Sunscreen composition as well as preparation method and application thereof

Abstract

The invention relates to the technical field of skin care products, in particular to a sunscreen composition as well as a preparation method and application thereof. The sunscreen composition is prepared from a carrier, a sunscreen agent component and a sunscreen synergistic component, wherein the sunscreen agent component and the sunscreen synergistic component are entrapped by the carrier; the sunscreen agent component is prepared from avobenzone, diethylhexyl butyrylamide triazinone and bis-ethylhexyloxyphenol methoxyphenyl triazine; the sunscreen synergistic component is prepared from carrot seed oil and herba siegesbeckiae extract. According to the sunscreen composition, AVB, DHBT and BEMT are combined with sunscreen synergistic components including carrot seed oil and herba siegesbeckiae extract, and the sunscreen composition with remarkably excellent sunscreen capacity and safety is obtained through the synergistic effect of all the components and has important value in the related production field of skin care products.

Description

Technical Field

[0001] The present invention relates to the technical field of skin care products, and particularly to a sunscreen composition, a preparation method thereof, and an application thereof. Background Art

[0002] Skin aging mainly includes two mechanisms: natural aging and photoaging. Natural aging, as an endogenous process, results from the physiological changes of skin tissues with age, specifically manifested as epidermal thinning and reduced elasticity caused by subcutaneous tissue atrophy and collagen loss. Photoaging is triggered by ultraviolet radiation, and research data shows that about 3 / 4 of skin aging phenomena are related to ultraviolet exposure. In the ultraviolet spectrum, long-wave UVA (320 - 400 nm) has the characteristic of deep penetration, which can reach the lower layer of the dermis directly and cause direct tanning; medium-wave UVB (290 - 320 nm) causes damage to the basal layer of the epidermis due to its higher energy, leading to indirect pigmentation through an inflammatory reaction and having the potential risk of inducing skin lesions.

[0003] With the improvement of consumers' awareness of ultraviolet protection, higher requirements are put forward for the research and development of sunscreen products, and products with high protection efficacy are increasingly favored. Currently, the evaluation of sunscreen efficacy mainly adopts two major index systems: the SPF value quantifies the immediate protection effect against erythema caused by UVB, and the current standard upper limit is marked as SPF50+; the PA grade represents the defensive ability against the melanization effect caused by UVA, and the highest protection is calibrated as PA++++.

[0004] Sunscreen agents, as the core function, can be divided into two types: organic components absorb and convert ultraviolet energy through molecular structure, and inorganic components achieve protection through physical reflection and scattering. Each type of component has its own characteristics, but there is a balance problem between dosage and effect in actual application: to obtain a higher protection index, the dosage of sunscreen agents needs to be increased, but this will not only cause problems of skin tolerance and use comfort, but also objectively increase the production cost. Therefore, developing an innovative formula that takes into account high-efficiency protection and good skin feel has become the key breakthrough direction in the industry. Summary of the Invention

[0005] In order to solve the problems existing in the prior art, the present invention provides a sunscreen composition, a preparation method thereof, and an application thereof.

[0006] One of the methods to solve the technical problems existing in the prior art is the compound combination and optimization of sunscreen agents. Different sunscreen agents are compounded through a special process, their ratios and structures are optimized, and at the same time, active substances with sunscreen enhancement and anti-inflammatory and soothing effects are added. On the one hand, it enables them to exert the best UVB / UVA protection efficacy, and on the other hand, it effectively reduces the possible irritation and inflammation during the use of the product. By achieving both goals simultaneously, not only can the usage amount of sunscreen agents be effectively reduced, but also the skin feel and cost of the product can be optimized, achieving the best cost performance.

[0007] Nanostructured Lipid Carriers (NLC) is a new generation of lipid-based drug delivery system developed in recent years on the basis of 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 drug-loaded carriers, which can obtain a higher encapsulation efficiency and at the same time adjust the drug release behavior of SLN and improve stability. Applying the nanostructured lipid carrier technology to sunscreen 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. On the other hand, through scientific combination, each component can synergistically enhance the effect, optimize costs and processes. Finally, by optimizing the components and processes, the carrier particle size is controlled within a certain range, reducing the penetration of the sunscreen while enabling the sunscreen to form a dense protective film on the skin surface, further enhancing the sunscreen performance and safety, which has obvious practical application significance.

[0008] First, the present invention provides a sunscreen composition, comprising: a carrier, and a sunscreen component and a sunscreen synergistic component encapsulated by the carrier: The sunscreen component includes: avobenzone, diethylhexyl butamido triazone, and bis-ethylhexyloxyphenol methoxyphenyl triazine; The sunscreen synergistic component includes: carrot seed oil and Siegesbeckia orientalis extract.

[0009] Avobenzone (INCI: Butyl Methoxydibenzoylmethane, abbreviated as AVB) is a commercial chemical sunscreen mainly targeting UVA, with broad-band and high-protection ultraviolet protection ability, and it is also one of the few organic sunscreens that can absorb UVA1. AVB can provide strong protection in the UVA1 range and, when combined with other UVB absorbers, enables the entire formulation to provide broad-spectrum UVA / UVB protection. However, its stability is poor. Under ultraviolet irradiation, AVB will transform from the highly photo-absorbing enol form into the keto isomer with a shorter absorption wavelength and stronger photoreactivity. The keto isomer then undergoes photodegradation, decomposing into other products and completely losing its sun protection function, resulting in a reduction in the ultraviolet protection of AVB. In addition, free radicals are generated during the decomposition of AVB, which also has a high irritation to the skin. AVB can lose 36% of its absorption capacity after 1 hour of sunlight exposure, and only 42% remains after 2 hours. Moreover, its compatibility is poor. It will undergo a cycloaddition reaction with ethylhexyl methoxycinnamate and lose its ability to protect against ultraviolet rays. In addition, it will produce colored compounds when it encounters metal ions.

[0010] Diethylhexylbutamidotriazone (abbreviated as DHBT or HEB), with an off-white to light brown powder appearance, is a highly efficient new type of ultraviolet UVB sunscreen, with a relatively high absorption rate. Only a small concentration is required to achieve a high SPF value. DHBT 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 give the product a sticky and heavy skin feel.

[0011] Bis-ethylhexyloxyphenol methoxyphenyl triazine, also known as ultraviolet absorber UV-627, abbreviated as BEMT, is a highly efficient oil-soluble broad-spectrum ultraviolet filter, with a slightly yellow powder appearance. It can protect against a part of UVB and most of UVA, with an absorption wavelength between 290 - 370 nm. It can absorb both UVA and UVB simultaneously, with two absorption peaks at 310 nm for UVB and 343 nm for UVA, and it has good light stability and can be used as a stabilizer for photosensitive ultraviolet filters. In terms of sun protection efficacy, BEMT can effectively resist the dual damage of UVB and UVA. It can effectively improve the SPF value and UVA-PF protection index at low dosages. However, BEMT has a relatively large molecular weight and poor solubility, with a sticky and heavy skin feel, and there is a risk of crystallization during low-temperature storage.

[0012] The present invention combines AVB, DHBT, and BEMT for use. The three work synergistically to provide a higher degree of ultraviolet protection effect.

[0013] Most traditional sunscreen compositions only consider the synergistic effect among sunscreens, while ignoring the safety risks of the sunscreens themselves. Since most sunscreen components have certain safety risks to both humans and the environment, national regulations for chemical sunscreens require limited addition. Secondly, chemical sunscreens have a certain risk of penetration, especially for sensitive skin, which may cause irritation and allergies. Finally, ultraviolet radiation can directly cause the skin to turn red and get sunburned, resulting in inflammation. The photo-instability problem of some chemical sunscreens themselves will exacerbate the skin's inflammatory response. Therefore, the present invention further combines chemical sunscreens with plant sunscreen synergistic active ingredients to form an ultra-broad-spectrum (full-band ultraviolet absorption) and multi-functional sunscreen composition, which on the one hand has anti-inflammatory and soothing effects and reduces the irritation of sunscreens; on the other hand, it increases the photo-stability of sunscreens and has a synergistic effect, so as to better protect the skin from ultraviolet damage.

[0014] The plant sunscreen synergistic active ingredients added in the present invention include carrot seed oil and Siegesbeckia orientalis extract. Carrot seed oil contains 50-60% sesquiterpenol (mainly carotol and carotol), which has a very strong repair ability for damaged skin, can stimulate the regeneration of cells at the bottom layer of the skin, and at the same time activate the subcutaneous tissue. Long-term use helps to improve skin immunity and better resist external stimuli. Secondly, carrot seed oil contains umbelliferone, also known as 7-hydroxycoumarin, which has a good absorption effect on several specific wavelengths of ultraviolet light, helps prevent pigmentation, and has a certain sunscreen effect. When combined with chemical sunscreens, on the one hand, it has anti-inflammatory and soothing effects, prevents sunburn and sunburn, and on the other hand, it has a synergistic effect and improves the sun protection index.

[0015] Siegesbeckia orientalis extract is rich in various active ingredients such as terpenoids, polyphenols, flavonoids, sterols, organic acids, etc., which endows it with powerful skin care effects. On the one hand, Siegesbeckia orientalis extract can reduce the formation of melanin by inhibiting the activity of tyrosinase. This inhibitory effect can effectively reduce skin pigmentation and prevent and reduce skin sunburn and tanning when used in sunscreen. On the other hand, Siegesbeckia orientalis extract has strong antioxidant and anti-inflammatory effects. In the process of skin photoaging, inflammation often occurs. Inhibiting inflammation is beneficial to counteract the process of skin photoaging. Polyphenol and flavonoid components are strong antioxidants with good free radical scavenging ability. They can promote the scavenging of excess free radicals in cells, resist oxidative stress caused by UV irradiation, reduce damage to keratinocytes, and at the same time have a soothing effect. Its protection of keratinocytes can prevent the areas with existing spots from being damaged by external factors such as ultraviolet rays and generating more pigmentation. When used in combination with chemical sunscreen agents, on the one hand, it can prevent chemical sunscreen agents from generating excessive oxygen free radicals due to ultraviolet irradiation, with anti-inflammatory and soothing effects, and at the same time can also slow down the skin irritation and inflammation that may occur during the penetration process of the sunscreen, reducing the risks that may be brought during the penetration process of the sunscreen; on the other hand, it has a synergistic effect, improving the sun protection index and helping to prevent skin sunburn and tanning.

[0016] Based on parts by weight, the mass ratio of avobenzone, diethylhexyl butamido triazone and bis-ethylhexyloxyphenol methoxyphenyl triazine is: (5~20):(5~20):(1~20); and / or, Based on parts by weight, the sunscreen synergistic component includes: 0.1~5 parts of carrot seed oil and 0.1~5 parts of Siegesbeckia orientalis extract.

[0017] Furthermore, based on parts by weight, the sunscreen component includes: 8~10 parts of avobenzone, 8~12 parts of diethylhexyl butamido triazone and 8~10 parts of bis-ethylhexyloxyphenol methoxyphenyl triazine.

[0018] Based on parts by weight, the sunscreen synergistic component includes: 0.4~3 parts of carrot seed oil and 0.4~3 parts of Siegesbeckia orientalis extract.

[0019] Further, the mass ratio of the sunscreen component to the sunscreen synergistic component is (10~40):(0.5~8).

[0020] Further, the carrier is a nanostructured lipid carrier, and the mass ratio of the sunscreen component to the nanostructured lipid carrier is: (10~40):(30~120).

[0021] Meanwhile, aiming at the physical and chemical properties of the core sunscreen agents AVB, DHBT, and BEMT, a safe and effective co-loading carrier technology is constructed using nanostructured lipid carriers (NLC). Research on the carrier formulation and preparation process of sunscreen efficacy components is carried out to solve the solubility of AVB and BEMT, as well as the photo-stability of AVB. By optimizing the ratio of sunscreen agents and the combination of co-loaded phytochemicals, the potential irritation during the use of sunscreen agents can be effectively reduced, the damage to the skin caused by ultraviolet rays can be alleviated, and the overall sunscreen performance of the sunscreen carrier can be further improved.

[0022] According to the physical and chemical properties of AVB, BEMT, and DHBT, the present invention combines the co-loaded active ingredient combinations of carrot seed oil and Siegesbeckia extract, and uses nanostructured lipid carriers for encapsulation. The encapsulation methods include the carrier components completely encapsulating the sunscreen synergistic components, the carrier components partially encapsulating the sunscreen synergistic components, or the carrier components adjacent to the sunscreen synergistic components. By optimizing the combination of emulsifiers and the nano-carrier treatment process, the co-encapsulation of sunscreen agent components and sunscreen synergistic components can be achieved, the release behavior of the sunscreen synergistic components can be adjusted, the stability of the sunscreen synergistic components can be improved, the solubility of AVB, BEMT, and DHBT can be solved while optimizing the ratio of sunscreen agents, enabling the components to work synergistically, reducing the potential irritation during the use of sunscreen agents, alleviating the damage to the skin caused by ultraviolet rays, optimizing the skin feel, and enhancing the overall sunscreen performance of the sunscreen carrier.

[0023] Furthermore, by weight, the nanostructured lipid carrier includes 5 - 30 parts of emulsifier, 0.1 - 10 parts of co-emulsifier, 5 - 30 parts of polyol, 5 - 40 parts of oil, and 5 - 30 parts of water.

[0024] Furthermore, the emulsifier includes: one or more of fatty alcohol polyoxyethylene ether emulsifiers, polyethylene glycol fatty acid ester emulsifiers, polyol polyoxyethylene ether emulsifiers, glyceride emulsifiers, polyglycerol fatty acid ester emulsifiers, sorbitan fatty acid ester emulsifiers, polyoxyethylene sorbitan fatty acid ester emulsifiers, glucoside emulsifiers, sucrose ester emulsifiers, silicone oil emulsifiers, phosphate ester emulsifiers, fatty acid salt emulsifiers, amino acid emulsifiers, or phospholipid emulsifiers; and / or, The co-emulsifier includes: one or more of fatty acid co-emulsifiers, fatty alcohol co-emulsifiers, jojoba esters, rice bran wax, carnauba wax, beeswax, or paraffin wax; and / or, The polyol includes one or more of glycerol, propylene glycol, 1,3 - butanediol, 1,3 - propanediol, 1,2 - pentanediol, ethoxydiglycol, 1,2 - hexanediol, dipropylene glycol, isopropanol, polyethylene glycol, PPG - 10 sorbitol, octyldodecanol, hexyldecanol, 2,3 - propanediol, decyltetradecanol, hexanediol, methylpropanediol, octyldecanol, isopentanediol or octyldecanol; and / or, The oil includes one or more of triglyceride caprylate / caprate, isononyl isononanoate, dicaprylyl carbonate, cetyl ethylhexanoate, C12 - 15 alkyl 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 isopropyl carboxylate, phenethyl benzoate, butanediol dicaprylate / dicaprate, C12 - 15 - alkanol polyether - 9 isopropyl carboxylate or tridecyl salicylate.

[0025] Furthermore, the particle size of the sunscreen composition is 100 - 1000 nm; the particle size distribution PDI of the sunscreen composition is less than 0.3.

[0026] In the present invention, the particle size of the nanostructured lipid carriers containing AVB, BEMT and DHBT is controlled between 100 nm - 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 carriers (NLC) with appropriate particle size and particle size distribution can reduce skin penetration while enabling the sunscreen to adhere more evenly to the skin, forming a dense protective film on the skin surface, effectively reducing transdermal water loss of the skin, enhancing the safety of the product and enabling the sunscreen to exert its best efficacy.

[0027] In a second aspect, the present invention provides a product, which includes the aforementioned sunscreen composition; the product is a skin care product, a cosmetic or a drug.

[0028] The sunscreen composition provided by the present invention has good water dispersibility. When the finished product formula is applied, it can be directly added to the water phase (W / O), or added to the oil phase (O / W) at the end of the formula, and stirred evenly. There is no dosage form limitation, and it can be prepared into various forms such as emulsions, creams and sprays, which is very convenient in application. Moreover, compared with the free components, the sunscreen effect is better.

[0029] In a third aspect, the present invention provides a preparation method of the aforementioned sunscreen composition, including: Mix avobenzone, diethylhexylbutamide triazone, bis - ethylhexyloxyphenol methoxyphenyl triazine, an emulsifier, a co - emulsifier, an oil, carrot seed oil and a first part of the polyol, and mix well to obtain a first mixed solution; Mix the Siegesbeckia orientalis extract, the second part of polyol and water, and mix evenly to obtain a second mixed solution; Mix the first mixed solution and the second mixed solution evenly to obtain a third mixed solution; Perform nanometer treatment on the third mixed solution.

[0030] Furthermore, the conditions for mixing evenly include: stirring and mixing evenly under the condition of 70-80°C; and / or, The methods for nanometer treatment include: high-pressure homogenization, high-speed microfluidics or high shear, and the pressure of the high-pressure homogenization is 500-1500 bar.

[0031] The present invention has the following beneficial effects: The present invention provides a sunscreen combination including three active ingredients of AVB, BEMT and DHBT. By nanocarrierizing these three components, a super-broad-spectrum (full-band) multi-effect composite sunscreen carrier is obtained. The multi-components of AVB, BEMT, DHBT, carrot seed oil and Siegesbeckia orientalis extract synergistically enhance the effects, significantly improving the sunscreen effect and safety performance of the sunscreen composition.

[0032] The sunscreen composition provided by the present invention can be used for the preparation of various skin care products, cosmetics or drugs, and has important significance in the field of sunscreen. Description of the Drawings

[0033] In order to more clearly illustrate the technical solutions in the present invention or the prior art, the following will briefly introduce the drawings required for use in the description of the embodiments or the prior art. Obviously, the drawings in the following description are some embodiments of the present invention. For those of ordinary skill in the art, other drawings can be obtained based on these drawings without creative efforts.

[0034] Figure 1 It is the TEM electron micrograph of the sunscreen carrier provided in Embodiment 1 of the present invention; the sunscreen carrier in the figure is the super-broad-spectrum multi-effect composite sunscreen carrier prepared in Embodiment 1, and the same hereinafter.

[0035] Figure 2 It is the column chart of the skin retention amount of the sunscreen carrier and the free sunscreen provided in Embodiment 1 of the present invention.

[0036] Figure 3 It is the column chart of the skin retention amount of the sunscreen carrier and the free sunscreen provided in Embodiment 5 of the present invention.

[0037] Figure 4 It is the diffusion diagram of the RhoB sunscreen nanocarrier in the skin observed by the laser confocal microscope provided in Experimental Example 4 of the present invention.

[0038] Figure 5It is the statistical result of the diffusion of the RhoB sunscreen nanocarrier in the skin observed by a laser confocal microscope provided in Experimental Example 4 of the present invention.

[0039] Figure 6 It is the calculated result of the sun protection factor of the BASF sunscreen calculator provided in Experimental Example 8 of the present invention. Detailed implementation manners

[0040] To make the objectives, technical solutions and advantages of the present invention clearer, the technical solutions in the present invention will be clearly and completely described below with reference to the accompanying drawings in the present invention. Apparently, the described embodiments are some but not all of the embodiments of the present invention. All other embodiments obtained by those of ordinary skill in the art based on the embodiments in the present invention without creative efforts shall fall within the protection scope of the present invention.

[0041] Unless otherwise specified, the experimental methods involved in the following embodiments are all conventional methods in the art. For example, they can be referred to the experimental manuals in the art or carried out according to the conditions recommended in the manufacturer's instructions.

[0042] Unless otherwise specified, the experimental materials and reagents involved in the following embodiments can all be obtained through commercial channels.

[0043] The parts mentioned in the following embodiments are all parts by mass, and the mass unit can be determined according to the implementation scale, preferably grams (g).

[0044] In the following embodiments, the Siegesbeckia extract is preferably the whole-plant extract of Siegesbeckia orientalis L., and the extraction method is preferably the solvent extraction method, or it can also be purchased commercially.

[0045] Example 1 Preparation of an ultra-broad-spectrum multi-effect composite sunscreen carrier 1. Mix 10 parts of AVB, 10 parts of BEMT, 10 parts of DHBT, 4 parts of cetearyl olivate, 4 parts of sorbitan olivate, 10 parts of PEG-40 hydrogenated castor oil, 2 parts of polyglyceryl-6 distearate, 0.8 part of cetearyl alcohol, 10 parts of ethoxydiglycol, 10 parts of butyl octyl salicylate, and 2 parts of carrot seed oil at 70 - 80 °C with stirring to form a homogeneous and clear liquid 1. The parts mentioned in the present invention are all parts by mass.

[0046] 2. Mix 2 parts of the Siegesbeckia extract, 10 parts of glycerol, and 18 parts of water at 70 - 80 °C with stirring to form a homogeneous and clear liquid 2.

[0047] 3. Pour liquid 1 into liquid 2 and mix, and stir at 70 - 80 °C to form a homogeneous liquid 3.

[0048] 4. After homogenizing the liquid 3 at 500 bar in a high-pressure homogenizer, an ultra-broad-spectrum multi-effect composite sunscreen carrier is obtained. Its average particle size is 618.8 nm, PDI is 0.171, and the TEM electron micrograph is shown in the appendix. Figure 1 .

[0049] Among them, AVB, BEMT, and DHBT are sunscreen agents, and carrot seed oil and Siegesbeckia orientalis are sunscreen synergistic components.

[0050] Example 2 Preparation of Ultra-broad-spectrum Multi-effect Composite Sunscreen Carrier 1. Mix 10 parts of AVB, 10 parts of BEMT, 10 parts of DHBT, 7 parts of polyglyceryl-3 methylglucose distearate, 3 parts of polyglyceryl-6 distearate, 5 parts of PEG-40 hydrogenated castor oil, 10 parts of Tween-80, 1 part of behenyl alcohol, 10 parts of ethoxydiglycol, 15 parts of butyl octyl salicylate, and 2 parts of carrot seed oil at 70 - 80 °C and stir to form a homogeneous and clear liquid 1.

[0051] 2. Mix 2 parts of Siegesbeckia orientalis extract, 12 parts of glycerol, and 5 parts of water at 70 - 80 °C and stir 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 the liquid 3 at 200 bar in a high-pressure homogenizer, a full-spectrum composite sunscreen carrier is obtained. Its average particle size is 924.9 nm, and PDI is 0.253.

[0054] Example 3 Preparation of Ultra-broad-spectrum Multi-effect Composite Sunscreen Carrier 1. Mix 5 parts of AVB, 15 parts of BEMT, 5 parts of DHBT, 5 parts of PEG-60 glyceryl isostearate, 8 parts of Tween-80, 10 parts of PEG-40 hydrogenated castor oil, 2 parts of PEG-100 stearate, 2 parts of glyceryl stearate, 1 part of behenyl alcohol, 10 parts of ethoxydiglycol, 5 parts of butyl octyl salicylate, and 0.5 parts of carrot seed oil at 70 - 80 °C and stir to form a homogeneous and clear liquid 1.

[0055] 2. Mix 1 part of Siegesbeckia orientalis extract, 10 parts of glycerol, and 20 parts of water at 70 - 80 °C and stir to form a homogeneous and clear liquid 2.

[0056] 3. Pour liquid 1 into liquid 2 and mix, then stir at 70 - 80 °C to form a homogeneous liquid 3.

[0057] 4. After homogenizing the liquid 3 at 800 bar in a high-pressure homogenizer, a full-spectrum composite sunscreen carrier is obtained. Its average particle size is 539.3 nm, and PDI is 0.232.

[0058] Example 4 Preparation of Ultra-Broad Spectrum Multi-Effect Composite Sunscreen Carrier 1. Take 5 parts of AVB, 10 parts of BEMT, 10 parts of DHBT, 7 parts of polyglyceryl-3 methylglucose distearate, 5 parts of polyglyceryl-6 stearate, 8 parts of PEG-40 hydrogenated castor oil, 10 parts of Tween-80, 1 part of behenyl alcohol, 5 parts of ethoxydiglycol, 5 parts of C12-15 alkyl benzoate, 10 parts of butyl octyl salicylate, and 0.5 part of carrot seed oil. Stir at 70 - 80 °C to form a homogeneous and clear liquid 1.

[0059] 2. Take 1 part of Siegesbeckia orientalis extract, 10 parts of propylene glycol, and 15 parts of water. Stir at 70 - 80 °C to form a homogeneous and clear liquid 2.

[0060] 3. Pour liquid 1 into liquid 2 and mix. Stir at 70 - 80 °C to form a homogeneous liquid 3.

[0061] 4. Homogenize liquid 3 at 400 bar in a high-pressure homogenizer to obtain a full-spectrum composite sunscreen carrier with an average particle size of 623.4 nm and a PDI of 0.192.

[0062] Example 5 Preparation of Ultra-Broad Spectrum Multi-Effect Composite Sunscreen Carrier 1. Take 10 parts of AVB, 10 parts of BEMT, 10 parts of DHBT, 3 parts of cetyl stearyl olivate, 3 parts of sorbitan olivate, 15 parts of Tween-80, 2 parts of polyglyceryl-3 methylglucose distearate, 1 part of behenyl alcohol, 5 parts of ethoxydiglycol, 5 parts of C12-15 alkyl benzoate, 10 parts of butyl octyl salicylate, and 1 part of carrot seed oil. Stir at 70 - 80 °C to form a homogeneous and clear liquid 1.

[0063] 2. Take 0.5 part of Siegesbeckia orientalis extract, 10 parts of butylene glycol, and 15 parts of water. Stir at 70 - 80 °C to form a homogeneous and clear liquid 2.

[0064] 3. Pour liquid 1 into liquid 2 and mix. Stir at 70 - 80 °C to form a homogeneous liquid 3.

[0065] 4. Homogenize liquid 3 at 1000 bar in a high-pressure homogenizer to obtain a full-spectrum composite sunscreen carrier with an average particle size of 436.7 nm and a PDI of 0.227.

[0066] Example 6 Preparation of Ultra-Broad Spectrum Multi-Effect Composite Sunscreen Carrier 1. Take 5 parts of AVB, 5 parts of BEMT, 5 parts of DHBT, 4 parts of C12-20 alkyl glucoside, 2 parts of polyglyceryl-3 methyl glucoside distearate, 7 parts of PEG-40 hydrogenated castor oil, 8 parts of Tween-80, 4 parts of C14-22 alcohol, 10 parts of ethoxydiglycol, 5 parts of C12-15 alcohol benzoate, 5 parts of butyl octyl salicylate, and 0.5 part of carrot seed oil. Stir at 70-80 °C to form a homogeneous and clear liquid 1.

[0067] 2. Take 0.5 part of Siegesbeckia orientalis extract, 20 parts of glycerol, and 20 parts of water. Stir at 70-80 °C to form a homogeneous and clear liquid 2.

[0068] 3. Pour liquid 1 into liquid 2 and mix. Stir at 70-80 °C to form a homogeneous liquid 3.

[0069] 4. After homogenizing liquid 3 at 1400 bar in a high-pressure homogenizer, a full-spectrum composite sunscreen carrier is obtained, with an average particle size of 131.8 nm and a PDI of 0.206.

[0070] Comparative Example 1 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. Replace the sunscreen agent with: 10 parts of AVB, 10 parts of BEMT, do not use sunscreen synergistic components, and the other components and preparation methods are the same as those in Example 1.

[0071] Comparative Example 2 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. Replace the sunscreen agent with: 10 parts of DHBT, do not use sunscreen synergistic components, and the other components and preparation methods are the same as those in Example 1.

[0072] Comparative Example 3 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. Still use: 10 parts of AVB, 10 parts of BEMT, 10 parts of DHBT as the sunscreen agent, do not use sunscreen synergistic components, and the other components and preparation methods are the same as those in Example 1.

[0073] Comparative Example 4 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. Replace the sunscreen agent with: 10 parts of AVB, 10 parts of BEMT, and replace the sunscreen synergistic component with: 2 parts of carrot seed oil, and the other components and preparation methods are the same as those in Example 1.

[0074] Comparative Example 5 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. Replace the sunscreen agent with: 10 parts of DHBT, and replace the sunscreen synergistic component with: 2 parts of carrot seed oil, and the other components and preparation methods are the same as those in Example 1.

[0075] Comparative Example 6 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. The sunscreen agent is replaced with: 10 parts of AVB and 10 parts of BEMT. The sunscreen synergistic component is replaced with: 2 parts of Siegesbeckia orientalis extract. Other components and the preparation method are the same as those in Example 1.

[0076] Comparative Example 7 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. The sunscreen agent is replaced with: 10 parts of DHBT. The sunscreen synergistic component is replaced with: 2 parts of Siegesbeckia orientalis extract. Other components and the preparation method are the same as those in Example 1.

[0077] Comparative Example 8 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. The sunscreen agent is replaced with: 10 parts of AVB and 10 parts of BEMT. The sunscreen synergistic component still uses: 2 parts of carrot seed oil and 2 parts of Siegesbeckia orientalis extract. Other components and the preparation method are the same as those in Example 1.

[0078] Comparative Example 9 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. The sunscreen agent is replaced with: 10 parts of DHBT. The sunscreen synergistic component still uses: 2 parts of carrot seed oil and 2 parts of Siegesbeckia orientalis extract. Other components and the preparation method are the same as those in Example 1.

[0079] Comparative Example 10 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. The sunscreen agent still uses: 10 parts of AVB, 10 parts of BEMT, and 10 parts of DHBT. The sunscreen synergistic component is replaced with: 2 parts of carrot seed oil. Other components and the preparation method are the same as those in Example 1.

[0080] Comparative Example 11 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. The sunscreen agent still uses: 10 parts of AVB, 10 parts of BEMT, and 10 parts of DHBT. The sunscreen synergistic component is replaced with: 4 parts of carrot seed oil. Other components and the preparation method are the same as those in Example 1.

[0081] Comparative Example 12 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. The sunscreen agent still uses: 10 parts of AVB, 10 parts of BEMT, and 10 parts of DHBT. The sunscreen synergistic component is replaced with: 2 parts of Siegesbeckia orientalis extract. Other components and the preparation method are the same as those in Example 1.

[0082] Comparative Example 13 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. The sunscreen agent still uses: 10 parts of AVB, 10 parts of BEMT, and 10 parts of DHBT. The sunscreen synergistic component is replaced with: 4 parts of Siegesbeckia orientalis extract. Other components and the preparation method are the same as those in Example 1.

[0083] Comparative Example 14 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. No sunscreen agent is used, and the sunscreen synergistic component is replaced with: 2 parts of carrot seed oil, and the other components and preparation method are the same as those in Example 1.

[0084] Comparative Example 15 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier. No sunscreen agent is used, and the sunscreen synergistic component is replaced with: 2 parts of Siegesbeckia orientalis extract, and the other components and preparation method are the same as those in Example 1.

[0085] Comparative Example 16 The present invention provides a comparative example of an ultra-broad-spectrum multi-effect composite sunscreen carrier: The dosages of the sunscreen agent and the sunscreen synergistic component are the same as those in Example 1, but they are not prepared in the form of a nano-carrier. The sunscreen synergistic components, carrot seed oil and Siegesbeckia orientalis extract, are liquid components. The solid sunscreen agents AVB, BEMT, and DHBT are dissolved in butyl octyl salicylate to obtain a free sunscreen composition with the same content of the sunscreen agent and the sunscreen synergistic component as the sunscreen carrier in Example 1.

[0086] The average particle size of the ultra-broad-spectrum multi-effect composite sunscreen carriers obtained in the above Examples 1-6 and Comparative Examples 1-15 is within 100 nm - 1000 nm, and the PDI is 0.1 - 0.3. Each of the obtained ultra-broad-spectrum multi-effect composite sunscreen carriers was placed in a sealed container at -20°C, room temperature, 4°C, and 45°C for 3 months respectively, and no layering or precipitation occurred, and the particle size did not change significantly either, indicating that the ultra-broad-spectrum multi-effect composite sunscreen carrier of the present invention has good stability.

[0087] Experimental Example 1 Evaluation of Chicken Embryo Chorioallantoic Membrane Irritation The sunscreen carriers of Examples 1-6 and the free composition of Comparative Example 16 were each diluted 5 times with water and mixed evenly. Then, 0.2 mL of each sample was respectively taken and dropped on the surface of the chorioallantoic membrane. The changes in the CAM blood vessels were observed within 5 minutes, and the initial times when hyperemia, bleeding, and blood coagulation occurred in the CAM blood vessels were recorded, and the irritation score IS was calculated. The irritation score (irritation score, IS) was calculated according to the following formula: IS = [(301 - secH) × 5 + (301 - secL) × 7 + (301 - secC) × 9] / 300 In the above formula, secH represents the initial time of hyperemia (s); secL represents the initial time of bleeding (s); secC represents the initial time of blood coagulation (s).

[0088] The results of Examples 1-6 were similar. When the sunscreen carrier after being diluted 5 times was in contact with the chorioallantoic membrane of chicken embryos for 300 s, there was no capillary bleeding, no vascular lysis, and no coagulation phenomenon, 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 16) after being diluted 5 times was in contact with the chorioallantoic membrane of chicken embryos for 300 s, there was capillary bleeding, and the reaction score was 4.81, showing irritation. This shows that the sunscreen carrier of the present invention can reduce the irritation of the sunscreen itself.

[0089] Experimental Example 2 Patch Test The sunscreen carriers of Examples 1-6 containing 30 wt% were respectively added to a blank cream matrix (the main components are water, polyol, carbomer, and caprylic / capric triglyceride) 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.

[0090] The results showed that none of the 30 subjects had faint erythema, erythema, edematous erythema, significant swelling, infiltration or papules, and papules or blisters, indicating that the sunscreen carriers described in Examples 1-6 have no irritation to human skin.

[0091] Experimental Example 3 In Vitro Skin Penetration Experiment The transdermal experiment of excised pig skin was carried out by the vertical Franz diffusion cell method. Avobenzone (AVB), Diethylhexylbutamidotriazone (DHBT), and Bis-ethylhexyloxyphenol methoxyphenyl triazine (BEMT) were dissolved in butyl octyl salicylate to prepare free component 1 and free component 6 with the same sunscreen content as that in the sunscreen carrier of Example 1 or Example 6. The sunscreen carrier and the free component were respectively added to a blank cream (the main components are water, polyol, carbomer, and caprylic / capric triglyceride) 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, and 1.0 g was placed in the supply chamber. 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, and the supernatant was taken by centrifugation for HPLC analysis to calculate the skin retention amount per unit area of AVB (butyl methoxydibenzoylmethane), DHBT (diethylhexyl butanamidotriazone), and BEMT (bis-ethylhexyloxyphenol methoxyphenyl triazine).

[0092] The results are shown in Figure 2 and Figure 3 , the skin retention amounts per unit area of free AVB and AVB in the sunscreen carrier (Example 1) at 24 h were 9.49 μg / cm 2 and 0.94 μg / cm2 。Compared with the free components, the skin retention amount per unit area of AVB in the sunscreen carrier (Example 1) decreased by 90.10%. The skin retention amounts per unit area of free DHBT and DHBT in the sunscreen carrier (Example 1) for 24 h were 5.37 μg / cm 2 and 0.26 μg / cm 2 respectively. Compared with the free sunscreen agent, the skin retention amount per unit area of DHBT in the sunscreen carrier (Example 1) decreased by 95.16%. The skin retention amounts per unit area of free BEMT and BEMT in the sunscreen carrier (Example 1) for 24 h were 2.28 μg / cm 2 and 0.14 μg / cm 2 respectively. Compared with the free sunscreen agent, the skin retention amount per unit area of BEMT in the sunscreen carrier (Example 1) decreased by 93.86%. The skin retention amounts per unit area of free AVB and AVB in the sunscreen carrier (Example 6) for 24 h were 5.12 μg / cm 2 and 3.88 μg / cm 2 respectively. Compared with the free components, the skin retention amount per unit area of AVB in the sunscreen carrier (Example 6) decreased by 24.22%. The skin retention amounts per unit area of free DHBT and DHBT in the sunscreen carrier (Example 6) for 24 h were 2.83 μg / cm 2 and 2.05 μg / cm 2 respectively. Compared with the free sunscreen agent, the skin retention amount per unit area of DHBT in the sunscreen carrier (Example 6) decreased by 27.56%. The skin retention amounts per unit area of free BEMT and BEMT in the sunscreen carrier (Example 6) for 24 h were 1.32 μg / cm 2 and 0.94 μg / cm 2 respectively. Compared with the free sunscreen agent, the skin retention amount per unit area of BEMT in the sunscreen carrier (Example 6) decreased by 28.79%. It shows that the sunscreen carrier 1 (with an average particle size of 618.8 nm) prepared by encapsulating the sunscreen agent can significantly reduce the retention of the sunscreen agent in the skin, while there is no obvious difference in the skin retention between the sunscreen carrier 6 (with an average particle size of 131.8 nm) and the free components. It indicates that the larger the particle size of the sunscreen carrier, the safer it is as a sunscreen agent. It is recommended that the particle size of the sunscreen carrier be greater than 300 nm.

[0093] Experimental Example 4 Observation of Skin Penetration by Laser Confocal Microscopy Preparation of RhoB Nanocarriers and Free RhoB: Rhodamine B (RhoB) was added to the aqueous phase as a fluorescent label. The rhodamine B sunscreen nanocarriers (RhoB nanocarriers) were prepared using Example 1, and an equimolar solution of free rhodamine B (i.e., rhodamine B was added to the composition of Comparative Example 16) was prepared as a control sample (free RhoB). 20 g of free RhoB and 20 g of RhoB sunscreen nanocarriers were respectively added to 80 g of blank essence matrix (the main components were water, polyol, and carbomer), and stirred evenly to obtain the corresponding free RhoB compounded essence and RhoB sunscreen nanocarrier compounded essence.

[0094] The skin penetration experiment of ex vivo porcine skin was carried out using the vertical Franz diffusion cell method. The skin was fixed between the receiving chamber and the supply chamber. 0.5 g of RhoB-labeled free RhoB and 0.5 g of RhoB-labeled RhoB sunscreen carrier compounded essence were placed in the supply chamber, and PBS was used as the receiving solution. Stirring and diffusion were carried out 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 thoroughly dried after cleaning. The samples were cryosectioned, observed through a laser confocal microscope, and representative areas were selected for photography.

[0095] The results are shown in Figure 4 and Figure 5 , the RhoB sunscreen carrier concentrated in the stratum corneum at 4 h and failed to penetrate the stratum corneum barrier, while free RhoB had penetrated the stratum corneum barrier and entered the deep skin tissue at 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 246 μm, while the RhoB sunscreen carrier still concentrated mostly 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 penetration depth of free RhoB in the skin were significantly higher than those of the RhoB sunscreen carrier, revealing that the sunscreen nanocarriers prepared by encapsulating the sunscreen agent could significantly reduce the retention of the sunscreen agent in the skin and were safer as sunscreen agents.

[0096] Experimental Example 5 Skin Moisture Content Test (Skin Film-Forming Effect) Five volunteers aged 20 - 50 years old 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 16 + 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 are water, polyol, carbomer, and caprylic / capric triglyceride. 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. Before the test, the subjects washed the test site with clean water, dried it, and then exposed the test site. They needed to sit still for 20 min in an environment with constant temperature and humidity ((22 ± 2) °C, relative humidity 50% ± 10%).

[0097] Transepidermal water loss test: The level of the transepidermal water loss (TEWL) value is an important indicator for evaluating the strength of the skin barrier function. It 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 transepidermal water loss tester was used to measure the 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: Table 1 TEWL values of skin transepidermal water loss at different times before and after using the samples

[0098] It can be seen from the results in the above table that for the same volunteer, the transdermal water loss value of the control group (without applying any product) remained at a relatively high value over time, and the fluctuation with time was not particularly obvious. This shows that normal skin has a certain self-regulating ability without intervention, so the transdermal water loss value will not fluctuate greatly over time but will remain relatively stable at a relatively high level. The blank group, the free group, and the carrier group can all reduce the transdermal water loss value of the skin, indicating that they all have a positive effect on 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 large, 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 better moisturizing efficacy compared to the free components (i.e., the transdermal water loss of the skin is reduced). 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.

[0099] Experimental Example 6 Inflammatory Factor Inhibition Test 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 16 + 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 12 + 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 hairless skin of 1.0 cm × 1.0 cm. The bare skin of the mice in the control group was not irradiated with ultraviolet light and only coated with the blank matrix. The mice in the UV group and the sample groups were respectively placed in a special rectangular experimental box with a size of 3.0 cm × 6.0 cm, and 0.1 ml of the corresponding sample was coated on the bare skin, and the coating thickness was 0.1 cm; after pretreatment for 15 min, 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 the contents of biochemical indexes IL-1β, IL-6, and TNF-α were detected according to the instructions of the corresponding ELISA kit, and the measurement results are shown in Table 2 below.

[0100] Table 2 Detection values of IL-1β, IL-6, and TNF-α contents in different test groups

[0101] Note: Compared with the control group, ##p < 0.01; compared with the UV group, **p < 0.01; compared with the free group 1, aa p < 0.01, and compared with the sunscreen carrier group 1, bb p < 0.01.

[0102] 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 generated by UV irradiation (p < 0.01). Compared with the free group, the sunscreen carrier group had a more significant effect in reducing IL-1β, IL-6, and TNF-α after UV irradiation (p < 0.01), indicating that the nano-carrier could inhibit the generation of inflammation after UV irradiation more effectively than the free components 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 reduction 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 comparison carrier groups (comparison carrier group 1, comparison carrier group 2, comparison carrier group 3), the sunscreen carrier group had a very obvious inhibitory effect on IL-1β, IL-6, and TNF-α after UV irradiation, which was significantly better than the comparison carrier groups, indicating that carrot seed oil and Siegesbeckia extract both had a certain anti-inflammatory effect when applied to the sunscreen carrier, could help inhibit the generation of erythema after UV irradiation, and when used in combination, the synergistic effect was significant, which was very beneficial for improving the sun protection factor.

[0103] Experimental Example 7 Sun Protection Factor Test The test instrument used was UV2000S. Test method: The test sample was applied by weight on a rough PMMA plate (the rough side on the top), and the application amount was 1.3 mg / cm² (actual application amount). When applying, it was evenly applied in the form of small droplets with approximately equal volumes. The plate was weighed immediately before and after application and the evaporation of the product was controlled. The applied plate was 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 was prepared by applying a few microliters of glycerol or other appropriate ultraviolet-transparent substance on the rough surface of the substrate, and the transmittance of ultraviolet radiation through the reference plate was determined. Each sample to be tested was applied on at least three PMMA plates, and each plate should be measured at multiple different positions, the single-point area should exceed 0.5 cm², and it was ensured that the total measured area was at least 2 cm². The incident irradiance was measured in the plane of the surface of the treated plate during UV irradiation, and the transmittance measurement after UV irradiation was carried out at the same plate position as accurately as possible as the previous measurement. The final SPF, UVA-PF value, and critical wavelength value were equal to the average of the values derived from individual plates.

[0104] The sunscreen carriers of Example 1 and Comparative Examples 1-15 (corresponding to Example 1A and Comparative Examples 1A-15A in the table) were diluted 2.5 times with a blank cream matrix (the main components are water, polyol, carbomer, and triglyceride of caprylic acid / capric acid), and then the SPF and UVA-PF values were measured. The measurement results are shown in Table 3 below: Table 3 Measurement Results of Sunscreen Index after Diluting the Sunscreen Carriers of Example 1 and Comparative Examples by 2.5 Times

[0105] Judging from the machine measurement results of Comparative Examples 14A and 15A, when carrot seed oil and Siegesbeckia extract were added alone, they both had certain sunscreen index values, but the numbers were small. Excluding the possible errors in the experiment, the sunscreen efficacy of carrot seed oil and Siegesbeckia extract used alone could not be determined.

[0106] Comparing Comparative Example 1A with Comparative Examples 4A, 6A, and 8A, and Comparative Example 2A with Comparative Examples 5A, 7A, and 9A, the SPF and UVA-PF values of the sunscreen index of using AVB and BEMT compositions (Comparative Example 1A, Comparative Example 4A, Comparative Example 6A, Comparative Example 8A) and DHBT (Comparative Example 2A, Comparative Example 5A, Comparative Example 7A, Comparative Example 9A) alone were not very ideal. After adding carrot seed oil or Siegesbeckia extract to the two groups of sunscreens alone, there was a certain promoting effect on the sunscreen index, but the promoting effect was not obvious. After adding carrot seed oil and Siegesbeckia extract to the two groups of sunscreens at the same time, the promoting effect on the sunscreen index was greater than the sum of adding a single component alone, indicating that adding carrot seed oil and Siegesbeckia extract at the same time had a certain synergistic effect on a single sunscreen or a combination of sunscreens, and the promoting effect on the combination of sunscreens was more obvious.

[0107] Comparing Example 1A with Comparative Example 3A, Comparative Example 10A with Comparative Example 12A, AVB, BEMT and DHBT have obvious synergistic effects after compounding, and the SPF value of Example 1A is increased by about 1.47 times compared with the sum of each single component (the sum of Comparative Example 1A, Comparative Example 2A, Comparative Example 14A and Comparative Example 15A), and the UVA-PF value is increased by about 1.55 times; the SPF value of Comparative Example 3A is increased by about 1.14 times compared with the sum of each single component (the sum of Comparative Example 1A and Comparative Example 2A), and the UVA-PF value is increased by about 1.23 times; the SPF value of Comparative Example 10A is increased by about 1.22 times compared with the sum of each single component (the sum of Comparative Example 1A, Comparative Example 2A and Comparative Example 14A), and the UVA- The PF value is increased by about 1.32 times; the SPF value of comparative example 12A is increased by about 1.24 times compared with the sum of each single component (the sum of comparative example 1A, comparative example 2A and comparative example 15A), and the UVA-PF value is increased by about 1.32 times; while the SPF value of Example 1A is increased by about 1.37 times compared with comparative example 3A, and the UVA-PF value is increased by about 1.33 times; the SPF value of comparative example 10A is increased by about 1.11 times compared with comparative example 3A, and the UVA-PF value is increased by about 1.11 times; the SPF value of comparative example 12A is increased by about 1.13 times compared with comparative example 3A, and the UVA-PF value is increased by about 1.10 times. The comparison of the results of comparative example 11A and comparative example 10A, and the comparison of the results of comparative example 12A and comparative example 13A show that even the incremental effect is very limited when there is only one sunscreen synergistic component. The SPPF and UVA-PF effects of Comparative Example 11A and Comparative Example 10A are similar, and the SPPF and UVA-PF effects of Comparative Example 12A and Comparative Example 13A are similar.

[0108] The above results show that adding carrot seed oil or Siegesbeckia extract alone has a certain synergistic effect on the composite sunscreen system of AVB, BEMT and DHBT, but the effect is not obvious. The simultaneous use of carrot seed oil and Siegesbeckia extract has a more obvious effect on improving the sun protection index of the composite sunscreen system of AVB, BEMT and DHBT, indicating that the simultaneous use of carrot seed oil and Siegesbeckia extract has a significant synergistic effect. The anti-inflammatory and soothing effects of carrot seed oil and Siegesbeckia extract cannot be demonstrated in this test, but this aspect of the effect can play a better role in practical applications or human tests.

[0109] Experimental Example 8 Comparative test of sun protection index between Example 1 and Example 2 in actual application Taking the sunscreen carriers of Example 1 and Example 2 as references, directly applying them to emulsions and creams of O / W and W / O dosage forms is the application example; adding a free sunscreen composition with the same proportion of sunscreen agent and active substance content as that in the sunscreen carriers of Example 1 and Example 2 (for the preparation of the free sunscreen composition, see Comparative Example 16) to the same dosage form formula of the application example is the comparative application example.

[0110] Applied to the traditional O / W emulsification system, Application Example 1A is 30 wt% of the sunscreen carrier of Example 1 + 6 wt% of OMC (ethylhexyl methoxycinnamate) + O / W blank cream matrix formula; Comparative Application Example 1A is 30 wt% of the free composition with the same sunscreen agent and active substance content as that of the sunscreen carrier of Example 1 + 6 wt% of OMC (ethylhexyl methoxycinnamate) + O / W blank cream matrix formula. Application Example 2A is 30 wt% of the sunscreen carrier of Example 2 + 6 wt% of OMC (ethylhexyl methoxycinnamate) + O / W blank cream matrix formula; Comparative Application Example 2A is 30 wt% of the free composition with the same sunscreen agent and active substance content as that of the sunscreen carrier of Example 2 + 6 wt% of OMC (ethylhexyl methoxycinnamate). The main components of the above O / W blank cream matrix formula are water, polyol, acryloyldimethyltaurate / VP copolymer, behenyl alcohol, polydimethylsiloxane, acrylate / C10-30 alkyl acrylate cross-linked polymer, polymethyl methacrylate and tromethamine.

[0111] Applied to the W / O emulsion system, Application Example 1B is the sunscreen carrier of Example 1 at 30 wt% + OMC (ethylhexyl methoxycinnamate) at 2 wt% + PBSA (phenylbenzimidazole sulfonic acid) at 1.5 wt% + W / O blank cream matrix formulation; Application Comparative Example 1B is a free composition with the same content of sunscreen agent and active ingredient as the sunscreen carrier of Example 1 at 30 wt% + OMC (ethylhexyl methoxycinnamate) at 2 wt% + PBSA (phenylbenzimidazole sulfonic acid) at 1.5 wt% + W / O blank cream matrix formulation; Application Example 2B is the sunscreen carrier of Example 2 at 30 wt% + OMC (ethylhexyl methoxycinnamate 2% wt) + PBSA (phenylbenzimidazole sulfonic acid) at 1.5 wt% + W / O blank cream matrix formulation, and Application Comparative Example 2B is a free composition with the same content of sunscreen agent and active ingredient as the sunscreen carrier of Example 2 at 30 wt% + OMC (ethylhexyl methoxycinnamate) at 2 wt% + PBSA (phenylbenzimidazole sulfonic acid) at 1.5 wt% + W / O blank cream matrix formulation. The main components of the above W / O blank cream matrix formulation are water, polyols, cetyl PEG / PPG-10 / 1 dimethicone, lauryl PEG-8 dimethicone, dimethicone, dimethicone / dimethicone crosspolymer, polyglyceryl-3 polyricinoleate, polyglyceryl-3 ricinoleate, di-stearyldimonium hectorite, polymethylsilsesquioxane, polymethyl methacrylate, and sodium chloride.

[0112] Then, the sunscreen index was measured according to the method described in Experimental Example 7, and the test results are shown in Table 4 below: Table 4 Measurement results of the sunscreen index in the actual application of the sunscreen carriers of Example 1 and Example 2

[0113] Figure 6 are the SPF value and UVA-PF value calculated by BASF computer simulation at the same sunscreen agent content. From Table 4 and Figure 6As can be seen from the results, the measured SPF results of the comparative application example are relatively close to the simulated calculation results of the BASF sunscreen calculator. However, the measured results of Application Example 1A and Application Example 1B are much higher than the simulated calculation results, indicating that the composite sunscreen nanocarrier (Application Example 1) has an obvious promoting effect on the improvement of the sun protection factor. For Application Example 2A and Application Example 2B, the difference between the measured results and the simulated values of the comparative application example and the calculator is not obvious, indicating that the composite sunscreen nanocarrier (Application Example 2) has no obvious promoting effect on the improvement of the sun protection factor. This 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, on the one hand, the larger the carrier particle size, the worse the carrier stability and the more uneven the particle size distribution. Prolonged storage will cause the aggregation of sunscreen agent particles, thus affecting the sunscreen effect. On the other hand, the larger the carrier particle size, the more uneven the distribution of carrier particles on the skin surface, which will also affect the uniform distribution of the sunscreen agent on the skin surface and thus affect the sunscreen effect. Therefore, in actual formula applications, the particle size of the composite sunscreen carrier should be less than 800 nm. When actually formulating, sunscreen nanocarriers with appropriate particle sizes (preferably 300 - 800 nm) can greatly improve the sun protection value and reduce the overall amount of sunscreen agents used in the formula, especially applicable when preparing high-fold sunscreen products.

[0114] After placing the samples of the application examples and the comparative application examples at 4°C for 3 months, it can be felt that there are crystal particles of sunscreen agents precipitating when applying Comparative Application Example 1A, 1B, Comparative Application Example 2A, and 2B, indicating that the solid sunscreen agents have aggregated and precipitated at low temperatures. However, this is not the case when applying Application Example 1A, 1B, Application Example 2A, and 2B, indicating that the application of the sunscreen carrier has 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 during actual formula applications, simplifying the operation process. In summary, the sunscreen nanocarrier of the present invention can, on the one hand, improve the sunscreen performance and reduce costs, and on the other hand, improve the formula stability and simplify the operation process, having great market prospects and application value.

[0115] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and are not intended to limit them. Although the present invention has been described in detail with reference to the foregoing embodiments, those of ordinary skill in the art should understand that they can still modify the technical solutions recorded in the foregoing embodiments or perform equivalent replacements for some of the technical features. However, such modifications or replacements do not cause the essence of the corresponding technical solutions to deviate from the spirit and scope of the technical solutions of the embodiments of the present invention.

Claims

1. A sunscreen composition, characterized in that, Comprising: a carrier, and a sunscreen component and a sunscreen synergistic component encapsulated by the carrier: The sunscreen component includes: avobenzone, diethylhexyl butamido triazone, and bis-ethylhexyloxyphenol methoxyphenyl triazine; The sunscreen synergistic component includes: carrot seed oil and Siegesbeckia orientalis extract.

2. The sunscreen composition according to claim 1, characterized in that, By weight, the mass ratio of avobenzone, diethylhexyl butamido triazone, and bis-ethylhexyloxyphenol methoxyphenyl triazine is: (5~20):(5~20):(1~20); and / or, By weight, the sunscreen synergistic component includes: 0.1~5 parts of carrot seed oil and 0.1~5 parts of Siegesbeckia orientalis extract.

3. The sunscreen composition according to claim 2, characterized in that, The mass ratio of the sunscreen component to the sunscreen synergistic component is (10~40):(0.5~8).

4. The sunscreen composition according to any one of claims 1-3, characterized in that The carrier is a nanostructured lipid carrier, and the mass ratio of the sunscreen component to the nanostructured lipid carrier is: (10~40):(30~120).

5. The sunscreen composition according to claim 4, characterized in that, By weight, the nanostructured lipid carrier includes 5~30 parts of an emulsifier, 0.1~10 parts of a co-emulsifier, 5~30 parts of a polyol, 5~40 parts of an oil, and 5~30 parts of water.

6. The sunscreen composition according to claim 5, characterized in that, The emulsifier includes: one or more of fatty alcohol polyoxyethylene ether emulsifiers, polyethylene glycol fatty acid ester emulsifiers, polyol polyoxyethylene ether emulsifiers, glyceride emulsifiers, polyglycerol fatty acid ester emulsifiers, sorbitan fatty acid ester emulsifiers, polyoxyethylene sorbitan fatty acid ester emulsifiers, glucoside emulsifiers, sucrose ester emulsifiers, silicone oil emulsifiers, phosphate ester emulsifiers, fatty acid salt emulsifiers, amino acid emulsifiers, or phospholipid emulsifiers; and / or, The co-emulsifier includes: one or more of fatty acid co-emulsifiers, fatty alcohol co-emulsifiers, jojoba ester co-emulsifiers, rice bran wax, carnauba wax, beeswax, or paraffin wax; and / or, The polyol includes: one or more of glycerol, propylene glycol, 1,3-butanediol, 1,3-propanediol, 1,2-pentanediol, ethoxydiglycol, 1,2-hexanediol, dipropylene glycol, isopropanol, polyethylene glycol, PPG-10 sorbitol, octyldodecanol, hexyl decanol, 2,3-propanediol, decyltetradecanol, hexanediol, methylpropanediol, octyldecanol, isopentylene glycol, or octyldecanol; and / or, The oil includes: one or more of triglyceride caprylate / caprate, isononyl isononanoate, dicaprylyl carbonate, cetyl ethylhexanoate, C12-15 alkyl 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 isopropyl carboxylate, phenethyl benzoate, butanediol dicaprylate / dicaprate, C12-15-alkanol polyether-9 isopropyl carboxylate, or tridecyl salicylate.

7. The sunscreen composition according to any one of claims 1-6, characterized in that, The particle size of the sunscreen composition is 100~1000 nm; and / or, The particle size distribution PDI of the sunscreen composition is less than 0.

3.

8. A method for preparing the sunscreen composition according to any one of claims 1-7, characterized in that, Comprising: Mix avobenzone, diethylhexylbutamidotriazone, bis-ethylhexyloxyphenol methoxyphenyl triazine, an emulsifier, a co-emulsifier, an oil, carrot seed oil, and a first portion of polyol, and mix well to obtain a first mixed solution; Mix Siegesbeckia orientalis extract, a second portion of polyol, and water, and mix well to obtain a second mixed solution; Mix the first mixed solution and the second mixed solution well to obtain a third mixed solution; Subject the third mixed solution to nanosizing treatment.

9. The preparation method according to claim 8, characterized in that, The conditions for mixing well include: stirring and mixing well under the condition of 70-80 °C; and / or The nanosizing treatment method includes: high-pressure homogenization, high-speed microfluidization, or high shear, and the pressure of the high-pressure homogenization is 500-1500 bar.

10. A product, characterized in that, The product includes the sunscreen composition according to any one of claims 1-7 or the sunscreen composition prepared by the method according to any one of claims 8-9; the product is a skin care product, a cosmetic, or a drug.

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