Composition for improving transdermal absorption of hydroxytyrosol, method for preparing the same, and skin care product

Abstract

The present application relates to the skin care technical field, specifically, it relates to the composition for improving the transdermal absorption of hydroxytyrosol, its preparation method and skin care product, the raw materials of the composition for improving the transdermal absorption of hydroxytyrosol include 0.1-1.0 parts of hydroxytyrosol, 0.1-2.0 parts of ceramide substance and 0.1-5.0 parts of squalane by mass fraction.The compound can improve the transdermal absorption of hydroxytyrosol, and the biological activity of hydroxytyrosol can be maximized.

Description

Technical Field

[0001] This invention relates to the field of skincare technology, and more specifically, to compositions that enhance the transdermal absorption of hydroxytyrosol, their preparation methods, and skincare products thereof. Background Technology

[0002] Oxidation is the biggest threat to skin aging, typically manifesting as yellowing, dryness, wrinkles, dullness, and age spots. In daily life, many substances accelerate skin cell oxidation, such as cell phone radiation, electromagnetic waves, ultraviolet rays, air pollution, fried foods, and stress. Therefore, to achieve truly healthy skin care, it's essential to incorporate repair factors, or antioxidants, into skincare products to slow down skin oxidation.

[0003] Hydroxytyrosol (HT), also known as 3,4-dihydroxyphenylethanol, is a natural small-molecule phenolic compound, mainly found in the fruit and leaves of olives in ester form. It is considered one of the most powerful antioxidants, and also possesses various biological and pharmacological activities such as anticancer, antithrombotic, lipid-regulating, anti-atherosclerotic, antimicrobial, anti-aging, cartilage protection, and anti-osteoporosis effects. It is a natural product with significant application development value and can be widely used in medicine, food, daily chemicals, and animal feed. The antioxidant properties of hydroxytyrosol are primarily due to its phenolic hydroxyl groups acting as hydrogen donors, scavenging various reactive oxygen species. It can reduce singlet oxygen to less reactive triplet oxygen, reducing the likelihood of oxygen free radical generation. Furthermore, the less reactive polyphenolic free radicals generated by hydroxytyrosol through its reaction can also scavenge various free radicals, thus breaking the chain reaction of free radical oxidation. In addition, the two ortho- and posterior phenolic hydroxyl groups of hydroxytyrosol can chelate metal ions, reducing the chance of metal ion-catalyzed oxidation reactions.

[0004] Hydroxytyrosol and its derivatives typically exhibit amphiphilic properties, making them readily soluble in both water and oily substances. This surfactant-like characteristic, coupled with its strong antioxidant properties, facilitates the application of hydroxytyrosol in pharmaceutical and skincare formulations. However, in practical applications, the transdermal absorption performance of hydroxytyrosol and its derivatives is not ideal. For example, in an in vitro transdermal absorption study of hydroxytyrosol and other natural products such as bisabolol, researchers such as Cristina Alonso found that the in vitro transdermal absorption performance of hydroxytyrosol was lower than that of bisabolol, which is insoluble in water and glycerin, with an absorption rate (%) of only 2.98 ± 1.12. This study also indicated that the transdermal absorption performance of hydroxytyrosol ester derivatives was significantly lower than that of bisabolol ester derivatives, which will greatly reduce the likelihood of its application in topical formulations in the pharmaceutical or cosmetic industries.

[0005] The low transdermal absorption of hydroxytyrosol has significantly hindered its application in the pharmaceutical and daily chemical industries. Therefore, to enhance the application value of hydroxytyrosol and maximize its excellent biological activity, a technological method to improve its transdermal absorption is urgently needed.

[0006] In view of this, the present invention is proposed. Summary of the Invention

[0007] The purpose of this invention is to provide compositions, methods for their preparation, and skincare products that enhance the transdermal absorption of hydroxytyrosol. The compounds provided in the embodiments of this invention can improve the transdermal absorption of hydroxytyrosol and maximize its bioactivity.

[0008] This invention is implemented as follows:

[0009] In a first aspect, the present invention provides a composition for enhancing the transdermal absorption performance of hydroxytyrosol, wherein, by weight, the raw materials include 0.1-1.0 parts of hydroxytyrosol, 0.1-2.0 parts of ceramide substances and 0.1-5.0 parts of squalane.

[0010] In an optional embodiment, the hydroxytyrosol is 0.5-1.0 parts by weight;

[0011] Preferably, the ceramide substance is present in an amount of 0.5-1.0 parts;

[0012] Preferably, the squalane is 1.0-3.0 parts.

[0013] In an optional embodiment, the ceramide substance is selected from at least one of ceramide NP and ceramide 3B.

[0014] Secondly, the present invention provides a complex for enhancing the transdermal absorption performance of hydroxytyrosol, the raw materials of which include the composition for enhancing the transdermal absorption performance of hydroxytyrosol described in any of the foregoing embodiments.

[0015] In optional embodiments, the raw materials also include at least one of a humectant, an emulsifier, a pH adjuster, a matrix, and water.

[0016] In an optional embodiment, the raw materials, by mass percentage, include 0.1-1.0% hydroxytyrosol, 0.1-2.0% ceramides, 0.1-5.0% squalane, 0.1-3.0% humectant, 0.1-2.0% emulsifier, 0.05-0.1% pH adjuster, with the remainder being a matrix or water.

[0017] In an optional embodiment, the hydroxytyrosol is 0.5-1.0% by mass;

[0018] Preferably, the ceramide substance is 0.5-1.0%;

[0019] Preferably, the squalane content is 1.0-3.0%;

[0020] Preferably, the humectant is 1.0-2.0%;

[0021] Preferably, the emulsifier is 1.0-2.0%.

[0022] In an optional embodiment, the moisturizer is selected from one or more mixtures of hydrolyzed hyaluronic acid and its salts, acetylated hyaluronic acid and its salts;

[0023] The emulsifier is selected from one or more mixtures of rhamnolipin, sophorolipid, and mannosyl erythritol ester;

[0024] The pH adjuster is selected from citric acid and / or triethylamine.

[0025] Thirdly, the present invention provides a method for preparing the complex for enhancing the transdermal absorption performance of hydroxytyrosol as described in the foregoing embodiments, comprising: mixing raw materials to form the complex;

[0026] Preferably, it includes: mixing a ceramide-like substance, squalane, and an emulsifier to form an aqueous phase;

[0027] Hydroxytyrosol, humectant, pH adjuster and matrix or water are mixed to form an oil phase;

[0028] Mix the oil phase and the aqueous phase;

[0029] Preferably, the temperature at which the oil phase is formed is 50-60°C; the temperature at which the water phase is formed is 50-60°C.

[0030] Preferably, the step of mixing the oil phase and the aqueous phase includes: adding the oil phase dropwise to the aqueous phase at 50-60°C, and then homogenizing at 2000-5000 rpm for 10-20 minutes.

[0031] Fourthly, the present invention provides a skin care product comprising the composition for enhancing the transdermal absorption performance of hydroxytyrosol as described in any of the foregoing embodiments or the complex for enhancing the transdermal absorption performance of hydroxytyrosol as described in any of the foregoing embodiments.

[0032] Preferably, the skin care product includes any one of cream, gel, patch, spray, ointment, plaster, lotion, liniment, paste, and mud dressing.

[0033] The present invention has the following beneficial effects: The composition provided in the embodiments of the present invention not only improves the transdermal absorption performance of hydroxytyrosol and maximizes its biological activity, but also has a strong antioxidant effect on the skin, effectively reducing the occurrence of various skin diseases. Furthermore, the components of this composition are primarily natural products, unlikely to cause harm to the human body, environmentally friendly, mild and non-irritating, and have a wide range of applications. Detailed Implementation

[0034] To make the objectives, technical solutions, and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below. Where specific conditions are not specified in the embodiments, conventional conditions or conditions recommended by the manufacturer shall apply. Reagents or instruments whose manufacturers are not specified are all conventional products that can be purchased commercially.

[0035] In a first aspect, the present invention provides a composition for enhancing the transdermal absorption performance of hydroxytyrosol, wherein, by weight, the raw materials include 0.1-1.0 parts of hydroxytyrosol, 0.1-2.0 parts of ceramide substances and 0.1-5.0 parts of squalane.

[0036] The composition provided in this invention improves the transdermal absorption performance of hydroxytyrosol, maximizing its bioactivity. Secondly, this composition uses hydroxytyrosol as the main raw material, leveraging its excellent antioxidant, anti-inflammatory, and antibacterial activities; it is supplemented with ceramides and squalane. Ceramides, as a major component of the human stratum corneum, can penetrate deep into all layers of the epidermis, enhancing the absorption of other auxiliary active ingredients and delivering them into the cells of each epidermal layer to exert their effects. Squalane, as a lipid compound, can maintain the skin's moisture balance and form a protective barrier, further expanding the efficacy of the composition.

[0037] For example, by weight, the hydroxytyrosol is any value between 0.1 and 1.0 parts or any range between any two values, such as 0.1 parts, 0.2 parts, 0.3 parts, 0.4 parts, 0.5 parts, 0.6 parts, 0.7 parts, 0.8 parts, 0.9 parts, and 1.0 parts, preferably 0.5 to 1.0 parts.

[0038] The ceramide substance is any value between 0.1 and 2.0 parts, or any range between any two values, such as 0.1 parts, 0.5 parts, 1.0 parts, 1.5 parts, and 2.0 parts, preferably 0.5 to 1.0 parts.

[0039] The squalane is any value between 0.1 and 5.0 parts, or any range between any two values, such as 0.1 parts, 0.5 parts, 1.0 parts, 1.5 parts, 2.0 parts, 2.5 parts, 3.0 parts, 3.5 parts, 4.0 parts, 4.5 parts, and 5.0 parts, preferably 1.0 to 3.0 parts.

[0040] Preferably, the ceramide substances include, but are not limited to, at least one of ceramide NP and ceramide 3B.

[0041] Secondly, the present invention provides a complex for enhancing the transdermal absorption performance of hydroxytyrosol, the raw materials of which include the composition for enhancing the transdermal absorption performance of hydroxytyrosol as described in any of the foregoing embodiments. The raw materials may further include at least one of a humectant, emulsifier, pH adjuster, matrix, and water.

[0042] Specifically, the hydroxytyrosol content, by mass percentage, is 0.1-1.0%, for example, any value between 0.1-1.0% or any range between any two values, such as 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, and 1.0%, preferably 0.5-1.0%.

[0043] The ceramide substance is 0.1-2.0%, for example, any value between 0.1-2.0% or any range between any two values, such as 0.1%, 0.5%, 1.0%, 1.5%, and 2.0%, preferably 0.5-1.0%. The ceramide substance includes, but is not limited to, ceramide NP.

[0044] The squalane content is 0.1-5%, for example, any value between 0.1-5.0% or any range between any two values, such as 0.1%, 0.5%, 1.0%, 1.5%, 2.0%, 2.5%, 3.0%, 3.5%, 4.0%, 4.5%, and 5.0%, preferably 1.0-3.0%.

[0045] The humectant is 0.1-3.0%, preferably any value or range between any two values ​​from 0.1% to 3.0%, such as 0.1%, 0.5%, 1.0%, 1.5%, 2.0%, 2.5%, and 3.0%, and most preferably 1.0-2.0%. The humectant is selected from existing humectants with moisturizing effects that can be used in daily chemical products, including but not limited to one or more mixtures of hydrolyzed hyaluronic acid and its salts, acetylated hyaluronic acid and its salts.

[0046] The emulsifier is 0.1-2.0%, for example, any value between 0.1% and 2.0%, or a range between any two values, such as 0.1%, 0.5%, 1.0%, 1.5%, and 2.0%, preferably 1.0-2.0%. The emulsifier is selected from existing emulsifiers with emulsifying functions that can be used in daily chemical products, including but not limited to one or more mixtures of rhamnolipids, sophorolipids, and mannosyl erythritol esters.

[0047] pH adjusters are 0.05-0.1%, for example, any value or range between 0.05-0.1%, such as 0.05%, 0.06%, 0.07%, 0.08%, 0.09%, and 0.1%. These pH adjusters are substances known in the prior art that can adjust pH and can be used in the field of daily chemical products, including but not limited to one of citric acid and triethylamine.

[0048] The remaining amount is selected from active ingredients added to correspond to different effects. These active ingredients should not affect the transdermal absorption performance of hydroxytyrosol or the performance of the composition, and should be one or more of the commonly used bases, deionized water, purified water, and distilled water for cosmetic topical formulations.

[0049] Thirdly, the present invention provides a method for preparing the complex for enhancing the transdermal absorption performance of hydroxytyrosol as described in the foregoing embodiments, comprising: mixing raw materials to form the complex.

[0050] Specifically, the materials are allocated into aqueous phase raw materials and oil phase raw materials according to the following table:

[0051]

[0052] The process involves dissolving the raw material that forms the oil phase in a water bath at 50℃-60℃ to obtain a mixed oil phase for later use; and dissolving the raw material that forms the aqueous phase in distilled water in a water bath at 50℃-60℃ to obtain a mixed aqueous phase.

[0053] The oil phase was added dropwise to the mixed aqueous phase while stirring at 50℃-60℃, and then homogenized using a high-speed stirring mill disperser at a speed of 2000rpm-4500rpm for 10min-20min, and 3-5 cycles were performed.

[0054] The homogenized solution was allowed to stand at room temperature for 5-10 minutes to obtain a complex solution with improved transdermal absorption of hydroxytyrosol.

[0055] Fourthly, the present invention provides a skin care product comprising a composition for enhancing the transdermal absorption performance of hydroxytyrosol as described in any of the foregoing embodiments, or a complex for enhancing the transdermal absorption performance of hydroxytyrosol as described in any of the foregoing embodiments; wherein the skin care product includes, but is not limited to, any one of creams, gels, patches, sprays, ointments, plasters, lotions, liniments, pastes, and mud masks.

[0056] The composite provided in this invention does not introduce harmful substances during its preparation process, is produced in a green and environmentally friendly manner, and has a simple preparation process and low cost.

[0057] The features and performance of the present invention will be further described in detail below with reference to embodiments.

[0058] Example 1

[0059] This invention provides a composition for improving the transdermal absorption of hydroxytyrosol, the raw materials of which include hydroxytyrosol, ceramide NP and squalane, wherein the mass ratio of hydroxytyrosol, ceramide NP and squalane is 1:1:1.

[0060] This invention provides a complex that enhances the transdermal absorption of hydroxytyrosol, the components of which are as follows:

[0061] 1.0% hydroxytyrosol, 1.0% ceramide NP, 1.0% squalane, 2.0% hydrolyzed hyaluronic acid, 1.5% rhamnolipid, 0.05% citric acid, and the balance being deionized water.

[0062] This invention provides a method for preparing a complex that enhances the transdermal absorption of hydroxytyrosol, comprising:

[0063] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0064] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0065]

[0066]

[0067] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a 60°C water bath to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a 60°C water bath to obtain a mixed aqueous phase.

[0068] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 60°C, and then homogenized using a high-speed stirring mill disperser at a speed of 3000 rpm for a homogenization time of 15 min, and 4 cycles are performed.

[0069] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 10 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0070] Example 2

[0071] This invention provides a composition for improving the transdermal absorption of hydroxytyrosol, the raw materials of which include hydroxytyrosol, ceramide NP and squalane, wherein the mass ratio of hydroxytyrosol, ceramide NP and squalane is 1:1.5:3.

[0072] This invention provides a complex that enhances the transdermal absorption of hydroxytyrosol, the components of which are as follows:

[0073] 1.0% hydroxytyrosol, 1.5% ceramide NP, 3.0% squalane, 1.0% acetylated hyaluronic acid, 2.0% sophorolipid, 0.05% triethanolamine, and the balance being deionized water.

[0074] This invention provides a method for preparing a complex that enhances the transdermal absorption of hydroxytyrosol, comprising:

[0075] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0076] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0077]

[0078] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a 50°C water bath to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a 50°C water bath to obtain a mixed aqueous phase.

[0079] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 50°C, and then homogenized using a high-speed stirring mill disperser at a speed of 4500 rpm for a homogenization time of 10 min, and 3 cycles are performed.

[0080] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 8 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0081] Example 3

[0082] This invention provides a composition for improving the transdermal absorption of hydroxytyrosol, the raw materials of which include hydroxytyrosol, ceramide NP and squalane, wherein the mass ratio of hydroxytyrosol, ceramide NP and squalane is 0.5:1:1.

[0083] This invention provides a complex that enhances the transdermal absorption of hydroxytyrosol, the components of which are as follows:

[0084] 0.5% hydroxytyrosol, 1.0% ceramide NP, 1.0% squalane, 3.0% hydrolyzed sodium hyaluronate, 0.5% rhamnolipid, 1.0% mannosyl erythritol ester, 0.05% citric acid, and the balance being deionized water.

[0085] This invention provides a method for preparing a complex that enhances the transdermal absorption of hydroxytyrosol, comprising:

[0086] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0087] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0088]

[0089] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a water bath at 55°C to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a water bath at 55°C to obtain a mixed aqueous phase.

[0090] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 55°C, and then homogenized using a high-speed stirring mill disperser at a speed of 2000 rpm for a homogenization time of 20 min, and 5 cycles are performed.

[0091] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 10 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0092] Example 4

[0093] This invention provides a composition for improving the transdermal absorption of hydroxytyrosol, the raw materials of which include hydroxytyrosol, ceramide NP and squalane, wherein the mass ratio of hydroxytyrosol, ceramide NP and squalane is 1:2:5.

[0094] This invention provides a complex that enhances the transdermal absorption of hydroxytyrosol, the components of which are as follows:

[0095] 1.0% hydroxytyrosol, 2.0% ceramide NP, 5.0% squalane, 0.5% hydrolyzed hyaluronic acid, 0.5% hydrolyzed sodium hyaluronate, 1.0% sophorolipid, 1.0% mannosyl erythritol ester, 0.1% triethanolamine, and the balance being deionized water.

[0096] This invention provides a method for preparing a complex that enhances the transdermal absorption of hydroxytyrosol, comprising:

[0097] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0098] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0099]

[0100] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a water bath at 50℃-60℃ to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a water bath at 50℃-60℃ to obtain a mixed aqueous phase.

[0101] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 50℃-60℃, and then homogenized using a high-speed stirring mill disperser at a speed of 2000rpm-4500rpm. The homogenization time is set to 10min-20min, and 3-5 cycles are performed.

[0102] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 5 min-10 min to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0103] Example 5

[0104] This invention provides a composition for improving the transdermal absorption of hydroxytyrosol, the raw materials of which include hydroxytyrosol, ceramide NP and squalane, wherein the mass ratio of hydroxytyrosol, ceramide NP and squalane is 1:1.5:4.

[0105] This invention provides a complex that enhances the transdermal absorption of hydroxytyrosol, the components of which are as follows:

[0106] 1.0% hydroxytyrosol, 1.5% ceramide NP, 4.0% squalane, 0.3% acetylated sodium hyaluronate, 1.2% hydrolyzed hyaluronic acid, 1.0% sophorolipid, 1.0% rhamnolipid, 0.05% citric acid, and the balance being deionized water.

[0107] This invention provides a method for preparing a complex that enhances the transdermal absorption of hydroxytyrosol, comprising:

[0108] (1) Weigh out the raw materials of the above mass percentages, with 100g as the total mass of the raw materials forming the complex.

[0109] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0110]

[0111]

[0112] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a 60°C water bath to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a 60°C water bath to obtain a mixed aqueous phase.

[0113] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 60°C, and then homogenized using a high-speed stirring mill disperser at a speed of 3500 rpm for a homogenization time of 15 min, and 4 cycles are performed.

[0114] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 10 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0115] Comparative Example 1

[0116] This comparative example provides a complex that, compared to Example 1, lacks the addition of ceramide NP. Specifically, the preparation steps of the complex in this comparative example are as follows:

[0117] (1) Weigh out the following raw materials in the mass percentages, with a total mass of 100g as the total mass of the raw materials forming the complex. Specifically, 1.0% hydroxytyrosol, 1.0% squalane, 2.0% hydrolyzed hyaluronic acid, 1.5% rhamnolipid, 0.05% citric acid, and the balance being deionized water.

[0118] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0119]

[0120] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a 60°C water bath to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a 60°C water bath to obtain a mixed aqueous phase.

[0121] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 60°C, and then homogenized using a high-speed stirring mill disperser at a speed of 3000 rpm for a homogenization time of 15 min, and 4 cycles are performed.

[0122] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 10 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0123] Comparative Example 2

[0124] This comparative example provides a complex that, compared to Example 1, lacks the addition of squalane. Specifically, the preparation steps of the complex in this comparative example are as follows:

[0125] (1) Weigh out the following raw materials in the mass percentages, with a total mass of 100g as the total mass of the raw materials forming the complex. Specifically, 1.0% hydroxytyrosol, 1.0% ceramide NP, 2.0% hydrolyzed hyaluronic acid, 1.5% rhamnolipid, 0.05% citric acid, and the balance being deionized water.

[0126] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0127]

[0128] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a 60°C water bath to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a 60°C water bath to obtain a mixed aqueous phase.

[0129] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 60°C, and then homogenized using a high-speed stirring mill disperser at a speed of 3000 rpm for a homogenization time of 15 min, and 4 cycles are performed.

[0130] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 10 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0131] Comparative Example 3

[0132] This comparative example provides a complex that, compared to Example 5, lacks the addition of squalane and contains an excess of ceramide NP. Specifically, the preparation steps of the complex in this comparative example are as follows:

[0133] (1) Weigh out the following raw materials in the mass percentages, with a total mass of 100g as the total mass of the raw materials forming the complex. Specifically, 1.0% hydroxytyrosol, 5.5% ceramide NP, 0.3% acetylated sodium hyaluronate, 1.2% hydrolyzed hyaluronic acid, 1.0% sophorolipid, 1.0% rhamnolipid, 0.05% citric acid, and the balance being deionized water.

[0134] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0135]

[0136] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a 60°C water bath to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a 60°C water bath to obtain a mixed aqueous phase.

[0137] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 60°C, and then homogenized using a high-speed stirring mill disperser at a speed of 3500 rpm for a homogenization time of 15 min, and 4 cycles are performed.

[0138] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 10 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0139] Comparative Example 4

[0140] This comparative example provides a complex that, compared to Example 5, lacks squalane and ceramide NP. Specifically, the preparation steps of the complex in this comparative example are as follows:

[0141] (1) Weigh out the following raw materials in the mass percentages, with a total mass of 100g as the total mass of the raw materials forming the complex. Specifically, 1.0% hydroxytyrosol, 0.3% acetylated sodium hyaluronate, 1.2% hydrolyzed hyaluronic acid, 1.0% sophorolipid, 1.0% rhamnolipid, 0.05% citric acid, and the balance being deionized water.

[0142] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0143]

[0144] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a 60°C water bath to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a 60°C water bath to obtain a mixed aqueous phase.

[0145] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 60°C, and then homogenized using a high-speed stirring mill disperser at a speed of 3500 rpm for a homogenization time of 15 min, and 4 cycles are performed.

[0146] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 10 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0147] Comparative Example 5

[0148] This comparative example provides a complex that, compared to Example 5, has an additional 2.0% of the humectant betaine. Specifically, the preparation steps of the complex in this comparative example are as follows:

[0149] (1) Weigh out the following raw materials in the mass percentages, with a total mass of 100g as the total mass of the raw materials forming the complex. Specifically, 1.0% hydroxytyrosol, 1.5% ceramide NP, 4.0% squalane, 0.3% acetylated sodium hyaluronate, 1.2% hydrolyzed hyaluronic acid, 1.0% sophorolipid, 1.0% rhamnolipid, 0.05% citric acid, 2.0% betaine, and the balance being deionized water.

[0150] (2) The raw materials weighed in step (1) are divided into oil phase and aqueous phase according to the following table:

[0151]

[0152] The oil phase is added and mixed according to the proportions in the table above, and then stirred and dissolved in a 60°C water bath to obtain a mixed oil phase for later use; the aqueous phase is dissolved in distilled water in a 60°C water bath to obtain a mixed aqueous phase.

[0153] (3) The mixed oil phase obtained in step (2) is added dropwise to the mixed water phase while stirring at 60°C, and then homogenized using a high-speed stirring mill disperser at a speed of 3500 rpm for a homogenization time of 15 min, and 4 cycles are performed.

[0154] (4) Based on the completion of step (3), the homogenized solution is allowed to stand at room temperature for 10 minutes to finally obtain a complex solution with improved transdermal absorption performance of hydroxytyrosol.

[0155] Test Example 1: Composition Stability Test

[0156] ① Heat resistance test

[0157] Take a portion of the final solution of the composite obtained in the above examples and comparative examples as a sample, pour it into two test tubes with specifications of 20mm×120mm, and make the liquid level about 80mm. Then, stopper the tubes with clean corks. Place one of the test tubes in a constant temperature incubator that has been pre-adjusted to a specified temperature ±1℃. After 24 hours, remove the tube, allow it to return to room temperature, and then visually compare it with the sample in the other test tube.

[0158] ② Cold resistance test

[0159] Take a portion of the final solution of the composite obtained in the above examples and comparative examples as a sample, and pour it into two test tubes with specifications of 20mm×120mm, so that the liquid level is about 80mm. Then, stopper the tubes with clean corks. Place one of the test tubes to be tested in a refrigerator that has been pre-adjusted to a specified temperature ±2℃. After 24 hours, take it out, allow it to return to room temperature, and then visually compare it with the sample in the other test tube.

[0160] ③ Alternating heat and cold resistance test

[0161] After completing the heat resistance test (or cold resistance test), perform the cold resistance test (or heat resistance test) next. This is called a hot-cold cycle. Repeat this process until the tested sample shows phenomena such as oil-water separation, color change, or oil seepage. Record the number of cycles, and according to the book "7 Steps to Cosmetic Formulation Design" published by Chemical Industry Press, 7 cycles are the minimum standard for a qualified cosmetic formulation composition.

[0162] ③ Centrifugation test

[0163] Take a portion of the final solution of the complex obtained in the above examples and comparative examples as a sample, fill the centrifuge tube with the sample to about two-thirds of its height and seal it with a cork. Then place it in an electric thermostatic incubator pre-adjusted to (38±1)℃, keep it at this temperature for 1 hour, and immediately transfer it to a centrifuge and adjust the centrifugation speed to 2000 r / min. Rotate for 30 minutes and then take it out for observation.

[0164] After completing all the steps in Test Example 1 above, the experimental results are as follows:

[0165]

[0166] As can be seen from the table above, the composite provided in the embodiments of the present invention has good stability, especially the number of cycles of alternating heat and cold resistance experiments can be greater than 7, and no oil-water separation occurs during centrifugation.

[0167] Test Example 2: Transdermal Absorption Performance Test of the Composition

[0168] Based on the relevant experiments in "2.4.3 Permeation Test Step" of the literature "Experimental Study on Transdermal Absorption of Neomycin Sulfate Ointment through Rat Ex vivo Burned Skin" published by Chen Yuebin et al., the transdermal absorption of the final composites obtained in the above examples and comparative examples was measured. The measurements were performed 6 times every 10 minutes using HPLC, and the cumulative permeation of the composition was calculated. The results are as follows:

[0169]

[0170] Based on the above results, it can be seen that the transdermal absorption of hydroxytyrosol in the complex provided by the embodiments of the present invention is significantly improved, and the complex can better exert the effect of hydroxytyrosol.

[0171] Test Example 3: Antioxidant Capacity Test of the Composition

[0172] Following the experimental procedures for "DPPH free radical scavenging capacity determination" in the Chinese literature "Preparation and Antioxidant Activity Study of Hydroxytyrosol from Olive Leaves" (DOI: 10.27345 / d.cnki.gsnyu.2020.001087), the antioxidant effects of the final complexes obtained in the above examples and comparative examples were determined. The absorbance of the reaction solution was measured every 10 minutes, for a total of 3 measurements, and the DPPH free radical scavenging rate was calculated. The results are as follows:

[0173]

[0174] Based on the above results, it can be seen that the complex provided in the embodiments of the present invention has good antioxidant effect and can be used in daily chemical products to resist skin oxidation.

[0175] The above description is merely a preferred embodiment of the present invention and is not intended to limit the invention. Various modifications and variations can be made to the present invention by those skilled in the art. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the scope of protection of the present invention.

Claims

1. A complex that enhances the transdermal absorption of hydroxytyrosol, characterized in that, By mass percentage, its raw materials include 0.1-1.0% hydroxytyrosol, 0.1-2.0% ceramides, 0.1-5.0% squalane, 0.1-3.0% humectant, 0.1-2.0% emulsifier, 0.05-0.1% pH adjuster, with the remainder being matrix or water; The moisturizer is selected from one or more mixtures of hydrolyzed hyaluronic acid and its salts, acetylated hyaluronic acid and its salts; The emulsifier is selected from one or more mixtures of rhamnolipin, sophorolipid, and mannosyl erythritol ester; The pH adjuster is selected from citric acid and / or triethylamine.

2. The complex for enhancing the transdermal absorption performance of hydroxytyrosol according to claim 1, characterized in that, The hydroxytyrosol is 0.5-1.0% by mass. The ceramide substance is 0.5-1.0%; The squalane content is 1.0-3.0%; The humectant concentration is 1.0-2.0%; The emulsifier is 1.0-2.0%.

3. A method for preparing the complex for enhancing the transdermal absorption performance of hydroxytyrosol as described in claim 1, characterized in that, include: The raw materials are mixed to form the complex.

4. The preparation method according to claim 3, characterized in that, include: Ceramides, squalane, and emulsifiers are mixed to form an oil phase; Hydroxytyrosol, humectant, pH adjuster and matrix or water are mixed to form an aqueous phase; Mix the oil phase and the water phase.

5. The preparation method according to claim 4, characterized in that, The temperature at which the oil phase forms is 50-60℃; the temperature at which the water phase forms is 50-60℃. The steps for mixing the oil phase and the aqueous phase include: adding the oil phase dropwise to the aqueous phase at 50-60°C, and then homogenizing at 2000-5000 rpm for 10-20 minutes.

6. A skincare product, characterized in that, It includes the complex described in claim 1 or 2 that enhances the transdermal absorption of hydroxytyrosol.

7. The skincare product according to claim 6, characterized in that, The skin care products include any one of creams, gels, patches, sprays, ointments, plasters, lotions, liniments, pastes, and mud masks.

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