High-permeability composition containing ascorbyl tetraisopalmitate and application thereof

Abstract

The invention discloses a high-permeability composition containing ascorbyl tetraisopalmitate and application of the high-permeability composition, and particularly belongs to the field of dressing preparations. The high-permeability composition is prepared from the following components in parts by mass: 5 to 10 parts of ascorbyl tetraisopalmitate, 0.6 to 1 part of radix angelicae sinensis royle root oil, 1 to 3 parts of geranium leaf oil and 0.2 to 0.4 part of evening primrose oil. When the Angelica rotundifolia root oil, the pelargonium hortorum leaf oil and the evening primrose oil provided by the invention are compounded for use, the transdermal effect of ascorbyl tetraisopalmitate can be remarkably enhanced, and absorption and utilization of ascorbyl tetraisopalmitate by skin are promoted. The high-permeability composition provided by the invention can be used for preparing skin whitening and moistening essence, and the prepared skin whitening and moistening essence has a remarkable skin whitening effect.

Description

Technical Field

[0001] The invention belongs to the field of cosmetic preparations, and in particular relates to a high-penetration composition containing ascorbyl tetraisopalmitate and application thereof. Background Art

[0002] Ascorbyl Tetraisopalmitate (VC-IP) is an esterified vitamin C derivative that has occupied a place in the beauty field with its unique molecular structure and excellent skin care effects. VC-IP not only has the multiple effects of vitamin C, such as anti-oxidation, promoting collagen regeneration, anti-inflammatory and inhibiting pigmentation, but also overcomes the shortcomings of the original vitamin C, such as poor transdermal permeability and insufficient stability. The fat-soluble characteristics of VC-IP give it excellent transdermal absorption ability, which can easily penetrate sebum, penetrate into the epidermis and dermis, and bring deep nourishment to the skin. At the same time, by introducing hydroxyl esterification into the molecular structure of vitamin C, VC-IP shows excellent stability and can maintain its activity both in air and under light conditions.

[0003] However, although VC-IP has shown high permeability and stability, there is still room for further improvement of its permeability efficiency and bioavailability in practical applications. Although the permeability of VC-IP is better than that of the prototype vitamin C, the process of permeation through the hair follicles is relatively slow, and it shows high mobility and low affinity in the hair follicles.

[0004] Therefore, it is urgently necessary to develop a composition that improves the permeability of VC-IP. By optimizing the formula ingredients and proportions, the penetration ability and affinity of VC-IP to the stratum corneum can be further improved, allowing it to penetrate the skin barrier more efficiently and achieve a deep nourishing effect. Summary of the invention

[0005] In view of the deficiencies in the prior art, the present invention aims to provide a high permeability composition containing ascorbyl tetraisopalmitate and its application, further improve the permeability, stability and conversion rate of ascorbyl tetraisopalmitate, expand its application field, and provide consumers with more efficient, safe and multi-effect skin care products.

[0006] To achieve the above object, the present invention discloses the following technical solutions: In a first aspect, the present invention provides a high permeability composition, which comprises the following components by weight: 5-10 parts of ascorbyl tetraisopalmitate; 0.6-1 part of angelica root oil; 1-3 parts geranium leaf oil; Evening primrose oil 0.2-0.4 parts.

[0007] Preferably, the composition comprises the following components in parts by mass: Ascorbyl tetraisopalmitate 7 parts; 0.8 parts of angelica root oil; 2 parts geranium leaf oil; 0.3 parts of evening primrose oil.

[0008] In a second aspect, the present invention provides use of the high permeability composition described in the first aspect in the preparation of a skin care product with whitening, spot-lightening and / or anti-oxidation effects.

[0009] In a third aspect, the present invention provides a whitening and moisturizing essence, wherein the essence contains the high permeability composition described in the first aspect.

[0010] Preferably, the high permeability composition is added in an amount of 0.5-2 wt % in the whitening and moisturizing essence.

[0011] More preferably, the whitening and moisturizing essence also includes a moisturizer, a base oil, a chelating agent, an emulsifier, a preservative, and a solvent.

[0012] More preferably, the moisturizing agent is selected from at least one of 1,3-butylene glycol, sodium hyaluronate, glycerol, propylene glycol, and butylene glycol; The base oil is selected from at least one of squalane, grape seed oil, and caprylic / capric triglyceride; The chelating agent is selected from disodium EDTA; The emulsifier is selected from laureth-23; The preservative is selected from phenoxyethanol; The solvent is deionized water.

[0013] In a fourth aspect, the present invention provides a method for preparing the aforementioned whitening and moisturizing essence, the preparation method comprising the following steps: S1-1. Mix 1,3-butylene glycol, sodium hyaluronate, glycerin, propylene glycol, butylene glycol, disodium EDTA, laureth-23, and deionized water, heat to 80 ° C, and stir to completely dissolve to obtain a mixture; S1-2. After cooling the mixture of step S1-1 to 45°C, add the high permeability composition, base oil and phenoxyethanol in sequence, stir evenly at a speed of 500r / min, deaerate, and discharge to obtain the whitening and moisturizing essence.

[0014] In the present invention: Ascorbyl tetraisopalmitate is an ingredient with multiple functions in cosmetics. It has a strong antioxidant effect, can neutralize free radicals, reduce their damage to skin cells and DNA, and protect other antioxidants in cosmetics, enhancing the overall antioxidant effect. In addition, it also has the effect of whitening and removing spots. By inhibiting tyrosinase activity and reducing melanin production, long-term use can improve the uniformity of skin color and lighten spots. At the same time, its oil-soluble characteristics make it have good transdermal absorption and high absorption rate. It can quickly penetrate the cell membrane and transport the active ingredients to the deep layers of the skin.

[0015] Angelica dahurica root oil is rich in active ingredients such as α-pinene, α-phellandrene, β-phellandrene, limonene, 3-carene, etc., and has antioxidant, anti-inflammatory, antibacterial, penetration-promoting, and blood circulation-promoting effects; geranium leaf oil contains l-citronellol, geraniol, geranyl formate, citronellal, geranial, eugenol and other active ingredients, and has excellent antioxidant, anti-inflammatory, antibacterial, penetration-promoting, blood circulation-promoting, and skin-soothing and irritation-reducing effects; evening primrose oil has excellent anti-inflammatory and soothing properties, which can effectively reduce skin inflammation, relieve discomfort such as redness, swelling, pain, itching and tingling, and bring gentle care to sensitive and easily inflamed skin. At the same time, it can also promote skin microcirculation, improve dull skin tone, and restore the skin to a healthy luster. It also has antibacterial effects, which helps prevent and treat skin infections, clean pores, and reduce acne and blackheads.

[0016] The present invention has found that when ascorbyl tetraisopalmitate, angelica root oil, geranium leaf oil and evening primrose oil are used in combination, the transdermal effect of ascorbyl tetraisopalmitate can be enhanced, and the absorption of ascorbyl tetraisopalmitate by the skin can be promoted.

[0017] Beneficial effects of the present invention: 1. When the angelica root oil, geranium leaf oil and evening primrose oil provided by the present invention are used in combination, the transdermal effect of ascorbyl tetraisopalmitate can be significantly enhanced, and the absorption and utilization of ascorbyl tetraisopalmitate by the skin can be promoted.

[0018] 2. The whitening and moisturizing essence provided by the present invention has a significant whitening effect, and the whitening performance is positively correlated with the concentration of the high permeability composition containing ascorbyl tetraisopalmitate provided by the present invention, that is, it has a certain concentration dependence. DETAILED DESCRIPTION

[0019] To better illustrate the purpose, technical solutions and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments. It should be understood by those skilled in the art that the specific embodiments described herein are only used to explain the present invention and are not intended to limit the present invention.

[0020] Unless otherwise specified, the test methods used in the specific implementation methods are all conventional methods; the materials, reagents, etc. used, unless otherwise specified, can be obtained from commercial channels; the percentages mentioned in the specific implementation methods, unless otherwise specified, are all mass percentages.

[0021] In the present invention: Ascorbyl tetraisopalmitate: INCI name ASCORBYL TETRAISOPALMITATE, purchased from Jisheng (Shanghai) Industrial Co., Ltd.; Angelica ARCHANGELICA root oil: Angelica ARCHANGELICA root oil, INCI name ANGELICAARCHANGELICA ROOT OIL, purchased from Jiangxi Yisenyuan Plant Spice Co., Ltd.; Geranium leaf oil: Pelargonium graaveolens leaf oil, INCI name PELARGONIUM GRAVEOLENS LEAF OIL, purchased from Sichuan Xingsanxing Technology Co., Ltd.; Evening primrose oil: Evening primrose (OENOTHERA BIENNIS) oil, INCI name OENOTHERA BIENNIS (EVENING PRIMROSE) OIL, purchased from Shanghai Jingchun Biotechnology Co., Ltd.; Other raw materials are commercially available.

[0022] Preparation of composition Accurately weigh the components in Table 1 according to their mass fractions, place the weighed components in a reaction kettle, mix and stir evenly, and obtain high permeability compositions 1-11.

[0023] Table 1 Components of high permeability composition and their mass fractions Composition 1 Composition 2 Composition 3 Composition 4 Composition 5 Composition 6 Composition 7 Composition 8 Composition 9 Composition 10 Composition 11 Ascorbyl Tetraisopalmitate 5 7 10 7 7 7 7 7 7 7 7 Angelica Root Oil 0.6 0.8 1 - 2.25 0.886 3.1 - - 1 2 Geranium leaf oil 1 2 3 2.7 - 2.214 - 3.1 - 1 0.5 Evening Primrose Oil 0.2 0.3 0.4 0.4 0.85 - - - - 1.1 0.6 Note: “-” in the table means no addition.

[0024] In order to verify the transdermal diffusion performance of composition 1-11, the above composition 1-11 was diluted with base oil to a sample 1-11 with a concentration of 1wt%, and the following performance test was performed, wherein the base oil was prepared by squalane and caprylic / capric triglyceride in a mass ratio of 1:5, and composition 4-11 was set based on composition 2, see Table 1 and the following settings for details: Composition 4: Composition 2 lacks angelica root oil, and the lacking mass fraction is distributed to geranium leaf oil and evening primrose oil at a mass ratio of 2:0.3, and the rest is consistent with composition 2; Composition 5: Composition 2 lacks geranium leaf oil, and the lacking mass fraction is distributed to angelica root oil and evening primrose oil at a mass ratio of 0.8:0.3, and the rest is consistent with composition 2; Composition 6: Composition 2 lacks evening primrose oil, and the missing mass portion is distributed to Angelica dahurica root oil and Pelargonium graveolens leaf oil at a mass ratio of 0.8:2, and the rest is consistent with Composition 2; Composition 7: Composition 2 is based on the fact that geranium leaf oil and evening primrose oil are missing, and the missing mass parts are equally distributed to angelica root oil, and the rest is the same as composition 2; Composition 8: Composition 2 lacks angelica root oil and evening primrose oil, and the missing parts are equally distributed to geranium leaf oil, and the rest is consistent with composition 2; Composition 9: ascorbyl tetraisopalmitate only; Composition 10: Based on composition 2, the mass ratio of angelica root oil, geranium leaf oil and evening primrose oil is adjusted to 1:1:1.1, and the rest is consistent with composition 2; Composition 11: Based on composition 2, the mass ratio of angelica root oil, geranium leaf oil and evening primrose oil is adjusted to 2:0.5:0.6, and the rest is consistent with composition 2.

[0025] Performance Experiment Experimental animals: 44 male ICR mice (20±2 g) were purchased from Beijing Weitonglihua Experimental Animal Technology Co., Ltd.

[0026] In this test example, the in vitro transdermal effect of compositions 1 to 11 was evaluated by a transdermal diffusion tester.

[0027] Healthy male ICR mice with intact skin were selected, and their abdominal hair was removed after anesthesia with 2wt% chloral hydrate. They were killed by cervical dislocation, and the skin of the lower abdomen was peeled off. Excess fat and mucous tissue were carefully removed and washed. They were placed in physiological saline and stored at -20℃ for future use. 11 experimental groups (i.e., samples 1-11 to be tested) were set up, with 4 mice in each group.

[0028] After the mouse skin was thawed at room temperature, it was fixed between the upper and lower chambers of the Franz diffusion cell, with the stratum corneum facing upward. The upper chamber was the supply chamber, and 0.5 g of each group of samples to be tested was added to the supply chamber. The lower chamber was the receiving cell, and the receiving solution in the receiving cell was 30% ethanol saline, which was just in contact with the dermis of the skin. A magnetic stirring bar was built into the receiving cell. The in vitro transdermal experiment was carried out at a stirring speed of 300 rpm and a water bath temperature of (37±1)℃. 0.2 mL of sample was taken every 1 hour within 1-12 hours, and fresh blank receiving solution of equal volume was immediately added at isothermal temperature to measure the cumulative permeation per unit area (Q) for 12 hours. 12 ).

[0029] The calculation formula is as follows: .

[0030] In the formula, C n is the drug (ascorbyl tetraisopalmitate) concentration (μg / mL) at the nth sampling point, Ci is the drug (ascorbyl tetraisopalmitate) concentration (μg / mL) at the ith sampling point, A is the effective drug delivery area (3.14 cm 2 ), V is the volume of the receiving solution (mL). The specific results are shown in Table 2.

[0031] Table 2 In vitro transdermal test results Group <![CDATA[Ascorbyl Tetraisopalmitate / Q 12 (μg / cm 2 )]]> Sample 1 43.49 Sample 2 43.67 Sample 3 42.73 Sample 4 30.92 Sample 5 31.77 Sample 6 31.38 Sample 7 29.43 Sample 8 29.22 Sample 9 26.06 Samples to be tested 10 38.51 Sample 11 31.29 Note: The concentration of ascorbyl tetraisopalmitate was determined by HPLC.

[0032] Result analysis: According to the results, the angelica root oil, geranium leaf oil and evening primrose oil provided by the present invention can significantly increase the cumulative permeation amount of ascorbyl tetraisopalmitate when used in combination, and the lack of any one or more of angelica root oil, geranium leaf oil and evening primrose oil will lead to a significant decrease in the cumulative permeation amount of ascorbyl tetraisopalmitate, indicating that the angelica root oil, geranium leaf oil and evening primrose oil provided by the present invention can enhance the transdermal effect of ascorbyl tetraisopalmitate when used in combination, and the three have a synergistic effect on improving the permeability of ascorbyl tetraisopalmitate.

[0033] Preparation of application examples Accurately weigh each component according to the mass percentage of each component in Table 3; S1-1. Mix 1,3-butylene glycol, sodium hyaluronate, glycerin, propylene glycol, butylene glycol, disodium EDTA, laureth-23, and deionized water, heat to 80 ° C, and stir to completely dissolve to obtain a mixture; S1-2. After cooling the mixture of step S1-1 to 45°C, add composition 2, squalane, grape seed oil and phenoxyethanol in Table 1 in sequence, stir evenly at a speed of 500 r / min, degas, and discharge to obtain the whitening and moisturizing essence.

[0034] Table 3 Components and their mass percentages in the application examples

[0035] Human skin patch test The application examples 1-3 prepared above were subjected to the human skin patch test in reference to the "2015 Cosmetic Safety Technical Specifications".

[0036] The skin reaction was observed according to the standard at 30 minutes (after the indentation disappears), 24 hours and 48 hours, and the observation results were recorded (see Table 4).

[0037] Table 4 Human safety test results serial number 30min 24h 48h Application Example 1 Level 0, 30 players Level 0, 30 players Level 0, 30 players Application Example 2 Level 0, 30 players Level 0, 30 players Level 0, 30 players Application Example 3 Level 0, 30 players Level 0, 30 players Level 0, 30 players Application example whitening effect evaluation Test sample: the whitening and moisturizing essence of Application Example 1-3.

[0038] 15 volunteers with similar facial skin conditions and darker facial complexion, aged 25-27 years old, were selected and divided into 3 groups according to the number of people. They were grouped according to Application Examples 1-3 respectively. Each group used corresponding test samples and conducted detection tests according to the test method in "Test Method for the Anti-freckle and Whitening Efficacy of Cosmetics on Ultraviolet-Induced Human Skin Melanization Model" in the Technical Specifications for Safety of Cosmetics (2015 Edition).

[0039] The test subjects used the test samples prepared above after cleaning their faces in the morning and evening for 4 consecutive weeks. A skin red-melanin tester and a test probe (Mexameter MX18, CK Company, Germany) were used to collect data on the test subjects' faces before use (week 0), in week 1, and after week 4 of use. The changes in skin melanin content / MI before and after use of cosmetics were calculated. The higher the MI measurement value, the higher the melanin content in the skin. The average value of the test results of each group was taken. The specific results are shown in Table 5.

[0040] Table 5 Whitening effect results

[0041] Result analysis: According to the results in Table 5, the whitening and moisturizing essence provided by the present invention has a significant whitening effect, and the whitening performance is positively correlated with the concentration of composition 2, that is, it has a certain concentration dependence, which proves that the composition provided by the present invention has excellent antioxidant and whitening effects.

[0042] Finally, it should be noted that the above embodiments and comparative examples are only used to illustrate the technical solution of the present invention rather than to limit the protection scope of the present invention. Although the present invention has been described in detail with reference to the preferred embodiments, those skilled in the art should understand that the technical solution of the present invention can be modified or replaced by equivalents without departing from the essence and scope of the technical solution of the present invention.

Claims

1. A high permeability composition, characterized in that The composition comprises the following components by weight: 5-10 parts of ascorbyl tetraisopalmitate; 0.6-1 part of angelica root oil; 1-3 parts geranium leaf oil; Evening primrose oil 0.2-0.4 parts.

2. The high permeability composition according to claim 1, characterized in that The composition comprises the following components by weight: Ascorbyl tetraisopalmitate 7 parts; 0.8 parts of angelica root oil; 2 parts geranium leaf oil; 0.3 parts of evening primrose oil.

3. Use of the high permeability composition according to claim 1 or 2 in the preparation of skin care products with whitening, spot-lightening and / or anti-oxidation effects.

4. A whitening and moisturizing essence, characterized in that: The essence contains the high-penetration composition according to claim 1 or 2.

5. The whitening and moisturizing essence according to claim 4, characterized in that: The high permeability composition is added in an amount of 0.5-2 wt % in the whitening and moisturizing essence.

6. The whitening and moisturizing essence according to claim 5, characterized in that: The whitening and moisturizing essence also includes a moisturizer, a base oil, a chelating agent, an emulsifier, a preservative, and a solvent.

7. The whitening and moisturizing essence according to claim 6, characterized in that: The moisturizer is selected from at least one of 1,3-butylene glycol, sodium hyaluronate, glycerin, propylene glycol, and butylene glycol; The base oil is selected from at least one of squalane, grape seed oil, and caprylic / capric triglyceride; The chelating agent is selected from disodium EDTA; The emulsifier is selected from laureth-23; The preservative is selected from phenoxyethanol; The solvent is deionized water.

8. The method for preparing the whitening and moisturizing essence according to claim 7, characterized in that: The preparation method comprises the following steps: S1-1. Mix 1,3-butylene glycol, sodium hyaluronate, glycerin, propylene glycol, butylene glycol, disodium EDTA, laureth-23, and deionized water, heat to 80 ° C, and stir to completely dissolve to obtain a mixture; S1-2. After cooling the mixture of step S1-1 to 45°C, add the high permeability composition, base oil and phenoxyethanol in sequence, stir evenly at a speed of 500r / min, deaerate, and discharge to obtain the whitening and moisturizing essence.

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