High-Permeability Composition Containing Ascorbyl Tetraisopalmitate and Its Application

Abstract

The present invention discloses a highly permeable composition containing tetraisopalmitate ascorbate and its application, specifically belonging to the field of toilet preparations. The highly permeable composition comprises the following components in parts by mass: 5-10 parts of tetraisopalmitate ascorbate, 0.6-1 part of angelica archangelica root oil, 1-3 parts of pelargonium graveolens leaf oil, and 0.2-0.4 part of evening primrose oil. When the angelica archangelica root oil, pelargonium graveolens leaf oil, and evening primrose oil provided by the present invention are used in combination, the transdermal effect of tetraisopalmitate ascorbate can be significantly enhanced, and the absorption and utilization of tetraisopalmitate ascorbate by the skin can be promoted. The highly permeable composition provided by the present invention can be used for preparing a whitening and moisturizing essence, and the prepared whitening and moisturizing essence has a remarkable 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:

[0007] In a first aspect, the present invention provides a high permeability composition, which comprises the following components by weight:

[0008] 5-10 parts of ascorbyl tetraisopalmitate;

[0009] 0.6-1 part of Angelica sinensis root oil;

[0010] 1 - 3 parts of pelargonium leaf oil;

[0011] 0.2 - 0.4 parts of evening primrose oil.

[0012] Preferably, by mass parts, the composition comprises the following components:

[0013] 7 parts of ascorbyl tetraisopalmitate;

[0014] 0.8 part of angelica archangelica root oil;

[0015] 2 parts of pelargonium leaf oil;

[0016] 0.3 part of evening primrose oil.

[0017] In a second aspect, the present invention provides the use of the high - permeability composition described in the first aspect in the preparation of a skin - care product having whitening, freckle - lightening and / or antioxidant effects.

[0018] In a third aspect, the present invention provides a whitening and moisturizing essence, and the essence contains the high - permeability composition described in the first aspect.

[0019] Preferably, the addition amount of the high - permeability composition in the whitening and moisturizing essence is 0.5 - 2 wt%.

[0020] More preferably, the whitening and moisturizing essence further comprises a humectant, a base oil, a chelating agent, an emulsifier, a preservative, and a solvent.

[0021] Even more preferably, the humectant is selected from at least one of 1,3 - butanediol, sodium hyaluronate, glycerol, propylene glycol, and butylene glycol;

[0022] The base oil is selected from at least one of squalane, grape seed oil, and caprylic / capric triglyceride;

[0023] The chelating agent is selected from disodium EDTA;

[0024] The emulsifier is selected from laureth - 23;

[0025] The preservative is selected from phenoxyethanol;

[0026] The solvent is deionized water.

[0027] In a fourth aspect, the present invention provides a preparation method of the aforementioned whitening and moisturizing essence, and the preparation method comprises the following steps:

[0028] S1 - 1. Mix 1,3 - butanediol, sodium hyaluronate, glycerol, propylene glycol, butylene glycol, disodium EDTA, laureth - 23, and deionized water, heat to 80°C, and stir until completely dissolved to obtain a mixture;

[0029] S1-2. After cooling the mixture in step S1-1 to 45°C, add the high-permeability composition, base oil, and phenoxyethanol in sequence, stir evenly at a rotation speed of 500 r / min, defoam, and discharge to obtain the whitening and moisturizing essence.

[0030] In the present invention:

[0031] Tetrahexyldecyl ascorbate is a component with multiple functions in cosmetics. It has a powerful antioxidant effect, can neutralize free radicals, reduce their damage to skin cells and DNA, and at the same time can also protect other antioxidants in cosmetics, enhancing the overall antioxidant effect. In addition, it also has the effect of whitening and removing spots. By inhibiting the activity of tyrosinase, it reduces melanin production. Long-term use can improve skin color uniformity and fade spots. At the same time, its oil-soluble characteristics make it have good transdermal absorbability and high absorption rate, and can quickly penetrate cell membranes to deliver active ingredients to the deep layer of the skin.

[0032] Angelica archangelica root oil is rich in active ingredients such as α-pinene, α-phellandrene, β-phellandrene, limonene, 3-carene, etc., and has the effects of antioxidant, anti-inflammatory, antibacterial, promoting penetration, and promoting blood circulation; Geranium leaf oil contains active ingredients such as l-citronellol, geraniol, geranyl formate, citronellyl formate, neral, geranial, and eugenol, and has excellent antioxidant, anti-inflammatory, antibacterial, promoting penetration, promoting blood circulation, and soothing the skin to reduce irritation effects; Evening primrose oil has excellent anti-inflammatory and soothing properties, can effectively reduce skin inflammation, relieve discomfort such as swelling, pain, itching, and stinging, bring gentle care to sensitive and easily inflamed skin. At the same time, it can also promote skin microcirculation, improve dull skin color, make the skin regain a healthy glow, and has antibacterial effects, helping to prevent and treat skin infections, clean pores, and reduce acne and blackheads.

[0033] The present invention studies and finds that when tetrahexyldecyl ascorbate, angelica archangelica root oil, geranium leaf oil, and evening primrose oil are used in combination, the transdermal effect of tetrahexyldecyl ascorbate can be enhanced, and the absorption of tetrahexyldecyl ascorbate by the skin can be promoted.

[0034] The beneficial effects of the present invention:

[0035] 1. When the angelica archangelica root oil, geranium leaf oil, and evening primrose oil provided by the present invention are used in combination, the transdermal effect of tetrahexyldecyl ascorbate can be significantly enhanced, and the absorption and utilization of tetrahexyldecyl ascorbate by the skin can be promoted.

[0036] 2. The whitening and moisturizing essence provided by the present invention has a significant whitening effect, and the level of whitening performance is positively correlated with the concentration of the high-permeability composition containing tetrahexyldecyl ascorbate provided by the present invention, that is, it has a certain concentration dependence. Detailed implementation mode

[0037] To better illustrate the purpose, technical solution and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments. Those skilled in the art should understand that the specific embodiments described herein are only used to explain the present invention and are not used to limit the present invention.

[0038] Unless otherwise specified, the test methods used in the detailed implementation mode are all conventional methods; the materials, reagents, etc. used, unless otherwise specified, can all be obtained from commercial channels; the percentages mentioned in the detailed implementation mode, unless otherwise specified, are all mass percentages.

[0039] In the present invention:

[0040] Ascorbyl tetraisopalmitate: The INCI name is ASCORBYL TETRAISOPALMITATE, purchased from Jisheng (Shanghai) Industrial Co., Ltd.;

[0041] Angelica archangelica root oil: Angelica archangelica root oil, the INCI name is ANGELICA ARCHANGELICA ROOT OIL, purchased from Jiangxi Yisenyuan Plant Spice Co., Ltd.;

[0042] Geranium leaf oil: Pelargonium graveolens leaf oil, the INCI name is PELARGONIUM GRAVEOLENS LEAF OIL, purchased from Sichuan Xingsanhang Technology Co., Ltd.;

[0043] Evening primrose oil: Oenothera biennis oil, the INCI name is OENOTHERA BIENNIS (EVENING PRIMROSE) OIL, purchased from Shanghai Jingchun Biotechnology Co., Ltd.;

[0044] Other raw materials are commercially available.

[0045] Preparation of the composition

[0046] Accurately weigh according to the mass parts of each component in Table 1, and place the weighed components in a reaction kettle and mix and stir evenly to obtain the high-permeability compositions 1-11.

[0047] Table 1 Components and their mass parts of the high-permeability composition

[0048] Composition 1 Composition 2 Composition 3 Composition 4 Composition 5 Composition 6 Composition 7 Composition 8 Composition 9 Composition 10 Composition 11 Tetra - isopalmitoyl ascorbate 5 7 10 7 7 7 7 7 7 7 7 Angelica archangelica root oil 0.6 0.8 1 - 2.25 0.886 3.1 - - 1 2 Pelargonium graveolens 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

[0049] Note: "-" in the table means no addition.

[0050] To verify the transdermal diffusion performance of Compositions 1-11, the above Compositions 1-11 were diluted with a base oil into Test Samples 1-11 with a concentration of 1 wt%, and the following performance tests were carried out. The base oil was prepared from squalane and caprylic / capric triglyceride in a mass ratio of 1:5. Compositions 4-11 were set based on Composition 2. For specific details, refer to Table 1 and the following settings:

[0051] Composition 4: On the basis of Composition 2, the angelica archangelica root oil was missing, and the missing mass fraction was distributed to geranium leaf oil and evening primrose oil according to a mass ratio of 2:0.3, and the rest was the same as Composition 2;

[0052] Composition 5: On the basis of Composition 2, the geranium leaf oil was missing, and the missing mass fraction was distributed to angelica archangelica root oil and evening primrose oil according to a mass ratio of 0.8:0.3, and the rest was the same as Composition 2;

[0053] Composition 6: On the basis of Composition 2, the evening primrose oil was missing, and the missing mass fraction was distributed to angelica archangelica root oil and geranium leaf oil according to a mass ratio of 0.8:2, and the rest was the same as Composition 2;

[0054] Composition 7: On the basis of Composition 2, the geranium leaf oil and evening primrose oil were missing, and the missing mass fraction was equally distributed to angelica archangelica root oil, and the rest was the same as Composition 2;

[0055] Composition 8: On the basis of Composition 2, the angelica archangelica root oil and evening primrose oil were missing, and the missing mass fraction was equally distributed to geranium leaf oil, and the rest was the same as Composition 2;

[0056] Composition 9: Only ascorbyl tetraisopalmitate;

[0057] Composition 10: On the basis of Composition 2, the mass ratio of angelica archangelica root oil, geranium leaf oil and evening primrose oil was adjusted to 1:1:1.1, and the rest was the same as Composition 2;

[0058] Composition 11: On the basis of Composition 2, the mass ratio of angelica archangelica root oil, geranium leaf oil and evening primrose oil was adjusted to 2:0.5:0.6, and the rest was the same as Composition 2.

[0059] Performance Experiment

[0060] Test animals: 44 male ICR mice (20±2 g), purchased from Beijing Vital River Laboratory Animal Technology Co., Ltd.

[0061] In this test example, the in vitro transdermal effects of Compositions 1-11 were evaluated by a transdermal diffusion tester.

[0062] Healthy male ICR mice with intact skin were selected. After anesthesia with 2wt% chloral hydrate, the hair on their abdomens was removed. They were sacrificed by cervical dislocation, and the abdominal skin was dissected. After carefully removing excess fat and mucus tissue, it was washed and placed in physiological saline, and stored at -20 °C for later use. 11 experimental groups (i.e., test samples 1 - 11) were set up, with 4 mice in each group.

[0063] After the excised mouse skin was thawed at room temperature, it was fixed between the upper and lower chambers of a Franz diffusion cell, with the stratum corneum facing upwards. The upper chamber was the supply chamber, and 0.5 g of each test sample was added to the supply chamber. The lower chamber was the receiving chamber, and the receiving fluid in the receiving chamber was 30% ethanol physiological saline. The receiving fluid just contacted the dermal layer of the skin. A magnetic stir bar was placed in the receiving chamber. An in vitro transdermal experiment was carried out under the conditions of a stirring speed of 300 rpm and a water bath temperature of (37 ± 1) °C. 0.2 mL of the sample was taken every 1 h within 1 - 12 h, and fresh blank receiving fluid of the same temperature and volume was immediately replenished. The cumulative amount permeated per unit area (Q 12 ) was measured at 12 h.

[0064] The calculation formula is as follows:

[0065]

[0066] In the formula, C n is the concentration (μg / mL) of the drug (tetraisopalmitate ascorbate) at the nth sampling point, Ci is the concentration (μg / mL) of the drug (tetraisopalmitate ascorbate) at the ith sampling point, A is the effective drug delivery area (3.14 cm 2 ), and V is the volume (mL) of the receiving fluid. The specific results are shown in Table 2.

[0067] Table 2 Results of in vitro transdermal experiment

[0068] Group <![CDATA[Ascorbyl Tetraisopalmitate / Q 12 (μg / cm 2 )]]> Sample to be tested 1 43.49 Sample to be tested 2 43.67 Sample to be tested 3 42.73 Sample to be tested 4 30.92 Sample to be tested 5 31.77 Sample to be tested 6 31.38 Sample to be tested 7 29.43 Sample to be tested 8 29.22 Sample to be tested 9 26.06 Sample to be tested 10 38.51 Sample to be tested 11 31.29

[0069] Note: The concentration of tetraisopalmitate ascorbate was detected by high performance liquid chromatography.

[0070] Result analysis:

[0071] According to the results, it can be seen that when the oil of Angelica archangelica roots, the oil of Pelargonium graveolens leaves and the oil of Oenothera biennis seeds provided by the present invention are used in combination, the cumulative amount permeated of tetraisopalmitate ascorbate can be significantly increased. However, the absence of any one or more of the oil of Angelica archangelica roots, the oil of Pelargonium graveolens leaves and the oil of Oenothera biennis seeds will lead to a significant decrease in the cumulative amount permeated of tetraisopalmitate ascorbate, indicating that when the oil of Angelica archangelica roots, the oil of Pelargonium graveolens leaves and the oil of Oenothera biennis seeds provided by the present invention are used in combination, the transdermal effect of tetraisopalmitate ascorbate can be enhanced, and the three have a synergistic effect on improving the permeability of tetraisopalmitate ascorbate.

[0072] Preparation of application examples

[0073] Accurately weigh each component according to the mass percentage of each component in Table 3;

[0074] 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;

[0075] 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.

[0076] Table 3 Components and their mass percentages in the application examples

[0077]

[0078] Human skin patch test

[0079] The application examples 1-3 prepared above were subjected to the human skin patch test in reference to the "2015 Cosmetic Safety Technical Specifications".

[0080] 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).

[0081] Table 4 Human safety test results

[0082] Number 30 min 24h 48h Application Example 1 Grade 0, 30 people Grade 0, 30 people Grade 0, 30 people Application Example 2 Grade 0, 30 people Grade 0, 30 people Grade 0, 30 people Application Example 3 Grade 0, 30 people Grade 0, 30 people Grade 0, 30 people

[0083] Application example whitening effect evaluation

[0084] Test sample: the whitening and moisturizing essence of Application Example 1-3.

[0085] 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).

[0086] The testers used the aforementioned prepared test samples after cleaning their faces in the morning and evening for 4 consecutive weeks. The skin red and black pigment tester and the test probe (Mexameter MX18, CK Company, Germany) were used to collect data on the testers' faces before use (week 0), after 1 week of use, and after 4 weeks of use. The change in the skin melanin content / MI of the testers before and after using the cosmetics was calculated. The higher the MI measurement value, the higher the melanin content in the skin. The average value was taken for the test results of each group, and the specific results are shown in Table 5.

[0087] Table 5 Whitening efficacy results

[0088]

[0089] Result analysis:

[0090] According to the results in Table 5, it can be seen that the whitening and moisturizing essence provided by the present invention has a significant whitening effect. 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.

[0091] Finally, it should be noted that the above examples and comparative examples are only used to illustrate the technical solutions 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 of ordinary skill in the art should understand that the technical solutions of the present invention can be modified or equivalently replaced without departing from the essence and scope of the technical solutions of the present invention.

Claims

1. A highly permeable composition, characterized in that, By mass parts, the composition consists of the following components: Tetra - isopalmitoyl ascorbate 5 - 10 parts; Angelica archangelica root oil 0.6 - 1 part; Pelargonium graveolens leaf oil 1 - 3 parts; Evening primrose oil 0.2 - 0.4 part.

2. The highly permeable composition according to claim 1, characterized in that, By mass parts, the composition consists of the following components: Tetra - isopalmitoyl ascorbate 7 parts; Angelica archangelica root oil 0.8 part; Pelargonium graveolens leaf oil 2 parts; Evening primrose oil 0.3 part.

3. Use of the high - permeability composition according to claim 1 or 2 in the preparation of a skin - care product having whitening, freckle - lightening and / or antioxidant effects.

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

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

6. The whitening and moisturizing essence according to claim 5, characterized in that, The whitening skin - care essence further 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 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 disodium EDTA; The emulsifier is laureth - 23; The preservative is phenoxyethanol; The solvent is deionized water.

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