Lipid composition with full-wave-band sunscreen function as well as preparation method and application of lipid composition
By using a specific formula of lipid composition, the problem of insufficient effectiveness of existing sunscreen products in taking into account both UVA and UVB protection is solved, and the stability of full-band sunscreen and sunscreen agents is improved, making its application in cosmetics safer and more efficient.
Patent Information
- Application Number
- CN202510163944.9
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-02-14
- Publication Date
- 2025-05-09
AI Technical Summary
Existing sun protection products are difficult to achieve ideal results in taking into account both UVA and UVB protection.
Using a lipid composition, including 4-tert-butyl-4'-methoxydiphenylmethane, UVA sunscreen component, UVB sunscreen component, broad spectrum sunscreen component, composite lipids, alcohols and emulsifiers, nanoemulsions are formed to improve the stability and water dispersion of the sunscreen agent through specific formula ratios and preparation methods.
It realizes full-band sun protection for UVA and UVB, improves the stability and water dispersion of sunscreen, making its application in skin care products/cosmetics more convenient, safe and efficient.
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Figure CN119950334A_ABST
Abstract
Description
Technical Field
[0001] The present invention relates to the technical field of cosmetics, and more specifically to a lipid composition with full-band sunscreen function, and a preparation method and application thereof. Background Art
[0002] The ultraviolet rays contained in sunlight are divided into long-wave ultraviolet rays (UVA) of 320-400nm, medium-wave ultraviolet rays (UVB) of 280-320nm, and short-wave ultraviolet rays (UVC) of 200-280nm by the dermatology community. Ultraviolet rays below 280nm are absorbed by the ozone layer and cannot reach the ground. The ultraviolet rays that reach the ground will have various effects on people's skin. Among them, UVB may cause erythema or blisters on the skin, promote the formation of melanin, and cause pigmentation on the skin, resulting in the formation of brown spots. The energy of UVA can reach the dermis of the skin, causing slow changes in the elastic fibers in the blood vessel wall or the conjunctural tissue, thereby causing the skin to turn brown, reduce the elasticity of the skin, and aggravate wrinkles. In addition, it may promote erythema reactions and even induce phototoxicity or photosensitivity reactions. Sensitive skin may also suffer from decreased immunity and even induce skin cancer if it is continuously exposed to UVB and UVA in sunlight. Therefore, it is very important to protect the human body from damage caused by excessive exposure to UVA and UVB.
[0003] Sunscreen cosmetics have been a hot spot in the development of the global cosmetics industry in recent years. With the improvement of living standards, people's demand for sunscreen products has also developed from UVB protection only to UVA protection. However, existing products are difficult to achieve ideal effects in terms of balancing UVA protection and UVB protection. Summary of the invention
[0004] The present invention provides a lipid composition with full-band sunscreen function and a preparation method and application thereof, so as to solve the problem that sunscreen products in the prior art are difficult to achieve ideal effects in terms of taking into account both UVA protection and UVB protection.
[0005] In the first aspect, the present invention provides a lipid composition, comprising the following components, in parts by weight: 1 to 15 parts of 4-tert-butyl-4'-methoxydibenzoylmethane, 0 to 15 parts of UVA sunscreen components, 5 to 40 parts of UVB sunscreen components, 0 to 25 parts of broad-spectrum sunscreen components, 10 to 35 parts of complex lipids, 1 to 25 parts of alcohols, and 10 to 35 parts of emulsifiers; wherein the UVB sunscreen component is any one of octocrylene, ethylhexyl methoxycinnamate, and ethylhexyl triazone.
[0006] As a possible implementation method, the following components are included, in parts by weight: 5 to 15 parts of 4-tert-butyl-4'-methoxydibenzoylmethane, 0 to 20 parts of the UVA sunscreen component, 0 to 20 parts of the broad-spectrum sunscreen component, 10 to 30 parts of the complex lipid, 1 to 20 parts of the alcohol, and 10 to 30 parts of the emulsifier.
[0007] As a possible implementation method, the following components are included, in parts by weight: 12 parts of 4-tert-butyl-4'-methoxydibenzoylmethane, 8 parts of the UVA sunscreen component, 20 parts of the UVB sunscreen component, 20 parts of the broad-spectrum sunscreen component, 22 parts of the complex lipids, 10 parts of the alcohols, and 18 parts of the emulsifier.
[0008] As a possible implementation, the broad-spectrum sunscreen component is bis-ethylhexyloxyphenol methoxyphenyl triazine; and / or the complex lipid is any one or a combination of C12-15 alcohol benzoate, dicaprylyl carbonate, diethylhexyl carbonate, dibutyl adipate, caprylic capric triglyceride, diisopropyl sebacate, isononyl isononanoate, triethylhexyl glycerol, isopropyl palmitate, isopropyl myristate, polydimethylsiloxane, isopropyl lauroyl sarcosine, squalane, triglyceride, phospholipid, and sterols; and / or the alcohol is 1,2-propylene glycol, 1,3-propylene glycol, dipropylene glycol, 1,2-butylene glycol, 1 ,2-pentanediol, pentaerythritol, 1,2-hexanediol, hexyldecanol, octyldodecanol, 16-18 alcohol, behenyl alcohol, glycerol, sorbitol, polyethylene glycol-400, any one or a combination of several thereof; and / or, the emulsifier is PEG-15 lauryl glyceride, polysorbate-20, polysorbate-60, polysorbate-80, dimethyl isosorbide, PEG-8 caprylic capric triglyceride, PEG-12 stearate, PEG-24 cholesterol ether, PEG-40 hydrogenated castor oil, sucrose stearate, PEG-20 methyl glucose sesquistearate, any one or a combination of several thereof.
[0009] In a second aspect, the present invention provides a method for preparing the lipid composition described in any possible implementation of the first aspect, comprising the following steps: mixing and heating the 4-tert-butyl-4'-methoxydibenzoylmethane, the UVA sunscreen component, the broad-spectrum sunscreen component, the complex lipid and the alcohol according to a formula ratio to obtain an oil phase system; adding the emulsifier to the oil phase system according to the formula ratio, mixing evenly and rotating to homogenize to obtain a nanoemulsion; cooling the nanoemulsion to room temperature to obtain the lipid composition.
[0010] As a possible implementation, the conditions for the rotary homogenization are: temperature 45-70° C., pressure 500-2000 bar.
[0011] In a third aspect, the present invention provides an application of the lipid composition described in any possible implementation of the first aspect or the lipid composition prepared by the preparation method described in any possible implementation of the second aspect in skin care products / cosmetics.
[0012] As a possible implementation method, the lipid composition can protect against both UVA and UVB.
[0013] Octyl Methoxycinnamate (OMC) is a sunscreen that protects against UVB. It has good formula applicability, high safety, and a large UV absorption coefficient. It is also cheap. A survey shows that OMC is the most frequently used raw material in the preparation of sunscreen cosmetics. Ethylhexyl Triazone (EHT) is the oil-soluble absorber with the strongest absorption capacity among sunscreens that protect against UVB. It has strong photostability and water resistance, and has good affinity for skin keratin. Octocrylene is an absorber in sunscreens that protect against UVB. It is photostability and can be used to stabilize 4-tert-butyl-4'-methoxydibenzoylmethane (trade name Avobenzone, Parsol 1789, Eusolex 9020, etc., AVO). There are very few chemical sunscreens that can block UVA, especially UVAI (340-400nm) ultraviolet rays. Avobenzone is one of the UVA filters currently widely approved for use in various countries. AVO exists in two forms: enol form (CE) and keto form (K). In AVO, these two forms are in equilibrium, with the enol form being dominant. The enol form has a strong absorption band in the UVA region at a wavelength of 357nm, while the keto form has a strong absorption capacity in the 260nm wavelength region, so it has no absorption effect on UVA or UVB. However, due to the light instability of AVO, the proportion of the keto form will increase under long-term light exposure, so sunscreen products containing this filter cannot effectively provide light protection. Bis-ethylhexyloxyphenol methoxyphenyl triazine (BEMT) is well-known in the chemical industry for its unique photostability and broad-spectrum ultraviolet absorption ability. This compound can absorb ultraviolet rays in both UVA and UVB bands at the same time, with its absorption peaks at wavelengths of 310nm and 340nm, respectively. This property makes it excellent in protecting the skin from ultraviolet damage. It can not only effectively block the invasion of ultraviolet rays, but also maintain a high degree of photostability. Even under strong ultraviolet rays, it can maintain a high absorption efficiency and is not prone to photodecomposition reactions. In addition, it can synergize with other sunscreens such as avobenzone to further enhance the sunscreen effect and inhibit the photodecomposition reactions that these sunscreens may produce.
[0014] In view of the problem that the UVA sunscreen avobenzone is easily degraded and discolored under light, the present invention is combined with BEMT that can inhibit its photodecomposition, so that the sunscreen can achieve stable, continuous and efficient synergistic protection in the entire band. At the same time, the lipid carrier technology also solves the problems of poor water solubility and inconvenient application of sunscreen, making it possible to use sunscreen conveniently, safely, continuously and efficiently.
[0015] The lipid composition obtained by the present invention is loaded with active ingredients: a full-band composite sunscreen, which includes a UVA sunscreen, a UVB sunscreen, and a broad-spectrum sunscreen. The UVA sunscreen is avobenzone, the UVB sunscreen is selected from at least one of octocrylene, ethylhexyl methoxycinnamate, or ethylhexyl triazone; and the broad-spectrum sunscreen is bis-ethylhexyloxyphenol methoxyphenyl triazine. The lipid composition has good stability and water dispersibility, and the preparation method is simple and controllable, with good repeatability, and is convenient for application in the preparation of sunscreen cosmetics.
[0016] The formula of the present invention breaks through the existing composite sunscreen application technology, and the prepared carrier itself has a safe, efficient, stable and continuous shielding effect on ultraviolet rays. The special structure of the lipid composition obtained by the present invention can improve the compatibility and release properties of the sunscreen. Using a certain proportion of liquid oil or other different lipids and solid lipids as a mixed lipid matrix not only increases the drug loading, but also can control the release of the sunscreen. BRIEF DESCRIPTION OF THE DRAWINGS
[0017] In order to more clearly illustrate the embodiments of the present invention or the technical solutions in the prior art, the drawings required for use in the embodiments or the description of the prior art will be briefly introduced below. Obviously, the drawings described below are only some embodiments of the present invention. For ordinary technicians in this field, other drawings can be obtained based on these drawings without paying creative work.
[0018] Figure 1 A schematic diagram of the preparation process of a lipid composition provided in an embodiment of the present invention.
[0019] Figure 2 The retention rates of avobenzone in lipid compositions A to lipid composition C and lipid compositions a to lipid composition c provided in the embodiments of the present invention under light irradiation of different durations. DETAILED DESCRIPTION
[0020] The following will be combined with the drawings in the embodiments of the present invention to clearly and completely describe the technical solutions in the embodiments of the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.
[0021] In order to solve the problem that sunscreen products in the prior art are difficult to achieve ideal effects in terms of both UVA protection and UVB protection, the embodiments of the present invention provide a lipid composition with full-band sunscreen function and a preparation method and application thereof.
[0022] Figure 1The following is a flow chart showing the preparation of a lipid composition having a full-band sunscreen function provided by an embodiment of the present invention. Figure 1 The preparation experiment and characterization were carried out according to the process shown. It can be seen that the lipid composition prepared by the present invention has good stability and good water dispersibility, which makes the process of compounding it into a sunscreen product more convenient; the stability of composition A to lipid composition C is good; the lipid composition A to lipid composition C have high physical stability; the composition A to lipid composition C have significantly higher sun protection factors and protection indexes against UVA.
[0023] The technical solution of the present invention will be further described below in conjunction with specific embodiments.
[0024] Example 1
[0025] This example provides an experiment for preparing a lipid composition.
[0026] according to Figure 1 The preparation experiments were carried out according to the process shown.
[0027] 10 g of avobenzone, 20 g of OMC, 20 g of octocrylene, 5 g of isopropyl lauroyl sarcosinate, 15 g of squalane, 5 g of lecithin, and 10 g of dipropylene glycol were heated and mixed in a water bath at 65 ° C to obtain the oil phase system A; 5 g of dimethyl isosorbide and 10 g of Tween 80 were added, heated and mixed in a water bath at 65 ° C, and then homogenized twice in a high-pressure homogenizer at 65 ° C and 800 bar, and cooled to room temperature to obtain a lipid composition A.
[0028] The difference from lipid composition A was that squalane was not added to obtain lipid composition a.
[0029] 12g of avobenzone, 8g of ethylhexyl triazone, 20g of bis-ethylhexyloxyphenol methoxyphenyl triazine, 15g of polydimethylsiloxane, 2g of lecithin, 5g of glyceryl stearate, and 10g of 1,2-hexanediol were heated and mixed in a water bath at 65°C to obtain the oil phase system B; 8g of dimethyl isosorbide and 10g of PEG-40 hydrogenated castor oil were added, the mixture was heated and mixed in a water bath at 65°C, and then homogenized twice in a high-pressure homogenizer at 65°C and 800 bar, and cooled to room temperature to obtain a lipid composition B.
[0030] The difference from lipid composition B is that PEG-40 hydrogenated castor oil is not added to obtain lipid composition b.
[0031] 5 g of avobenzone, 20 g of OMC, 20 g of octocrylene, 5 g of bis-ethylhexyloxyphenol methoxyphenyl triazine, 10 g of caprylic capric triglyceride, 15 g of glyceryl stearate, and 5 g of octyldodecanol were heated and mixed in a water bath at 65°C to obtain the oil phase system C; 10 g of dimethyl isosorbide, 5 g of lecithin, and 5 g of Tween 80 were added, the mixture was heated and mixed in a water bath at 65°C, and then homogenized twice in a high-pressure homogenizer at 65°C and 800 bar, and cooled to room temperature to obtain a lipid composition C.
[0032] The difference from lipid composition C is that octyldodecanol is not added to obtain lipid composition c.
[0033] The prepared lipid compositions A to C and lipid compositions a to c were diluted 10 times with deionized water, respectively, and the particle sizes were measured by a laser particle size analyzer to obtain the results shown in Table 1.
[0034] Table 1 Particle size results
[0035] Particle size / μm Lipid composition A 193.5 Lipid composition B 186.7 Lipid composition C 208.6 Lipid compositiona 0.218 Lipid compositionb 0.264 Lipid compositionc 0.262
[0036] The retention rates of avobenzone in the prepared lipid compositions A to lipid compositions C and lipid compositions a to lipid compositions c under different light exposure times were detected, and the following results were obtained: Figure 2 The results shown. Figure 2 It can be seen that compared with lipid compositions A to C, lipid compositions a to c reduce or remove lipids, emulsifiers, and alcohols in the formula, and as time goes by, the retention rate of avobenzone in the system is lower than that of lipid compositions A to C. This is because the reduction or absence of lipids, emulsifiers, and alcohols in the system leads to poor stability of the system, larger or precipitated particles of the sunscreen actives, and weakened interactions between active substances.
[0037] Good system stability enables active octocrylene and bis-ethylhexyloxyphenol methoxyphenyl triazine to continuously play the role of stabilizing the active substance avobenzone (AVO), promoting the long-term absorption of ultraviolet rays by the active substances AVO, EHT, and OMC in the skin surface layer, and is conducive to giving full play to the efficacy of the active substances in protecting the skin from ultraviolet damage. The lipid composition prepared by the present invention has good stability and good water dispersibility, making the process of compounding it into a sunscreen product more convenient.
[0038] Example 2
[0039] This example provides a characterization experiment of a lipid composition.
[0040] The particle size stability tests were performed on lipid compositions A to C and lipid compositions a to c prepared in Example 1, respectively, and the results shown in Table 2 were obtained.
[0041] Table 2 Particle size stability
[0042]
[0043] Since the particle size affects the physical stability, drug release and chemical stability of the sample, it can be used as an important indicator of stability. As shown in Table 2, the particle size of lipid compositions A to lipid compositions C did not change significantly after being placed for 90 days, indicating that lipid compositions A to lipid compositions C have better stability.
[0044] The interfacial potential tests were performed on lipid compositions A to C and lipid compositions a to c prepared in Example 1 at different times, and the results shown in Table 3 were obtained.
[0045] Table 3 Average potential detection results
[0046]
[0047] The measurement of interface potential can evaluate physical stability. Generally, when the absolute value of the interface potential is above 30 mV, it indicates that the system has low particle aggregation and is in a stable state, mainly due to the electrostatic repulsion between particles. When the absolute value of the interface potential is between 15 and 30 mV, it indicates that the system may condense. When the absolute value of the interface potential is higher than 60 mV, the system has extremely high stability. When the absolute value of the interface potential is lower than 5 mV, it indicates that the system may condense seriously. As shown in Table 3, the absolute values of the interface potential of lipid compositions A to lipid compositions C on the first day are all higher than 30 mV, which is a particle dispersion state with good stability. After 90 days of storage, the absolute values of the interface potential are still above 30 mV, indicating that lipid compositions A to lipid compositions C have high physical stability.
[0048] The SPF value (sun protection factor) and PFA value (protection index against UVA) of the lipid compositions A to C and lipid compositions a to c prepared in Example 1 were measured by the method specified in Chapter 8 of the 2015 edition of the Technical Specifications for Safety of Cosmetics. The results are shown in Table 4.
[0049] Table 4 SPF value and PFA value test results
[0050] SPF value PFA value Lipid composition A 33.5 11.3 Lipid composition B 36.4 13.4 Lipid composition C 37.2 12.7 Lipid compositiona 19.3 7.5 Lipid compositionb 20.4 6.3 Lipid compositionc 21.6 8.4
[0051] As can be seen from Table 4, the SPF values and PFA values of lipid compositions A to C are significantly higher than those of lipid compositions a to c. It can be seen that the lipid compositions provided by the present invention have significantly higher sun protection factors and protection indexes against UVA.
[0052] Although the preferred embodiments of the present invention have been described, those skilled in the art may make other changes and modifications to these embodiments once they have learned the basic creative concept. Therefore, the appended claims are intended to be interpreted as including the preferred embodiments and all changes and modifications that fall within the scope of the present invention.
[0053] Obviously, those skilled in the art can make various changes and modifications to the present invention without departing from the spirit and scope of the present invention. Thus, if these modifications and variations of the present invention fall within the scope of the claims of the present invention and their equivalents, the present invention is also intended to include these modifications and variations.
Claims
1. A lipid composition, characterized in that In parts by weight, it includes the following components: 1-15 parts of 4-tert-butyl-4'-methoxydibenzoylmethane, 0-15 parts of UVA sunscreen component, 5-40 parts of UVB sunscreen component, 0-25 parts of broad-spectrum sunscreen component, 10-35 parts of complex lipids, 1-25 parts of alcohols, and 10-35 parts of emulsifiers; Wherein, the UVB sunscreen component is any one of octocrylene, ethylhexyl methoxycinnamate, and ethylhexyl triazone.
2. The lipid composition according to claim 1, characterized in that In parts by weight, it includes the following components: The 4-tert-butyl-4'-methoxydibenzoylmethane is 5 to 15 parts, the UVA sunscreen component is 0 to 20 parts, the broad-spectrum sunscreen component is 0 to 20 parts, the complex lipid is 10 to 30 parts, the alcohol is 1 to 20 parts, and the emulsifier is 10 to 30 parts.
3. The lipid composition according to claim 1, characterized in that In parts by weight, it includes the following components: The 4-tert-butyl-4'-methoxydibenzoylmethane comprises 12 parts, the UVA sunscreen component comprises 8 parts, the UVB sunscreen component comprises 20 parts, the broad-spectrum sunscreen component comprises 20 parts, the complex lipid comprises 22 parts, the alcohol comprises 10 parts, and the emulsifier comprises 18 parts.
4. The lipid composition according to any one of claims 1 to 3, characterized in that The broad-spectrum sunscreen component is bis-ethylhexyloxyphenol methoxyphenyl triazine; And / or, the complex lipid is any one or a combination of C12-15 alcohol benzoate, dicaprylyl carbonate, diethylhexyl carbonate, dibutyl adipate, caprylic capric triglyceride, diisopropyl sebacate, isononyl isononanoate, triethylhexyl glycerol, isopropyl palmitate, isopropyl myristate, polydimethylsiloxane, isopropyl lauroyl sarcosine, squalane, triglycerides, phospholipids, and sterols; And / or, the alcohol is any one of 1,2-propylene glycol, 1,3-propylene glycol, dipropylene glycol, 1,2-butylene glycol, 1,2-pentanediol, pentaerythritol, 1,2-hexanediol, hexyldecanol, octyldodecanol, 16-18 alcohol, behenyl alcohol, glycerol, sorbitol, polyethylene glycol-400, or a combination of several thereof; And / or, the emulsifier is any one or a combination of PEG-15 lauryl glyceride, polysorbate-20, polysorbate-60, polysorbate-80, dimethyl isosorbide, PEG-8 caprylic capric triglyceride, PEG-12 stearate, PEG-24 cholesterol ether, PEG-40 hydrogenated castor oil, sucrose stearate, and PEG-20 methyl glucose sesquistearate.
5. The method for preparing the lipid composition according to any one of claims 1 to 4, characterized in that: The following steps are involved: The 4-tert-butyl-4'-methoxydibenzoylmethane, the UVA sunscreen component, the broad-spectrum sunscreen component, the complex lipid and the alcohol are mixed and heated according to a formula ratio to obtain an oil phase system; Adding the emulsifier to the oil phase system according to the formula ratio, mixing evenly and rotating to homogenize, to obtain a nanoemulsion; The nanoemulsion is cooled to room temperature to obtain the lipid composition.
6. The preparation method according to claim 5, characterized in that: The conditions for the rotary homogenization are: temperature 45-70° C., pressure 500-2000 bar.
7. Use of the lipid composition according to any one of claims 1 to 4 or the lipid composition prepared by the preparation method according to any one of claims 5 to 6 in skin care products / cosmetics.
8. The use according to claim 7, characterized in that: The lipid composition is capable of protecting against both UVA and UVB.