the skin surface, which will also affect the uniform distribution of the sunscreen agent on the skin surface, thus affecting the sunscreen effect. Therefore, in the actual formula application, the particle size of the composite sunscreen carrier is preferably less than 800 nm. When actually applying the formula, a sunscreen nanocarrier with a suitable particle size (preferably 300-800 nm) can greatly improve the sun protection value and reduce the overall amount of sunscreen agents used in the formula, especially suitable for preparing high-fold sunscreen products.

[0152] After the application example and comparative application example samples were placed at 4 °C for 3 months, it was felt that sunscreen agent crystal particles precipitated when applying Comparative Application Examples 1A, 1B and Comparative Application Examples 4A, 4B, indicating that the solid sunscreen agent aggregated and precipitated at low temperature, while this was not the case when applying Application Examples 1A, 1B and Application Examples 4A, 4B, indicating that the application of the sunscreen carrier greatly improved the low-temperature stability problem of the solid sunscreen agent. On the other hand, the water dispersibility of the sunscreen carrier is also good and can be directly dispersed in the aqueous phase in actual formulation applications, simplifying the operation process. In summary, on the one hand, the sunscreen nano-carrier of the present invention can improve the sunscreen performance and reduce the cost, and on the other hand, it can improve the formulation stability and simplify the operation process, having great market prospects and application value.

[0153] The above embodiments are only used to help illustrate the present invention, but the implementation manners of the present invention are not limited by the above embodiments. Any modifications, equivalent replacements and improvements made by any person skilled in the technical field within the technical scope disclosed by the present invention are all included in the protection scope of the invention.

Claims

1. An ultra-broad-spectrum multi-effect composite sunscreen carrier, characterized in that: Contains sunscreens, sunscreen boosting active ingredients and nanocarrier raw materials; The sunscreen is diethylaminohydroxybenzoyl hexyl benzoate, isopentyl p-methoxycinnamate, and diethylhexyl butyramido triazone; The sunscreen synergistic active ingredients are pomegranate seed oil and thick-leaved Bergenia extract; The nano-carrier raw materials include emulsifier, co-emulsifier, oil, polyol and water.

2. The ultra-broad-spectrum multi-effect composite sunscreen carrier according to claim 1, characterized in that: The invention comprises the following ingredients in parts by mass: 5-20 parts of diethylaminohydroxybenzoyl hexyl benzoate, 5-20 parts of isopentyl p-methoxycinnamate, 5-20 parts of diethylhexyl butyramido triazone, 0.1-10 parts of pomegranate seed oil, 0.1-5 parts of thick-leaved Bergenia extract, 5-40 parts of emulsifier, 0.1-10 parts of co-emulsifier, 0.1-20 parts of oil, 5-40 parts of polyol and 10-40 parts of water.

3. The ultra-broad-spectrum multi-effect composite sunscreen carrier according to claim 1, characterized in that: The emulsifier includes one or more combinations of fatty alcohol polyoxyethylene ethers, polyethylene glycol fatty acid esters, polyol polyoxyethylene ethers, glycerides, polyglycerol fatty acid esters, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, glucosides, sucrose esters, silicone oils, phosphates, fatty acid salts, amino acids, and phospholipids.

4. The ultra-broad-spectrum multi-effect composite sunscreen carrier according to claim 1, characterized in that: The auxiliary emulsifier includes one or more combinations of fatty alcohols, fatty acids, jojoba esters, rice bran wax, carnauba wax, and beeswax.

5. The ultra-broad-spectrum multi-effect composite sunscreen carrier according to claim 1, characterized in that: The oil includes one or more combinations of caprylic / capric triglyceride, isononyl isononanoate, dicaprylyl carbonate, cetyl ethylhexanoate, C12-15 alcohol benzoate, isopropyl myristate, neopentyl glycol diheptanoate, butyl octyl salicylate, dibutyl adipate, diethylhexyl malate, diethylhexyl maleate, diisopropyl adipate, diisopropyl sebacate, hexyl laurate, PPG-2 isodecyl polyether-7 carboxylate, phenethyl alcohol benzoate, butylene glycol dicaprylate / dicaprate, C12-15-chain alcohol polyether-9 carboxylate isopropyl, and tridecyl alcohol salicylate.

6. The ultra-broad-spectrum multi-effect composite sunscreen carrier according to claim 1, characterized in that: The polyol preferably includes one or more combinations of glycerol, propylene glycol, 1,3-butylene glycol, 1,3-propanediol, 1,2-pentanediol, ethoxydiglycol, 1,2-hexanediol, dipropylene glycol, isopropyl alcohol, polyethylene glycol, PPG-10 sorbitol, octyldodecanol, hexyldecanol, 2,3-propanediol, decyltetradecyl alcohol, hexylene glycol, methylpropylene glycol, octyldecanol, isopentyl glycol, and caprylyl glycol.

7. The ultra-broad-spectrum multi-effect composite sunscreen carrier according to claim 1, characterized in that: The particle size is 300-800nm.

8. The method for preparing the ultra-broad-spectrum multi-effect composite sunscreen carrier according to any one of claims 1 to 7, characterized in that: The steps include: (1) mixing diethylaminohydroxybenzoyl hexyl benzoate, isopentyl p-methoxycinnamate, diethylhexyl butyramido triazone, an emulsifier, an auxiliary emulsifier, pomegranate seed oil, and a polyol to obtain a mixed solution 1; (2) mixing the Bergenia crassifolia extract, polyol and water to obtain a mixed solution 2; (3) Pour the mixed solution 1 into the mixed solution 2 and mix them evenly to obtain a mixed solution 3; (4) The mixed solution 3 is subjected to nano-processing to obtain the ultra-broad-spectrum multi-effect composite nano-sunscreen carrier.

9. Use of the ultra-broad-spectrum multi-effect composite sunscreen carrier according to any one of claims 1 to 7 in the preparation of sunscreen cosmetics.

10. A sunscreen cosmetic, characterized in that: It comprises the ultra-broad-spectrum multi-effect composite sunscreen carrier described in any one of claims 1 to 7.

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