CN112107506B - Retinols wrap and preparation method and application thereof - Google Patents

Retinols wrap and preparation method and application thereof Download PDF

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Publication number
CN112107506B
CN112107506B CN202011064343.6A CN202011064343A CN112107506B CN 112107506 B CN112107506 B CN 112107506B CN 202011064343 A CN202011064343 A CN 202011064343A CN 112107506 B CN112107506 B CN 112107506B
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Prior art keywords
retinol
retinoid
thickening agent
thickener
polydimethylsiloxane
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CN112107506A (en
Inventor
钱进
向琼彪
李华真
黄建珍
李传茂
邓慧
张伟杰
曾伟丹
张楚标
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Guangdong Danz Group Co Ltd
Guangzhou Keneng Cosmetic Research Co Ltd
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Guangdong Danz Group Co Ltd
Guangzhou Keneng Cosmetic Research Co Ltd
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Priority to CN202011064343.6A priority Critical patent/CN112107506B/en
Publication of CN112107506A publication Critical patent/CN112107506A/en
Priority to PCT/CN2021/086675 priority patent/WO2022068173A1/en
Priority to JP2022546684A priority patent/JP2023513098A/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/671Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/81Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
    • A61K8/8188Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bonds, and at least one being terminated by a bond to sulfur or by a hertocyclic ring containing sulfur; Compositions of derivatives of such polymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/89Polysiloxanes
    • A61K8/891Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/89Polysiloxanes
    • A61K8/895Polysiloxanes containing silicon bound to unsaturated aliphatic groups, e.g. vinyl dimethicone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations

Abstract

The invention relates to a retinoid wrap and a preparation method and application thereof, belonging to the field of cosmetics. The invention provides a retinoid package, which comprises the following components: mixed oils of retinoids; a thickener; and polydimethylsiloxane; wherein the thickening agents comprise a first thickening agent, a second thickening agent, and a third thickening agent; the mass ratio of the retinol mixed oil to the first thickening agent is (2-4) to 1; also, the first, second and third thickeners may be the same or different. The retinoid envelope of the present invention can form a stable envelope of a retinoid compound, and realize sustained release of the retinoid compound without causing damage to the retinoid compound. Furthermore, the retinol wrap is applied to the skin care product, can improve the utilization rate of the retinol compound in the skin care product, and enables the skin care product to realize the effects of effectively removing wrinkles and resisting aging.

Description

Retinols wrap and preparation method and application thereof
Technical Field
The invention relates to a retinoid wrap and a preparation method and application thereof, in particular to a retinoid wrap and a preparation method and application thereof, belonging to the field of cosmetics.
Background
Tretinoin (also called vitamin A acid, retinoic acid) is a metabolic intermediate product of vitamin A in vivo, and plays an important role in regulation and control in the processes of human growth, development and cell differentiation. Tretinoin can not only promote the synthesis of collagen, but also promote the generation of elastin fiber, and has good wrinkle removing effect. However, tretinoin is irritating to the skin and may cause redness, itching, etc. after application. Compared with tretinoin, tretinoin (also called retinol) and tretinoin ester (also called retinol) have low irritation, and are usually used in cosmetics instead of tretinoin.
When the retinol or retinol ester penetrates into the skin, it is gradually metabolized into retinoic acid under the oxidation action of enzyme, and retinoic acid again plays a role in promoting epidermal cell renewal. Through the metabolic process, the retinoic acid is slowly released on the skin, so that the skin can be prevented from being strongly stimulated, and the function of activating cell renewal can be achieved. But the retinol has poor stability, is easy to decompose when being exposed to light and heat, and is easy to be catalytically decomposed particularly under the action of ultraviolet rays; furthermore, retinol is fat-soluble and poorly soluble in water. Therefore, the retinol has the disadvantages of instability and low utilization rate when applied to cosmetics. How to make retinol stably exist in cosmetics and slowly release the retinol on the skin is an important problem to be solved urgently in the industry at present.
Citation 1 discloses a pulsed electric field-based production method of emulsion gel embedding fat-soluble vitamins, which is to dissolve octenyl succinic acid starch ester in water, heat in a water bath, stir until completely gelatinized and dissolved, and cool to room temperature; adding edible oil dissolved with fat-soluble vitamins to obtain a mixed solution; shearing and homogenizing the obtained mixed solution by using a high-speed shearing machine and a high-pressure homogenizer to obtain a coarse emulsion; adding starch into the coarse emulsion, and uniformly stirring to obtain emulsion; adding methyl cellulose solution into the emulsion, uniformly mixing, then carrying out pulsed electric field treatment, heating in water bath, degassing, and cooling to obtain emulsion gel. Wherein the fat-soluble vitamin is one or more of retinol, beta-carotene, lycopene, lutein, tocopherol, sterols and vitamin K. However, in the method, the emulsion embedded with the fat-soluble vitamin needs to be heated in a water bath at the temperature of 80-95 ℃, and the retinol is not light-resistant and heat-resistant and is easy to be damaged in the process.
Citation 2 discloses a preparation method of hydroxypropyl cyclodextrin inclusion retinol, which comprises the following steps: (1) Taking 1 part of retinol, adding 10-30 parts of purified water, heating to 40-80 ℃, stirring for 0.5-2 hours, and dissolving; (2) Adding 3-10 parts of hydroxypropyl cyclodextrin into the dissolved retinol solution, and stirring for 1-4 hours at 40-80 ℃ to fully include to obtain hydroxypropyl cyclodextrin inclusion retinol. The method encapsulates the retinol by hydroxypropyl cyclodextrin to form a slow-release high-efficiency product, however, the retinol is easily damaged by heating treatment at the temperature of 40-80 ℃ in the preparation process.
Cited documents:
cited document 1: CN110693003A
Cited document 2: CN110623859A
Disclosure of Invention
Problems to be solved by the invention
In view of the technical problems in the prior art, for example: the invention provides a retinol wrap, which has the problems of poor stability and low utilization rate in cosmetics, and the retinol wrap is easy to damage the retinol in the retinol wrapping process. The retinoid envelope of the present invention can form a stable envelope of a retinoid compound, and realize sustained release of the retinoid compound without causing damage to the retinoid compound.
Further, the present invention provides a method for preparing a retinoid package, which does not require heating of the retinoid compound during the preparation process and does not cause damage to the retinoid compound.
Furthermore, the invention also provides application of the retinol wrap in skin care products, and the retinol compound has high utilization rate in the skin care products and can effectively remove wrinkles and resist aging.
Means for solving the problems
The invention provides a retinoid wrap, which comprises the following components:
mixed oils of retinoids;
a thickener; and
polydimethylsiloxane; wherein, the first and the second end of the pipe are connected with each other,
the thickening agents comprise a first thickening agent, a second thickening agent and a third thickening agent;
the mass ratio of the retinol mixed oil to the first thickening agent is (2-4) to 1; and the number of the first and second electrodes,
the first, second and third thickeners may be the same or different.
The retinoid package according to the invention is characterized in that the mass ratio of the mixture of the retinoid mixed oil and the first thickener, the second thickener and the third thickener is (1-1.4): (0.05-0.08): (0.02-0.05).
The retinoid package according to the invention, wherein the retinoid mixed oil, the first thickener, the second thickener and the third thickener form a blend, and the mass ratio of the blend to polydimethylsiloxane is (1-2): 1.
the retinoid package according to the present invention, wherein the retinoid mixed oil includes a retinoid compound and polydimethylsiloxane; preferably, the mass ratio of the retinol compound to the polydimethylsiloxane is (1-2): (1-2).
The retinoid package according to the present invention, wherein the retinoid compound includes retinol and/or retinol ester.
The retinoid package according to the present invention, wherein the thickener includes one or a combination of two or more of a vinyl dimethicone/methicone silsesquioxane crosspolymer, a dimethicone/vinyl dimethicone crosspolymer, and a hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer.
The invention also provides a preparation method of the retinol wrap, which comprises the step of mixing the components of the retinol wrap.
The preparation method comprises the following steps:
mixing a mixed retinol oil with a first thickener;
mixing the mixed retinol oil with the mixture of the first thickening agent, the second thickening agent and the third thickening agent to obtain a blend;
the blend was dispersed in polydimethylsiloxane to give a retinoid encapsulate.
The invention also provides an application of the retinoid envelope in skin care products; preferably, the skin care product comprises a lotion, cream, emulsion, gel or essence.
According to the application of the invention, the addition amount of the retinol wrap in the skin care product is 1-5%.
ADVANTAGEOUS EFFECTS OF INVENTION
The retinoid envelope of the present invention can stably encapsulate a retinoid compound, and can realize sustained release of the retinoid compound without causing damage to the retinoid compound.
Furthermore, the invention also provides a preparation method of the retinol wrap, which is simple and easy to operate, has easily obtained raw materials, does not need to heat the retinol compound in the preparation process, does not damage the retinol compound, and meets the requirement of mass production.
Furthermore, the application of the retinol wrap in the skin care product provided by the invention improves the utilization rate of the retinol compound in the skin care product, can effectively lighten fine lines, improve the skin elasticity and has the anti-aging effect.
Detailed Description
Various exemplary embodiments, features and aspects of the invention will be described in detail below. The word "exemplary" is used exclusively herein to mean "serving as an example, embodiment, or illustration. Any embodiment described herein as "exemplary" is not necessarily to be construed as preferred or advantageous over other embodiments.
Furthermore, in the following detailed description, numerous specific details are set forth in order to provide a better understanding of the present invention. It will be understood by those skilled in the art that the present invention may be practiced without some of these specific details. In other instances, methods, means, devices and steps which are well known to those skilled in the art have not been described in detail so as not to obscure the invention.
All units used in the specification are international standard units unless otherwise specified, and numerical values and numerical ranges appearing in the present invention should be understood to include systematic errors inevitable in industrial production.
In the present specification, "%" denotes mass% unless otherwise specified.
In the present specification, the term "may" includes both the case where a certain process is performed and the case where no process is performed.
In the present specification, reference to "some particular/preferred embodiments," "other particular/preferred embodiments," "embodiments," and the like, means that a particular element (e.g., feature, structure, property, and/or characteristic) described in connection with the embodiment is included in at least one embodiment described herein, and may or may not be present in other embodiments. In addition, it is to be understood that the described elements may be combined in any suitable manner in the various embodiments.
In the present specification, the numerical range represented by "a value a to B value" means a range including the endpoint value A, B.
In the present specification, the term "water" includes any available water that can be used in the cosmetic field, such as deionized water, distilled water, ion-exchanged water, double distilled water, high purity water, and purified water.
In the present specification, when "normal temperature" or "room temperature" is used, the temperature may be 10 to 40 ℃.
First aspect
In a first aspect of the present invention, there is provided a retinoid-based wrap comprising the following components:
mixed oils of retinoids;
a thickener; and
polydimethylsiloxane; wherein the content of the first and second substances,
the thickening agents comprise a first thickening agent, a second thickening agent and a third thickening agent;
the mass ratio of the retinol mixed oil to the first thickening agent is (2-4) to 1; and the number of the first and second electrodes,
the first, second and third thickeners may be the same or different.
The retinol wrap comprises a thickening agent and a mixed retinol oil as an inner phase, and polydimethylsiloxane wrapped thickening agent and the mixed retinol oil as an outer phase, so that the retinol compound can be stably contained in the wrap layer by layer, the slow release effect is achieved, and the activity of the retinol compound cannot be damaged. The thickening agent in the retinene-based package can form stable adsorption on the retinene-based mixed oil and reduce desorption of the retinene-based mixed oil. After the retinol wrap is applied to the skin surface, the wrap is spread layer by layer, so that the retinol compound is slowly released to the skin surface to play the effects of removing wrinkles and resisting aging.
Polydimethylsiloxane
Polydimethylsiloxane is also called simethicone, has the functions of lubricating property and ultraviolet resistance in cosmetics, has good air permeability and obvious dustproof function, and can be used for replacing the traditional grease raw material. The polydimethylsiloxane has very good permeability to the skin, can increase the smooth and refreshing feeling of the skin care product smeared on the skin, and has good effect on increasing the softness of the skin. The polydimethylsiloxane provided by the invention is used as an external phase for wrapping the mixed oil of retinol, the first thickening agent, the second thickening agent and the third thickening agent, and can effectively stabilize the retinol compound; after the retinol wrap is applied to a skin care product, the outer layer of polydimethylsiloxane wraps a layer of water phase, and finally an easily-spreading oil-in-water stable system is formed.
The mixed oil of retinol, the first thickening agent, the second thickening agent and the third thickening agent form a blend, and the mass ratio of the blend to polydimethylsiloxane is (1-2): 1. specifically, the mass ratio of the blend to polydimethylsiloxane can be 1.1, 1.2. When the mass ratio of the blend to the polydimethylsiloxane is (1-2): 1, the blend is fully dispersed in polydimethylsiloxane, so that the inner retinol compound is effectively wrapped, and the system stability is high.
Further, in other specific embodiments, the polydimethylsiloxane is added in an amount of 35 to 55% by mass based on the total mass of the retinoid inclusions, for example: 40%, 45%, 50%, etc. When the addition amount of the polydimethylsiloxane is 35 to 55%, the coating can be better realized. Preferably, in the present invention, the polydimethylsiloxane has a viscosity of 5 to 10 η.
Mixed oil of retinoids
The mixed oil of retinol of the present invention is formed by mixing retinol compound and polydimethylsiloxane. The retinol compound is fat soluble, can be dispersed in polydimethylsiloxane, and is helpful for the first layer of the retinol compound to wrap. In addition, the compatibility and stability of the system can be improved by mixing the same polydimethylsiloxane as the outermost layer as an oil component with a retinoid mixture. Preferably, the viscosity of the polydimethylsiloxane in the mixed oil of retinoids may be 5 to 10 η.
Specifically, in the mixed oil of retinol, the mass ratio of the retinol compound to the polydimethylsiloxane is (1-2): (1-2). For example, the mass ratio of the retinol compound to the polydimethylsiloxane is 1,1. When the mass ratio of the retinol compound to the polydimethylsiloxane is (1-2): (1-2), the retinoid compound can be sufficiently dispersed in the polydimethylsiloxane.
Further, the retinol-based compound includes retinol and/or retinol ester. In some specific embodiments, the retinol wrap is formed by wrapping retinol, which has small irritation to skin, can be gradually metabolized into retinoic acid on the skin surface, activate and promote skin cell renewal, improve skin elasticity, so as to weaken fine lines, effectively remove wrinkles and resist aging. In other embodiments, the retinoid-based coating can be a retinoid ester coating formed by coating retinol ester, or a mixture of retinol and retinol ester. Retinol esters are more stable than retinol and can also be metabolized to retinoic acid to provide wrinkle-removing, anti-aging benefits.
In some particular embodiments, the retinol esters of the present invention can be retinol palmitate and/or retinol propionate.
Further, in other specific embodiments, the retinol blend oil is added in an amount of 35-55% based on the total mass of the retinol based wrap, for example: 40%, 45%, 50%, etc. When the addition amount of the mixed oil of retinol is 35-55%, the effect of the retinol compound can be better exerted.
Thickening agent
The thickening agent comprises a first thickening agent, a second thickening agent and a third thickening agent, wherein the first thickening agent, the second thickening agent and the third thickening agent can use some thickening agents commonly used in the field, and the first thickening agent, the second thickening agent and the third thickening agent can be the same or different. By adding the first thickening agent, the second thickening agent and the third thickening agent, effective adsorption on the retinol mixed oil can be formed, the viscosity of an inner phase is increased, and desorption of a retinol compound in a retinol inclusion is reduced.
In some specific embodiments, the mass ratio of the mixed retinol oil to the first thickener is (2-4): 1. For example, the mass ratio of the retinol mixed oil to the first thickener may be from 2.2. When the mass ratio of the mixed oil of the retinol to the first thickening agent is (2-4): 1, the first thickening agent can effectively adsorb the mixed oil of the retinol and reduce the desorption of the retinol compounds in the mixed oil of the retinol.
Specifically, the mass ratio of the mixture of the mixed oil of retinol and the first thickening agent, the second thickening agent and the third thickening agent is (1-1.4): (0.05-0.08): (0.02-0.05). For example, the mass ratio of the mixture of the mixed retinol oil and the first thickener, the second thickener and the third thickener may be (1-1.4): (0.06-0.08): (0.02-0.05), and also (1-1.4): (0.05-0.07): (0.02-0.05), or 1: (0.06-0.08): (0.02-0.05), 1.4: (0.05-0.07): (0.02-0.05), etc. When the mass ratio of the mixture of the mixed retinol oil and the first thickener to the second thickener to the third thickener is (1-1.4): (0.05-0.08): (0.02-0.05), the coating can fully coat the mixed oil of retinol, is compatible with polydimethylsiloxane of an external phase, and is beneficial to obtaining a coating with stable system and high adsorption fastness of retinol compounds.
In the invention, the thickening agent comprises one or the combination of more than two of vinyl polydimethylsiloxane/polymethylsiloxane silsesquioxane cross-linked polymer, polydimethylsiloxane/vinyl polydimethylsiloxane cross-linked polymer and hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer. The thickener component has good compatibility with other system components while adsorbing the mixed oil of retinol.
In some embodiments, the first thickening agent is a vinyl dimethicone/methicone silsesquioxane crosspolymer that is a silicone powder that absorbs silicone oil and has thickening and skin feel improving effects. The second thickener is polydimethylsiloxane/vinyl polydimethylsiloxane cross-linked polymer, and the polydimethylsiloxane/vinyl polydimethylsiloxane cross-linked polymer is a kind of silicon-philic thickener and can form effective adsorption on mixed retinol oil. The third thickener is hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer which has an emulsifying effect and can improve the system stability of the retinoid inclusion.
Further, in other specific embodiments, the first thickener is added in an amount of 8 to 16% based on the total mass of the retinoid package, for example: 10%, 12%, 14%, etc.; the second thickener is added in an amount of 1 to 5%, for example: 2%, 3%, 4%, etc.; the third thickener is added in an amount of 0.1 to 2%, for example: 0.5%, 1%, 1.5%, etc. When the contents of the first, second and third thickeners are within the above ranges, the obtained retinoid house is more excellent in performance.
The retinol wrap is formed by mixing the thickening agent, the mixed oil of retinol and polydimethylsiloxane, and the thickening agent wraps the mixed oil of retinol layer by layer, so that the retinol compound stably exists in the retinol wrap and can be slowly released on the surface of skin.
Second aspect of the invention
A second aspect of the present invention provides a method for preparing the retinoid package according to the first aspect, including a step of mixing the components of the retinoid package.
Further, a method for preparing the retinoid package includes a step of mixing the components of the retinoid package at room temperature.
In some embodiments, the method of making a retinoid package comprises the steps of:
mixing a mixed retinol oil with a first thickener;
mixing the mixed retinol oil with the mixture of the first thickening agent, the second thickening agent and the third thickening agent to obtain a blend;
the blend was dispersed in polydimethylsiloxane to give a retinoid encapsulate.
The mixing of the mixed oil of retinoids with the first thickener means that the mixed oil of retinoids is mixed with the first thickener of powder, and the first thickener is stirred until the mixed oil of retinoids in the oil body is sucked dry to obtain a mixture of the mixed oil of retinoids and the first thickener.
Further, as the mixed oil of retinoids, a mixed oil of retinoids obtained by mixing a retinoids compound with polydimethylsiloxane may be used.
For the blend, the powder of the first thickener, the second thickener and the third thickener is formed by wrapping the mixed oil of retinol.
The dispersion of the blend in the polydimethylsiloxane means that the blend is dispersed in the polydimethylsiloxane with the viscosity of 5-10 eta, and the outer side of the blend is finally coated with a layer of oil-phase polydimethylsiloxane to obtain the retinol wrap which is prepared by wrapping the mixed retinol oil with oil-phase wrapping powder.
Further, the mixing step and the dispersing step are both performed at room temperature, and finally the mixture of the mixed oil of retinol and the first thickener, the mixture of the second thickener and the third thickener, which are uniformly mixed, is uniformly dispersed in the polydimethylsiloxane.
The preparation method of the retinol inclusion compound of the invention does not need heating treatment in the process of inclusion of the retinol compound, can be implemented at room temperature, does not cause damage to the activity of the retinol compound, is simple and easy to implement, has easily obtained raw materials, and is suitable for large-scale industrial preparation.
Third aspect of the invention
The third aspect of the present invention provides a use of the retinoid envelope according to the first aspect in a skin care product; preferably, the skin care product comprises a lotion, cream, emulsion, gel or essence.
After the retinol wrap is added into a skin care product, a layer of water phase wrap is formed on the outer side of polydimethylsiloxane, and a stable oil-in-water system is finally obtained, so that the skin care product has the effects of resisting aging and removing wrinkles, and the retinol compound serving as an active ingredient has stable performance and long acting time.
Specifically, the addition amount of the retinoid based on the total mass of the skin care product is 1 to 5%, preferably 1.4 to 4%. For example, the amount of retinoid based wrap added may be 1.5%, 1.7%, 1.9%, 2.0%, 2.2%, 2.4%, 2.6%, 3%, 3.5%, 4.5%, etc. When the addition amount of the retinol wrap is 1-5%, the effects of wrinkle removal and aging resistance can be achieved, the stimulation to the skin of a human body can be avoided, and the product is mild and safe.
Wrinkle-removing face cream
In some specific embodiments, the present invention provides a wrinkle-removing cream comprising a retinoid-based wrap according to the first aspect of the invention. After the wrinkle-removing cream is applied to the surface of skin, the retinol coating layer spreads to release the retinol compound in the innermost layer, thereby playing the roles of promoting the renewal of epidermal cells and fading fine wrinkles. The retinol inclusion added in the wrinkle-removing cream has high stability and slow release effect, and can exert the wrinkle-removing and anti-aging effects of the retinol compound to the maximum extent.
Specifically, the amount of the retinoid based on the total mass of the wrinkle-removing cream is 1 to 3%, preferably 1.4 to 2.8%. For example, the amount of retinoid based wrap added may be 1.5%, 1.7%, 1.9%, 2.0%, 2.2%, 2.4%, 2.6%, 2.8%, etc.
In the present invention, the retinol wrap includes one or both of a retinol wrap and a retinol ester wrap. The retinol wrap and the retinol ester wrap have the effects of high stability, slow release, anti-aging and wrinkle removal. In some more specific embodiments, the wrinkle-removing cream of the present invention is added with a retinol wrap and a retinol ester wrap at the same time, wherein the retinol wrap is added in an amount of 0.5 to 1.5%, preferably 0.7 to 1.4%, and the retinol ester wrap is added in an amount of 0.5 to 1.5%, preferably 0.7 to 1.4%, based on the total mass of the wrinkle-removing cream. In some more specific embodiments, the retinol ester wrap is a retinol palmitate wrap and/or retinol propionate wrap.
In some embodiments, the wrinkle-removing cream further comprises one or a combination of two or more of a moisturizer, an emulsifier, a grease, a thickener, a solvent, a skin conditioner, and a preservative. The wrinkle-removing cream has mild formula composition, and can fully exert the efficacy of the retinol wrap.
In the invention, the humectant can be added to play a role in moisturizing. In order to further exert the efficacy of the moisturizer, the moisturizer of the present invention may be added in an amount of 1 to 10%, preferably 2 to 6%, based on the total mass of the wrinkle-removing cream. Further, the humectant of the present invention is propylene glycol.
In the invention, the system stability of the wrinkle-removing cream can be increased by adding the emulsifier, specifically, the adding amount of the emulsifier is 0.5-2%, preferably 0.6-1.2% based on the total mass of the wrinkle-removing cream.
Further, the emulsifier comprises one or more of PEG-20 methyl glucose sesquistearate, sorbitan isostearate, polyglyceryl-3 methyl glucose distearate, laureth-7, isosteareth-20.
In other specific embodiments, the wrinkle-removing cream is added with PEG-20 methyl sesqui glucose stearate and methyl sesqui glucose stearate; wherein, the addition amount of PEG-20 methyl sesqui glucose stearate is 0.3-1.2% and the addition amount of methyl sesqui glucose stearate is 0.2-0.8% based on the total mass of the wrinkle removing cream.
In the invention, the wrinkle-removing cream also comprises grease, and the grease is added into the wrinkle-removing cream, so that the evaporation of water on the surface of the skin can be reduced, and the skin can be prevented from being dried and cracked. In addition, by adding oil or fat, a hydrophobic film can be formed on the skin surface to prevent the invasion of harmful substances from the outside. Specifically, the addition amount of the oil is 1-20%, preferably 3-15% based on the total mass of the wrinkle-removing cream.
Further, the oil or fat comprises one or a combination of two or more of behenyl alcohol, isononyl isononanoate, dimethiconol and dimethiconol.
In some more specific embodiments, the wrinkle-removing cream is added with behenyl alcohol, isononyl isononanoate, dimethiconol and dimethicone. Wherein, the addition amount of the behenyl alcohol is 0.5-2 percent, preferably 0.5-1.5 percent based on the total mass of the wrinkle-removing cream; the addition amount of isononyl isononanoate is 1-5%, preferably 1.5-2.5%; the adding amount of the dimethiconol is 0.5-5%, preferably 1-3%; the polydimethylsiloxane is added in an amount of 0.5 to 5%, preferably 1 to 3%.
In the present invention, a proper consistency is obtained by adding a thickener to control the texture of the wrinkle-removing cream, and the stability is excellent. Specifically, the thickener in the wrinkle-removing cream is added in an amount of 0.05-6%, preferably 0.7-2.5%, based on the total mass of the wrinkle-removing cream.
Further, the thickener of the present invention includes a dimethicone/vinyl dimethicone crosspolymer, an ammonium acryloyldimethyl taurate/VP copolymer, xanthan gum, acrylic acid (ester)/C 10-30 One or the combination of more than two of alkanol acrylate cross-linked polymer and hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer.
In some specific embodiments, the wrinkle-removing cream is added with polydimethylsiloxane/vinyl polydimethylsiloxane cross-linked polymer, acryloyl dimethyl ammonium taurate/VP copolymer and acrylic acid (ester)/C 10-30 An alkanol acrylate cross-linked polymer; wherein, the total mass of the wrinkle-removing cream is countedThe addition amount of the polydimethylsiloxane/vinyl polydimethylsiloxane crosspolymer is from 0.05 to 2%, preferably from 0.5 to 1.5%; the addition amount of the acryloyl dimethyl ammonium taurate/VP copolymer is 0.01-2%, preferably 0.1-0.5%; acrylic acid (ester)/C 10-30 The addition amount of the alkanol acrylate cross-linked polymer is 0.01 to 2%, preferably 0.1 to 0.5%.
In the present invention, the generation of wrinkles can be reduced by adding a skin conditioner to the wrinkle-removing cream. The effective components in the skin conditioner can penetrate into the deep part of skin and be absorbed by skin, thereby improving the state of skin. Specifically, the skin conditioner is added in an amount of 1.05-6%, preferably 1.4-4%, based on the total mass of the wrinkle-removing cream.
Further, the skin conditioning agent comprises one or both of D-panthenol and niacinamide. Wherein, after being absorbed by skin, the D-panthenol can increase the content of hyaluronic acid of the skin, give the skin luster and moisture retention effects, and can stimulate cell division and regeneration and repair tissues. The addition amount of D-panthenol in the wrinkle removing cream is 0.05-2%, preferably 0.8-1.2%. Nicotinamide can maintain the level of ceramide and free fatty acid in skin, maintain the water content of skin, and improve microcirculation of dermis. The addition amount of nicotinamide in the wrinkle-removing cream is 1-4%, preferably 1.5-2.5%.
In the invention, a certain amount of preservative can be added into the wrinkle-removing cream, and specifically, the addition amount of the preservative is 0.5-2%, preferably 0.6-1% based on the total mass of the wrinkle-removing cream.
Further, the preservative comprises one or more of methyl hydroxybenzoate, ethylparaben, phenoxyethanol and ethylhexylglycerin.
Furthermore, other components which do not influence the efficacy of the wrinkle-removing cream can be added into the wrinkle-removing cream.
In the invention, the components of the wrinkle-removing cream can be fully dissolved by adding the solvent, and the wrinkle-removing effect can be synergistically exerted. Specifically, the addition amount of the solvent is such that the sum of the mass of the solvent and the rest of the components reaches 100% based on the total mass of the wrinkle-removing cream. Further, water may be selected as the solvent.
The wrinkle-removing cream provided by the invention is mild in components and can realize synergistic interaction; the retinol inclusion can exist stably, and the retinol compound is slowly released on the surface of the skin after the wrinkle-removing cream is applied to the hair, thereby playing the effects of removing wrinkles and resisting aging.
Further, the invention also provides a preparation method of the wrinkle-removing cream in the third aspect, which comprises the step of mixing the components of the wrinkle-removing cream.
In some specific embodiments, the wrinkle-removing cream is prepared by a method comprising the steps of:
mixing humectant, skin conditioner, part of thickener, part of antiseptic and solvent to obtain phase A, heating phase A to 80-90 deg.C, and stirring to mix phase A uniformly;
mixing emulsifier, oil and the rest thickener to obtain phase B, heating phase B to 80-90 deg.C, and stirring to mix phase B uniformly;
adding phase B into phase A at 80-90 deg.C, homogenizing and mixing;
taking the rest antiseptic and retinol wrap as C phase, adding C phase when the temperature of the system is reduced to below 40 deg.C, homogenizing, and discharging.
Emulsion
In the present invention, there is also provided an emulsion comprising a retinoid package according to the first aspect of the invention. The retinol inclusion added in the emulsion has high stability and slow release effect, and can exert the wrinkle removing and anti-aging effects of the retinol compound to the maximum extent.
Specifically, the retinoid-based coating is added in an amount of 1 to 5%, preferably 2 to 4%, based on the total mass of the emulsion. For example, the amount of retinoid based wrap added may be 1.5%, 1.7%, 1.9%, 2.0%, 2.2%, 2.4%, 2.6%, 2.8%, 3%, 3.5%, 4.5%, etc.
In some embodiments, the emulsion further comprises one or a combination of two or more of a humectant, an emulsifier, a thickener, a solvent, and a preservative. The emulsion of the invention has mild formulation composition, and can fully exert the efficacy of the retinoid envelope of the invention.
In the invention, the humectant can be added to play a role in moisturizing. In order to further exert the efficacy of the moisturizer, the moisturizer of the present invention may be added in an amount of 1 to 10%, preferably 2 to 6%, based on the total mass of the emulsion. Further, the humectant of the present invention is propylene glycol.
In the present invention, the system stability of the emulsion can be increased by adding an emulsifier, specifically, the emulsifier is added in an amount of 0.1 to 2%, preferably 0.3 to 1.2%, based on the total mass of the emulsion.
Further, the emulsifier comprises one or more of PEG-20 methyl glucose sesquistearate, sorbitan isostearate, polyglyceryl-3 methyl glucose distearate, laureth-7, isosteareth-20.
In other embodiments, PEG-20 methylsilsesquioxane stearate and methylsilsesquioxane stearate are added to the emulsion at the same time; wherein, the addition amount of PEG-20 methyl sesqui glucose stearate is 0.05-1.2%, and the addition amount of methyl sesqui glucose stearate is 0.05-0.8% based on the total mass of the emulsion.
In the present invention, a proper consistency is obtained by adding a thickener to control the texture of the emulsion, and the stability is excellent. Specifically, the thickener is added in the emulsion of the present invention in an amount of 0.05 to 2%, preferably 0.1 to 0.8%, based on the total mass of the emulsion.
Further, the thickener of the present invention includes a dimethicone/vinyl dimethicone crosspolymer, an ammonium acryloyldimethyl taurate/VP copolymer, xanthan gum, acrylic acid (ester)/C 10-30 One or a combination of two or more of the alkanol acrylate crosslinked polymer and the hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, and xanthan gum is preferably used.
In the present invention, a certain amount of preservative may also be added to the emulsion, specifically, the preservative is added in an amount of 0.5 to 2%, preferably 0.6 to 1%, based on the total mass of the emulsion. Further, the preservative comprises one or more of methyl hydroxybenzoate, ethylparaben, phenoxyethanol and ethylhexylglycerin.
Further, the present invention provides a method for preparing the emulsion of the third aspect, comprising the step of mixing the components of the emulsion.
In some embodiments, the emulsion is prepared by a method comprising the steps of:
mixing humectant, thickener, emulsifier, part of antiseptic and solvent to obtain phase A, heating phase A to 80-90 deg.C, stirring, and homogenizing to obtain phase A;
mixing the rest antiseptic and the retinol wrap to obtain phase B, adding phase B when the temperature of the system is reduced to below 40 deg.C, homogenizing, and discharging.
Examples
Embodiments of the present invention will be described in detail below with reference to examples, but those skilled in the art will appreciate that the following examples are only illustrative of the present invention and should not be construed as limiting the scope of the present invention. The examples, in which specific conditions are not specified, were conducted under conventional conditions or conditions recommended by the manufacturer. The reagents or instruments used are not indicated by the manufacturer, and are all conventional products commercially available.
Examples 1 to 3
Three groups of retinyl-type wraps of examples 1-3 were prepared according to the component amounts provided in table 1, and the preparation method of each group of retinyl-type wraps specifically included the following steps:
(1) Mixing retinol or retinol palmitate with polydimethylsiloxane having a viscosity of 6 eta at room temperature in a ratio of 1: mixing at a ratio of 1 to obtain mixed oil of retinoids.
Wherein, the retinol palmitate is added in example 1, the retinol is added in example 2, and the mixture of retinol and retinol palmitate is added in example 3, wherein the mass ratio of retinol to retinol palmitate is 1:1.
(2) And (2) mixing the mixed oil of retinol obtained in the step (1) with the vinyl polydimethylsiloxane/polymethylsiloxane silsesquioxane cross-linked polymer to form powder, and sucking the oil body to dryness.
(3) And (3) mixing the mixture obtained in the step (3) with a polydimethylsiloxane/vinyl polydimethylsiloxane cross-linked polymer and a hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer at room temperature, and then dispersing the mixture in polydimethylsiloxane with the viscosity of 6 eta to obtain the retinoid envelope.
TABLE 1
Figure BDA0002713312560000161
Comparative examples 1 to 2
Two groups of retinoid envelopes in comparative examples 1-2 were prepared according to the preparation methods provided in examples 1-3, respectively, based on the data provided in table 2. Wherein, the retinol palmitate is added in the comparative example 1, the retinol palmitate is added in the comparative example 2, and in the mixed oil of retinol, the mass ratio of the retinol or the retinol palmitate to the polydimethylsiloxane is 1:1.
TABLE 2
Figure BDA0002713312560000162
Application example a and comparative application examples b to d
Emulsion was prepared by selecting the retinyl wraps prepared in example 1 and comparative examples 1-2 and retinol palmitate as the components of phase B, according to the following procedure:
(1) Mixing phase A components, heating to 85 deg.C, homogenizing, and mixing;
(2) When the temperature of the system is reduced to below 40 ℃, adding the phase B component, homogenizing uniformly and discharging.
TABLE 3
Figure BDA0002713312560000171
Application examples 1 to 3
The retinoid envelopes prepared in examples 1 to 3 were selected as phase C components to prepare wrinkle-removing creams in application examples 1 to 3, respectively, wherein the retinoid envelopes prepared in examples 1 to 3 correspond to the wrinkle-removing creams in application examples 1 to 3, and the other material components in the wrinkle-removing cream are specifically shown in table 4, and the preparation method of the wrinkle-removing cream comprises the following steps:
(1) Mixing A, B two-phase components, heating to 85 deg.C, and stirring to uniformly mix A, B two phases;
(2) Adding phase B into phase A at 85 deg.C, homogenizing and mixing;
(3) When the temperature of the system is reduced to below 40 ℃, adding the phase C, homogenizing uniformly and discharging.
Table 4 application examples 1-3
Figure BDA0002713312560000181
Application of comparative examples 1 to 3
The two sets of wrinkle-removing creams in application comparative examples 1 to 3 were respectively prepared according to the preparation methods provided in application examples 1 to 3 with the data provided in table 5.
TABLE 5 application comparative examples 1-3
Figure BDA0002713312560000191
Effect evaluation experiment
1. Evaluation of wrapping Effect
And selecting the samples a-d in the package effect evaluation as samples to be detected. The samples to be tested were separately packaged in four groups of two 50g transparent PET bottles, one of which was placed under natural light for 7 days, and the other was refrigerated in the dark. And 7 days later, respectively carrying out quantitative analysis on the retinol palmitate in the two batches of samples to be detected by adopting a high performance liquid chromatograph at the same time under the same condition, and calculating the residual effective components. The results are shown in table 6:
TABLE 6 evaluation of the effects of encapsulation
Sample (I) Refrigerated in the dark (%) Content after light irradiation (%) Residual (%)
Sample a 0.482 0.285 59.1%
Sample b 0.474 0.172 36.4%
Sample c 0.465 0.155 33.4%
Sample d 0.468 0.189 40.9%
As can be seen from the results of the evaluation of the wrapping effect in Table 6, after the experiment of 7 days under illumination, the residual amount of the retinol palmitate in the sample a is the highest and can reach 59.1%, the residual amount of the retinol palmitate in the sample d is 40.9%, and the residual amounts of the samples b and c are the lowest. According to the experimental results, the residual amount of the retinol-based wrap provided by the invention can be improved by about 20% compared with that of the non-wrapped retinol palmitate after being illuminated for 7 days, which shows that the retinol-based wrap can effectively improve the stability of the retinol-based compound.
2. Evaluation of wrinkle-removing Effect
The face creams prepared in examples 1 to 3 and comparative examples 4 to 6 were placed under room temperature and in a non-dark condition for one week and then used as test samples for wrinkle removal effect test, wherein 30 women of 25 to 35 years old with canthus wrinkles and infraocular wrinkles were selected as the test subjects. The user applies the medicine to the whole face twice a day, morning and evening, and uses two droppers (the amount of each dropper is 0.3-0.5 g) at one time together with sun protection (the dosage is about 0.6-0.8g according to the individual use amount each time) (the dosage is determined according to the face area of the user, and the same content is used in equal areas). After 28 days of use, the fine grain fading effect was observed, and 10 is marked with fine grain fading and 1 is unchanged, wherein the result is counted by 10 points. The details are shown in table 7 below:
TABLE 7 wrinkle-dispelling Effect evaluation Table
Tester number 1 2 3 4 5 6 7 8 9 10 Mean value of
Application example 1 8 8 8 9 9 8 9 8 9 9 8.5
Application example 2 8 8 8 8 9 8 8 8 8 9 8.2
Application example 3 8 8 9 9 9 8 9 8 8 9 8.5
Application comparative example 1 7 7 7 7 7 8 7 7 7 7 7.1
Comparative application example 2 6 6 6 7 6 6 6 6 6 7 6.2
Comparative application example 3 6 7 7 7 7 7 7 7 7 7 6.9
As can be seen from the evaluation of wrinkle-removing effects in table 7, the wrinkle-removing creams prepared by the application examples 1-3 are superior to the wrinkle-removing creams prepared by the application comparative examples 1-3 in that the actives of the application examples 1-3 are all retinol-based encapsulates and maintain the active effects better than the uncoated actives. This is the case where the wrinkle-removing cream effects of application example 1 and application example 3 were comparable, and the effect of application comparative example 1 was better than that of application comparative example 3, probably because the rate of complete decomposition failure was slower for retinol palmitate than for retinol.
Industrial applicability
The retinoid envelope provided by the invention, and the preparation method and application thereof can be applied to industry.
The above examples of the present invention are merely examples for clearly illustrating the present invention and are not intended to limit the embodiments of the present invention. Other variations and modifications will be apparent to persons skilled in the art in light of the above description. And are neither required nor exhaustive of all embodiments. Any modification, equivalent replacement, and improvement made within the spirit and principle of the present invention should be included in the protection scope of the claims of the present invention.

Claims (9)

1. A retinoid package comprising the following components:
the mixed oil of retinol comprises a retinol compound and first polydimethylsiloxane, and the mass ratio of the retinol compound to the first polydimethylsiloxane is (1-2): (1-2);
a thickener; and
a second polydimethylsiloxane; wherein the content of the first and second substances,
the thickening agents comprise a first thickening agent, a second thickening agent and a third thickening agent;
the mass ratio of the retinol mixed oil to the first thickening agent is (2-4) to 1; and the number of the first and second electrodes,
the first, second and third thickeners may be the same or different;
the mass ratio of the mixture of the mixed retinol oil and the first thickener to the second thickener to the third thickener is (1-1.4): (0.05-0.08): (0.02-0.05).
2. The retinoid package according to claim 1, wherein the retinoid blend oil, the first thickener, the second thickener, and the third thickener form a blend, and the mass ratio of the blend to the second polydimethylsiloxane is (1-2): 1.
3. the retinoid package according to claim 1, wherein the retinoid compound comprises retinol and/or retinol esters.
4. The retinoid package according to any of claims 1-3, wherein the thickener comprises one or a combination of two or more of vinyl dimethicone/polymethylsiloxane silsesquioxane crosspolymer, dimethicone/vinyl dimethicone crosspolymer, and hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer.
5. A method for preparing a retinoid package according to any one of claims 1 to 4, comprising a step of mixing the components of the retinoid package.
6. The method of claim 5, comprising the steps of:
mixing the mixed retinol oil with a first thickening agent;
mixing the mixed retinol oil with the mixture of the first thickening agent, the second thickening agent and the third thickening agent to obtain a blend;
the blend was dispersed in a second polydimethylsiloxane to give a retinoid encapsulate.
7. Use of a retinoid coating according to any one of claims 1 to 4 in skin care products.
8. The use according to claim 7, wherein the skin care product comprises a lotion, cream, emulsion, jelly or essence.
9. Use according to claim 7 or 8, wherein said retinoid based coating is added in an amount of 1-5% of the skin care product.
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