Cosmetic composition comprising lotus leaf extract and ferulic acid

Incorporating lotus leaf extract into cosmetic compositions with ferulic acid addresses solubility and stability issues, improving formulation stability and skin benefits.

WO2025249801A1PCT designated stage Publication Date: 2025-12-04LG HOUSEHOLD & HEALTH CARE LTD
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Patent Information

Application Number
PCT/KR2025/006518
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2025-02-17
Filing Date
2025-05-14
Publication Date
2025-12-04

AI Technical Summary

Technical Problem

Ferulic acid's low solubility and stability issues limit its use in cosmetics, leading to precipitation and skin irritation concerns, particularly at pH levels similar to human skin pH, and existing derivatives fail to maintain skin improvement effects.

Method used

Incorporating lotus leaf extract into cosmetic compositions with ferulic acid enhances solubility and stability, preventing decarboxylation and discoloration, while maintaining effective skin benefits.

Benefits of technology

The combination of lotus leaf extract and ferulic acid improves formulation stability, reduces skin irritation, and enhances moisturizing and anti-inflammatory effects compared to individual use.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present invention relates to a cosmetic composition comprising a lotus leaf extract and ferulic acid. The present invention can provide a cosmetic composition which can reduce concerns about precipitation by adding a lotus leaf extract to a composition containing ferulic acid to improve the solubility of ferulic acid and has excellent formulation stability. In addition, the composition exhibited superior moisturizing and anti-inflammatory effects compared to the use of lotus leaf extract or ferulic acid alone.
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Description

Cosmetic composition containing lotus leaf extract and ferulic acid

[0001] The present invention relates to a cosmetic composition comprising lotus leaf extract and ferulic acid.

[0002] Ferulic acid exhibits a wide range of antibacterial activities, is effective in neutralizing active oxygen, and has various effects as an external skin agent, such as antioxidant, UV protection, and skin whitening effects. Therefore, efforts are ongoing to develop cosmetics containing ferulic acid.

[0003] However, ferulic acid has very low solubility and stability, limiting its use in cosmetics. Specifically, because ferulic acid has a pKa of 4.61, there are concerns about precipitation at pH values ​​below 5. Above pH 5, ferulic acid decomposes through decarboxylation, resulting in discoloration of the formulation, decreased potency, and decreased efficacy.

[0004] Therefore, to address the issue of ferulic acid precipitation at pH values ​​below 5, attempts have been made to improve solubility and storage stability by adding glycols and nonvolatile polyols together with ferulic acid. However, the glycol content must also increase in proportion to the ferulic acid content, and excessive use of glycols poses a risk of skin irritation.

[0005] Furthermore, the pH of human skin is 5.5 to 6, but the pKa of ferulic acid is lower than this, raising concerns about skin irritation. Therefore, from a human safety perspective, there was a need to develop a product that uses a small amount of polyol while maintaining a pH similar to skin pH or that of conventional cosmetics.

[0006] At pH 5 or higher, the solubility of ferulic acid improves, reducing the amount of polyol used and alleviating concerns about skin irritation. However, at pH 5 or higher, decarboxylation of ferulic acid occurs, rapidly discoloring the composition, reducing potency and efficacy, and potentially disrupting the distribution of cosmetics.

[0007] In addition, attempts were made to improve the formulation stability of ferulic acid by derivatizing ferulic acid in the past, but these derivatives did not show the same skin improvement effect as ferulic acid, despite improving formulation stability. Therefore, a method was needed to stably include ferulic acid itself at a certain content or more, rather than derivatizing ferulic acid.

[0008] Under the above background, the inventors of the present invention conducted research to improve the stability of ferulic acid, and as a result, confirmed that adding lotus leaf extract to ferulic acid inhibits the decarboxylation decomposition reaction, thereby preventing discoloration, decrease in potency, and decrease in efficacy of the composition, thereby completing the present invention.

[0009] Accordingly, an object of the present invention is to provide a cosmetic composition comprising lotus leaf (Nelumbo NuciferaLeaf) extract and ferulic acid.

[0010] Another object of the present invention is to provide a use of a composition comprising lotus leaf extract and ferulic acid for the manufacture of a cosmetic composition for improving skin.

[0011] Another object of the present invention is to provide a method for improving skin, comprising a step of applying a cosmetic composition comprising an effective amount of lotus leaf extract and ferulic acid to the skin of a subject in need thereof.

[0012] Hereinafter, the present invention will be described in detail.

[0013] When a part of the present invention is said to "include" a certain component, this does not mean that other components are excluded, but rather that other components may be additionally included, unless otherwise specifically stated.

[0014] One aspect of the present invention is a cosmetic composition comprising a lotus leaf (Nelumbo NuciferaLeaf) extract and ferulic acid.

[0015] In the present invention, the lotus leaf extract may be an extract obtained by extracting the leaf or petal portion of the lotus (Nelumbo Nucifera). The lotus is a perennial herb with circular, shield-shaped leaves and flowers that bloom at the end of long peduncles emerging from the water around July or August. The flower has 4 to 5 sepals and multiple petals. The fruit is called lotus seed, and the underground stem is called lotus root.

[0016] In the present invention, the lotus leaf is the dried leaf of the lotus flower. The leaves are picked in summer and dried in the sun or shade. They are bitter in flavor and neutral in nature. They are used as a medicinal herb to treat diarrhea caused by dampness, dizziness, edema caused by water vapor, vomiting blood, bloody stool, and postpartum hematuria.

[0017] In the present invention, "ferulic acid (or 4-hydroxy-3-methoxycinnamic acid)" is a phenolic compound with a structure represented by the following chemical formula 1. Ferulic acid is a precursor of lignin, which forms cell walls, and is abundantly contained in plant cell walls, helping to neutralize active oxygen such as hydroxyl radicals. In addition, ferulic acid can exhibit effective effects in antioxidant, whitening, wrinkle suppression, photoaging prevention, antibacterial, anti-inflammation, and moisturizing.

[0018] [Chemical Formula 1]

[0019]

[0020] However, ferulic acid has very low water solubility and is easily oxidized, limiting its use in cosmetics. Accordingly, the present invention provides a cosmetic composition containing lotus leaf extract to improve the formulation stability of ferulic acid.

[0021] In the present invention, the composition may be for skin moisturizing, skin regeneration, skin soothing, skin elasticity enhancement or wrinkle improvement, or anti-inflammation, but is not limited thereto.

[0022] According to Experimental Example 2 of the present invention, when HaCaT cells were treated with a combination of lotus leaf extract and ferulic acid, the expression of AQP3 was statistically significantly increased compared to the group treated alone. In addition, according to Experimental Example 3, when HaCaT cells were treated with a combination of lotus leaf extract and ferulic acid, the amount of hyaluronic acid was statistically significantly increased compared to the group treated alone. In addition, according to Experimental Example 4, when HaCaT cells were treated with a combination of lotus leaf extract and ferulic acid, the amount of IL-10 was statistically significantly decreased compared to the group treated alone.

[0023] In the present invention, the lotus leaf extract may be extracted with a solvent selected from the group consisting of water, alcohol having 1 to 6 carbon atoms, dichloromethane, acetone, and a mixed solvent thereof, and may preferably be a water extract, but is not limited thereto.

[0024] In the present invention, the lotus leaf extract may be included in an amount of 0.0001 to 99.9 wt%, 10 to 99.9 wt%, 30 to 99.9 wt%, 50 to 99.9 wt%, 70 to 99.9 wt%, 0.0001 to 90 wt%, 10 to 90 wt%, 30 to 90 wt%, 50 to 90 wt%, or 70 to 90 wt% relative to the weight of the total composition, but is not limited thereto.

[0025] In the present invention, ferulic acid may be included in an amount of 0.0001 to 1.0 wt%, 0.1 to 1.0 wt%, 0.5 to 1.0 wt%, 0.0001 to 0.8 wt%, 0.1 to 0.8 wt%, or 0.5 to 0.8 wt% relative to the weight of the entire composition, but is not limited thereto.

[0026] In the present invention, ferulic acid and lotus leaf extract may be included in a weight ratio of 1:10 to 1:100, 1:20 to 1:100, 1:30 to 1:100, 1:40 to 1:100, 1:50 to 1:100, 1:60 to 1:100, 1:70 to 1:100, 1:80 to 1:100, 1:90 to 1:100, but is not limited thereto.

[0027] In the present invention, the cosmetic composition may additionally contain one or more polyols.

[0028] In the present invention, the polyol may be at least one selected from the group consisting of pentylene glycol, ethylhexylglycerin, ethoxydiglycol, 2,3-butanediol, 1,2-hexanediol, glycerin, dipropylene glycol, butylene glycol, and propanediol, but is not limited thereto.

[0029] In the present invention, the cosmetic composition may have a pH of 4.0 to 6.0.

[0030] The ingredients included in the cosmetic composition of the present invention may include ingredients commonly used in cosmetic compositions in addition to the effective ingredients, and may include, for example, conventional auxiliary agents such as antioxidants, stabilizers, solubilizers, vitamins, ultraviolet absorbers, preservatives, pH regulators, colorants, pigments, and fragrances, and carriers.

[0031] The cosmetic composition of the present invention can be manufactured into any formulation commonly manufactured in the art, and for example, can be formulated into a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, cleansing oil, powder foundation, emulsion foundation, wax foundation, pack, massage cream, and spray, but is not limited thereto. More specifically, it can be manufactured into a formulation of skin, lotion, emollient toner, nourishing toner, nourishing cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray, or powder.

[0032] Another aspect of the present invention is a skin external preparation comprising the cosmetic composition described above.

[0033] When the cosmetic composition of the present invention is used as an external preparation, it may additionally contain adjuvants commonly used in the field of dermatology, such as fatty substances, organic solvents, solubilizers, thickening and gelling agents, emollients, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, water, ionic or nonionic emulsifiers, fillers, sequestering and chelating agents, preservatives, vitamins, blocking agents, humectants, essential oils, dyes, pigments, hydrophilic or lipophilic active agents, lipid vesicles, or any other ingredients commonly used in external preparations for skin. In addition, the above ingredients may be introduced in amounts commonly used in the field of dermatology. When provided in the form of a skin external preparation, it may have a formulation such as, but not limited to, an ointment, a patch, a gel, a cream, or a spray.

[0034] Another aspect of the present invention is the use of a composition comprising lotus leaf extract and ferulic acid for the manufacture of a cosmetic composition for improving skin.

[0035] In the present invention, skin improvement may be skin moisturizing, skin regeneration, skin elasticity enhancement, wrinkle improvement, or anti-inflammation.

[0036] Another aspect of the present invention is a method for improving skin, comprising the step of applying a cosmetic composition comprising an effective amount of lotus leaf extract and ferulic acid to the skin of a subject in need thereof.

[0037] The present invention relates to a cosmetic composition comprising lotus leaf extract and ferulic acid. The present invention improves the solubility of ferulic acid by adding lotus leaf extract to a composition comprising ferulic acid, thereby reducing concerns about precipitation and providing a cosmetic composition with excellent formulation stability. Furthermore, the composition exhibits superior moisturizing and anti-inflammatory effects compared to when lotus leaf extract and ferulic acid are used alone.

[0038] Figure 1 is a diagram comparing the appearance of the compositions of Comparative Example 1 and Example 4 according to Experimental Example 1.

[0039] Figure 2 is a graph showing the expression level of the AQP3 gene evaluated when treated with lotus leaf extract and ferulic acid according to Experimental Example 2.

[0040] Figure 3 is a graph showing the evaluation of the amount of hyaluronic acid when treated with lotus leaf extract and ferulic acid according to Experimental Example 3.

[0041] Figure 4 is a graph showing the expression level of the IL-10 gene, an inflammation expression marker, after treatment with lotus leaf extract and ferulic acid according to Experimental Example 4.

[0042] The advantages and features of the present invention, and the methods for achieving them, will become clearer with reference to the embodiments described in detail below. However, the present invention is not limited to the embodiments disclosed below, but may be implemented in various different forms. These embodiments are provided only to ensure that the disclosure of the present invention is complete and to fully inform those skilled in the art of the scope of the invention, and the present invention is defined only by the scope of the claims.

[0043] Manufacturing Example 1. Manufacturing of lotus leaf extract

[0044] Dried lotus leaves (origin: Yeongcheon, Gyeongsangbuk-do; source: Human Hub) were extracted with hot water and filtered through filter paper. Next, a porous adsorbent (HP20) was used as a propellant, and the extract was adsorbed onto a column. The extract was sequentially fractionated with ethanol from 10% to 100%, and subjected to porous gel column chromatography. The fractions were then concentrated under reduced pressure to obtain a final 1 g fraction. The fractions were then dissolved in purified water to prepare a 0.5% extract.

[0045]

[0046] Example

[0047] In this example, the solubility of ferulic acid according to the content of lotus leaf extract (Experimental Example 1), the moisturizing effect of a composition containing lotus leaf extract and ferulic acid (Experimental Example 2), the production amount of hyaluronic acid, a moisturizing factor, of a composition containing lotus leaf extract and ferulic acid (Experimental Example 3), and the anti-inflammatory effect of a composition containing lotus leaf extract and ferulic acid (Experimental Example 4) were confirmed.

[0048]

[0049] Experimental Example 1. Evaluation of Ferulic Acid Solubility According to Lotus Leaf Extract Content

[0050] A composition was prepared by adding lotus extract and ferulic acid at room temperature in the amounts (weight %) listed in Table 1, and then vortexing for about 1 minute.

[0051] Unit: weight % Comparative Example 1 Comparative Example 3 Example 1 Example 2 Comparative Example 2 Comparative Example 4 Example 3 Example 4 Ferulic acid 0.8 0.8 0.8 0.8 0.8 0.9 0.9 0.9 Lotus leaf extract 0 7 0 8 0 9 0 0 8 0 9 0 9 9.1 Purified water To 100 To 100 To 100 To 100 To 100 To 100 To 100 To 100 Ferulic acid: content ratio of lotus leaf extract - 1:87.5 1:100 1:112.5 - 1:88.9 1:100 1:110.1

[0052]

[0053] The manufactured Comparative Examples 1 and 2 and Examples 1 to 4 were allowed to stand for one week, and the macroscopic changes in appearance were observed with the naked eye to conduct a solubility evaluation, and the results are shown in Table 2 and Figure 1 below.

[0054] Precipitation Evaluation Comparative Example 1 Comparative Example 3 Example 1 Example 2 Comparative Example 2 Comparative Example 4 Example 3 Example 4 XXOOXXOO

[0055] ○: Good, ×: Precipitation

[0056]

[0057] As can be seen from Table 2 above, in Comparative Example 1 containing 0.8 wt% of ferulic acid and Comparative Example 3 containing 70 wt% or less of lotus leaf extract, ferulic acid was precipitated. On the other hand, Examples 1 and 2 containing 80 wt% or more of lotus leaf extract exhibited good formulation stability without precipitation. In addition, in Comparative Example 2 containing 0.9 wt% of ferulic acid and Comparative Example 4 containing 80 wt% or less of lotus leaf extract, ferulic acid was precipitated. On the other hand, Examples 3 and 4 containing 90 wt% or more of lotus leaf extract exhibited good formulation stability without precipitation (Fig. 1).

[0058] Through this, it was confirmed that when a certain concentration of ferulic acid is included in the composition, precipitation occurs, and when lotus leaf extract is prescribed at 100 times or more compared to ferulic acid, the phenomenon of improved solubility was confirmed.

[0059]

[0060] Experimental Example 2. Evaluation of the moisturizing effect of a composition containing lotus leaf extract and ferulic acid.

[0061] As shown in Table 3 below, HaCaT cells, a keratinocyte cell line, were treated with non-cytotoxic concentrations of lotus leaf extract (100, 500 ppm) and ferulic acid (1, 10 ppm), either alone or in combination, and the expression level of moisturizing gene AQP3 (Aquaporin-3) was measured by PCR (real time PCR). A group not treated with ferulic acid or lotus leaf extract was compared as a control group.

[0062] Treatment group Ferulic acid (ppm) 0 1 1 0 0 0 1 0 1 0 Lotus leaf extract (ppm) 0 0 1 0 0 5 0 1 0 0 5 0 AQP3 expression (fold) average 10.96 9 6 0.93 0 4 1.46 5 9 1.69 48 2.42 9 5 2.99 46 st dev 0.07 9 4 0.03 7 5 0.04 27 0.14 4 10.29 47 0.40 56 0.39 7 4 p-value (vs control group) -0.59 4 5 0.27 25 0.01 48 0.04 6 9 0.02 23 0.01 0 6 p-value (vs ferulic acid) ----- 0.02 25 0.01 14 p-value (vs lotus leaf extract) ----- 0.04 18 0.01 25

[0063]

[0064] As can be seen in Table 3 and Figure 2 above, it was confirmed that the AQP3 gene expression level increased when the two components were mixed and treated, compared to when either lotus leaf extract or ferulic acid was treated alone.

[0065]

[0066] Experimental Example 3. Evaluation of the amount of hyaluronic acid, a moisturizing factor, produced in a composition containing lotus leaf extract and ferulic acid.

[0067] As shown in Table 4 below, HaCaT cells, a keratinocyte cell line, were treated with 100 and 500 ppm of lotus leaf extract and 1 and 10 ppm of ferulic acid, which are non-cytotoxic concentrations, alone or in combination, and the amount of hyaluronic acid (HA), a moisturizing factor, was confirmed by ELISA.

[0068] Treatment group Ferulic acid (ppm) 0 1 1 0 0 1 0 1 0 Lotus leaf extract (ppm) 0 0 1 0 0 5 0 1 0 0 5 0 0 HA production (ng / ml) average 79.1 9 0 5 8 3.1 0 6 9 5.0 6 9 2.5 4 6 8 115.4 3 2 9 15 8.6 7 9 7 22 8.4 3 4 7 st dev 7.1 3 2 9 4.2 4 12 3.4 5 0 7 4.7 9 4 9 12.0 2 3 7 26.3 0 4 4 3 1.3 1 8 7 p-value (vs control group) -0.46 6 8 0.0 4 2 8 0.0 6 2 9 0.0 1 7 3 0.0 2 7 7 0.0 1 2 p-value (vs ferulic acid) ----- 0.0 4 9 0.0 1 5 1 0 Lotus leaf extract (ppm) 0 0 1 0 0 0 0 0 5 ... Lotus leaf extract)-----0.05030.0169

[0069]

[0070] As can be seen in Table 4 and Figure 3 above, it was confirmed that the amount of hyaluronic acid increased when the two components were mixed and treated, compared to when either lotus leaf extract or ferulic acid was treated alone.

[0071]

[0072] Experimental Example 4. Evaluation of the anti-inflammatory efficacy of a composition containing lotus leaf extract and ferulic acid.

[0073] As shown in Table 5 below, HaCaT cells, a keratinocyte cell line, were treated with 100 and 500 ppm of lotus leaf extract and 1 and 10 ppm of ferulic acid, which are non-cytotoxic concentrations, alone or in combination, and then an inflammatory response was induced by LPS (lipopolysaccharide) treatment, and the expression level of IL-10 gene, an inflammatory expression marker, was measured by PCR (real time PCR).

[0074] Treatment group LPS (μg / ml) 0 1 1 1 1 1 1 Ferulic acid (ppm) 0 1 1 0 0 1 0 1 0 Lotus leaf extract (ppm) 0 0 0 0 0 0 0 0 0 0 IL-10 expression (fold) average 0.00 1 9 1.0 9 8 0 0.83 1 7 0.81 5 3 0.71 9 9 0.51 3 3 0.34 5 8 0.21 6 3 st dev 0.00 1 1 0.1 6 7 10.04 1 3 0.08 3 9 0.04 5 7 0.04 5 6 0.02 5 8 0.00 8 7 p-value (vs control group) -0.00 76 --- p-value (vs LPS) --0.10 2 5 0.08 0 6 0.05 0 9 0.02 0 2 0.01 4 0.01 1 6 p-value (vs Ferulic acid)------0.00640.0060p-value(vs lotus leaf extract)------0.00090.0062

[0075]

[0076] As can be seen in Table 5 and Figure 4 above, it was confirmed that the expression level of IL-10 was significantly reduced when the two components were mixed and treated, compared to when either lotus leaf extract or ferulic acid was treated alone.

Claims

1. A cosmetic composition comprising lotus leaf (Nelumbo NuciferaLeaf) extract and ferulic acid.

2. In paragraph 1, The above composition is a cosmetic composition for moisturizing the skin, regenerating the skin, soothing the skin, increasing skin elasticity or improving wrinkles, or for anti-inflammation.

3. In paragraph 1, A cosmetic composition wherein the lotus leaf extract is extracted with a solvent selected from the group consisting of water, alcohol having 1 to 6 carbon atoms, dichloromethane, acetone, and a mixed solvent thereof.

4. In paragraph 3, A cosmetic composition wherein the lotus leaf extract is a water extract.

5. In paragraph 1, A cosmetic composition comprising the above ferulic acid and lotus leaf extract in a weight ratio of 1:10 to 1:

100.

6. In paragraph 1, A cosmetic composition further comprising one or more polyols.

7. In paragraph 6, A cosmetic composition wherein the polyol is at least one selected from the group consisting of pentylene glycol, ethylhexylglycerin, ethoxydiglycol, 2,3-butanediol, 1,2-hexanediol, glycerin, dipropylene glycol, butylene glycol, and propanediol.

8. In paragraph 1, The above cosmetic composition is a cosmetic composition having a pH of 4.0 to 6.

0.

9. A skin external preparation comprising a cosmetic composition according to any one of claims 1 to 8.

Citation Information

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