A skin barrier repair-enhancing composition and its application

Abstract

This invention discloses a skin barrier repair-enhancing composition and its application. The composition comprises the following raw materials in parts by weight: 20-70 parts meadowfoam seed oil, 29-79 parts squalane, and 0.1-2 parts phytol. This invention, by mixing meadowfoam seed oil, squalane, and phytol in a specific ratio, achieves a gentle penetration-enhancing effect while maintaining good permeability and providing a certain degree of repair to the skin barrier.

Description

Technical Field

[0001] This invention relates to the field of cosmetic technology for skin barrier repair, and more specifically, to a penetration-enhancing composition with skin barrier repair function and its application. Background Technology

[0002] The outermost layer of the skin is the stratum corneum, which is composed of corneocytes and intercellular lipids, forming a "brick-and-mortar" structure and serving as the main barrier restricting the penetration of substances. Molecules can enter the skin through the following main pathways:

[0003] 1. Cellular pathway: Molecules directly cross keratinocytes. This pathway requires crossing alternating structures of hydrophilic cytoplasm and hydrophobic cell membranes. It places high demands on the physicochemical properties of the molecules and is generally suitable for small molecules that have a certain degree of lipophilicity / hydrophilicity.

[0004] 2. Intercellular pathway: Active molecules diffuse along lipid channels between keratinocytes. Because the lipid layer has a highly ordered layered structure, most lipophilic substances can penetrate more easily along this pathway.

[0005] 3. Accessory pathways: These include accessory structures such as hair follicles, sebaceous glands, and sweat glands. Although these pathways account for less than 0.1% of the skin surface area, they provide alternative pathways for macromolecules or particulate substances due to their relatively weak barrier function.

[0006] These three pathways work together to determine the penetration efficiency and site of different active molecules. Understanding and rationally utilizing these pathways is the theoretical basis for designing penetration-enhancing strategies.

[0007] Transdermal penetration is a crucial process for the delivery of active ingredients across the skin barrier. Research addressing the core scientific question of "how active substances overcome the skin barrier" is of paramount importance to both the daily chemical and pharmaceutical industries. Traditional penetration-enhancing methods often damage the skin barrier function, leading to irritation, erythema, and even long-term barrier dysfunction. This contradicts the fundamental requirements of "mild and safe" for daily chemical products and limits the application of transdermal formulations in chronic disease management, localized treatment, and other scenarios.

[0008] To overcome the stratum corneum barrier, existing technologies have proposed a variety of methods to enhance penetration, which can be broadly classified into three categories: physical methods, chemical methods, and biological methods.

[0009] 1. Physical methods: These include microneedles, iontophoresis, electroporation, ultrasound, and thermal effects. These methods can significantly improve drug permeability, and are especially suitable for large molecular active substances (such as peptides, proteins, and polynucleotides). However, their limitations lie in their strong equipment dependence, high cost, and the potential for barrier damage and irritation risks associated with some methods (such as microneedles and electroporation), making them difficult to widely apply in daily chemical products.

[0010] 2. Chemical methods: These mainly involve adding chemical penetration enhancers, such as surfactants, alcohols, fatty acids, terpenes, and urea derivatives. These methods are simple to operate, inexpensive, and easily integrated into formulation systems. However, a drawback is that some penetration enhancers can damage the lipids or proteins of the stratum corneum, and long-term use may lead to skin barrier damage, resulting in irritation or dryness.

[0011] 3. Biological methods: These include the use of carrier systems (liposomes, solid lipid nanoparticles, cyclodextrin inclusion complexes, etc.) and biomimetic lipid or peptide penetration enhancers. The advantage of these methods lies in their relative gentleness, balancing safety and targeting; some systems can also synergistically exert moisturizing or repairing effects. However, the stability of the carrier system, raw material costs, and process complexity remain challenges to their industrialization.

[0012] In summary, existing penetration enhancement technologies each have their advantages, but they generally face a contradiction between penetration efficiency and skin barrier safety.

[0013] Therefore, there is an urgent need to provide a penetration-enhancing composition that can significantly improve the transdermal delivery efficiency of active ingredients without damaging the skin's natural barrier function, and can even support barrier repair to a certain extent. Summary of the Invention

[0014] In view of this, the present invention provides a penetration-enhancing composition that can significantly improve the transdermal delivery efficiency of active ingredients without damaging the skin's natural barrier function, and can even support barrier repair to a certain extent.

[0015] On the one hand, a penetration-enhancing composition with skin barrier repair function includes the following raw materials in parts by weight: 20-70 parts of meadowfoam seed oil, 29-79 parts of squalane, and 0.1-2 parts of phytol;

[0016] The penetration-enhancing composition is prepared according to the following method:

[0017] Take the above-mentioned parts by weight of meadowfoam seed oil, squalane, and phytol;

[0018] Add to a beaker and stir at 200 rpm for 10 minutes to obtain the permeation-enhancing composition.

[0019] Optional ingredients may include the following parts by weight: 50-70 parts meadowfoam seed oil, 29-49 parts squalane, and 0.1-1 parts phytol.

[0020] On the other hand, the present invention also provides the application of the above-mentioned penetration-enhancing composition with skin barrier repair function in the preparation of a product for enhancing penetration and repairing the skin barrier, wherein the product further includes coenzyme Q10 or vitamin E acetate.

[0021] Optionally, the content of coenzyme Q10 is 0.5% based on the mass of the product (100%).

[0022] Optionally, the content of the vitamin E acetate is 0.5%.

[0023] Compared with the prior art, the penetration-enhancing composition and its application with skin barrier repair function provided by the present invention achieve at least the following beneficial effects:

[0024] This invention presents a composition of meadowfoam seed oil, squalane, and phytol mixed in a specific ratio. While ensuring permeability, it also has a certain repairing effect on the skin barrier, achieving a gentle method of promoting penetration.

[0025] Phytol is a long-chain, non-cyclic diterpenoid alcohol (C 20 H 40 Phytol (O), containing an unsaturated double bond and a hydroxyl group, is a small molecule with permeation-enhancing properties. It does have certain research and application value in the field of transdermal permeation enhancement, but its mechanism differs from common chemical permeation enhancers (such as alcohols, surfactants, and terpenes), exhibiting strong hydrophobicity and the ability to intercalate within the lipid bilayer. The stratum corneum barrier mainly relies on the "intercellular lipid bilayer," in which cholesterol, fatty acids, and ceramides are key components. Phytol can partially replace cholesterol, embedding itself within the skin's lipid bilayer, thereby altering its order and fluidity. Phytol can intercalate and perturb the lipid arrangement of the stratum corneum, causing the lipid bilayer to transform from a highly ordered crystalline form to a more loosely liquid crystal form, thus increasing the diffusion rate of small molecules. This mechanism and structural characteristics determine that phytol has a relatively mild advantage compared to other chemical permeation enhancers. However, its perturbation of the lipid layer structure of the skin barrier also poses a certain risk of irritation. In this invention, phytol is used in combination with meadowfoam seed oil and squalane. While achieving penetration, it also has a certain damaging effect on the skin barrier. Surprisingly, it was found that when meadowfoam seed oil, squalane, and phytol are mixed in a specific ratio, they simultaneously maintain permeability and also have a certain repairing effect on the skin barrier. This invention plays a very important role in the development of gentle penetration-enhancing methods.

[0026] Of course, any product implementing this invention does not necessarily need to achieve all of the technical effects described above at the same time.

[0027] Other features and advantages of the invention will become clear from the following detailed description of exemplary embodiments of the invention with reference to the accompanying drawings. Attached Figure Description

[0028] The accompanying drawings, which are incorporated in and form part of this specification, illustrate embodiments of the invention and, together with their description, serve to explain the principles of the invention.

[0029] Figure 1This is a flowchart of a method for preparing a penetration-enhancing composition with skin barrier repair function provided by the present invention;

[0030] Figure 2 This is the infrared spectrum corresponding to sample 3;

[0031] Figure 3 It is 2855 cm of samples 1 to 9. -1 The graph showing the change of normalized intensity corresponding to the characteristic peak over time;

[0032] Figure 4 These are micro Raman permeation data of coenzyme Q10 in pig skin in samples 10 and 11;

[0033] Figure 5 These are micro Raman permeation data of vitamin E acetate in pigskin in samples 12 and 13. Detailed Implementation

[0034] Various exemplary embodiments of the present invention will now be described in detail with reference to the accompanying drawings. It should be noted that, unless otherwise specifically stated, the relative arrangement, numerical expressions, and values ​​of the components and steps set forth in these embodiments do not limit the scope of the invention.

[0035] The following description of at least one exemplary embodiment is merely illustrative and is in no way intended to limit the invention or its application or use.

[0036] Techniques, methods, and equipment known to those skilled in the art may not be discussed in detail, but where appropriate, such techniques, methods, and equipment should be considered part of the specification.

[0037] In all the examples shown and discussed herein, any specific values ​​should be interpreted as merely exemplary and not as limitations. Therefore, other examples of exemplary embodiments may have different values.

[0038] It should be noted that similar labels and letters in the following figures indicate similar items; therefore, once an item is defined in one figure, it does not need to be discussed further in subsequent figures.

[0039] Meadowfoam seed oil is a plant oil extracted from the seeds of meadowfoam (scientific name: Limnanthes alba). More than 97% of its fatty acids are C20-C22 long-chain fatty acids. It contains phytosterols and meadowfoam oligolactone, which can replenish the lipids needed for the skin barrier and promote the repair of the stratum corneum.

[0040] Squalane is a hydrocarbon oil derived from the hydrogenation of squalene extracted from the liver of deep-sea sharks. Also known as deep-sea shark liver oil, squalane is formed by the hydrogenation of squalene (a highly unsaturated hydrocarbon compound). Its fully saturated hydrocarbon structure gives it extremely high chemical stability, making it resistant to oxidation and deterioration. It can form a breathable, moisture-locking film on the skin's surface, preventing moisture evaporation while promoting the skin's absorption of moisture and nutrients.

[0041] Phytol is a long-chain, non-cyclic diterpenoid alcohol (C 20 H 40 Phytol (O), containing an unsaturated double bond and a hydroxyl group, is a small molecule with permeation-enhancing properties. It does have certain research and application value in the field of transdermal permeation enhancement, but its mechanism differs from common chemical permeation enhancers (such as alcohols, surfactants, and terpenes), exhibiting strong hydrophobicity and the ability to intercalate within the lipid bilayer. The stratum corneum barrier mainly relies on the "intercellular lipid bilayer," in which cholesterol, fatty acids, and ceramides are key components. Phytol can partially replace cholesterol, embedding itself within the skin's lipid bilayer, thereby altering its order and fluidity. Phytol can intercalate and perturb the lipid arrangement of the stratum corneum, causing the lipid bilayer to transform from a highly ordered crystalline form to a more loosely liquid crystal form, thus increasing the diffusion rate of small molecules. This mechanism and structural characteristics determine that phytol has a relatively mild advantage compared to other chemical permeation enhancers. However, its perturbation of the lipid layer structure of the skin barrier also poses a certain risk of irritation.

[0042] This invention provides a method for preparing a penetration-enhancing composition with skin barrier repair function:

[0043] S1, take parts by weight of meadowfoam seed oil, squalane and the phytol;

[0044] Add S2 to a beaker and stir at 200 rpm for 10 minutes to obtain the permeation-enhancing composition.

[0045] The present invention prepares the following sample examples according to the above method:

[0046] Sample 1: Take 99 parts squalane and 1 part phytol, add them to a beaker, and stir at 200 rpm for 10 minutes.

[0047] Sample 2: Take 20 parts meadowfoam seed oil, 79 parts squalane, and 1 part phytol. Add all three to a beaker and stir at 200 rpm for 10 minutes.

[0048] Sample 3: Take 40 parts meadowfoam seed oil, 59 parts squalane, and 1 part phytol. Add all three to a beaker and stir at 200 rpm for 10 minutes.

[0049] Sample 4: Take 50 parts meadowfoam seed oil, 49 parts squalane, and 1 part phytol. Add all three to a beaker and stir at 200 rpm for 10 minutes.

[0050] Sample 5: Take 70 parts meadowfoam seed oil, 29 parts squalane, and 1 part phytol. Add all three to a beaker and stir at 200 rpm for 10 minutes.

[0051] Sample 6: Take 80 parts meadowfoam seed oil, 19 parts squalane, and 1 part phytol. Add all three to a beaker and stir at 200 rpm for 10 minutes.

[0052] Sample 7: Take 99 parts meadowfoam seed oil and 1 part phytol, add them to a beaker, and stir at 200 rpm for 10 minutes.

[0053] Sample 8: Take 50 parts meadowfoam seed oil, 49.9 parts squalane, and 0.1 parts phytol. Add the three to a beaker and stir at 200 rpm for 10 minutes.

[0054] Sample 9: Take 50 parts meadowfoam seed oil, 48 parts squalane, and 2 parts phytol. Add all three to a beaker and stir at 200 rpm for 10 minutes.

[0055] Table 1. Formulation ratio of oil samples

[0056] meadowfoam seed oil (%) Squalane (%) Phytosterol (%) Sample 1 99 1 Sample 2 20 79 1 Sample 3 40 59 1 Sample 4 50 49 1 Sample 5 70 29 1 Sample 6 80 19 1 Sample 7 99 0 1 Sample 8 50 49．9 0.1 Sample 9 50 48 2

[0057] Cut the pigskin into 1-square-centimeter squares. Take 30g of oil sample and immerse 9 pieces of pigskin in each sample (samples 1-9). Before each test, remove the pigskin from the oil. Carefully wipe away any remaining oil stains. Perform infrared testing.

[0058] It should be noted that the meadowfoam seed oil was purchased from Huatu Technology, the squalane from Yichun Sea Turtle, the phytol from BASF, and the pigskin from Chongqing Meisheng Trading Co., Ltd.

[0059] Select sample 3 for infrared testing. The infrared spectrum is shown below (e.g.) Figure 2 ), 2855 cm -1 The peaks were lipid-ordered, and the soaking time of pigskin in sample 3 increased with the extension of the soaking time. Figure 2 (0h corresponds to 0 hours of soaking, 1h corresponds to 1 hour of soaking, 2h corresponds to 2 hours of soaking, 4h corresponds to 4 hours of soaking) 2855 cm -1 The peak intensity gradually increases, indicating a gradual increase in the lipid order of the pigskin. This increased lipid order represents a gradual increase in the molecular order of the skin barrier, thus enhancing the skin barrier function.

[0060] Samples 1 through 9 were tested according to the above method, and 2855cm was used.-1 The corresponding characteristic peaks are integrated, and the peak intensities are normalized. The changes in peak intensity over time are plotted on [the graph]. Figure 3 In the middle, by Figure 3 It can be known that:

[0061] As time increased, the peak intensity of Sample 1 showed a trend of first increasing and then decreasing. This means that after the pigskin was soaked in the essential oil of Sample 1, the barrier order first increased and then decreased with prolonged soaking time.

[0062] The peak intensity of Sample 2 increased over time. This indicates that after soaking in the essential oil of Sample 2, the barrier order of the pigskin increased over time.

[0063] The peak intensity of Sample 3 increased over time. This indicates that after soaking in the essential oil of Sample 3, the barrier order of the pigskin increased over time.

[0064] The peak intensity of Sample 4 increased over time. This indicates that after soaking in the essential oil of Sample 4, the barrier order of the pigskin increased over time.

[0065] The peak intensity of Sample 5 increased over time. This indicates that after soaking in the essential oil of Sample 5, the barrier order of the pigskin increased over time.

[0066] For Sample 6, the peak intensity initially increased and then decreased over time. This indicates that after soaking in the essential oil of Sample 6, the barrier order of the pigskin initially increased and then decreased over time.

[0067] For Sample 7, the peak intensity initially increased and then decreased over time. This indicates that after soaking in the essential oil of Sample 7, the barrier order of the pigskin initially increased and then decreased over time.

[0068] The peak intensity of sample 8 increased over time. This indicates that after soaking in the essential oil of sample 4, the barrier order of the pigskin increased over time.

[0069] The peak intensity of sample 9 increased over time. This indicates that after soaking in the essential oil of sample 4, the barrier order of the pigskin increased over time.

[0070] Therefore, in this invention, with 20-70 parts of meadowfoam seed oil, 29-79 parts of squalane, and 0.1-2 parts of phytol, the barrier order increases over time under this specific ratio.

[0071] The following are examples of applications of the penetration-enhancing composition in the preparation of products that enhance skin barrier penetration.

[0072] Samples 10 to 13 were prepared according to the following method:

[0073] For sample 10, take 60 parts of meadowfoam seed oil, 39 parts of squalane, and 0.5 parts of coenzyme Q10. Add all three to a beaker and stir at 200 rpm for 10 minutes.

[0074] Sample 11: Take 60 parts meadowfoam seed oil, 39 parts squalane, 1 part phytol, and 0.5 parts coenzyme Q10. Add all four to a beaker and stir at 200 rpm for 10 minutes.

[0075] For sample 12, take 60 parts meadowfoam seed oil, 39 parts squalane, and 0.5 parts vitamin E acetate. Add all three to a beaker and stir at 200 rpm for 10 minutes.

[0076] Sample 13: Take 60 parts meadowfoam seed oil, 39 parts squalane, 1 part phytol, and 0.5 parts vitamin E acetate. Add all four to a beaker and stir at 200 rpm for 10 minutes.

[0077] Table 2. Formulation ratios in each sample

[0078]

[0079] Microscopic Raman spectroscopy was performed on samples 10 and 11. The results showed that before application of samples 10 and 11 respectively, no coenzyme Q10 scattering signal was observed in the pigskin. However, after 1 hour, the scattering signal of coenzyme Q10 in the pigskin sample coated with sample 11 was significantly higher than that in sample 10. This indicates that the combination of meadowfoam seed oil, squalane, and phytol can significantly promote the penetration of coenzyme Q10.

[0080] It should be noted that micro Raman spectroscopy is a high-sensitivity, high-spatial-resolution spectroscopic analysis technique based on the Raman scattering effect. By detecting the frequency changes of scattered light generated by the interaction between incident laser and the vibration of molecules, it can accurately analyze the composition, structure, and relative content of substances.

[0081] Figure 4 The text indicates the Raman intensity (...). The Raman intensity at the location ranged from blue (150) to red (200). Experimental parameters included: location 16 μm, laser wavelength 532 nm, energy 3 mW, exposure frequency 2 Hz, step size 2 μm, and number of scans 3.

[0082] Microscopic Raman spectroscopy was performed on samples 12 and 13. It was found that before applying samples 12 and 13 respectively, no scattering signal of vitamin E acetate was observed in the pigskin. However, after 1 hour, the scattering signal of vitamin E acetate in the pigskin sample with sample 13 was significantly higher than that in sample 12. This indicates that the combination of meadowfoam seed oil, squalane, and phytol can significantly promote the penetration of vitamin E acetate.

[0083] In summary, when meadowfoam seed oil and squalane are mixed with phytol, they can disrupt the skin barrier's balance. However, when meadowfoam seed oil and squalane are present in a specific ratio (20:79-70:29), and combined with 0.1-2 parts of phytol, they can both enhance skin penetration and repair the skin barrier.

[0084] While specific embodiments of the invention have been described in detail by way of examples, those skilled in the art should understand that these examples are for illustrative purposes only and not intended to limit the scope of the invention. Those skilled in the art should understand that modifications can be made to the above embodiments without departing from the scope and spirit of the invention. The scope of the invention is defined by the appended claims.

Claims

1. A penetration-enhancing composition with skin barrier repair function, characterized in that, The ingredients include the following parts by weight: meadowfoam seed oil 20-70 parts, squalane 29-79 parts, phytol 0.1-2 parts; The penetration-enhancing composition is prepared according to the following method: Take the above-mentioned parts by weight of meadowfoam seed oil, squalane, and phytol; Add to a beaker and stir at 200 rpm for 10 minutes to obtain the permeation-enhancing composition.

2. The penetration-enhancing composition with skin barrier repair function according to claim 1, characterized in that, It includes the following raw materials in parts by weight: 50-70 parts meadowfoam seed oil, 29-49 parts squalane, and 0.1-1 parts phytol.

3. The use of the skin barrier repair-enhancing composition according to claims 1 to 2 in the preparation of products that enhance skin barrier repair, characterized in that, The product also includes coenzyme Q10 or vitamin E acetate.

4. The application of the penetration-enhancing composition with skin barrier repair function according to claim 3 in the preparation of products that enhance skin barrier repair, characterized in that, The product is 100% pure, and the coenzyme Q10 content is 0.5%.

5. The application of the penetration-enhancing composition with skin barrier repair function according to claim 3 in the preparation of products that enhance penetration and repair the skin barrier, characterized in that, The content of vitamin E acetate is 0.5%.

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