Solubilized compositions and uses thereof

Abstract

The application provides a solubilizing composition and its use, and a cosmetic composition comprising the solubilizing composition. The solubilizing composition comprises a polar oil and a PEG solubilizer, wherein the mass ratio of the PEG solubilizer and the polar oil is greater than 1:1. The solubilizing composition of the application can realize solubilization without relying on a complex composition system, has a good solubilization effect on fat-soluble active substances, can reduce the amount of solubilizer, ensures the transparency of the solution, reduces the stickiness and irritation on the skin, and is very suitable for practical product application.

Description

Technical Field

[0001] This application belongs to the field of cosmetic technology, specifically relating to a solubilizing composition and its use. Background Technology

[0002] Lipid-soluble cosmetic active ingredients such as retinol and its derivatives, tocopherol and its derivatives, lipid-soluble ascorbic acid derivatives, bakuchiol, and coenzyme Q10 are widely used in whitening and anti-aging cosmetics due to their excellent functionality. However, these active ingredients are all lipid-soluble and almost insoluble in water, which greatly limits their practical application. In particular, how to add these lipid-soluble active ingredients to transparent aqueous products has always been a problem that needs to be solved in this field.

[0003] Solubilization technology refers to the technique of increasing the solubility of poorly soluble oils by adding surfactants with high HLB values. The solubilization mechanism involves the surfactant spontaneously forming micelles in water. Based on the principle of "like dissolves like," the surfactant can dissolve poorly soluble oils by encapsulating them within the hydrocarbon core, on the hydrophilic chains of polyethylene oxide, or by binding them to the micelle grid layer or surface. In practical applications, to maximize the transparency of aqueous products and provide consumers with a clear and refreshing appearance, a relatively large amount of solubilizer is often added. However, this results in a sticky feel on the skin. Summary of the Invention

[0004] To address the above problems, this application provides a solubilizing composition comprising polar oils and PEG-based solubilizers. The solubilizing composition can act as a novel solubilizer to effectively dissolve lipophilic active ingredients in water, thereby reducing the amount of solubilizer required.

[0005] Specifically, this application relates to the following aspects:

[0006] 1. A solubilizing composition comprising a polar oil and a PEG-based solubilizer, wherein the mass ratio of the PEG-based solubilizer to the polar oil is greater than 1:1;

[0007] The polar oils include one or both of the following: polar oils containing triglycerides and polar oils containing amino acid structures.

[0008] 2. The solubilizing composition according to claim 1, wherein the mass ratio of the PEG-based solubilizer to the polar oil is (2.5-9):1.

[0009] 3. The solubilizing composition according to item 1 or 2, wherein the degree of polymerization of the PEG-based solubilizer is 30-80, preferably including one or both of PEG-40 hydrogenated castor oil and PEG-60 hydrogenated castor oil.

[0010] 4. Use of the solubilizing composition according to any one of items 1-3 in improving the solubility of a fat-soluble active ingredient in water.

[0011] 5. The use according to item 4, wherein the fat-soluble active ingredient comprises one or more of retinol and its derivatives, tocopherol and its derivatives, fat-soluble ascorbic acid derivatives, psoralen, and coenzyme Q10.

[0012] 6. The use according to item 4 or 5, wherein the mass ratio of the lipid-soluble active ingredient to the PEG-based solubilizer is 1:(1.5-9).

[0013] 7. A cosmetic composition comprising the solubilizing composition and the fat-soluble active ingredient as described in any one of claims 1-3.

[0014] 8. The cosmetic composition according to item 7, wherein the mass ratio of the fat-soluble active ingredient to the PEG-based solubilizer is 1:(1.5-9).

[0015] 9. The cosmetic composition according to item 7 or 8, wherein the fat-soluble active ingredient is selected from one or more of retinol and its derivatives, tocopherol and its derivatives, fat-soluble ascorbic acid derivatives, bakuchiol, and coenzyme Q10.

[0016] 10. The cosmetic composition according to any one of claims 7-9, wherein the fat-soluble active ingredient is present in a mass content of 0.01%-5%, the polar oil is present in a mass content of 0.002%-10%, and the PEG-based solubilizer is present in a mass content of 0.015%-10%.

[0017] The solubilizing composition of this application can achieve solubilization without relying on a complex composition system. It not only has a good solubilizing effect on fat-soluble active ingredients, but also reduces the amount of solubilizer used. While ensuring the transparency of the solution, it reduces the stickiness and irritation on the skin, making it very suitable for practical product applications. Detailed Implementation

[0018] The present application is further illustrated below with reference to embodiments. It should be understood that the embodiments are only used to further illustrate and explain the present application and are not intended to limit the present application.

[0019] Unless otherwise defined, technical and scientific terms used in this specification have the same meaning as commonly understood by one of ordinary skill in the art. While similar or identical methods and materials may be applied in experimental or practical applications, materials and methods are described herein. In case of conflict, the definitions included herein shall prevail. Furthermore, materials, methods, and examples are for illustrative purposes only and are not intended to be limiting. The present application is further described below with reference to specific embodiments, but is not intended to limit the scope of the application.

[0020] Composition

[0021] One subject matter of this application relates to compositions, which are defined as long as they achieve the effects of this application. The "composition" includes, but is not limited to, the simultaneous or sequential use of the components. "Simultaneous use" includes using them together in the same formulation or separately in different formulations. "Sequential use" includes using them sequentially in different formulations, with no restriction on the order of sequential use.

[0022] This application provides a solubilizing composition comprising a polar oil and a PEG-based solubilizer, wherein the mass ratio of the PEG-based solubilizer to the polar oil is greater than 1:1, for example, it can be 1.01:1, 1.1:1, 1.2:1, 1.3:1, 1.4:1, 1.5:1, 1.6:1, 1.7:1, 1.8:1, 1.9:1, 2:1, 2.1:1, 2.2:1, 2.3:1, 2.4:1, etc. 2.5:1, 2.6:1, 2.7:1, 2.8:1, 2.9:1, 3:1, 3.1:1, 3.2:1, 3.3:1, 3.4:1, 3.5:1, 3.6:1, 3.7:1, 3.8:1, 3.9:1, 4:1, 4.1:1, 4.2:1, 4.3:1, 4.4:1, 4.5:1, 4.6:1, 4.7:1, 4.8:1, 4.9:1, 5:1 5.1:1, 5.2:1, 5.3:1, 5.4:1, 5.5:1, 5.6:1, 5.7:1, 5.8:1, 5.9:1, 6:1, 6.1:1, 6.2:1, 6.3:1, 6.4:1, 6.5:1, 6.6:1, 6.7:1, 6.8:1, 6.9:1, 7:1, 7.1:1, 7.2:1, 7.3:1, 7.4:1, 7.5:1, 7.6: 1, 7.7:1, 7.8:1, 7.9:1, 8:1, 8.1:1, 8.2:1, 8.3:1, 8.4:1, 8.5:1, 8.6:1, 8.7:1, 8.8:1, 8.9:1, 9:1, 10:1, 11:1, 12:1, 13:1, 14:1, 15:1, 16:1, 17:1, 18:1, 19:1, 20:1, and any range between these values.

[0023] In one specific embodiment, the mass ratio of the PEG-based solubilizer to the polar oil is (2.5-9):1.

[0024] In one specific embodiment, the polar oil includes one or both of the following: polar oil containing triglycerides and polar oil containing amino acid structures.

[0025] In one specific embodiment, the triglyceride-containing polar oil can be a triglyceride-containing polar synthetic oil or a triglyceride-containing polar vegetable oil. The triglyceride-containing polar synthetic oil may include caprylic / capric triglycerides, etc., and the triglyceride-containing vegetable oil may include sunflower seed oil, castor seed oil, sweet almond oil, jojoba seed oil, shea butter, grape seed oil, camellia seed oil, meadowfoam seed oil, coconut oil, oat kernel oil, olive fruit oil, etc. The amino acid-containing polar oil includes N-lauroyl glutamate isopropyl ester, etc.

[0026] In one specific embodiment, the degree of polymerization of the PEG-based solubilizer is 30-80, for example, the degree of polymerization can be 30, 35, 40, 45, 50, 55, 60, 65, 70, 75, 80, etc.

[0027] In one specific embodiment, the PEG-based solubilizer includes one or both of PEG-40 hydrogenated castor oil and PEG-60 hydrogenated castor oil.

[0028] In one specific embodiment, the solubilizing composition includes a polar oil and a PEG-based solubilizer, wherein the mass ratio of the PEG-based solubilizer to the polar oil is greater than 1:1, the polar oil includes one or both of the following: a triglyceride-containing polar oil and a polar oil containing an amino acid structure, and the degree of polymerization of the PEG-based solubilizer is 30-80.

[0029] In one specific embodiment, the solubilizing composition includes a polar oil and a PEG-based solubilizer, wherein the mass ratio of the PEG-based solubilizer to the polar oil is (2.5-9):1, the polar oil includes one or both of triglyceride-containing polar oil and amino acid-containing polar oil, and the degree of polymerization of the PEG-based solubilizer is 30-80.

[0030] In one specific embodiment, the solubilizing composition comprises a polar oil and a PEG-based solubilizer, wherein the mass ratio of the PEG-based solubilizer to the polar oil is (2.5-9):1, the polar oil comprises one or more of caprylic / capric triglycerides, N-lauroyl glutamate isopropyl ester, sunflower seed oil, and castor seed oil, and the PEG-based solubilizer comprises one or two of PEG-40 hydrogenated castor oil and PEG-60 hydrogenated castor oil.

[0031] In one specific embodiment, the solubilizing composition comprises a polar oil and a PEG-based solubilizer, wherein the mass ratio of the PEG-based solubilizer to the polar oil is greater than 1:1, the polar oil includes one or both of the following: a triglyceride-containing polar oil and a polar oil containing an amino acid structure, and the degree of polymerization of the PEG-based solubilizer is 30-80.

[0032] In one specific embodiment, the solubilizing composition comprises a polar oil and a PEG-based solubilizer, wherein the mass ratio of the PEG-based solubilizer to the polar oil is (2.5-9):1, the polar oil includes one or both of the following: a triglyceride-containing polar oil and a polar oil containing an amino acid structure, and the degree of polymerization of the PEG-based solubilizer is 30-80.

[0033] In one specific embodiment, the solubilizing composition comprises a polar oil and a PEG-based solubilizer, wherein the mass ratio of the PEG-based solubilizer to the polar oil is (2.5-9):1, the polar oil includes one or more of caprylic / capric triglycerides, N-lauroyl glutamate isopropyl ester, sunflower seed oil, and castor seed oil, and the PEG-based solubilizer includes one or two of PEG-40 hydrogenated castor oil and PEG-60 hydrogenated castor oil.

[0034] The solubilizing composition of this application has a simple composition and can achieve solubilization without relying on a complex system. It can reduce the stickiness and irritation on the skin while ensuring the transparency of the solution, making it very suitable for practical product applications.

[0035] This application also provides the use of any of the above-mentioned solubilizing compositions in improving the solubility of lipophilic active ingredients in water.

[0036] The fat-soluble active ingredients may include one or more of retinol and its derivatives, tocopherol and its derivatives, fat-soluble ascorbic acid derivatives, psoralen, and coenzyme Q10.

[0037] Retinol and its derivatives include one or more of retinol, retinyl palmitate, retinyl propionate, retinyl acetate, hydroxypinazone retinoate, retinyl linoleate, and retinyl retinoate.

[0038] Tocopherol and its derivatives include one or more of tocopherol, tocopherol acetate, tocopherol succinate, tocopherol nicotinate, tocopherol palmitate, tocopherol linoleate, and tocopherol linoleate / oleate.

[0039] Fat-soluble ascorbic acid derivatives include one or more of ascorbic acid tetraisopalmitate, ascorbic acid palmitate, ascorbic acid stearate, and ascorbic acid dipalmitate.

[0040] In one specific embodiment, the mass ratio of the lipid-soluble active ingredient to the PEG-based solubilizer is 1:(1.5-9), for example, it can be 1.5:1, 1.6:1, 1.7:1, 1.8:1, 1.9:1, 2:1, 2.1:1, 2.2:1, 2.3:1, 2.4:1, 2.5:1, 2.6:1, 2.7:1, 2.8:1, 2.9:1, 3:1, 3.1:1, 3.2:1, 3.3:1, 3.4:1, 3.5:1, 3.6:1, 3.7:1, 3.8:1, 3.9:1, 4:1, 4.1:1, 4.2:1, 4.3:1, 4.4:1, 4.5:1, 4.6:1, 4.7:1, 4.8:1, 4.9:1, etc. 5:1, 5.1:1, 5.2:1, 5.3:1, 5.4:1, 5.5:1, 5.6:1, 5.7:1, 5.8:1, 5.9:1, 6:1, 6.1:1, 6.2:1, 6.3:1, 6.4:1, 6.5:1, 6.6:1, 6.7:1, 6.8:1, 6.9:1, 7:1, 7.1:1, 7.2:1, 7.3:1, 7.4:1, 7.5:1, 7.6:1, 7.7:1, 7.8:1, 7.9:1, 8:1, 8.1:1, 8.2:1, 8.3:1, 8.4:1, 8.5:1, 8.6:1, 8.7:1, 8.8:1, 8.9:1, 9:1, and any range between these values.

[0041] This application also provides a cosmetic composition comprising any one of the above-described solubilizing compositions and a fat-soluble active ingredient. The fat-soluble active ingredient is as defined above.

[0042] In one specific embodiment, the fat-soluble active ingredient in the cosmetic composition has a mass content of 0.01%-5%, for example, 0.01%, 0.1%, 0.5%, 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, and any range between these values; the polar oil has a mass content of 0.002%-10%, for example, 0.002%, 0.01%, 0.1%, 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%. The mass content of the PEG-based solubilizer is 0.015%-10%, for example, it can be 0.015%, 0.05%, 1%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, 5.5%, 6%, 6.5%, 7%, 7.5%, 8%, 8.5%, 9%, 9.5%, 10%, and any range between these values.

[0043] In one specific embodiment, in the cosmetic composition, the mass content of the fat-soluble active ingredient is 0.1%-2%, the mass content of the polar oil is 0.02%-5%, and the mass content of the PEG-based solubilizer is 0.2%-5%.

[0044] The cosmetic composition may be an aqueous cosmetic composition or a non-aqueous cosmetic composition.

[0045] In one specific embodiment, the cosmetic composition is an aqueous cosmetic composition, wherein the water content in the aqueous cosmetic composition is greater than 40% by mass, for example, it can be 41%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, and any range between such values.

[0046] In one specific embodiment, the cosmetic composition is an aqueous cosmetic composition, wherein the water content in the aqueous cosmetic composition is greater than 50% by mass.

[0047] In one specific embodiment, the particle size of the cosmetic composition is <120nm, preferably <90nm. The smaller the particle size, the more transparent the cosmetic composition appears, and the better the transdermal effect of the cosmetic.

[0048] In one specific embodiment, the cosmetic composition is an aqueous cosmetic composition, wherein the mass content of the fat-soluble active ingredient is 0.1%-2%, the mass content of the polar oil is 0.02%-5%, the mass content of the PEG-based solubilizer is 0.2%-5%, and the mass content of water is greater than 40%.

[0049] Example

[0050] Example 1

[0051] Take 1g of vitamin E, add 3g of PEG-40 hydrogenated castor oil and 1g of N-lauroyl glutamate isopropyl ester, heat and stir at 60℃, add water to 100g after mixing, stir evenly to obtain the composition.

[0052] Example 2

[0053] The only difference between Example 2 and Example 1 is that PEG-40 hydrogenated castor oil is replaced with PEG-60 hydrogenated castor oil.

[0054] Examples 3-5

[0055] The only difference between Examples 3-5 and Example 1 is the type of oil used. In Example 3, the oil was castor seed oil; in Example 4, the oil was sunflower seed oil; and in Example 5, the oil was caprylic / capric triglyceride.

[0056] Examples 6-12

[0057] The only difference between Examples 6-12 and Example 4 is the amount of PEG-40 hydrogenated castor oil and / or sunflower seed oil added. Specifically,

[0058] In Example 6, the amount of PEG-40 hydrogenated castor oil added was 2g, and the amount of sunflower seed oil added was 0.5g.

[0059] In Example 7, the amount of sunflower seed oil added was 0.2g.

[0060] In Example 8, the amount of sunflower seed oil added was 0.5g.

[0061] In Example 9, 5g of PEG-40 hydrogenated castor oil was added.

[0062] In Example 10, the amount of PEG-40 hydrogenated castor oil added was 5g, and the amount of sunflower seed oil added was 2g.

[0063] In Example 11, 9g of PEG-40 hydrogenated castor oil was added.

[0064] In Example 12, 7g of PEG-40 hydrogenated castor oil was added.

[0065] Example 13

[0066] The difference between Example 13 and Example 4 is that the amount of PEG-40 hydrogenated castor oil added is 1.5g, the amount of fat-soluble active ingredient is 1g of coenzyme Q10, and the amount of sunflower seed oil added is 0.5g.

[0067] Example 14

[0068] The only difference between Example 14 and Example 1 is that the solubilizer also includes 0.5g of polyglycerol-10 laurate.

[0069] Example 15

[0070] The only difference between Example 15 and Example 1 is that the oil also includes 0.5g of squalane.

[0071] Example 16

[0072] The only difference between Example 16 and Example 12 is that the fat-soluble active ingredient is psoralen.

[0073] Comparative Example 1

[0074] The only difference between Comparative Example 1 and Example 1 is that N-lauroyl glutamate isopropyl ester was not added.

[0075] Comparative Examples 2-4

[0076] The only difference between Comparative Examples 2-4 and Comparative Example 1 is the amount of PEG-40 hydrogenated castor oil added. Specifically, 5g of PEG-40 hydrogenated castor oil was added in Comparative Example 2, 7g in Comparative Example 3, and 9g in Comparative Example 4.

[0077] Comparative Example 5

[0078] The only difference between Comparative Example 5 and Example 2 is that N-lauroyl glutamate isopropyl ester was not added.

[0079] Comparative Example 6

[0080] The only difference between Comparative Example 6 and Example 1 is that PEG-40 hydrogenated castor oil was replaced with polyglycerol-10 laurate.

[0081] Comparative Example 7

[0082] The only difference between Comparative Example 7 and Example 1 is that PEG-40 hydrogenated castor oil was replaced with PPG-13-decyltetradecyl alcohol polyether-24.

[0083] Comparative Examples 8-9

[0084] The only difference between Comparative Examples 8-9 and Example 1 is that the types of oils used are different. In Comparative Example 8, N-lauroyl glutamate isopropyl ester was replaced with squalane, and in Comparative Example 9, N-lauroyl glutamate isopropyl ester was replaced with octyldodecyl alcohol.

[0085] Comparative Example 10

[0086] The only difference between Comparative Example 10 and Example 4 is the amount of PEG-40 hydrogenated castor oil added. In Comparative Example 10, the amount of PEG-40 hydrogenated castor oil added was 1g.

[0087] Comparative Example 11

[0088] The only difference between Comparative Example 11 and Example 1 is that PEG-40 hydrogenated castor oil was not added.

[0089] The specific components and their amounts in the above embodiments and comparative examples are shown in Table 1.

[0090] Table 1

[0091]

[0092]

[0093] The particle size and transmittance of the samples prepared in the above examples and comparative examples were measured using an Anton Paar Litesizer 500 instrument, and the results are shown in Table 2.

[0094] Table 2. Performance test results of the solubilizing composition

[0095]

[0096]

[0097] As shown in Table 2, when the solubilizer is a PEG-based solubilizer and a polar oil, it has a good solubilizing effect on lipophilic active ingredients, the solution is transparent, and the particle size is below 50 nm. When the polar oil is replaced with a non-polar oil, squalane, the solubilizing effect is significantly worse, the solution is milky white, and the particle size increases to 413.7 nm. When the PEG-based solubilizer is replaced with other types of solubilizers, it cannot effectively solubilize lipophilic active ingredients, the solution is milky white, and the particle size is generally above 100 nm.

[0098] The comparison between Examples 1-10, 12-16 and Comparative Example 4 shows that, while achieving the same solubilizing effect on lipophilic active ingredients, the solubilizing composition of this application uses a lower content of solubilizer and has a smaller particle size. The comparison between Examples 1-5, 7-8, 15 and Comparative Example 1, and the comparison between Examples 9-10 and Comparative Example 2, all show that, when using the same content of PEG-based solubilizer, the compositions of the examples of this application can achieve the effect of solubilizing lipophilic active ingredients, while the comparative examples cannot achieve the solubilizing effect.

Claims

1. Use of a solubilizing composition in improving the solubility of a fat-soluble active ingredient in water; The solubilizing composition is: (a) One or more of the following: caprylic / capric triglyceride, N-lauroyl glutamate isopropyl ester, sunflower seed oil, and castor seed oil; and (b) One or both of PEG-40 hydrogenated castor oil and PEG-60 hydrogenated castor oil; The mass ratio of (b) to (a) is (2.5-20):1; The mass ratio of the fat-soluble active ingredient to (b) is 1:(1.5-9). The fat-soluble active ingredients include one or more of retinol and its derivatives, tocopherol and its derivatives, fat-soluble ascorbic acid derivatives, psoralen, and coenzyme Q10. Retinol and its derivatives are one or more of retinol, retinyl palmitate, retinyl propionate, retinyl acetate, hydroxypinazone retinate, retinyl linoleate, and retinyl retinoate. Tocopherol and its derivatives are one or more of tocopherol, tocopherol acetate, tocopherol succinate, tocopherol nicotinate, tocopherol palmitate, tocopherol linoleate, and tocopherol linoleate / oleate. The fat-soluble ascorbic acid derivative is one or more of ascorbic acid tetraisopalmitate, ascorbic acid palmitate, ascorbic acid stearate, and ascorbic acid dipalmitate.

2. The use according to claim 1, wherein the mass ratio of (b) to (a) is (2.5-9):

1.

3. A cosmetic composition comprising a solubilizing composition and a fat-soluble active ingredient; The solubilizing composition is: (a) One or more of the following: caprylic / capric triglyceride, N-lauroyl glutamate isopropyl ester, sunflower seed oil, and castor seed oil; and (b) One or both of PEG-40 hydrogenated castor oil and PEG-60 hydrogenated castor oil; The mass ratio of (b) to (a) is (2.5-20):1; The mass ratio of the fat-soluble active ingredient to (b) is 1:(1.5-9). The fat-soluble active ingredients include one or more of retinol and its derivatives, tocopherol and its derivatives, fat-soluble ascorbic acid derivatives, psoralen, and coenzyme Q10. Retinol and its derivatives are one or more of retinol, retinyl palmitate, retinyl propionate, retinyl acetate, hydroxypinazone retinate, retinyl linoleate, and retinyl retinoate. Tocopherol and its derivatives are one or more of tocopherol, tocopherol acetate, tocopherol succinate, tocopherol nicotinate, tocopherol palmitate, tocopherol linoleate, and tocopherol linoleate / oleate. The fat-soluble ascorbic acid derivative is one or more of ascorbic acid tetraisopalmitate, ascorbic acid palmitate, ascorbic acid stearate, and ascorbic acid dipalmitate.

4. The cosmetic composition according to claim 3, wherein the mass content of the fat-soluble active ingredient in the cosmetic composition is 0.01%-5%, the mass content of (a) is 0.002%-10%, and the mass content of (b) is 0.015%-10%.

5. The cosmetic composition according to claim 3, wherein the mass ratio of (b) to (a) is (2.5-9):1.

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