Extended-spectrum multi-effect composite sunscreen carrier containing AVB, OCR and OMC 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 AVB, OCR and OMC 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 is prepared from AVB (butyl methoxy dibenzoylmethane), OCR (octocrylene), OMC (ethylhexyl methoxycinnamate), baobab seed oil, a radix bupleuri root extract and a nano-carrier raw material, wherein the nano-carrier raw material is prepared from an emulsifying agent, a co-emulsifying agent, 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 invention belongs to the field of cosmetics, relates to sunscreen cosmetics, and specifically relates to an ultra-broad-spectrum multi-effect composite sunscreen carrier containing AVB, OCR and OMC, and the preparation and application thereof. Background Art

[0002] The aging of human skin is mainly divided into natural aging and photoaging. Natural aging belongs to endogenous aging. With the increase of age, the subcutaneous tissue begins to shrink, collagen is lost, the skin becomes thinner, elasticity decreases, and wrinkles gradually appear. This process cannot be avoided. Photoaging belongs to exogenous aging, which refers to skin aging caused by sunlight (ultraviolet rays). Studies have shown that 75% of skin aging factors are caused by ultraviolet rays. Among them, long-wavelength UVA (320-400nm) has weaker energy, but can penetrate into the lower dermis and directly cause skin tanning. Medium-wavelength UVB (290-320nm) has higher energy and can penetrate into the basal layer of the epidermis or the upper part of the dermis to damage DNA, causing skin sunburn, which in turn causes the skin to be indirectly tanned. There is also a risk of skin cancer. At present, with the continuous development of environmental biology and medicine, people's cognitive level is constantly improving, and their understanding and demand for sun protection are also deepening and increasing, prompting more and more cosmetics companies to focus on the research and development of sun protection related products and raw materials, making the cosmetics sun protection market grow rapidly, especially for high sun protection index products, which are becoming more and more popular in the market. This is also the development trend of sun protection products in the future.

[0003] The SPF value is a measure of protection against UVB and refers to the ability to immediately prevent skin from getting sunburned. The amount of erythema is a clinical evaluation indicator. The stronger the protection, the greater the SPF value. Currently, the highest SPF value in China is marked as SPF50+. The PA value is a measure of protection against UVA and refers to the ability to immediately prevent skin from getting sunburned. The melanization value is a clinical evaluation indicator, and the highest PA value is marked as PA++++. The sunscreen ability of sunscreen cosmetics mainly depends on the addition and use of sunscreen agents. Sunscreen agents are divided into organic sunscreen agents and inorganic sunscreen agents according to different sunscreen mechanisms. Organic sunscreen agents achieve protection by absorbing ultraviolet rays, while inorganic sunscreen agents achieve protection by reflecting and scattering light. Both have their own advantages and disadvantages. Sunscreen products are characteristic products in China, and the use of sunscreens is also limited. The higher the SPF requirement, the more sunscreen is added. This not only increases product safety and skin feel issues, but also leads to increased costs. The key to solving these problems lies in the compounding, combination and optimization of sunscreens. Different sunscreens are compounded through special processes to optimize their ratios and structures. At the same time, they are combined with active ingredients that enhance sunscreen and provide anti-inflammatory and soothing effects. On the one hand, they can exert the best UVB / UVA protection effect, and on the other hand, they can effectively reduce irritation and inflammation that may occur during product use. This two-pronged approach can not only effectively reduce the amount of sunscreen used, but also optimize product skin feel and costs, achieving the best cost-effectiveness.

[0004] Nanostructured lipid carriers (NLC) are a new generation of lipid nano drug delivery systems developed in recent years based on solid lipid nanoparticles (SLN). They are lipid nanoparticles prepared using a mixture of liquid lipids (such as medium-chain glycerides, IPM, IPP, liquid paraffin, etc.) and solid lipids as matrix materials. Compared with the overly perfect solid lipid crystal structure of SLN, NLC mixes solid lipids with liquid lipids with greatly different physical properties to prepare drug-containing carriers, which can achieve a higher encapsulation rate and adjust the drug release behavior of SLN to improve stability. The nanostructured lipid carrier technology is applied to sunscreen cosmetics. Chemical sunscreens with different functions are encapsulated through carrier technology. On the one hand, it solves the problems of some chemical sunscreens being difficult to apply and easy to crystallize. On the other hand, through scientific combination, the various ingredients can synergize and optimize costs and processes.

[0005] AVB: Avobenzone (INCI: Butyl Methoxydibenzoylmethane) is the first commercial chemical sunscreen that targets UVA and the only globally approved UVA1 absorber. It has a wide-band high-protection UV protection capability and is one of the few organic sunscreens that can absorb UVA1. UVA1 is the largest span of UV rays and is the wavelength that most UV absorbers cannot protect against: 340-400nm. Protecting against UVA is of great significance and may be more important than sun protection: UVA reaching the earth's surface accounts for 95% of the total UV rays. UVA is not only the main cause of skin photoaging, but also participates in the carcinogenesis caused by sunlight. The special thing about AVB is that it can provide strong protection in the UVA1 range, and with other UVB absorbers, the entire formula can provide broad-spectrum UVA / UVB protection. But it has a huge flaw - it is very photo-unstable. Under ultraviolet irradiation, AVB will transform from the enol form with high light absorption to the keto isomer with shorter absorption wavelength and stronger photoreactivity. The keto isomer will then undergo photodegradation and decompose into other products, completely losing the sunscreen effect, resulting in reduced ultraviolet protection of AVB; in addition, sunscreens will also produce free radicals during the decomposition process, which are also highly irritating to the skin. Without stabilization, AVB can lose 36% of its absorption capacity after 1 hour of sunlight exposure, and only 42% will remain after 2 hours. Therefore, the previous sunscreens emphasized reapplying every two hours. One of the important reasons is that chemical sunscreens are unstable (another reason is that the waterproof and sweat-proof performance is poor and loss occurs). Another disadvantage of AVB is that it has poor compatibility and is difficult to get along with. It will undergo a cycloaddition reaction with ethylhexyl methoxycinnamate, and both will perish together, losing the ability to protect against ultraviolet rays. In addition to not being able to pair with ethylhexyl methoxycinnamate, it will produce colored compounds when it encounters metal ions, so you should also pay attention when applying it. In short, AVB is a highly efficient UVA absorber that is cheap, but unstable and not very compatible, which greatly limits its use in sunscreen products.

[0006] OCR: Octocrylene, also known as UV absorber 3039, is an oil-soluble UV absorber that can absorb 280-350nm ultraviolet light (UVB + short-wave UVA), with an absorption peak of 303nm. It has the advantages of high ultraviolet absorption rate, non-toxicity, non-teratogenicity, good light and thermal stability, etc. It is a Class I sunscreen approved by the US FDA and is widely used in the United States and Europe. Another purpose of Octocrylene is to help other chemical sunscreens maintain the stability of the ultraviolet absorption process. For example, when used with AVB, it can effectively improve the light instability of AVB and has a wide range of applications. However, studies have pointed out that the transdermal absorption rate of OCR far exceeds that of other sunscreen ingredients, and OCR will release oxygen free radicals when exposed to sunlight, which greatly increases the risk of skin irritation and allergies, limiting the use of OCR in sunscreen products. In addition, OCR itself is an oily liquid with high viscosity, which feels sticky and heavy on the skin. When used in high concentrations, it will affect the overall skin feel of the sunscreen product. Therefore, optimizing the skin feel of OCR and reducing transdermal absorption can effectively improve the usage rate of OCR.

[0007] OMC: Ethylhexyl methoxycinnamate is currently the most widely used UVB sunscreen in the world. It is an oily chemical sunscreen that can absorb UVB 290-320 bands, with a maximum absorption wavelength of 311nm, an absorbance of 0.76, and a molecular weight of 290.4. Due to its relatively small molecular weight, the risk of penetrating into the skin becomes greater, and there is a certain degree of irritation and sensitization. The European Consumer Safety Scientific Committee (SCCS) found in its evaluation that OMC has potential endocrine disrupting properties, including significant estrogenic activity and weak anti-androgenic activity. In addition, OMC has low sun resistance and light stability, mainly manifested in poor durability. It is reported that usually after 10MED of sunlight radiation, about 70% of the active ingredients are photodegraded, so a higher dose needs to be added to the formula to work effectively. With the increase in usage, the potential safety risks of sunscreens are also greater, especially the risk of excessive irritation reactions in sunlight after use by consumers with sensitive skin; at the same time, high content addition increases product costs on the one hand, and also worsens the product experience on the other.

[0008] The existing technology combines AVB and OCR to 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. It is not recommended to use AVB and OMC together in traditional sunscreen products, because AVB and OMC will undergo a cycloaddition reaction together, and they will perish together and lose the ability to protect against ultraviolet rays. 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 AVB, OCR and OMC, and its preparation and application.

[0010] In view of the physicochemical properties of the core sunscreens AVB, OMC and OCR, the present invention uses nanostructured lipid carriers (NLC) to co-load chemical sunscreens and anti-inflammatory and soothing plant active ingredients, which solves the light stability and solubility of AVB, and also solves the problem that AVB and OMC will lose their protective ability when used together, greatly improving the sunscreen effect while effectively reducing costs and optimizing the product skin feel. At the same time, by optimizing the sunscreen ratio and the combination of plant active ingredients, a synergistic effect is generated, effectively reducing the irritation that may occur during the use of sunscreens, alleviating the damage of ultraviolet rays to the skin, and further improving the overall sunscreen performance of the sunscreen carrier. In addition, the particle size of the sunscreen carrier is controlled between 100-1000nm (preferably 300-800nm), and the particle size distribution PDI (polydispersity index) is less than 0.300, ensuring uniform particle size distribution. This can reduce skin penetration while allowing the sunscreen to adhere more evenly to the skin, forming a dense protective film on the skin surface, effectively reducing transepidermal water loss, and enhancing product safety while also allowing the sunscreen to exert its best efficacy.

[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 a sunscreen agent and a sunscreen synergistic active ingredient, and the raw materials include a sunscreen agent, a sunscreen synergistic active ingredient, and a nanocarrier raw material. Among them, the sunscreen agent is AVB (butyl methoxydibenzoylmethane), OCR (octocrylene), OMC (ethylhexyl methoxycinnamate); the sunscreen synergistic active ingredient is baobab seed oil and bupleurum extract; the nanocarrier raw material includes an emulsifier, an emulsifier, oil, polyol, and water.

[0013] In some preferred embodiments, the ultra-broad-spectrum multi-effect composite sunscreen carrier comprises the following ingredients in parts by mass: 5-20 parts of AVB (butyl methoxydibenzoylmethane), 5-20 parts of OCR (octocrylene), 5-30 parts of OMC (ethylhexyl methoxycinnamate), 0.5-10 parts of baobab seed oil, 0.1-5 parts of Altai Bupleurum 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 bupleurum extract is preferably an Altai bupleurum extract, and more preferably an Altai bupleurum root extract.

[0015] The emulsifier preferably 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, phospholipids, etc.

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

[0017] The oil preferably 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, tridecyl alcohol salicylate, etc.

[0018] 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, caprylyl glycol, etc.

[0019] In some preferred embodiments, the particle size of the ultra-broad-spectrum multi-effect composite sunscreen carrier is 100-1000nm. For the numerical range in the present invention, it includes each intermediate value between the upper limit and the lower limit of the range, and also includes each smaller range within the range. The particle size of the ultra-broad-spectrum multi-effect composite sunscreen carrier can be 100, 101, 102...998, 999 or 1000nm, or it can be a range between any two of these values. Further preferably, the particle size of the ultra-broad-spectrum multi-effect composite sunscreen carrier is 300-800nm. When the particle size is 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 ultra-broad-spectrum multi-effect composite nano sunscreen carrier, which comprises the following steps:

[0021] (1) OMC, baobab seed oil, emulsifier and co-emulsifier are mixed to obtain a mixed solution 1.

[0022] (2) Mix AVB, OCR and oil to obtain mixed solution 2.

[0023] (3) Mix the Bupleurum chinense extract, polyol and water to obtain a mixed solution 3.

[0024] (4) Pour the mixed solution 1 and the mixed solution 2 into the mixed solution 3 respectively and mix them evenly to obtain a mixed solution 4.

[0025] (5) The mixed solution 4 is subjected to nano-processing to obtain the ultra-broad-spectrum multi-effect composite nano-sunscreen carrier.

[0026] In the above steps (1), (2), (3) and (4), the mixing is preferably carried out under heating and stirring conditions, and the conditions are not limited. Uniform mixing and dissolution can be achieved under conditions that do not affect the activity of the components. It is further preferred that the mixing is carried out under heating and stirring conditions at 70-80°C.

[0027] In step (5), the nano-treatment method includes high-pressure homogenization, high-speed microfluidization or high-speed shearing, etc., preferably, the high-pressure homogenization method is used, and the homogenization pressure is preferably 100-1500 bar, and more preferably 500-1200 bar.

[0028] In a third aspect, the present invention also provides the use of the ultra-broad-spectrum multi-effect composite sunscreen carrier in the preparation of sunscreen cosmetics.

[0029] In a fourth aspect, the present invention further provides a sunscreen cosmetic comprising the above-mentioned ultra-broad-spectrum multi-effect composite sunscreen carrier.

[0030] The dosage form of the sunscreen cosmetics is not limited, and includes sunscreen lotion, sunscreen cream, sunscreen spray, etc.

[0031] The present invention has the following advantages and beneficial effects:

[0032] The present invention comprehensively considers the sunscreen mechanism and selects AVB, OCR and OMC for compound combination, which, on the one hand, helps AVB to dissolve better, and on the other hand, by improving the process, AVB and OMC are separately packaged and processed, thereby solving the problem that traditional OMC and AVB are prone to failure when used at the same time, better promoting the light stability of AVB and OMC, and achieving a broad-spectrum sunscreen effect.

[0033] The present invention simultaneously adds plant sunscreen synergistic active ingredients baobab seed oil and Altai bupleurum root extract, the baobab seed oil is obtained by cold-pressing extraction from the seeds of the baobab tree, is rich in unsaturated fatty acids, such as oleic acid, linoleic acid, fat accompanying substances, etc., and also contains a large amount of nutrients such as vitamins A, C, D, E, F and sterols, vitamin A and vitamin F (gamma-linolenic acid) have the effect of stimulating cell tissue renewal and regeneration, can prevent scars, vitamin C and vitamin E are super antioxidants, can help the skin clear free radicals, and delay aging. At the same time, plant sterols and some fat accompanying substances also have certain anti-inflammatory effects, so the use of baobab seed oil in sunscreen products can help resist cell damage caused by oxidative stress (ultraviolet rays) and improve the SPF value. The main component of the Altai Bupleurum root extract is bupleurum saponin, followed by phytosterols, adonisol, flavonoids, lignans, coumarins, and a small amount of volatile oils, polysaccharides, saponins and other ingredients. Therefore, the Altai Bupleurum root extract has significant antioxidant, anti-inflammatory and antiviral effects. Its main active ingredient, saikosaponin, can enhance the immune mechanism of human cells, improve skin metabolism, increase capillary permeability, and promote keratinocyte proliferation and regeneration. Active ingredients such as phytosterols, adonisol, and flavonoids can enhance the efficacy of saikosaponin, giving it synergistic effects such as healing wounds, smoothing rough skin, and preventing skin aging. At the same time, saikosaponin can absorb ultraviolet rays and inhibit the formation of melanin. The two are used in combination with chemical sunscreens to synergistically enhance their effectiveness. On the one hand, they prevent chemical sunscreens from producing excessive oxygen free radicals due to ultraviolet radiation, and have anti-inflammatory and soothing effects. At the same time, they can also slow down skin irritation and inflammation that may occur during the penetration of sunscreens, and reduce the risks that may be caused by the penetration of sunscreens. On the other hand, they can further increase the sun protection index and help prevent skin sunburn and tanning.

[0034] According to the physicochemical properties of AVB, OCR and OMC, the present invention uses baobab seed oil and Altai bupleurum root extract to co-load the active ingredient combination, and optimizes the emulsifier combination and the formulation process to solve the problems of AVB photostability and solubility, and also solves the problem that AVB and OMC lose their protective ability when used simultaneously, so that the components can synergize and enhance the sunscreen effect, effectively reduce the cost, optimize the skin feel of the product, reduce the irritation that may occur during the use of the sunscreen, alleviate the damage of ultraviolet rays to the skin, optimize the skin feel and improve the overall sunscreen performance of the sunscreen carrier.

[0035] The present invention can control the particle size of the sunscreen carrier to be between 100-1000nm (preferably 300-800nm) through the formulation process, and the particle size distribution PDI (polydispersity index) is less than 0.300, ensuring that the particle size distribution is uniform and controllable. The nanostructured lipid carrier (NLC) of the particle size and particle size distribution can reduce skin penetration while also allowing the sunscreen to be more evenly attached to the skin, forming a dense protective film on the skin surface, enhancing the safety of the product, and allowing the sunscreen to exert its best efficacy.

[0036] The ultra-spectrum multi-effect composite sunscreen carrier prepared by the present invention has good water dispersibility. When the finished product formula is used, it can be directly added to the water phase (W / O) or added at the end of the formula (O / W) and stirred evenly. There is no dosage form restriction and it can be used in sunscreen lotions, creams and sprays. It is very convenient to use and has better sunscreen effect than free ingredients. BRIEF DESCRIPTION OF THE DRAWINGS

[0037] Figure 1 This is a TEM electron microscope image of the sunscreen carrier of Example 1.

[0038] Figure 2 4 is a bar graph showing the skin retention of the sunscreen carrier and free sunscreen of Example 1.

[0039] Figure 3 4 is a bar graph showing the skin retention of the sunscreen carrier and free sunscreen of Example 5.

[0040] Figure 4 Laser confocal microscopy was used to observe the diffusion of RhoB sunscreen nanocarriers in the skin. Compared with free RhoB, ** P<0.01.

[0041] Figure 5 It is the calculated value of the sun protection factor by the BASF sun protection calculator. DETAILED DESCRIPTION

[0042] The present invention is further described in detail below through specific examples. It should be understood that these examples are only part of the embodiments of the present invention, rather than all of the embodiments, and the protection scope of the present invention is not limited to the following examples.

[0043] The materials, reagents, etc. used in the following examples can all be obtained from commercial sources, such as the Bupleurum chinense root extract can be purchased from Croda, UK.

[0044] Example 1

[0045] An ultra-broad-spectrum multi-effect composite sunscreen carrier, which is prepared as follows:

[0046] (1) 20 parts of OMC, 3 parts of polyglyceryl-3 methylglucose distearate, 5 parts of Tween-80, 22 parts of steareth-2, 3 parts of PEG-40 hydrogenated castor oil, 3 parts of polyglyceryl-6 distearate, 1 part of cetyl alcohol, and 4 parts of baobab seed oil were stirred at 70-80° C. to form a uniform and clear liquid 1. The parts mentioned in the present invention are all parts by mass.

[0047] (2) 10 parts of AVB, 11 parts of OCR, 5 parts of C12-15 alcohol benzoate, and 5 parts of butyl octyl salicylate were stirred at 70-80° C. to form a uniform clear liquid 2.

[0048] (3) 2 parts of Bupleurum chinense root extract, 10 parts of glycerol and 16 parts of water were stirred at 70-80° C. to form a uniform clear liquid 3.

[0049] (4) Liquid 1 and Liquid 2 are poured into Liquid 3 respectively, mixed, and stirred at 70-80° C. to form a uniform Liquid 4.

[0050] (5) Liquid 4 was homogenized by a high-pressure homogenizer at 1100 bar to obtain an ultra-broad-spectrum multi-effect composite sunscreen carrier with an average particle size of 408.4 nm and a PDI of 0.204. The TEM electron microscope image is shown in FIG. Figure 1 .

[0051] Example 2

[0052] An ultra-broad-spectrum multi-effect composite sunscreen carrier, which is prepared as follows:

[0053] (1) 10 parts of OMC, 5 parts of polyglyceryl-3 methylglucose distearate, 10 parts of Tween-80, 3 parts of cetearyl glucoside, 3 parts of PEG-40 hydrogenated castor oil, 2 parts of sorbitan olivate, 3 parts of cetearyl alcohol and 1 part of baobab seed oil were stirred at 70-80° C. to form a uniform clear liquid 1.

[0054] (2) 5 parts of AVB, 5.5 parts of OCR and 10 parts of butyl octyl salicylate were stirred at 70-80°C to form a homogeneous clear liquid 2.

[0055] (3) 1 part of Bupleurum chinense root extract, 10 parts of glycerol and 32 parts of water were stirred at 70-80° C. to form a uniform clear liquid 3.

[0056] (4) Liquid 1 and Liquid 2 are poured into Liquid 3 respectively, mixed, and stirred at 70-80° C. to form a uniform Liquid 4.

[0057] (5) Liquid 4 was homogenized by a high-pressure homogenizer at 800 bar to obtain an ultra-broad-spectrum multi-effect composite sunscreen carrier with an average particle size of 588.3 nm and a PDI of 0.226.

[0058] Example 3

[0059] An ultra-broad-spectrum multi-effect composite sunscreen carrier, which is prepared as follows:

[0060] (1) 10 parts of OMC, 4 parts of polysorbate 60, 10 parts of Tween 80, 2 parts of polyglyceryl-10 laurate, 5 parts of PEG-150 distearate, 4 parts of ceteareth-20, 3 parts of sorbitan olivate, 1 part of cetyl alcohol, and 0.5 parts of baobab seed oil were stirred at 70-80° C. to form a uniform clear liquid 1.

[0061] (2) 8 parts of AVB, 8.8 parts of OCR, and 10 parts of C12-15 alcohol benzoate were stirred at 70-80°C to form a uniform and clear liquid 2.

[0062] (3) 0.5 parts of Bupleurum chinense root extract, 10 parts of glycerol and 23 parts of water were stirred at 70-80° C. to form a uniform clear liquid 3.

[0063] (4) Liquid 1 and Liquid 2 are poured into Liquid 3 respectively, mixed, and stirred at 70-80° C. to form a uniform Liquid 4.

[0064] (5) Liquid 4 was homogenized by a high-pressure homogenizer at 600 bar to obtain an ultra-broad-spectrum multi-effect composite sunscreen carrier with an average particle size of 648.8 nm and a PDI of 0.249.

[0065] Example 4

[0066] An ultra-broad-spectrum multi-effect composite sunscreen carrier, which is prepared as follows:

[0067] (1) 20 parts of OMC, 3 parts of cetearyl olivate, 10 parts of Tween-80, 0.5 parts of hydrogenated lecithin, 4 parts of sucrose stearate, 4 parts of sorbitan olivate, 1 part of behenyl alcohol and 4 parts of baobab seed oil were stirred at 70-80° C. to form a uniform clear liquid 1.

[0068] (2) 10 parts of AVB, 11 parts of OCR and 8 parts of butyl octyl salicylate were stirred at 70-80° C. to form a homogeneous clear liquid 2.

[0069] (3) 2 parts of Bupleurum chinense root extract, 10 parts of butylene glycol and 10 parts of water were stirred at 70-80° C. to form a uniform clear liquid 3.

[0070] (4) Liquid 1 and Liquid 2 are poured into Liquid 3 respectively, mixed, and stirred at 70-80° C. to form a uniform Liquid 4.

[0071] (5) Liquid 4 was homogenized by a high-pressure homogenizer at 400 bar to obtain an ultra-broad-spectrum multi-effect composite sunscreen carrier with an average particle size of 973.2 nm and a PDI of 0.241.

[0072] Example 5

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

[0074] (1) 10 parts of OMC, 4 parts of PEG-4 olive oil ester, 4 parts of olive oil PEG-7 ester, 2 parts of PEG-150 distearate, 8 parts of PEG-40 hydrogenated castor oil, 2 parts of polyglyceryl-6 distearate, 1 part of cetyl alcohol, and 1 part of baobab seed oil were stirred at 70-80° C. to form a uniform clear liquid 1.

[0075] (2) 5 parts of AVB, 5.5 parts of OCR and 10 parts of butyl octyl salicylate were stirred at 70-80°C to form a homogeneous clear liquid 2.

[0076] (3) 0.5 parts of Bupleurum chinense root extract, 21 parts of glycerol and 27 parts of water were stirred at 70-80° C. to form a uniform clear liquid 3.

[0077] (4) Liquid 1 and Liquid 2 are poured into Liquid 3 respectively, mixed, and stirred at 70-80° C. to form a uniform Liquid 4.

[0078] (5) Liquid 4 was homogenized by a high-pressure homogenizer at 1300 bar to obtain an ultra-broad-spectrum multi-effect composite sunscreen carrier with an average particle size of 192.5 nm and a PDI of 0.241.

[0079] Example 6

[0080] An ultra-broad-spectrum multi-effect composite sunscreen carrier, which is prepared as follows:

[0081] (1) 20 parts of OMC, 3 parts of cetearyl olivate, 12 parts of Tween-80, 2 parts of PEG-150 distearate, 2 parts of olive oil PEG-7 esters, 3 parts of sorbitan olivate, and 0.5 parts of baobab seed oil were stirred at 70-80° C. to form a uniform clear liquid 1.

[0082] (2) 10 parts of AVB, 11 parts of OCR, and 10 parts of C12-15 alcohol benzoate were stirred at 70-80°C to form a uniform clear liquid 2.

[0083] (3) 0.5 parts of Bupleurum chinense root extract, 10 parts of glycerol and 16 parts of water were stirred at 70-80° C. to form a uniform clear liquid 3.

[0084] (4) Liquid 1 and Liquid 2 are poured into Liquid 3 respectively, mixed, and stirred at 70-80° C. to form a uniform Liquid 4.

[0085] (5) Liquid 4 was homogenized by a high-pressure homogenizer at 1000 bar to obtain an ultra-broad-spectrum multi-effect composite sunscreen carrier with an average particle size of 332.4 nm and a PDI of 0.194.

[0086] Comparative Examples 1-13 use Example 1 as a control, adjust the sunscreen agent and sunscreen synergistic ingredients therein, and use the same method to prepare sunscreen carriers containing different active ingredients.

[0087] Comparative Example 1

[0088] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 10 parts of sunscreen AVB and 11 parts of OCR, and the other ingredients and preparation method are the same as those in Example 1.

[0089] Comparative Example 2

[0090] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: only containing 20 parts of OMC as a sunscreen agent, and other ingredients and preparation method are the same as Example 1.

[0091] Comparative Example 3

[0092] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only sunscreen agents including 10 parts of AVB, 11 parts of OCR, and 20 parts of OMC, and other ingredients and preparation method are the same as those in Example 1.

[0093] Comparative Example 4

[0094] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 10 parts of sunscreen AVB, 11 parts of OCR, and 4 parts of baobab seed oil, a sunscreen synergistic ingredient, and other ingredients are the same as those in Example 1 of the preparation method.

[0095] Comparative Example 5

[0096] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 20 parts of sunscreen OMC and 4 parts of sunscreen synergistic ingredient baobab seed oil, and other ingredients are the same as those in Example 1 of the preparation method.

[0097] Comparative Example 6

[0098] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 10 parts of sunscreen AVB, 11 parts of OCR, 2 parts of the sunscreen synergistic ingredient, Bupleurum chinense root extract, and other ingredients are the same as those in Example 1 of the preparation method.

[0099] Comparative Example 7

[0100] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 20 parts of sunscreen OMC and 2 parts of the sunscreen synergistic ingredient, Bupleurum chinense root extract, and other ingredients are the same as those in Example 1 of the preparation method.

[0101] Comparative Example 8

[0102] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 10 parts of sunscreen AVB, 11 parts of OCR, 4 parts of sunscreen synergistic ingredient baobab seed oil, and 2 parts of Altai Bupleurum root extract, and other ingredients are the same as the preparation method embodiment 1.

[0103] Comparative Example 9

[0104] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 20 parts of sunscreen OMC, 4 parts of sunscreen synergistic ingredient baobab seed oil, and 2 parts of Altai Bupleurum root extract, and other ingredients are the same as those in Example 1 of the preparation method.

[0105] Comparative Example 10

[0106] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 10 parts of sunscreen AVB, 11 parts of OCR, 20 parts of OMC, and 4 parts of baobab seed oil, a sunscreen synergistic ingredient, and other ingredients are the same as those in Example 1 of the preparation method.

[0107] Comparative Example 11

[0108] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains only 10 parts of sunscreen AVB, 11 parts of OCR, 20 parts of OMC, 2 parts of sunscreen synergistic ingredient Altai Bupleurum root extract, and other ingredients are the same as those in Example 1 of the preparation method.

[0109] Comparative Example 12

[0110] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains 4 parts of baobab seed oil, a sunscreen synergistic ingredient, and other ingredients are the same as those in Example 1 of the preparation method.

[0111] Comparative Example 13

[0112] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention contains 2 parts of the sunscreen synergistic ingredient, Bupleurum chinense root extract, and other ingredients are the same as those in Example 1 of the preparation method.

[0113] Comparative Example 14

[0114] A comparative example of the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention: a certain amount of OMC, AVB 10, OCR, baobab seed oil, and Altai Bupleurum root extract are added to butyl octyl salicylate and mixed to obtain a sunscreen free composition having the same content of sunscreen agent and sunscreen synergistic ingredient as the sunscreen carrier of Example 1.

[0115] The average particle size of the sunscreen carriers obtained in the above Examples 1-6 and Comparative Examples 1-13 is within 100nm-1000nm, and the PDI is 0.1-0.3. The sunscreen carriers obtained were placed in a sealed container at -20°C, room temperature, 4°C, and 45°C for 3 months, respectively, and no stratification or precipitation occurred, and the particle size did not change significantly, indicating that the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention has good stability.

[0116] Test Example 1 Evaluation of the irritation of chicken embryo chorioallantoic membrane

[0117] The sunscreen carriers of Examples 1-6 and the free composition of Comparative Example 14 were diluted 5 times with water, mixed evenly, and then 0.2 mL of each sample was taken and dripped onto the surface of the chorioallantoic membrane. The changes in the CAM blood vessels were observed within 5 minutes, and the initial time of congestion, bleeding and coagulation of the CAM blood vessels was recorded, and the irritation score IS was calculated. The irritation score (IS) was calculated according to the following formula:

[0118] IS=[(301-secH)×5+(301-secL)×7+(301-secC)×9] / 300

[0119] In the above formula, secH represents the initial time of congestion (s); secL represents the initial time of bleeding (s); and secC represents the initial time of coagulation (s).

[0120] The results of Examples 1-6 are similar. When the sunscreen carrier diluted 5 times is in contact with the chicken embryo chorioallantoic membrane for 300 seconds, there is no bleeding in the capillaries, no vascular melting, and no coagulation phenomenon, and the reaction integral is 0.07, indicating that the sunscreen carrier of the present invention is safe and non-irritating. However, after the free composition (Comparative Example 14) diluted 5 times is in contact with the chicken embryo chorioallantoic membrane for 300 seconds, there is bleeding in the capillaries, and the reaction integral is 4.53, which is irritating. This shows that the sunscreen carrier of the present invention can reduce the irritation of the sunscreen itself.

[0121] Test Example 2 Patch Test

[0122] The sunscreen carriers of Examples 1-6 were added to a blank cream base (mainly composed of water, polyols, carbomer, caprylic / capric triglyceride) to prepare samples with a sunscreen carrier content of 30 wt% as experimental groups, and 30 subjects were selected. Each experimental group and the blank control (blank cream base) were applied to the curved side of the forearm of the subjects for 24 hours, and the spot tester was removed for 30 minutes. The skin reaction was observed after the indentation disappeared. The skin reaction was observed again 24 hours and 48 hours after the spot tester was removed.

[0123] The results showed that none of the 30 subjects developed light red spots, erythema, edematous erythema, significant redness and swelling, infiltration or papules, and papules or blisters, etc., indicating that the sunscreen carrier of the present invention is non-irritating to human skin.

[0124] Test Example 3 In vitro skin penetration test

[0125] The vertical Franz diffusion cell method was used to conduct a transdermal experiment on in vitro pig skin. AVB, OCR and OMC were dissolved in butyl octyl salicylate to prepare free component 1 and free component 5 with the same content of sunscreen agent as in the sunscreen carrier of Example 1 or Example 5. The sunscreen carrier and free component were added to a blank cream (mainly composed of water, polyol, carbomer, caprylic / capric triglyceride) and stirred to prepare a test sample containing 40wt% sunscreen carrier or free component. The skin was fixed between the receiving chamber and the supply chamber, 1.0g of each of the above test samples was taken in the supply chamber, PBS (pH7.4) was used as the receiving solution, and it was stirred and diffused at 32°C. 0.5mL of receiving solution was taken at 4, 8, 12, and 24h, and an equal amount of constant temperature fresh receiving solution was immediately supplemented. After 24 hours, the skin was removed, washed and cut into pieces, ground into a homogenate with an appropriate amount of solvent, and the supernatant was centrifuged for HPLC analysis to calculate the skin retention per unit area of ​​AVB (butyl methoxydibenzoylmethane), OCR (octocrylene), and OMC (ethylhexyl methoxycinnamate).

[0126] Results Figure 2 and Figure 3The 24h skin retention of OMC per unit area in free component 1 and sunscreen carrier 1 (Example 1) was 25.38 μg / cm 2 and 4.17 μg / cm 2 Compared with free ingredient 1, the skin retention per unit area of ​​OMC in the sunscreen carrier (Example 1) was reduced by 83.57%. The skin retention per unit area of ​​OCR in free ingredient 1 and sunscreen carrier 1 (Example 1) for 24 hours was 12.34 μg / cm 2 and 2.04 μg / cm 2 Compared with free component 1, the skin retention per unit area of ​​OCR in sunscreen carrier 1 (Example 1) was reduced by 83.47%. The skin retention per unit area of ​​AVB in free component 1 and sunscreen carrier 1 (Example 1) for 24 hours was 11.69 μg / cm 2 and 1.72 μg / cm 2 Compared with the free sunscreen, the skin retention per unit area of ​​AVB in the sunscreen carrier (Example 1) was reduced by 85.19%. The skin retention per unit area of ​​OMC in the free ingredient 5 and the sunscreen carrier 5 (Example 5) for 24 hours was 12.43 μg / cm 2 and 8.25 μg / cm 2 Compared with free ingredient 5, the skin retention per unit area of ​​OMC in sunscreen carrier 5 (Example 5) was only reduced by 33.63%. The skin retention per unit area of ​​OCR in free ingredient 5 and sunscreen carrier 5 (Example 5) for 24 hours was 6.78 μg / cm 2 and 4.64 μg / cm 2 Compared with free ingredient 5, the skin retention per unit area of ​​OCR in sunscreen carrier 5 (Example 5) was only reduced by 31.56%. The skin retention per unit area of ​​AVB in free ingredient 5 and sunscreen carrier 5 (Example 5) for 24 hours was 6.16 μg / cm 2 and 4.47 μg / cm 2 . Compared with free component 5, the skin retention of AVB per unit area in sunscreen carrier 5 (Example 5) is only reduced by 27.44%. This indicates that the sunscreen carrier 1 (average particle size of 408.4 nm) prepared by encapsulating the sunscreen can significantly reduce the retention of the sunscreen in the skin, while the retention difference of sunscreen carrier 5 (average particle size of 192.5 nm) compared with the free component in the skin is not obvious, indicating that the larger the particle size of the sunscreen carrier, the safer it is to use as a sunscreen, and the particle size of the sunscreen carrier should be greater than 300 nm.

[0127] Test Example 4 Laser Confocal Microscope Observation of Skin Penetration

[0128] Preparation of RhoB nanocarriers and free RhoB: Rhodamine B (RhoB) was added to the aqueous phase as a fluorescent marker, and Rhodamine B sunscreen nanocarriers (RhoB nanocarriers) were prepared according to the method of Example 1, and a free Rhodamine B solution of equal concentration (i.e., Rhodamine B was added 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 nanocarriers were added to 80 g of blank essence matrix (mainly composed of water, polyols, and carbomer), respectively, and stirred evenly to obtain the corresponding free RhoB compound essence and RhoB sunscreen nanocarrier compound essence.

[0129] The skin permeation experiment of ex vivo pig skin was carried out by vertical Franz diffusion cell method. The skin was fixed between the receiving chamber and the supply chamber, and 0.5 g of RhoB-labeled free RhoB and RhoB sunscreen nanocarrier compound essence 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 for each group. After 4h and 8h, the residual sample on the skin was gently wiped off, the skin in the target area was removed, and the skin was rinsed again. After thorough cleaning, the residual moisture was wiped off. The sample was frozen and sectioned, and the sections were observed by laser confocal microscopy, and representative areas were selected for photography.

[0130] Results Figure 4 , RhoB sunscreen nanocarriers were concentrated in the stratum corneum at 4 hours and failed to penetrate the stratum corneum barrier, while free RhoB had penetrated the stratum corneum barrier and entered the deep tissue of the skin at 4 hours. As time went on, the fluorescence penetration depth of free RhoB in the skin increased further at 8 hours, reaching a skin depth of 174.3μm, while RhoB sunscreen nanocarriers were still mostly concentrated in the stratum corneum at 8 hours and failed to penetrate the stratum corneum barrier. The experimental results show that within the same period of time, the fluorescence intensity and penetration depth of free RhoB in the skin were significantly higher than those of RhoB sunscreen nanocarriers, revealing that sunscreen nanocarriers prepared by encapsulating sunscreen can significantly reduce the retention of sunscreen in the skin, making it safer to use as a sunscreen.

[0131] Test Example 5 Skin Moisture Content Test (Skin Film Forming Effect)

[0132] Five volunteers aged 20-50 were selected on a voluntary basis, and the inner sides of the left and right arms of the subjects were randomly set up with a blank cream group, a free composition group (20wt% comparative example 14 + blank cream matrix) and a sunscreen carrier (Example 1) group (20wt% Example 1 + blank cream matrix). The main components of the blank cream matrix are water, polyols, carbomer, caprylic / capric triglyceride. A control site without any sample was set up. The test was conducted before use (0h), 0.5h after use, 1h after use, 2h after use, 4h after use, and 8h after use. Before the test, the subject washed the test site with clean water and exposed the test site after drying it. It was necessary to sit for 20min in a constant temperature and humidity environment (22±2)℃, relative humidity 50%±10%).

[0133] Transepidermal water loss test: The TEWL value is an important indicator for evaluating the strength of the skin barrier function, which can reflect the water retention capacity of the skin stratum corneum and is one of the important indicators for evaluating the efficacy of moisturizing cosmetics. The TEWL value of the skin on the inner side of the subject's arm was measured using the Tewameter TM300 transepidermal water loss tester before and after using the sample for different periods of time. The test results are shown in Table 1 below.

[0134] Table 1: TEWL values ​​of the skin at different times before and after use of the samples

[0135]

[0136]

[0137] From the results in the table above, it can be seen that the transepidermal water loss value of the same volunteer control group (no product applied) has been maintained at a relatively high value over time, and the fluctuation over time is not particularly obvious, indicating that normal skin has a certain self-regulation ability without intervention, so the transepidermal water loss value will not fluctuate greatly over time, but will be relatively stable at a higher level. The blank group, free group and carrier group can all reduce the transepidermal water loss value of the skin, indicating that it has a positive effect on the skin and moisturizing (NLC carrier technology can allow sunscreen and other related components to form a dense protective film on the skin surface). The difference in transepidermal water loss between the blank group and the free group is not very large, but both are significantly higher than the carrier group, indicating that the free group and the blank group have no obvious film-forming effect (moisturizing effect) on the skin, and the sunscreen carrier has a better moisturizing effect (i.e., the skin transepidermal water loss is reduced) than the free component, indicating that the NLC technology is applied to the sunscreen carrier. By controlling the carrier particle size and structure, the carrier component can be better spread on the skin surface during the application process to form a dense protective film, thereby reducing the water loss of the skin epidermis.

[0138] Test Example 6 Inflammatory Factor Inhibition Test

[0139] 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 (20wt% comparative example 14 + blank matrix), sunscreen carrier group (20wt% embodiment 1 + blank matrix), comparative carrier group 1 (20wt% comparative example 3 + blank matrix), comparative carrier group 2 (20wt% comparative example 10 + blank matrix), comparative carrier group 3 (20wt% comparative example 11 + blank matrix). The main components of the above blank matrix are water, polyols, carbomer, caprylic / capric triglyceride. The mice were depilated to expose 1.0cm×1.0cm of hairless skin. The exposed skin of the mice in the control group was not exposed to ultraviolet radiation, and only the blank matrix was applied. The mice in the UV group and the sample group were placed in a special rectangular experimental box of 3.0 cm × 6.0 cm in size, and 0.1 mL of the corresponding sample was applied to the exposed skin with a coating thickness of 0.1 cm for 15 min. Then, they were exposed to long-wave ultraviolet rays (UVA, 1.55 J / cm 2 , 18min) and medium-wave ultraviolet rays (UVB, 0.95J / cm 2 , 11min) irradiation was performed to prepare a skin model damaged by ultraviolet irradiation. The skin model damaged by ultraviolet irradiation was prepared once a day for 7 consecutive days. After the irradiation, the skin tissue of the mice was taken and processed according to the instructions of the corresponding ELISA kit to detect the content of biochemical indicators IL-1β, IL-6 and TNF-α. The measurement results are shown in Table 2 below.

[0140] Table 2: Detection values ​​of IL-1β, IL-6 and TNF-α in different test groups

[0141] Grouping IL-1β (pg / mL) IL-6 (pg / mL) TNF-α(pg / mL) Control group 65.45±4.15 83.67±3.82 72.74±3.87 UV Groups <![CDATA[189.16±7.74 ## ]]> <![CDATA[214.73±7.26 ## ]]> <![CDATA[196.82±8.12 ## ]]> Free group <![CDATA[92.57±2.36 ** ]]> <![CDATA[111.72±2.58 ** ]]> <![CDATA[118.41±2.52 ** ]]> Sunscreen carrier set <![CDATA[71.35±3.26 **aa ]]> <![CDATA[92.38±2.84 **aa ]]> <![CDATA[79.66±2.03 **aa ]]> Comparative carrier group 1 <![CDATA[103.48±3.06 **bb ]]> <![CDATA[125.37±2.23 **bb ]]> <![CDATA[107.31±1.85 **bb ]]> Comparative vehicle group 2 <![CDATA[94.17±2.06 **bb ]]> <![CDATA[113.68±2.75 **bb ]]> <![CDATA[99.45±1.87 **bb ]]> Comparative vehicle group 3 <![CDATA[97.35±2.32 **bb ]]> <![CDATA[115.42±2.15 **bb ]]> <![CDATA[102.83±1.59 **bb ]]>

[0142] Note: Compared with the control group, ##p<0.01; compared with UV, **p<0.01; compared with the free group, aap<0.01; compared with the sunscreen carrier group, bbp<0.01.

[0143] The experimental results in Table 2 show that compared with the blank control group, the secretion of IL-1β, IL-6 and TNF-α in the UV group after ultraviolet irradiation increased significantly (p<0.01); compared with the UV group, the free group, the sunscreen carrier group, the comparison carrier group 1, the comparison carrier group 2 and the comparison carrier group 3 can significantly reduce the secretion of IL-1β, IL-6 and TNF-α produced by UV irradiation (p<0.01). Compared with the free group, the sunscreen carrier group has a more significant effect on reducing IL-1β, IL-6 and TNF-α after UV irradiation (p<0.01), indicating that the nanocarrier can better inhibit the production of inflammation after UV irradiation than the free component, and is more conducive to the efficacy of the sunscreen active composition. The 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 those of comparison carrier group 1, but the difference was not significant; compared with the sunscreen carrier group and the comparison carrier group (compared with carrier group 1, comparison carrier group 2, and 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 the comparison carrier group, indicating that baobab seed oil and Altai Bupleurum root extract used in sunscreen carriers have certain anti-inflammatory effects, can help inhibit the occurrence of erythema after UV irradiation, and the combination of the two has significant synergistic effect, which is very beneficial for improving the sun protection index.

[0144] Test Example 7 Sun Protection Index Test

[0145] The test instrument used is UV2000S. Test method: The test sample is smeared on the rough PMMA plate (the rough side is on the top) according to the weight, and the smearing amount is 1.3mg / cm 2 (Actual coating amount). Apply evenly in the form of small droplets of approximately equal volume. Weigh the plate immediately before and after coating and control the amount of product evaporation. The coated plate is balanced in the dark at ambient temperature for at least 15 minutes to help form a standard stable product film. Prepare a 100% transmittance reference sample by applying a few microliters of glycerin or other appropriate UV transparent substance on the rough side of the substrate, and determine the transmittance of UV radiation through the reference plate. Each sample to be tested is coated on at least three PMMA plates, and each plate should be measured at multiple different locations, and the single point area should exceed 0.5cm 2 , and ensure that the total area measured is at least 2cm 2 UV irradiation measures the incident irradiance in the plane of the treated plate surface, and transmission measurements after UV irradiation are made as closely as possible at exactly the same plate position as the previous measurement. The final SPF and UVA-PF values ​​are equal to the average of the values ​​derived for the individual plates.

[0146] The sunscreen carriers of Example 1 and Comparative Examples 1-13 were diluted 4 times with a blank cream base (mainly composed of water, polyols, carbomer, caprylic / capric triglyceride) and then the SPF and UVA-PF values ​​were measured. The measurement results are shown in Table 3 below.

[0147] Table 3: Sun protection index measurement results after the sunscreen carrier of Example 1 and the comparative example was diluted 4 times

[0148] Measurement object SPF UVA-PF Example 1 25.18 9.78 Comparative Example 1 5.15 5.47 Comparative Example 2 9.06 0.87 Comparative Example 3 19.37 7.62 Comparative Example 4 6.85 5.94 Comparative Example 5 9.96 1.36 Comparative Example 6 6.63 5.86 Comparative Example 7 9.58 1.54 Comparative Example 8 7.54 6.83 Comparative Example 9 10.86 2.46 Comparative Example 10 21.18 8.36 Comparative Example 11 20.96 8.16 Comparative Example 12 0.31 0.28 Comparative Example 13 0.22 0.19

[0149] From the machine test results of Comparative Examples 12 and 13, it can be seen that adding baobab seed oil and Altai Bupleurum root extract alone has a certain sun protection index value, but the number is small. Excluding possible errors in the experiment, it is impossible to determine the sun protection effect of baobab seed oil and Altai Bupleurum root extract used alone. Comparing Comparative Example 1 with Comparative Example 4, Comparative Example 6 and Comparative Example 8, Comparative Example 2 with Comparative Example 5, Comparative Example 7 and Comparative Example 9, the SPF value and UVA-PF value of the sun protection index of the combination of AVB and OCR (mass ratio 1:1.1) (Comparative Example 1, Comparative Example 4, Comparative Example 6, Comparative Example 8) and OMC (Comparative Example 2, Comparative Example 5, Comparative Example 7, Comparative Example 9) are not very ideal. When a single sunscreen is added with baobab seed oil or Altai Bupleurum root extract, the sun protection index has a certain promoting effect, but the promoting effect is not obvious; when a single sunscreen is added with baobab seed oil and Altai Bupleurum root extract at the same time, the promoting effect on the sun protection index is greater than the sum of the single components added separately, indicating that the simultaneous addition of baobab seed oil and Altai Bupleurum root extract has a certain synergistic effect on the single sunscreen, but the effect is not obvious. Comparing Example 1 with Comparative Example 3, Comparative Example 10 with Comparative Example 11, AVB, OCR and OMC have obvious synergistic effects after compounding, and the SPF value of Example 1 is increased by about 1.91 times compared with the sum of each single component (the sum of Comparative Example 1, Comparative Example 2, Comparative Example 12 and Comparative Example 13), and the UVA-PF value is increased by about 1.44 times; the SPF value of Comparative Example 3 is increased by about 1.36 times compared with the sum of each single component (the sum of Comparative Example 1 and Comparative Example 2), and the UVA-PF value is increased by about 1.20 times; the SPF value of Comparative Example 10 is increased by about 1.6 times compared with the sum of each single component (Comparative Example 1, Comparative Example 2 and Comparative Example 1 2) is increased by about 1.46 times, and the UVA-PF value is increased by about 1.26 times; the SPF value of Comparative Example 11 is increased by about 1.45 times compared with the sum of each single component (the sum of Comparative Example 1, Comparative Example 2 and Comparative Example 13), and the UVA-PF value is increased by about 1.27 times; while Example 1 is increased by about 1.30 times compared with Comparative Example 3, and the UVA-PF value is increased by about 1.28 times; Comparative Example 10 is increased by about 1.09 times compared with Comparative Example 3, and the UVA-PF value is increased by about 1.10 times; Comparative Example 11 is increased by about 1.08 times compared with Comparative Example 3, and the UVA-PF value is increased by about 1.07 times. The above results indicate that adding baobab seed oil or Bupleurum chinense root extract alone has a certain synergistic effect on the AVB, OCR and OMC composite sunscreen system, but the effect is not obvious. The simultaneous use of baobab seed oil and Bupleurum chinense root extract has a more obvious effect on improving the sun protection index of the AVB, OCR and OMC composite sunscreen system, indicating that the simultaneous use of baobab seed oil and Bupleurum chinense root extract has an obvious synergistic effect.The anti-inflammatory and soothing effects of baobab seed oil and Altai Bupleurum root extract could not be demonstrated in this test, but this effect could play a better role in practical applications or human tests.

[0150] Test Example 8 Comparative test of sun protection index of sunscreen carriers of Example 1 and Example 4 in actual application

[0151] Taking the sunscreen carriers of Example 1 and Example 4 as references, they are directly applied to O / W and W / O dosage form lotions and creams as application examples; a sunscreen free composition with the same sunscreen agent and active ingredient content as those in the sunscreen carriers of Example 1 and Example 4 (the preparation of the sunscreen free composition is shown in Comparative Example 14) is added to the same dosage form formula as the application example as a comparative application example.

[0152] Applied to conventional O / W and W / O emulsified systems, Application Example 1A is the sunscreen carrier of Example 1 30 wt% + BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) 2 wt% + O / W or W / O blank cream base formula, and Comparative Application Example 1A is the free composition 30 wt% + BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) 2 wt% + O / W or W / O blank cream base formula with the same content of sunscreen and active ingredient as the sunscreen carrier of Example 1. Application Example 4A is the sunscreen carrier of Example 4 30 wt% + BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) 2 wt% + O / W or W / O blank cream base formula, and Comparative Application Example 4A is the free composition 30 wt% + BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) 2 wt% + O / W or W / O blank cream base formula with the same content of sunscreen and active ingredient as the sunscreen carrier of Example 4.

[0153] Applied to traditional O / W and W / O emulsified systems, Application Example 1B is the sunscreen carrier 30wt% of Example 1 + BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) 2wt% + PBSA (phenylbenzimidazole sulfonic acid) 2wt% + O / W or W / O blank cream base formula, and Comparative Application Example 1B is a free composition 30wt% + BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) 2wt% + PBSA (phenylbenzimidazole sulfonic acid) 2wt% + O / W or W / O blank cream base formula with the same content of sunscreen agent and active ingredient as the sunscreen carrier of Example 1. Application Example 4B is the sunscreen carrier 30wt% + BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) 2wt% + PBSA (phenylbenzimidazole sulfonic acid) 2wt% + O / W or W / O blank cream base formula of Example 4, and Comparative Application Example 4B is the free composition 30wt% + BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine) 2wt% + PBSA (phenylbenzimidazole sulfonic acid) 2wt% + O / W or W / O blank cream base formula with the same content of sunscreen agent and active ingredient as the sunscreen carrier of Example 4.

[0154] The main ingredients of the above O / W blank cream base formula are water, polyols, ammonium acryloyldimethyltaurate / VP copolymer, behenyl alcohol, polydimethylsiloxane, acrylates / C10-30 alkyl acrylate crosspolymer, polymethyl methacrylate and tromethamine. The main ingredients of the W / O blank cream base formula are water, polyols, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, lauryl PEG-8 polydimethylsiloxane, polydimethylsiloxane, polydimethylsiloxane / polydimethylsiloxane crosspolymer, polyglyceryl-3 polyricinoleate, polyglyceryl-3 ricinoleate, disteardimonium hectorite, polymethylsilsesquioxane, polymethyl methacrylate and sodium chloride.

[0155] Then the sun protection index was measured according to the method described in Test Example 7. The test results are shown in Table 4 below.

[0156] Table 4: SPF measurement results of sunscreen carriers in practical applications of Example 1 and Example 4

[0157]

[0158]

[0159] Figure 5 The SPF and UVA-PF values ​​at the same sunscreen content calculated by BASF computer simulation are shown in Table 4 and Figure 5As can be seen from the results, the SPF machine test results of the comparative application example are closer to the simulation calculation results of the BASF sunscreen calculator, while the machine test 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 a significant promoting effect on the improvement of the sunscreen index. The machine test results of application examples 4A and 4B are not significantly different from the comparative application examples and the calculator simulation values, indicating that the composite sunscreen nanocarrier (application example 4) has no significant promoting effect on the improvement of the sunscreen index. It shows that for the same type and content of sunscreen, the same plant sunscreen synergistic active components and carrier types, the promoting effect of the sunscreen composite nanocarrier on the sunscreen index is related to the carrier particle size. The larger the carrier particle size, the less obvious the sunscreen index promotion effect. This is because the larger the carrier particle size, on the one hand, the worse the carrier stability, the more uneven the particle size distribution, and long-term placement will cause the sunscreen particles to aggregate, thereby 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 on the skin surface and thus affect the sunscreen effect. Therefore, in actual formulation applications, the composite sunscreen carrier particle size is preferably less than 800nm. In actual formulation applications, sunscreen nanocarriers with appropriate particle sizes (preferably 300-800nm) can greatly increase the sunscreen value and reduce the amount of overall sunscreen in the formula, which is particularly applicable when preparing high-multiple sunscreen products.

[0160] After placing the application examples and comparative application example samples at 4°C for 3 months, it can be felt that the crystal particles of sunscreen agent are precipitated when the comparative application examples 1A, 1B and comparative application examples 4A, 4B are applied, indicating that the solid sunscreen agent has aggregated and precipitated at low temperatures, while there is no aggregation and precipitation in application examples 1A, 1B and application examples 4A, 4B when applied, indicating that the application of sunscreen carriers has greatly improved the low-temperature stability problem of solid sunscreen agents. On the other hand, the sunscreen carrier has good water dispersibility and can be directly dispersed in the aqueous phase in actual formulation applications, simplifying the operation process. In summary, the sunscreen nanocarrier of the present invention can improve the sunscreen performance and reduce costs on the one hand, and can improve the formulation stability and simplify the operation process on the other hand, and has great market prospects and application value.

[0161] The above embodiments are only used to help illustrate the present invention, but the implementation methods of the present invention are not limited to the above embodiments. Any modifications, equivalent substitutions and improvements made by any technician familiar with the technical scope disclosed by the present invention are 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 butyl methoxydibenzoylmethane, octocrylene, and ethylhexyl methoxycinnamate; The sunscreen synergistic active ingredients are baobab seed oil and bupleurum 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 butyl methoxydibenzoylmethane, 5-20 parts of octocrylene, 5-30 parts of ethylhexyl methoxycinnamate, 0.5-10 parts of baobab seed oil, 0.1-5 parts of bupleurum extract, 5-40 parts of emulsifier, 0.1-10 parts of auxiliary 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 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 ethylhexyl methoxycinnamate, baobab seed oil, an emulsifier, an emulsifier aid, oil, and a polyol to obtain a mixed solution 1; (2) mixing avobenzone, octocrylene, oil, and polyol to obtain a mixed solution 2; (3) mixing the Altai radix bupleuri extract, polyol, and water to obtain a mixed solution 3; (4) Pour the mixed solution 1 and the mixed solution 2 into the mixed solution 3 and mix well to obtain a mixed solution 4; (5) The mixed solution 4 is subjected to nano-processing to obtain the ultra-broad-spectrum multi-effect composite 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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