Preparation method of hydrogenated lysolecithin entrapped whitening composition and application of hydrogenated lysolecithin entrapped whitening composition in preparation of cosmetics

Abstract

The invention discloses a preparation method of a hydrogenated lysolecithin-entrapped whitening composition and application of the hydrogenated lysolecithin-entrapped whitening composition in preparation of cosmetics, and provides a synergistic ratio of pterostilbene and tetrahydromagnolol which are whitening active matters, a nano entrapment technology is adopted, hydrogenated lysolecithin is used as a main emulsifier, and the hydrogenated lysolecithin-entrapped whitening composition is prepared into a cosmetic. The proper co-emulsifier and polyol are searched to entrap the grease which efficiently dissolves the whitening active matter into a stable nano-emulsion, so that pterostilbene and tetrahydromagnolol can permeate into the deep layer of the skin to play an efficient mild whitening role.

Description

Technical Field

[0001] The present invention belongs to the technical field of cosmetics, and particularly relates to a preparation method of a whitening composition encapsulated by hydrogenated lysophosphatidylcholine and its application in the preparation of cosmetics. Background Art

[0002] Hydrogenated lysophosphatidylcholine is a modified phospholipid compound. Compared with hydrogenated phosphatidylcholine, it retains the hydrophilic and lipophilic structures of phospholipids, but reduces the non-polar groups (hydrophobic groups) and has a lower critical micelle concentration (CMC).

[0003] Pterostilbene is a polyphenolic compound of natural origin, and pterostilbene has certain effects in whitening, anti-inflammatory and anti-aging. Research has pointed out that pterostilbene can achieve skin whitening effects by inhibiting melanin and tyrosinase, regulating the Nrf2 pathway to reduce oxidative stress, inhibiting the MC1R / α-MSH pathway, inhibiting melanin transport, and activating autophagy.

[0004] Tetrahydromagnolol is a compound extracted from Magnolia officinalis. Tetrahydromagnolol can not only scavenge free radicals, but also has good inhibitory activity against tyrosinase.

[0005] However, tetrahydromagnolol and pterostilbene are crystalline, and it is easy to precipitate when directly added to the formula, with low bioavailability and limited ability to penetrate deep into the epidermis. Summary of the Invention

[0006] The purpose of this part is to outline some aspects of the embodiments of the present invention and briefly introduce some preferred embodiments.

[0007] As one aspect of the present invention, the present invention provides a preparation method of a whitening composition encapsulated by hydrogenated lysophosphatidylcholine, which includes the following steps:

[0008] Step 1: Dissolve pterostilbene, tetrahydromagnolol, co-emulsifier, and 2,3-butanediol in an oil ester by heating to obtain Composition 1;

[0009] Step 2: Dissolve water, polyol, and hydrogenated lysophosphatidylcholine by heating to obtain Composition 2;

[0010] Step 3: Add Composition 1 to Composition 2, and homogenize and stir until completely emulsified to obtain a primary emulsion;

[0011] Step 4: Prepare a whitening composition carrier by subjecting the primary emulsion obtained in Step 3 to high-pressure microfluidic homogenization;

[0012] Among them, by mass fraction, pterostilbene is 8-10 parts, tetrahydromagnolol is 3-7 parts, hydrogenated lysolecithin is 3-6 parts, oil ester is 15-30 parts, co-emulsifier is 2-5 parts, polyol is 10-30 parts, 2,3-butanediol is 1-3 parts, and the balance is water up to 100 parts.

[0013] As a preferred embodiment of the preparation method of the whitening composition encapsulated by hydrogenated lysolecithin of the present invention: in step 1, the heating temperature is 80-85 °C.

[0014] As a preferred embodiment of the preparation method of the whitening composition encapsulated by hydrogenated lysolecithin of the present invention: in step 1, the mass ratio of pterostilbene to tetrahydromagnolol is (4-5):(2-3).

[0015] As a preferred embodiment of the preparation method of the whitening composition encapsulated by hydrogenated lysolecithin of the present invention: in step 2, the heating temperature is 75-80 °C.

[0016] As a preferred embodiment of the preparation method of the whitening composition encapsulated by hydrogenated lysolecithin of the present invention: in step 3, the homogenization time is 2-5 min, and the rotation speed is 5000-10000 r / s.

[0017] As a preferred embodiment of the preparation method of the whitening composition encapsulated by hydrogenated lysolecithin of the present invention: in step 4, the pressure of high-pressure microfluidic homogenization is 500-800 bar.

[0018] As a preferred embodiment of the preparation method of the whitening composition encapsulated by hydrogenated lysolecithin of the present invention: the co-emulsifier is one or more of glyceryl stearate, glyceryl behenate, cetearyl alcohol, and cetyl palmitate.

[0019] As a preferred embodiment of the preparation method of the whitening composition encapsulated by hydrogenated lysolecithin of the present invention: the polyol is one or more of diglycerol, 1,3-butanediol, polyglycerol-3, and polyglycerol-10.

[0020] The beneficial effects of the present invention: The present invention provides a synergistic ratio of the whitening active substances pterostilbene and tetrahydromagnolol, and adopts a nano-encapsulation technology, using hydrogenated lysolecithin as the main emulsifier, and finding suitable co-emulsifiers and polyols to encapsulate the oil ester that can efficiently dissolve the whitening active substances into a stable nano-emulsion, which is beneficial for pterostilbene and tetrahydromagnolol to penetrate into the deep layer of the skin to exert an efficient and mild whitening effect. Description of the Drawings

[0021] In order to more clearly illustrate the technical solutions of the embodiments of the present invention, the following will briefly introduce the drawings required for the description of the embodiments. Among them:

[0022] Figure 1 Particle size distribution diagram measured by the Zeta potential and nanoparticle size analyzer for Example 1.

[0023] Figure 2 MI value tested for Example 1 within 28 days.

[0024] Figure 3 ITA° test value for Example 1 within 28 days. Detailed implementation manners

[0025] To make the above objects, features, and advantages of the present invention more obvious and understandable, the following detailed description of the specific implementation manners of the present invention will be given in conjunction with specific embodiments.

[0026] Example 1:

[0027] The whitening composition encapsulated by hydrogenated lysophosphatidylcholine of the present invention, calculated by mass fraction, includes 10 parts of pterostilbene (C 16 H 16 O3), 5 parts of tetrahydromagnolol, 3.5 parts of hydrogenated lysophosphatidylcholine (INCl name: HYDROGENATED LYSOLECITHIN, trade name: SLP-LPC70H), 20 parts of isopropyl lauroylsarcosinate, 3 parts of glyceryl stearate, 25 parts of diglycerol, 2 parts of 2,3-butanediol, and the balance is water up to 100 parts.

[0028] 1. Heat pterostilbene, tetrahydromagnolol, glyceryl stearate, isopropyl lauroylsarcosinate, and 2,3-butanediol to 80°C and dissolve them thoroughly to obtain Composition 1;

[0029] 2. Heat water, diglycerol, and hydrogenated lysophosphatidylcholine to 80°C and dissolve them thoroughly to obtain Composition 2;

[0030] 3. Keep at 80°C and add Composition 1 to Composition 2, and homogenize and stir at 5000 r / s for 3 min until completely emulsified to obtain the primary emulsion;

[0031] 4. Use high-pressure microfluidics to circulate the primary emulsion obtained in Step 3 5 times at a pressure of 500 bar to prepare the nanoemulsion of the whitening composition carrier.

[0032] Experimental results: The obtained nanoemulsion is a translucent viscous liquid. Measure its particle size using a Zeta potential and nanoparticle size analyzer; place it in a high and low temperature cycle (-15°C to 48°C) incubator to measure its high and low temperature stability. Figure 1 The particle size distribution diagram measured by the Zeta potential and nanoparticle size analyzer. It can be seen that the nanoemulsion has a relatively concentrated particle size distribution and good dispersion. As shown in Table 1, the average particle size of the nanoemulsion is 70.4 nm.

[0033] Results of the stability experiment: There was no obvious change after one month of cycling.

[0034] Principle of the transdermal experiment: The Franz diffusion cell method was adopted. Using piglet skin as the carrier, it was fixed between the supply chamber and the receiving chamber of the Franz diffusion cell. The diffusion cell was fixed in a transdermal absorption diffuser, and different test samples were added to the skin surface in the chamber for transdermal tests. High-performance liquid chromatography (HPLC) was used to detect the transdermal absorption of the active ingredients in the pig skin extract.

[0035] Experimental materials: Skin of Bama mini-pig.

[0036] Liquid chromatography conditions: Mobile phase: Phase A was acetonitrile, and Phase B was ultrapure water. Detection conditions: Acclaim120 / Thermoscientific C18 (5μm 4.6×250mm) chromatographic column, column temperature 25°C, injection volume 20μL, detection and peak emergence at 280nm. Mobile phase elution conditions: Methanol (A): 0.03 mM phosphate buffer (B) = 85:15, flow rate 1 mL / min, elution for 20 min. Calculate the cumulative permeation amount per unit area and the cumulative retention amount per unit area, expressed in μg / cm 2 ) = Mass of pterostilbene / tetrahydromagnolol cumulatively permeated / diffusion cell area. Cumulative storage amount per unit area (μg / cm 2 ) = Content of pterostilbene / tetrahydromagnolol * total volume of skin extract / permeation area. 2 ) = Mass of pterostilbene / tetrahydromagnolol cumulatively permeated / diffusion cell area. Cumulative storage amount per unit area (μg / cm

[0037] Experimental results: As shown in Tables 4 and 5, Example 1 had good permeation and storage amounts.

[0038] Patch test: Patch test method: Select qualified patch test equipment. Using the closed patch test method, place 0.020 - 0.025 g of the test substance in the patch tester, and apply it to the flexor side of the subject's forearm with a low-sensitization tape. After 24 hours, remove the test substance. 30 minutes after removing the patch tester with the test substance, observe the skin reaction after the indentation disappears. If the result is negative, observe again at 24 h and 48 h after the patch test. Record the reaction results according to the skin adverse reaction grading standard table (as shown in the following table).

[0039] Table 1 Skin reaction grading standard for skin closed patch test

[0040]

[0041] After detection, among 30 people in the human closed skin patch test, 30 people did not show skin adverse reactions. See Table 2 for details.

[0042] Table 2 Summary of results of human patch test for cosmetics

[0043]

[0044]

[0045] Human body whitening efficacy evaluation experiment: Use the Mexameter MX18 probe of the German CK skin tester to measure the skin melanin content (MI value). The higher the measured value, the higher the melanin content in the skin. Use the Colormeter probe to measure the skin brightness (dark yellow degree) (ITA° value): The ITA° value is the skin individual type angle. The larger the ITA° value, the brighter the skin, and vice versa, the darker the skin. After the subjects wash their faces every day, apply the whitening composition carrier at a coating density of 1.25 μL / cm 2 evenly coat the test area, once in the morning and once in the evening every day, and continuously apply for 28 days. Figure 2 is the MI value measured within 28 days, Figure 3 is the ITA° test value within 28 days. It can be seen from the figure that the whitening composition encapsulated by hydrogenated lysophosphatidylcholine can well reduce the skin melanin content and improve the brightness.

[0046] Example 2:

[0047] The difference from Example 1 is only that the co-emulsifier is glyceryl behenate, and other conditions and methods are the same as those in Example 1. Perform stability testing and particle size testing. Results: The stability did not change after one month of cycling. The particle size test is shown in Table 1, and the particle size is larger than that in Example 1.

[0048] Control Example 1:

[0049] In terms of mass fraction, dissolve and mix 10 parts of pterostilbene, 5 parts of tetrahydromagnolol, and 20 parts of isopropyl lauroylsarcosinate at 80 °C and then conduct a transdermal experiment. The results are shown in Tables 4 and 5. The average cumulative permeation amount and storage amount of the two active substances are much smaller than those in Example 1. It shows that the encapsulated whitening composition has better transdermal performance.

[0050] Control Example 2:

[0051] Replace hydrogenated lysophosphatidylcholine with hydrogenated phosphatidylcholine, and keep other conditions the same as those in Example 1. Conduct stability, particle size, and transdermal experiments. Experimental results: The particle size is shown in Table 1, which is larger than that in Example 1. The transdermal performance is shown in Tables 4 and 5.

[0052] Control Example 3:

[0053] The difference compared with Example 1 is only that the addition amount of pterostilbene is 5 parts and the addition amount of tetrahydromagnolol is 10 parts. After performing stability testing, it is found that solids precipitate. It shows that when the addition amount of tetrahydromagnolol is relatively high and the addition ratio is higher than that of pterostilbene, the nanoemulsion is unstable.

[0054] Comparative Example 4:

[0055] The difference compared with Example 1 is only that isopropyl lauroylsarcosinate is replaced with triglyceride caprylate / caprate, and other conditions are the same as those in Example 1. A stability test was carried out, and solids precipitated, indicating that the triglyceride caprylate / caprate has poor solubility in the whitening composition.

[0056] Comparative Example 5:

[0057] The difference compared with Example 1 is only that isopropyl lauroylsarcosinate is replaced with octyldodecanol, and other conditions are the same as those in Example 1. A stability test was carried out, and solids precipitated, indicating that the octyldodecanol has poor solubility in the whitening composition.

[0058] Comparative Example 6:

[0059] The difference compared with Example 1 is only that isopropyl lauroylsarcosinate is replaced with hexyl decanol, and other conditions are the same as those in Example 1. A stability test was carried out, and solids precipitated, indicating that this oil ester has poor solubility in the whitening composition.

[0060] Comparative Example 7:

[0061] Diglycerin was not added, and other conditions were the same as those in Example 1, and a stability test was carried out. The emulsion was white and stratified after being placed at high and low temperatures for a period of time.

[0062] Comparative Example 8:

[0063] The raw materials and their ratios were the same as those in Example 1, and the preparation process was as follows:

[0064] 1. Pterostilbene, tetrahydromagnolol, glyceryl stearate, isopropyl lauroylsarcosinate, and 2,3-butanediol were heated to 80 °C and dissolved thoroughly to obtain Composition 1;

[0065] 2. Water, diglycerin, and hydrogenated lysolecithin were heated to 80 °C and dissolved thoroughly to obtain Composition 2;

[0066] 3. While maintaining 80 °C, Composition 1 was added to Composition 2, and homogenized and stirred for 3 min until completely emulsified to obtain the whitening composition emulsion.

[0067] Stability, particle size, transdermal experiment, and human whitening efficacy evaluation experiment were carried out. The results showed that the emulsion was white, stratified after being placed for a period of time, and solids precipitated. It can also be seen from Table 1 that the particle size was within the range of ordinary emulsions. The transdermal performance was also worse than that of Example 1.

[0068] Table 3

[0069]

[0070]

[0071] Table 4

[0072]

[0073] Table 5

[0074]

[0075] The present invention uses hydrogenated lysophosphatidylcholine to encapsulate pterostilbene and tetrahydromagnolol with low bioavailability to achieve a better whitening and anti-inflammatory effect.

[0076] It should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and not to limit them. 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 spirit and scope of the technical solutions of the present invention, and they should all be covered by the scope of the claims of the present invention.

Claims

1. A method for preparing a whitening composition encapsulated with hydrogenated lysophosphatidylcholine, characterized in that: Comprising the following steps, Step 1: Dissolve pterostilbene, tetrahydromagnolol, co-emulsifier, and 2,3-butanediol by heating in an oil ester to obtain Composition 1; Step 2: Dissolve water, polyol, and hydrogenated lysolecithin by heating to obtain Composition 2; Step 3: Add Composition 1 to Composition 2, and homogenize and stir until completely emulsified to obtain a primary emulsion; Step 4: Use high-pressure microfluidic homogenization on the primary emulsion obtained in Step 3 to prepare a carrier for the whitening composition; wherein, by mass fraction, pterostilbene is 8-10 parts, tetrahydromagnolol is 3-7 parts, hydrogenated lysolecithin is 3-6 parts, oil ester is 15-30 parts, co-emulsifier is 2-5 parts, polyol is 10-30 parts, 2,3-butanediol is 1-3 parts, and the balance is water up to 100 parts.

2. The preparation method of the whitening composition encapsulated by hydrogenated lysophosphatidylcholine according to claim 1, characterized in that: In Step 1, the heating temperature is 80-85°C.

3. The preparation method of the whitening composition encapsulated by hydrogenated lysophosphatidylcholine according to claim 1 or 2, characterized in that: In Step 1, the mass ratio of pterostilbene to tetrahydromagnolol is (4-5):(2-3).

4. The preparation method of the whitening composition encapsulated by hydrogenated lysophosphatidylcholine according to claim 1 or 2, characterized in that: In Step 2, the heating temperature is 75-80°C.

5. The preparation method of the whitening composition encapsulated with hydrogenated lysophosphatidylcholine according to claim 1 or 2, characterized in that: In Step 3, the homogenization time is 2-5 min, and the rotation speed is 5000-10000 r / s.

6. The preparation method of the whitening composition encapsulated with hydrogenated lysophosphatidylcholine according to claim 1 or 2, characterized in that: In Step 4, the pressure of high-pressure microfluidic homogenization is 500-800 bar.

7. The preparation method of the whitening composition encapsulated by hydrogenated lysophosphatidylcholine according to claim 1 or 2, characterized in that: The co-emulsifier is one or more of glyceryl stearate, glyceryl behenate, cetearyl alcohol, and cetyl palmitate.

8. The preparation method of the whitening composition encapsulated with hydrogenated lysophosphatidylcholine according to claim 1 or 2, characterized in that: The polyol is one or more of diglycerol, 1,3-butanediol, polyglycerol-3, and polyglycerol-10.

9. The preparation method of the whitening composition encapsulated by hydrogenated lysophosphatidylcholine according to claim 1 or 2, characterized in that: The oil ester is isopropyl lauroyl sarcosinate.

10. Use of the whitening composition encapsulated with hydrogenated lysophosphatidylcholine prepared by the preparation method of the whitening composition encapsulated with hydrogenated lysophosphatidylcholine according to claim 1 in the preparation of a cosmetic having a whitening effect, characterized in that: The cosmetic includes essence, mask, lotion, or cream.

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