Retinol anti-wrinkle soothing nano composition

The microbead emulsification film formed by self-emulsification reaction of polyglycerol-6 benzene and polyglycerol-6 stearate encapsulate retinol, and combined with microjet and nano-treatment treatment, the problems of large emulsification dose and obvious side effects in the prior art are solved, and the efficient absorption and stability of retinol are achieved.

CN119499122APending Publication Date: 2025-02-25AIRONGZHUYAN (SHANGHAI) BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202411723213.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-11-28
Publication Date
2025-02-25

AI Technical Summary

Technical Problem

The emulsifiers used in existing retinol nanoemulsions contain a large amount of polysorbate-20/80 or polyglycerol-10 myristate, resulting in large emulsification doses, poor absorption of active substances, and possible introduction of petroleum-derived dimethyl ether and carcinogen oxopentane, resulting in transdermal malabsorption, irritation and obvious side effects.

Method used

Polyglycerol-6 benzyl ester and polyglycerol-6 stearate were used to form an emulsified film composed of microbead particles and encapsulate retinol. Combined with microjet treatment and nano-treatment treatment, a retinol anti-wrinkle soothing nanocomposition with good stability was prepared.

Benefits of technology

Through this method, the emulsified particle size of retinol is smaller, and it is easy to form a self-microemulsification system, with better stability, improved skin absorption effect and reduced side effects.

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Abstract

The invention relates to a retinol anti-wrinkle soothing nano composition, which is prepared from the following components in percentage by weight: 0.1 to 3 percent of polyglycerol-6 behenate, 0.5 to 10 percent of polyglycerol-6 stearate, 0.1 to 5 percent of hydrogenated lecithin, 0.1 to 15 percent of retinol, 5 to 35 percent of glycerol, 5 to 30 percent of GTCC and the balance of water. The adopted polyglycerol-6 behenate is used as a self-emulsifying emulsifier, can be emulsified in a small amount, and is subjected to a self-emulsifying reaction with the polyglycerol-6 stearate to form an emulsifying film consisting of microbead particles and wrap the retinol, so that a self-micro-emulsifying system which is smaller in emulsifying particle size and easy to form is formed, and the retinol is kept for a long time and absorbed by the skin; and the stability is better.
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Description

Technical Field

[0001] The invention relates to the technical field of cosmetic formulas, and in particular to a retinol anti-wrinkle and soothing nanometer composition and a preparation method thereof. Background Art

[0002] Retinol, also known as vitamin A alcohol, is a fat-soluble vitamin with powerful antioxidant effects. In the field of medical beauty, retinol can promote skin renewal, increase collagen production, and is used to treat acne, fine lines and sagging skin. In the cosmetics industry, retinol is added to skin care products for anti-aging, whitening and improving skin texture.

[0003] Therefore, based on the effects of retinol in promoting cell growth, accelerating cell regeneration, reducing fine lines, and anti-oxidation, it has become a widely used anti-wrinkle ingredient that is deeply loved by beauty lovers. For example, the invention patent with publication number CN118284402A discloses a cosmetic composition containing a large amount of retinol. The cosmetic composition also contains a variety of non-ionic emulsifiers, fatty alcohols, fatty compounds, thickening polymers and water. The cosmetic composition is applied to the skin to promote the production of collagen and / or elastin, and reduce the appearance of fine lines, wrinkles and uneven skin color.

[0004] However, the application of single retinol in cosmetics still has limitations. For example, the retinol nanoemulsions on the market mostly use emulsifiers containing a large amount of polysorbate-20 / 80 or polyglycerol-10 myristate, which are characterized by using high HLB values ​​for emulsification, but the required emulsifier dosage is relatively large, and the amount of emulsifier will have a negative effect on the absorption of active ingredients. In addition, the polyether-derived emulsifier will inevitably bring in dimethyl ether from petroleum during its synthesis process, and the product contains oxadiazine, which is a carcinogen and is difficult to remove. Therefore, these products often cause poor transdermal absorption, and obvious side effects such as irritation, itching, peeling, and erythema. Summary of the invention

[0005] In order to solve the above problems, the present invention provides a retinol anti-wrinkle soothing nanocomposition, a preparation method thereof and an application thereof.

[0006] In one aspect of the present invention, a retinol anti-wrinkle soothing nanocomposition is provided, comprising the following components in percentage by weight:

[0007] 0.1-3% polyglyceryl-6 behenate, 0.5-10% polyglyceryl-6 stearate, 0.1-5% hydrogenated lecithin, 0.1-15% retinol, 5-35% glycerol, 5-30% GTCC and the balance water.

[0008] As an optional embodiment of the present invention, optionally, the ratio of the polyglyceryl-6 behenate to the polyglyceryl-6 stearate is 1:3-6.

[0009] As an optional embodiment of the present invention, optionally, in the retinol anti-wrinkle soothing nanocomposition, the turbidity (NTU) of the retinol at a concentration of 0.1% satisfies:

[0010] NTU≤10.

[0011] In another aspect of the present invention, a method for preparing a retinol anti-wrinkle soothing nanocomposition is provided, comprising the following steps:

[0012] S1. Add GTCC, retinol, hydrogenated lecithin, polyglyceryl-6 behenate, polyglyceryl-6 stearate and glycerin in sequence at 50-65° C. and stir to disperse uniformly into phase A;

[0013] S2. Add 50-65° C. water to the phase A in step S1, and stir to disperse evenly to form phase B;

[0014] S3, homogenizing the phase B in step S2 at 50-65° C. and 3000 rpm for 5 min to obtain a crude emulsion;

[0015] S4, subjecting the crude emulsion in step S3 to microfluidization treatment three times at a pressure of 700 bar to obtain a crude emulsion dispersion;

[0016] S5, subjecting the crude emulsion dispersion in step S4 to nano-treatment to obtain the anti-wrinkle nano-composition.

[0017] As an optional embodiment of the present invention, optionally, the polyglyceryl-6 behenate and the polyglyceryl-6 stearate react through self-emulsification to form an emulsified film composed of micro-bead particles and encapsulate the retinol.

[0018] As an optional embodiment of the present invention, optionally, the particle size of the microbead particles is generally 25 to 65 nanometers.

[0019] As an optional embodiment of the present invention, optionally, the polyglycerol adopts liposome microcapsule encapsulation technology to form liposome microcapsules and encapsulate the emulsified membrane.

[0020] As an optional embodiment of the present invention, optionally, S4, subjecting the crude emulsion in step S3 to microfluidization treatment three times at a pressure of 700 bar to obtain a crude emulsion dispersion, comprising:

[0021] Crude emulsion preparation: preparing the crude emulsion to be processed, ensuring that its composition and proportion meet the requirements of subsequent processing;

[0022] Microfluidization treatment: Select suitable microfluidization emulsification equipment, and select a microfluidizer with a T-shaped structure, a flow focusing structure or a co-flow structure according to the needs; process the crude emulsion through the microfluidizer; under the action of high pressure, the particles in the crude emulsion are subjected to strong shearing and collision in the microchannel, thereby breaking into smaller droplets;

[0023] Collect the product: After the emulsion is treated with microfluidization, its particle size and dispersibility will be improved. Collect the treated product and conduct necessary tests and evaluations to determine whether the particle size and dispersibility of the product are qualified:

[0024] If qualified, the crude emulsion dispersion is obtained;

[0025] Otherwise, repeat the above microfluidization steps.

[0026] In another aspect, the present invention further provides a retinol anti-wrinkle soothing nano composition comprising the retinol anti-wrinkle soothing nano composition.

[0027] Technical effects of the present invention:

[0028] The polyglyceryl-6 behenate used in the present invention is a self-emulsifying emulsifier, which can be emulsified in a small amount, and through a self-emulsification reaction with polyglyceryl-6 stearate, an emulsified film composed of micro-bead particles is formed to encapsulate retinol, thereby forming a self-micro-emulsifying system with a smaller emulsified particle size and easy to form, so that retinol can be retained for a long time and absorbed by the skin, and its stability is better.

[0029] Further features and aspects of the present invention will become apparent from the following detailed description of exemplary embodiments with reference to the attached drawings. BRIEF DESCRIPTION OF THE DRAWINGS

[0030] The accompanying drawings, which are incorporated in and constitute a part of the specification, illustrate exemplary embodiments, features, and aspects of the invention and, together with the description, serve to explain the principles of the invention.

[0031] Figure 1 Shown is a composition ratio ingredient table of the present invention;

[0032] Figure 2 The experimental data table showing the influence of different proportions on stability of the present invention is shown;

[0033] Figure 3 The experimental data table showing the influence of the lowest ratio and the highest ratio on the stability of the present invention is shown;

[0034] Figure 4 The table shows the experimental data of the effects of different emulsifier types on stability of the present invention;

[0035] Figure 5 The experimental data table showing the effects of different phospholipid types on stability of the present invention is shown. DETAILED DESCRIPTION

[0036] Various exemplary embodiments, features and aspects of the present invention will be described in detail below with reference to the accompanying drawings. The same reference numerals in the accompanying drawings represent elements with the same or similar functions. Although various aspects of the embodiments are shown in the accompanying drawings, the drawings are not necessarily drawn to scale unless otherwise specified.

[0037] The word “exemplary” is used exclusively herein to mean “serving as an example, example, or illustration.” Any embodiment described herein as “exemplary” is not necessarily to be construed as preferred or advantageous over other embodiments.

[0038] In addition, in order to better illustrate the present invention, numerous specific details are provided in the following specific embodiments. It should be understood by those skilled in the art that the present invention can also be implemented without certain specific details. In some examples, means, components and circuits well known to those skilled in the art are not described in detail in order to highlight the subject matter of the present invention.

[0039] The present invention provides a retinol anti-wrinkle soothing nanocomposition, comprising the following components in percentage by mass:

[0040] 0.1-3% polyglyceryl-6 behenate, 0.5-10% polyglyceryl-6 stearate, 0.1-5% hydrogenated lecithin, 0.1-15% retinol, 5-35% glycerol, 5-30% GTCC and the balance water.

[0041] See the attached table for specific ratios. Figure 1 shown.

[0042] Wherein, the ratio of the polyglyceryl-6 behenate to the polyglyceryl-6 stearate is 1:3 to 6. In the retinol anti-wrinkle soothing nanocomposition, the turbidity (NTU) of the retinol at a concentration of 0.1% satisfies:

[0043] NTU≤10.

[0044] The present invention also provides a method for preparing a retinol anti-wrinkle soothing nanocomposition, comprising the following steps:

[0045] S1. Add GTCC, retinol, hydrogenated lecithin, polyglyceryl-6 behenate, polyglyceryl-6 stearate and glycerin in sequence at 50-65° C. and stir to disperse uniformly into phase A;

[0046] S2. Add 50-65° C. water to the phase A in step S1, and stir to disperse evenly to form phase B;

[0047] S3, homogenizing the phase B in step S2 at 50-65° C. and 3000 rpm for 5 min to obtain a crude emulsion;

[0048] S4, subjecting the crude emulsion in step S3 to microfluidization treatment three times at a pressure of 700 bar to obtain a crude emulsion dispersion;

[0049] S5, subjecting the crude emulsion dispersion in step S4 to nano-treatment to obtain the anti-wrinkle nano-composition.

[0050] In this embodiment, the reaction process of using polyglyceryl-6 behenate and polyglyceryl-6 stearate to form an emulsified film composed of micro-bead particles and encapsulate retinol molecules can be carried out by following the steps below:

[0051] 1. Raw material preparation

[0052] Polyglyceryl-6 Behenate: Ensure that the raw materials are pure and free of impurities, and weigh them according to the formula.

[0053] Polyglyceryl-6 Stearate: Also ensure that the raw materials are pure and free of impurities, and weigh according to the formula.

[0054] Retinol (Vitamin A): Accurately weigh the required amount and store it away from light to prevent oxidation.

[0055] Auxiliary solvent / emulsifier (if necessary): Depending on the formula, some auxiliary solvent or emulsifier may be needed to optimize the emulsification effect, so prepare them in advance.

[0056] Aqueous phase: Prepare an appropriate amount of deionized water or purified water as the aqueous phase.

[0057] 2. Preheating and mixing

[0058] Preheating: Preheat polyglyceryl-6 behenate and polyglyceryl-6 stearate to a suitable temperature (generally not exceeding their melting point to avoid damaging the structure) to facilitate the subsequent emulsification process.

[0059] Mixing the oil phase: uniformly mix the preheated polyglyceryl-6 behenate and polyglyceryl-6 stearate in a predetermined ratio to form an oil phase mixture.

[0060] 3. Emulsification pre-treatment

[0061] Retinol dissolution: Dissolve retinol in an appropriate amount of oil phase mixture, ensuring full dissolution to avoid crystallization.

[0062] Preparation of water phase: Heat the water phase to a temperature close to that of the oil phase to reduce the impact of temperature difference on the emulsification effect.

[0063] 4. Self-emulsification reaction

[0064] Slowly add the water phase: Under stirring, slowly add the preheated water phase to the oil phase mixture to start the self-emulsification process.

[0065] High-speed stirring: Use a high-speed stirrer to stir thoroughly to promote rapid mixing of the oil phase and the water phase and form a stable emulsified system.

[0066] Temperature control: Maintain appropriate temperature during the emulsification process to avoid excessively high or low temperatures that affect the emulsification effect.

[0067] 5. Microbead particle formation and encapsulation

[0068] Continue stirring: As stirring continues, the oil droplets in the emulsified system will gradually become smaller and form micro-bead particles.

[0069] Encapsulates retinol: These microbead particles will encapsulate the retinol molecules dissolved in them during the formation process, forming an emulsified film.

[0070] Stabilization treatment: By adjusting the pH value, adding stabilizers, etc., the stability of the emulsification system is improved to ensure that the micro-bead particles will not aggregate or break.

[0071] 6. Post-processing and testing

[0072] Cooling: Gradually cool the emulsified system to room temperature to avoid rapid cooling that may cause system instability.

[0073] Filtration and purification: Remove incompletely emulsified particles and impurities through filtration to improve the purity of the product.

[0074] Quality testing: Conduct quality testing on the final product, including particle size distribution, encapsulation efficiency, stability and other indicators to ensure that the product meets the requirements.

[0075] 7. Packaging and storage

[0076] Aseptic packaging: Packaging under aseptic conditions to prevent microbial contamination.

[0077] Store away from light: Because retinol is light-sensitive, the product should be stored in a dark, cool, dry place.

[0078] Through the above steps, an emulsion film composed of micro-bead particles formed by self-emulsification reaction of polyglyceryl-6 behenate and polyglyceryl-6 stearate can be successfully prepared, and a product that effectively encapsulates retinol molecules can be prepared.

[0079] The specific reagents and equipment used can be provided by a biochemical laboratory or purchased on the market, and the present invention is not limited thereto.

[0080] The following will combine various embodiments and comparative examples to describe in detail the application effects and characteristics of the present invention from the perspectives of proportion, emulsifier type, phospholipid type and process.

[0081] The material ratios of each embodiment and comparative example are as follows:

[0082] Example 1

[0083] 0.1% polyglyceryl-6 behenate, 0.3% polyglyceryl-6 stearate, 0.1% hydrogenated lecithin, 0.1% retinol, 5% glycerin, 5% GTCC and the balance water.

[0084] Example 2

[0085] 1% Polyglyceryl-6 Behenate, 4% Polyglyceryl-6 Stearate, 0.5% Hydrogenated Lecithin, 5% Retinol, 35% Glycerin, 10% GTCC and the balance Water.

[0086] Example 3

[0087] 1% Polyglyceryl-6 Behenate, 5% Polyglyceryl-6 Stearate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0088] Example 4

[0089] 1.67% polyglyceryl-6 behenate, 10% polyglyceryl-6 stearate, 3% hydrogenated lecithin, 15% retinol, 20% glycerin, 20% GTCC and the balance water.

[0090] Example 5

[0091] 3% Polyglyceryl-6 Behenate, 9% Polyglyceryl-6 Stearate, 2% Hydrogenated Lecithin, 15% Retinol, 20% Glycerin, 10% GTCC and the balance Water.

[0092] Example 6

[0093] 2% Polyglyceryl-6 Behenate, 6% Polyglyceryl-6 Stearate, 5% Hydrogenated Lecithin, 10% Retinol, 20% Glycerin, 16% GTCC and the balance Water.

[0094] Comparative Example 1

[0095] 1% Polyglyceryl-6 Behenate, 7% Polyglyceryl-6 Stearate, 5% Hydrogenated Lecithin, 10% Retinol, 20% Glycerin, 16% GTCC and the balance Water

[0096] Comparative Example 2

[0097] 2% Polyglyceryl-6 Behenate, 4% Polyglyceryl-6 Stearate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0098] Comparative Example 3

[0099] 3% Polyglyceryl-6 Behenate, 6% Polyglyceryl-6 Stearate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0100] Comparative Example 4

[0101] 1% self-emulsifying monoglyceride, 5% polyglyceryl-6 stearate, 2% hydrogenated lecithin, 10% retinol, 10% glycerin, 30% GTCC and the balance water.

[0102] Comparative Example 5

[0103] 1% Polyglyceryl-6 Behenate, 5% Polyglyceryl-10 Myristic Acid, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0104] Comparative Example 6

[0105] 1% polyglyceryl-6 behenate, 5% polyglyceryl-6 oleate, 2% hydrogenated lecithin, 10% retinol, 10% glycerin, 30% GTCC and the balance water.

[0106] Comparative Example 7

[0107] 1% Polyglyceryl-6 Behenate, 5% Polyglyceryl-6 Isostearate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0108] Comparative Example 8

[0109] 1% polyglyceryl-6 behenate, 5% polyglyceryl-4 oleate, 2% hydrogenated lecithin, 10% retinol, 10% glycerin, 30% GTCC and the balance water.

[0110] Comparative Example 9

[0111] 1% Polyglyceryl-6 Behenate, 5% Polyglyceryl-6 Ricinoleate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0112] Comparative Example 10

[0113] 3% Polyglyceryl-6 Behenate, 6% Polyglyceryl-6 Stearate, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0114] Comparative Example 11

[0115] 3% Polyglyceryl-6 Behenate, 6% Polyglyceryl-6 Stearate, 2% Phosphatidylserine, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0116] Comparative Example 12

[0117] 3% polyglyceryl-6 behenate, 6% polyglyceryl-6 stearate, 2% phosphatidylcholine, 10% retinol, 10% glycerin, 30% GTCC and the balance water.

[0118] Comparative Example 13

[0119] 3% Polyglyceryl-6 Behenate, 6% Polyglyceryl-6 Stearate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0120] Comparative Example 14

[0121] 6% Polyglyceryl-6 Stearate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0122] Comparative Example 15

[0123] 6% Polyglyceryl-6 Behenate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0124] Comparative Example 16

[0125] 8% Polyglyceryl-6 Stearate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0126] Comparative Example 17

[0127] 8% Polyglyceryl-6 Behenate, 2% Hydrogenated Lecithin, 10% Retinol, 10% Glycerin, 30% GTCC and the balance Water.

[0128] The embodiments and comparative examples relate to polyglycerol emulsifier HLB emulsification values ​​as follows:

[0129] Polyglyceryl-6 behenate (self-emulsifying), polyglyceryl-6 stearate (HLB 9), polyglyceryl-10 myristic acid (HLB 14), polyglyceryl-6 oleate (HLB 12), polyglyceryl-6 isostearate

[0130] (HLB 11), polyglyceryl-4 oleate (HLB 9), polyglyceryl-6 ricinoleate (HLB 4).

[0131] 1. Effect of different ratios on stability

[0132] In order to explore the characteristics of the performance of the composition with different ratios of components, based on the composition formula proposed in the present invention, 6 groups of compositions with different ratios were constructed: Example 1-Example 6 (see Appendix for details) Figure 2 ratio shown).

[0133] Under the same process (microfluidization) experimental conditions, studies were conducted from the dimensions of 0.1% retinol turbidity (NTU), appearance, stability and retinol transdermal detection.

[0134] As attached Figure 2 As shown, we can find that:

[0135] The formula used in the present invention maintains uniform test results in terms of water solubility, appearance and stability. As the proportion of polyglyceryl-6 behenate and polyglyceryl-6 stearate increases, the corresponding retinol meter transdermal absorption / test results also show an overall upward trend. This shows that the emulsified film composed of microbead particles formed by the self-emulsification reaction of polyglyceryl-6 behenate and polyglyceryl-6 stearate can effectively wrap retinol molecules and protect them from entering the subcutaneous layer and being absorbed by the skin layer.

[0136] Even with the lowest ratio, this formula can still maintain 80.9% of the retinol transdermal absorption / test results, and the highest is 92.0%.

[0137] 2. Effect of minimum and maximum ratios on stability

[0138] As attached Figure 3 As shown, comparative examples 1 to 3 are set here, wherein comparative example 1 adopts the lowest proportion of polyglycerol emulsifier, and comparative example 2 adopts the highest proportion of polyglycerol emulsifier.

[0139] By comparing Comparative Example 1 with Example 6, when the proportion of polyglyceryl-6 stearate is high (exceeding the maximum polyglyceryl-6 stearate limit of this formula), the prepared composition has stratification, emulsification exceeds the limit, and water-insoluble emulsifier appears. And because of the stratification caused by the presence of water-insoluble polyglyceryl-6 stearate in the composition, the retinol molecules cannot be absorbed through the skin, and its absorption rate is reduced to 30.3%.

[0140] On the contrary, in Comparative Example 2, compared with Example 3, a high proportion of polyglyceryl-6 behenate was used, and the above-mentioned stratification and the lowest transdermal absorption rate were also observed.

[0141] Therefore, the ratio of polyglyceryl-6 behenate and polyglyceryl-6 stearate needs to meet the reasonable proportion range of this formula, otherwise stratification will occur, resulting in the risk of over-emulsification and retinol molecules being difficult to be absorbed by the skin.

[0142] In order to further verify the effect of ratio on stability, comparative example 3 is set up here. By increasing the amount of emulsifier, compared with Example 6, while maintaining the minimum ratio for the best effect in Example 6, the proportion of polyglyceryl-6 behenate is increased simultaneously, and stratification also occurs, resulting in a decrease in the transdermal absorption rate of retinol.

[0143] Therefore, Example 3 and Example 6, as the upper and lower limit values ​​of the present formulation, can enable the present composition to achieve the best application effect (soluble in water and with a transdermal absorption rate of at least 80.9%).

[0144] 3. Effect of different emulsifier types on stability

[0145] As attached Figure 4 As shown, the effects of different emulsifier types are compared here and in Example 3 to study the influence of different emulsifier types on the stability of the composition.

[0146] Although the emulsifiers selected in the comparative examples have little difference in molecular weight, molecular structure, and emulsifying capacity (HLB) from those in the examples, there are huge differences in the stability and transdermal absorption of retinol. In general, for the same amount of emulsifier, the higher the HLB value of a single emulsifier, the more oil it can emulsify or the better the stability.

[0147] Here, comparative examples 4 (comparative example 4 has only one polyglycerol-6 stearate, and self-emulsifying monoglyceride is a common raw material for self-emulsifying systems. There is no need to consider the HLB value of compound emulsifiers and oils during self-emulsification) - comparative example 9 are set. While maintaining the same ratio of polyglycerol emulsifier, the emulsifiers therein are changed in variables.

[0148] Combined with the data in the table, it can be seen that only when both polyglyceryl-6 behenate and polyglyceryl-6 stearate in Example 3 are present, can the present composition be dissolved in water and maintain uniform stability. At the same time, the retinol transdermal absorption rate is maintained at more than 80.9% (the absorption rate of Example 3 here reaches 89.0%).

[0149] However, in Comparative Examples 4 to 9, a single emulsifier or a combination of emulsifiers other than "polyglyceryl-6 behenate and polyglyceryl-6 stearate" was used, and different emulsification stratification, turbidity and other phenomena occurred, and the final result showed that the transdermal absorption rate of retinol was far less than 80.9%.

[0150] It shows that the present invention adopts a combined emulsifier of "polyglyceryl-6 behenate and polyglyceryl-6 stearate", which can not only maintain uniform water solubility but also allow the transdermal absorption rate of retinol molecules to reach at least 80.9%.

[0151] The method of using polyglyceryl-6 behenate and polyglyceryl-6 stearate to form an emulsified film composed of micro-bead particles and encapsulate retinol molecules through a self-emulsification reaction can maximize the transdermal absorption effect of retinol molecules.

[0152] 4. Effect of different phospholipid types on stability

[0153] like Figure 5 As shown, in order to verify the effects of different phospholipid types and processes on transdermal absorption rate, comparative examples 10 to 13 were set. Under the condition of maintaining the same ratio and combined emulsifier:

[0154] It was found that the comparative example 10 lacking phospholipids had the lowest transdermal absorption rate of retinol, and stratification and turbidity occurred.

[0155] In other comparative examples 11 and 12, different types of phospholipids are added. Compared with Example 3, it can be found that the phospholipids in Comparative Examples 11 and 12 greatly reduce the transdermal absorption rate of retinol molecules. On the contrary, the hydrogenated lecithin used in Example 3 of the present invention makes the transdermal absorption rate of retinol as high as 89.0%, and it is easily soluble in water, not stratified, and not turbid.

[0156] Therefore, hydrogenated lecithin can effectively promote the transdermal absorption rate of retinol.

[0157] 5. Impact of different process types on stability

[0158] By comparing the processes of Example 3 and Comparative Example 13, it can be found that the composition prepared by the microfluidization process can allow the retinol molecules to be well wrapped by the emulsified film, and can maximize the effect of promoting the transdermal absorption of the retinol molecules.

[0159] If the composition prepared by ordinary homogenization (such as stirring and shaking) shows stratification and turbidity, the transdermal absorption rate of retinol is the lowest.

[0160] Therefore, the present invention prepares the composition through the microfluidization process, which can improve the emulsification effect, protect the retinol molecules from being lost, and achieve good transdermal absorption.

[0161] The embodiments of the present invention have been described above, and the above description is exemplary, not exhaustive, and is not limited to the disclosed embodiments. Many modifications and variations will be apparent to those of ordinary skill in the art without departing from the scope and spirit of the described embodiments. The selection of terms used herein is intended to best explain the principles of the embodiments, practical applications, or technical improvements in the market, or to enable other persons of ordinary skill in the art to understand the embodiments disclosed herein.

Claims

1. A retinol anti-wrinkle soothing nanocomposition, characterized in that: The composition includes the following mass percentages: 0.1-3% polyglyceryl-6 behenate, 0.5-10% polyglyceryl-6 stearate, 0.1-5% hydrogenated lecithin, 0.1-15% retinol, 5-35% glycerol, 5-30% GTCC and the balance water.

2. A retinol anti-wrinkle soothing nanocomposition according to claim 1, characterized in that: The ratio of the polyglyceryl-6 behenate to the polyglyceryl-6 stearate is 1:3-6.

3. The retinol anti-wrinkle soothing nanocomposition according to claim 1, characterized in that: In the retinol anti-wrinkle soothing nanocomposition, the turbidity (NTU) of the retinol at a concentration of 0.1% satisfies: NTU≤10.

4. A method for preparing a retinol anti-wrinkle soothing nanocomposition according to any one of claims 1 to 3, characterized in that: The steps include: S1. Add GTCC, retinol, hydrogenated lecithin, polyglyceryl-6 behenate, polyglyceryl-6 stearate and glycerin in sequence at 50-65° C. and stir to disperse uniformly into phase A; S2. Add 50-65° C. water to the phase A in step S1, and stir to disperse evenly to form phase B; S3, homogenizing the phase B in step S2 at 50-65° C. and 3000 rpm for 5 min to obtain a crude emulsion; S4, subjecting the crude emulsion in step S3 to microfluidization treatment three times at a pressure of 700 bar to obtain a crude emulsion dispersion; S5, subjecting the crude emulsion dispersion in step S4 to nano-treatment to obtain the anti-wrinkle nano-composition.

5. The preparation method according to claim 4, characterized in that: The polyglyceryl-6 behenate and the polyglyceryl-6 stearate undergo a self-emulsification reaction to form an emulsified film composed of micro-bead particles and encapsulate the retinol.

6. The preparation method according to claim 4, characterized in that: The particle size of the microbead particles is generally 25 to 65 nanometers.

7. The preparation method according to claim 4, characterized in that: The polyglycerol adopts liposome microcapsule encapsulation technology to form liposome microcapsules and encapsulate the emulsified membrane.

8. The preparation method according to claim 4, characterized in that: S4, subjecting the crude emulsion in step S3 to microfluidization treatment three times at a pressure of 700 bar to obtain a crude emulsion dispersion, comprising: Crude emulsion preparation: preparing the crude emulsion to be processed, ensuring that its composition and proportion meet the requirements of subsequent processing; Microfluidization treatment: Select suitable microfluidization emulsification equipment, and select a microfluidizer with a T-shaped structure, a flow focusing structure or a co-flow structure according to the needs; process the crude emulsion through the microfluidizer; under the action of high pressure, the particles in the crude emulsion are subjected to strong shearing and collision in the microchannel, thereby breaking into smaller droplets; Collect the product: After the emulsion is treated with microfluidization, its particle size and dispersibility will be improved. Collect the treated product and conduct necessary tests and evaluations to determine whether the particle size and dispersibility of the product are qualified: If qualified, the crude emulsion dispersion is obtained; Otherwise, repeat the above microfluidization steps. 9 . A retinol anti-wrinkle soothing nano composition comprising the retinol anti-wrinkle soothing nano composition according to any one of claims 1 to 4 .

Citation Information

Patent Citations

  • Cosmetic composition comprising high amounts of retinol

    CN118284402A