CN108451837B

CN108451837B - Whitening liquid crystal composition and preparation method and application thereof

Info

Publication number: CN108451837B
Application number: CN201810690246.4A
Authority: CN
Inventors: 刘卫; 洪延涵; 闻庆; 卞思静; 韩非; 郭赛红
Original assignee: Wuhan Best Carrier Biotechnology Co ltd
Current assignee: Wuhan Best Carrier Biotechnology Co ltd
Priority date: 2018-06-28
Filing date: 2018-06-28
Publication date: 2020-10-13
Anticipated expiration: 2038-06-28
Also published as: CN108451837A

Abstract

The invention relates to the field of cosmetics, and provides a whitening liquid crystal composition, which comprises whitening active ingredients and a liquid crystal carrier; the whitening active ingredients comprise at least two of an exfoliating promoting active substance, a tyrosinase inhibitor, a melanosome migration inhibiting active substance, an antioxidant active substance, an anti-inflammatory active substance and an anti-saccharification active substance; the raw materials of the liquid crystal carrier comprise a liquid crystal emulsifier, an auxiliary emulsifier and an emulsifying thickener; the whitening liquid crystal composition also comprises liquid lipid and water for dissolving the whitening active ingredients and the liquid crystal carrier raw material. According to the invention, through compounding of different whitening mechanisms and loading of the liquid crystal carrier, a remarkable synergistic effect is obtained, the stability and whitening effect of the whitening liquid crystal composition can be remarkably improved, and the problem that skin irritation is easily caused by loading of high-concentration whitening active ingredients is solved.

Description

Whitening liquid crystal composition and preparation method and application thereof

Technical Field

The invention relates to the field of cosmetics, and particularly relates to a whitening liquid crystal composition and a preparation method and application thereof.

Background

Healthy and fair skin is a hot spot of concern for most women, and oriental women have been advocated with the whitening effect of "skin like snow, and skin like fat". However, the whitening skin care products on the market generally have the following problems:

1. the whitening mechanism is single: most products only aim at the formation and transfer mechanism of melanin, and cannot realize full-effect whitening;

2. the product stability is poor: when most whitening products in the market are manufactured, the whitening components are directly added into the formula, so that the products are easy to discolor and smell, and even paste is layered and thickened;

3. the whitening efficiency is low: because the skin has a barrier, the whitening active ingredients are difficult to permeate into the basal layer of the skin and cannot directly act on melanocytes, so that the whitening efficiency is greatly reduced;

4. easily cause skin irritation: the conventional whitening agent, such as glabridin and phenethyl resorcinol, is directly added into skin care products, and if the concentration is controlled improperly, skin irritation and even inflammation are easily caused.

Therefore, promoting the penetration of active ingredients, improving the stability and reducing the irritation is a difficult problem to be solved in the process of realizing the efficacy of the whitening cosmetics.

Disclosure of Invention

In order to solve the problems of single effect, poor stability, insufficient whitening effect and easy skin irritation of whitening products in the prior art, the invention provides a whitening liquid crystal composition which can load high-concentration whitening components, effectively control the slow release of the whitening active components, promote the skin permeation quantity, reduce the irritation and improve the whitening effect.

In order to solve the above problems, the present invention provides the following technical solutions:

the invention provides a whitening liquid crystal composition, which comprises whitening active ingredients and a liquid crystal carrier;

the whitening active ingredients comprise at least two of an exfoliating promoting active substance, a tyrosinase inhibitor, a melanosome migration inhibiting active substance, an antioxidant active substance, an anti-inflammatory active substance and an anti-saccharification active substance;

the raw materials of the liquid crystal carrier comprise a liquid crystal emulsifier, an auxiliary emulsifier and an emulsifying thickener;

the whitening liquid crystal composition also comprises liquid lipid and water for dissolving whitening active ingredients and/or liquid crystal carrier raw materials.

Preferably, based on the total mass of the whitening liquid crystal composition:

when the whitening active component comprises an exfoliation promoting active substance, the exfoliation promoting active substance accounts for 0.1-3% of the total mass of the whitening liquid crystal composition;

when the whitening active ingredients comprise the tyrosinase inhibitor, the tyrosinase inhibitor accounts for 0.1-10% of the total mass of the whitening liquid crystal composition;

when the whitening active ingredients comprise the active substance for inhibiting the migration of the melanosomes, the active substance for inhibiting the migration of the melanosomes accounts for 0.1 to 10 percent of the total mass of the whitening liquid crystal composition;

when the whitening active ingredients comprise antioxidant active substances, the antioxidant active substances account for 0.1-5% of the total mass of the whitening liquid crystal composition;

when the whitening active ingredients comprise anti-inflammatory active substances, the anti-inflammatory active substances account for 0.1-5% of the total mass of the whitening liquid crystal composition;

when the whitening active component comprises the anti-saccharification active substance, the anti-saccharification active substance accounts for 0.1-5% of the total mass of the whitening liquid crystal composition.

the liquid crystal carrier comprises the following raw materials in percentage by mass: 1-10% of liquid crystal emulsifier, 2-25% of co-emulsifier and 0.01-5% of emulsion thickener.

Preferably, the liquid lipid accounts for 2-35% of the total mass of the whitening liquid crystal composition, and the water accounts for 5-35% of the total mass of the whitening liquid crystal composition.

Preferably, the active substance for promoting the exfoliation is selected from one or more of salicylic acid, papain and bitter almond;

the tyrosinase inhibitor is selected from one or more of glabridin, phenethyl resorcinol, alpha-arbutin, ferulic acid and kojic acid;

the active substance for inhibiting the migration of the melanosome is one or two of nicotinamide and heparin sodium;

the antioxidant active substance is selected from one or more of vitamin C and derivatives thereof, vitamin E and derivatives thereof, polypeptide and hydroxytyrosol;

the anti-inflammatory active substance is one or two selected from glycyrrhetinic acid and paeonol;

the anti-saccharification active substance is selected from one or more of tea polyphenol, silymarin, phloretin, phlorizin, quercetin, curcumin and alpha-lipoic acid.

Preferably, the liquid crystal emulsifier is selected from one or more of polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene (40) monostearate, polyglyceryl-3-methylglucdistearate, soya lecithin, hydrogenated lecithin, cetearyl alcohol (and) coco glucoside, C14-22 alcohol (and) C12-20 alkyl glucoside, coco glucoside (and) coco alcohol, C22 alcohol alkyl phosphate, cetearyl glucoside, hydroxystearyl and hydroxystearyl glycosides, arachidyl and behenyl alcohol and arachidyl alcohol glucoside, behenyl alcohol alkyl phosphate, cetearyl alcohol and cetearyl glucoside, cetearyl alcohol and coco glucoside, and tetradecyl glucoside;

the auxiliary emulsifier is one or more selected from stearyl alcohol, hexanediol, polyethylene glycol, propylene glycol, dipropylene glycol, glycerol, 1, 3-butanediol and 1, 2-pentanediol;

the emulsifying thickener is one or more of carbomer, hydroxyethyl acrylate, polyacrylamide, polyacrylate-13 (and) polyisobutylene (and) polysorbate-20, polyvinylpyrrolidone, hydroxypropyl methylcellulose, sodium carboxymethylcellulose, sodium acrylate/sodium acryloyldimethyl taurate copolymer (and) isohexadecane (and) polysorbate-80, guar gum and acacia.

Preferably, the liquid lipid is selected from one or more of isopropyl myristate, isopropyl palmitate, caprylic capric glyceride, caprylic capric triglyceride, polyethylene glycol lauric glyceride, polyethylene glycol stearic glyceride, linoleic glyceride, propylene glycol monocaprylate, propylene glycol dicaprylate, cocoa butter octadecanoate, isononyl isononanoate, glyceryl triacetate, dimethicone, vitamin E, white oil, squalene, sunflower seed oil and soybean oil.

The invention also provides a preparation method of the whitening liquid crystal composition, which comprises the following steps:

A. dissolving liquid crystal emulsifier and water-insoluble whitening active ingredient with liquid lipid to obtain oil phase;

B. dissolving the auxiliary emulsifier and the emulsifying thickener with water to obtain a water phase;

C. dissolving the water-soluble whitening active ingredient in water to obtain a whitening active ingredient water solution;

D. mixing and emulsifying the oil phase obtained in the step A and the water phase obtained in the step B, and carrying out micron treatment to obtain a micron-sized dispersion;

E. c, mixing and emulsifying the aqueous solution of the whitening active ingredients obtained in the step C and the micron-sized dispersoid obtained in the step D, and carrying out nanocrystallization treatment to obtain a whitening liquid crystal composition;

there is no restriction on the order between steps A, B and C.

Preferably, in the step D, the micronization treatment is a shearing treatment to a micrometer scale;

in the step E, the nano treatment is shearing, high-pressure homogenization or high-pressure micro-jet treatment to the nano level.

The invention also provides application of the whitening liquid crystal composition in the technical scheme in preparation of cosmetics.

Compared with the prior art, the technical scheme provided by the invention has the following advantages:

the invention provides a whitening liquid crystal composition, which comprises whitening active ingredients and a liquid crystal carrier; the whitening active ingredients comprise at least two of an exfoliating promoting active substance, a tyrosinase inhibitor, a melanosome migration inhibiting active substance, an antioxidant active substance, an anti-inflammatory active substance and an anti-saccharification active substance; the raw materials of the liquid crystal carrier comprise a liquid crystal emulsifier, an auxiliary emulsifier and an emulsifying thickener; the whitening liquid crystal composition also comprises liquid lipid and water for dissolving the whitening active ingredients and the liquid crystal carrier raw material. According to the whitening liquid crystal composition, the components of different whitening mechanisms are compounded and the liquid crystal carrier is loaded, so that the remarkable synergistic effect is achieved, the stability and the whitening effect of the whitening liquid crystal composition can be remarkably improved, and the problem that the skin is easily irritated due to the fact that the high-concentration whitening active ingredient is loaded is solved.

The whitening component is directly added to prepare the cosmetic, so that the product is easy to deteriorate and delaminate, and the stability is poor. The liquid crystal carrier is mainly applied to the field of medicine, and the self stability of the liquid crystal structure also has a certain problem, and the liquid crystal structure can be reduced along with the storage time. The whitening liquid crystal composition provided by the invention adopts the liquid crystal emulsifier, the co-emulsifier and the emulsifying thickener as raw materials to construct the liquid crystal carrier, so that the loading capacity of the liquid crystal carrier can be obviously improved, and a stable liquid crystal structure is formed. Tests show that the whitening liquid crystal composition provided by the invention does not delaminate and precipitate after being centrifuged for half an hour in a centrifuge with the rotating speed of 12000 r/min; the liquid crystal can be stored for 3 months at 45 ℃ without layering and discoloring, and the liquid crystal structure is not reduced; the product has no delamination and discoloration after being stored for 3 years at normal temperature, and has good stability.

The skin whitening cream fully considers the influence of the skin structure state and the skin renewal period on the skin color, selects at least two of an exfoliating promotion active substance, a tyrosinase inhibitor, a melanosome migration inhibition active substance, an antioxidant active substance, an anti-inflammatory active substance and an anti-saccharification active substance, fundamentally eliminates the phenomenon of color spots and uneven skin color through multi-target effect, and realizes the effect of multi-target full-effect whitening.

The whitening ingredients in conventional cosmetics cannot be added too much, otherwise skin irritation is easily caused. According to the invention, a large amount of whitening active substances are encapsulated in the carrier by using the liquid crystal carrier, and are gradually released by using the slow release performance, so that the irritation of the whitening product to the skin can be reduced, more whitening active substances can be absorbed by the skin through the sustained release of the whitening substances, and the whitening effect is improved.

The liquid crystal carrier adopted by the invention has a unique internal double-channel structure and a huge membrane surface area, and can coat whitening active substances with different polarities and contents. The water-soluble whitening active substance is encapsulated in the water-based channel of the liquid crystal carrier, and the fat-soluble whitening active substance can be encapsulated in a lipid bilayer membrane of liquid crystal, so that the stability of the whitening active substance under light and heat can be effectively improved compared with the conventional W/O or O/W emulsion-encapsulated active substance.

The whitening liquid crystal composition provided by the invention has a structure very similar to that of oil/horny layer/water of human skin, can be adsorbed with the horny layer of the skin, and promotes effective penetration of whitening active ingredients, so that the whitening effect is enhanced.

The whitening liquid crystal composition provided by the invention has excellent moisturizing performance, good skin feel, good water locking effect and long water locking time.

The whitening liquid crystal composition provided by the invention can be used for preparing cosmetics, so that the cosmetics have the advantages of high-efficiency whitening, excellent skin feeling, small irritation, high-efficiency moisture retention and good stability. Meanwhile, the whitening liquid crystal composition provided by the invention has the structure capable of stimulating the natural regeneration function of skin, accelerating the metabolism of skin, and realizing effective whitening effect by synergistic action with whitening active ingredients.

Drawings

FIG. 1 is a polarization microscope photograph of a whitening liquid crystal composition prepared in example 3, magnified 100 times;

fig. 2 is a polarization microscope photograph of the whitening and moisturizing liquid crystal cream of example 19, magnified 100 times.

Detailed Description

the whitening liquid crystal composition also comprises liquid lipid and water for dissolving the whitening active ingredients and the liquid crystal carrier raw material.

Preferably, the whitening active ingredients comprise at least one of an exfoliating promoting active substance, a tyrosinase inhibitor and a melanosome migration inhibiting active substance. In the present invention, the whitening active ingredient preferably accounts for 0.5% to 30%, more preferably 10% to 20%, of the total mass of the raw materials of the whitening liquid crystal composition.

In the invention, the whitening active ingredients are coated by the liquid crystal carrier, and the compounded whitening active ingredients are co-delivered to realize the multi-target multi-mechanism synergistic effect. In the invention, the co-delivery refers to compounding and co-acting of the whitening active ingredients with multiple target points and multiple mechanisms of action. Specifically, the exfoliating cutin active substances selected by the invention act on the cuticle, the melanosome transfer inhibiting active substances act on the basal layer, the antioxidant and the anti-sensitizing agent act on the epidermis layer and the dermis layer, the anti-saccharification active substances act on the dermis layer, and the tyrosinase inhibitor acts on the basal layer.

In the present invention, the exfoliation promoting active includes, but is not limited to, salicylic acid, papain, and almond. Based on the total mass of the whitening liquid crystal composition: when the whitening active ingredients comprise the exfoliation promoting active substances, the mass percentage of the exfoliation promoting active substances is preferably 0.1-3%; more preferably 1% to 2%. Substances promoting exfoliation such as salicylic acid can soften horny layer, promote exfoliation, and remove melanin from skin by exfoliating excessive horny layer to achieve whitening effect. However, the conventional active substances for promoting the exfoliation of the epidermis can ensure the skin whitening effect after exfoliation by combining with moisturizing and sun protection, and the exfoliation of the stratum corneum is easy to cause skin allergy. The invention takes the active substance for promoting the exfoliation of the epidermis as one of the whitening active ingredients, and the whitening active ingredients and the whitening active substances with other action mechanisms act together, so that the multi-target whitening effect is more excellent. The liquid crystal carrier can provide sufficient moisturizing effect to simplify whitening steps, and the good skin feeling of the liquid crystal carrier can reduce irritation.

In the present invention, the tyrosinase inhibitors include, but are not limited to, glabridin, phenethyl resorcinol, α -arbutin, ferulic acid, and kojic acid. Based on the total mass of the whitening liquid crystal composition: when the whitening active component comprises the tyrosinase inhibitor, the mass percent of the tyrosinase inhibitor is preferably 0.1-10%; more preferably 1% to 5%. Tyrosinase inhibitor such as glabridin can inhibit tyrosinase activity in vivo, and prevent melanin generation, thereby reducing skin pigmentation, and effectively removing mottle and freckle. The tyrosinase inhibitor usually needs to permeate into the bottom layer of the skin to exert the blocking effect, and the tyrosinase inhibitor is difficult to effectively permeate in the mode of directly adding the tyrosinase inhibitor into the conventional cosmetics and the like, so that the tyrosinase inhibitor cannot effectively exert the effect. The liquid crystal carrier structure adopted by the invention is very similar to the skin structure, and can be adsorbed on the horny layer to promote effective permeation of whitening active ingredients, so that the whitening effect of the tyrosinase inhibitor is effectively exerted.

In the present invention, the active substances inhibiting the migration of melanosomes include, but are not limited to, nicotinamide and heparin sodium. Based on the total mass of the whitening liquid crystal composition: when the whitening active ingredients comprise the active substance for inhibiting the migration of the melanosomes, the mass percentage of the active substance for inhibiting the migration of the melanosomes is preferably 0.1-10%; more preferably 1% to 6%. Nicotinamide and the like act on produced melanin, prevent the transfer of the melanin to keratinocytes and reduce pigmentation. The liquid crystal carrier adopted by the invention can promote skin to absorb the active substances for inhibiting the migration of melanosomes, so that the active substances can really contact with melanin already formed on the bottom layer of the skin, and the excellent whitening effect is exerted.

In the present invention, antioxidant actives include, but are not limited to, vitamin C and its derivatives, vitamin E and its derivatives, polypeptides, and hydroxytyrosol. Based on the total mass of the whitening liquid crystal composition: when the whitening active ingredients comprise antioxidant active substances, the mass percentage of the antioxidant active substances is preferably 0.1-5%; more preferably 0.5% to 3%. The antioxidant active substance can effectively organize the black oxidation process, remove oxygen free radicals, and reduce melanin intermediate and melanin polymer, thereby effectively inhibiting melanin production. The liquid crystal carrier is adopted to load the antioxidant active substance and encapsulate the antioxidant active substance in the carrier, so that the storage time of the antioxidant active substance can be effectively prolonged, and the overall stability is improved.

In the present invention, the anti-inflammatory active substances include, but are not limited to, glycyrrhetinic acid and paeonol. Based on the total mass of the whitening liquid crystal composition: when the whitening active ingredient comprises the anti-inflammatory active substance, the mass percentage of the anti-inflammatory active substance is preferably 0.1-5%; more preferably 1% to 3%. The anti-inflammatory active substances such as glycyrrhetinic acid and the like have stronger anti-inflammatory, anti-allergic reaction and skin hormone-like effects, can reduce the biosynthesis of PEG2 in inflammatory tissues, and has obvious inhibition effect on acute inflammation caused by overhigh local concentration of whitening active ingredients.

In the present invention, the anti-glycation active substances include, but are not limited to, tea polyphenol, silymarin, phloretin, phlorizin, quercetin, curcumin, and alpha-lipoic acid. Based on the total mass of the whitening liquid crystal composition: when the whitening active ingredient comprises the anti-saccharification active substance, the mass percentage of the anti-saccharification active substance is preferably 0.1-5%; more preferably 0.5% to 3%. The anti-glycation active ingredients such as tea polyphenol can promote the generation of collagen, prevent the collagen and sugar molecules in the dermis from being crosslinked, thereby inhibiting tyrosinase from being activated in the presence of sugar to generate melanin, improving the quality of the collagen, repairing damaged skin cells, eliminating dark spots, and recovering the elasticity and luster of the skin.

In the present invention, the total mass of the raw materials of the liquid crystal carrier is preferably 3.5% to 35%, more preferably 5.5% to 31%, and most preferably 8.5% to 22% of the total mass of the raw materials of the whitening liquid crystal composition.

In the invention, the mass percentage of the liquid crystal emulsifier is preferably 1-10%, more preferably 2-8%, and most preferably 3-6% of the total mass of the whitening liquid crystal composition. In the present invention, the liquid crystal emulsifier includes, but is not limited to, polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene (40) monostearate, polyglyceryl-3-methylglucdistearate, soybean lecithin, hydrogenated lecithin, cetearyl alcohol (and) coco glucoside, C14-22 alcohol (and) C12-20 alkyl glucoside, coco glucoside (and) coco alcohol, C22 alcohol alkyl phosphate, cetearyl glucoside, hydroxystearyl alcohol and hydroxystearyl glucoside, arachidyl alcohol and behenyl alcohol and arachidyl alcohol glucoside, behenyl alcohol alkyl phosphate, cetearyl alcohol and cetearyl glucoside, cetearyl alcohol and coco glucoside, and tetradecyl glucoside.

Further preferably, the liquid crystal emulsifier is a mixture of 2-5 liquid crystal emulsifiers; more preferred are cetearyl glucoside, mixtures of hydroxystearyl alcohol with hydroxystearyl glucoside, arachidyl alcohol and behenyl alcohol and arachidyl alcohol glucoside, alkyl behenyl phosphate and cetearyl alcohol and cetearyl glucoside. The proportion of each component in the liquid crystal emulsifier is not particularly limited.

In the invention, the liquid crystal emulsifier plays a main role in forming a liquid crystal structure, the liquid crystal structure can be formed within the dosage range of the liquid crystal emulsifier defined in the invention, and the liquid crystal structure cannot be formed beyond the dosage range.

In the present invention, based on the total mass of the whitening liquid crystal composition: the mass percentage of the co-emulsifier is preferably 2-25%, more preferably 3-20%, and most preferably 5-15%.

In the present invention, the co-emulsifier includes, but is not limited to, stearyl alcohol, hexylene glycol, polyethylene glycol, propylene glycol, dipropylene glycol, glycerin, 1, 3-butylene glycol, and 1, 2-pentanediol. The auxiliary emulsifier is preferably a mixture of 2-4 auxiliary emulsifiers; more preferably, the co-emulsifier is hexylene glycol, propylene glycol, glycerin, and 1, 3-butylene glycol. The proportion of each component in the co-emulsifier is not particularly limited.

In the invention, the coemulsifier can ensure that the interface arrangement of the liquid crystal emulsifier is more orderly and more rigid, and can also adjust the HLB (hydrophile-lipophile balance) value of the interface layer of the liquid crystal emulsifier, thereby ensuring that the liquid crystal structure is more stable and preventing the disappearance of the liquid crystal structure.

In the present invention, based on the total mass of the whitening liquid crystal composition: the weight percentage of the emulsifying thickener is preferably 0.01-5%, more preferably 0.1-3%, and most preferably 0.3-1%.

In the present invention, the emulsifying thickener includes, but is not limited to, carbomer, hydroxyethyl acrylate, polyacrylamide, polyacrylate-13 (and) polyisobutylene (and) polysorbate-20, polyvinylpyrrolidone, hydroxypropylmethylcellulose, sodium carboxymethylcellulose, sodium acrylate/sodium acryloyldimethyl taurate copolymer (and) isohexadecane (and) polysorbate-80, guar gum, and acacia. Preferably, the emulsifying thickener is a mixture of 2-4 emulsifying thickeners; more preferably, the mixture is hydroxyethyl acrylate, polyacrylamide, polyvinylpyrrolidone, and sodium carboxymethyl cellulose. The invention has no special limitation on the proportion of each component in the mixture of the emulsifying thickener.

In the invention, the emulsifying thickener can increase the stability of the liquid crystal emulsion, is beneficial to forming a liquid crystal network structure system and reduces the sensitivity of a liquid crystal carrier to temperature.

In the present invention, the whitening liquid crystal composition further comprises a solvent for dissolving the whitening active ingredient and the liquid crystal carrier material, namely, a liquid lipid for dissolving the water-insoluble ingredient and water for dissolving the water-soluble ingredient.

In the present invention, the water is preferably 5 to 35% by mass, and more preferably 10 to 25% by mass, based on the total mass of the whitening liquid crystal composition. In the present invention, the water is preferably distilled water.

In the present invention, the liquid lipid is preferably 2 to 35% by mass, more preferably 5 to 30% by mass, and most preferably 8 to 25% by mass, based on the total mass of the whitening liquid crystal composition.

In the present invention, the liquid lipid preferably includes isopropyl myristate, isopropyl palmitate, caprylic capric glyceride, caprylic capric triglyceride, polyethylene glycol lauric glyceride, polyethylene glycol stearic glyceride, linoleic glyceride, propylene glycol monocaprylate, propylene glycol dicaprylate, cocoa butter octadecanoate, isononyl isononanoate, triacetin, dimethicone, vitamin E, white oil, squalene, sunflower seed oil, and soybean oil. In the present invention, the liquid lipid is preferably a mixture of 2 to 4 kinds of the above liquid lipids; more preferably a mixture of hydroxyethyl acrylate, polyacrylamide, polyvinylpyrrolidone and sodium carboxymethyl cellulose. The present invention is not particularly limited to the ratio of the components in the liquid lipid mixture.

there is no restriction on the order between steps A, B and C.

The whitening composition is divided into a water-soluble whitening active ingredient and a water-insoluble whitening active ingredient according to the water solubility of the whitening active ingredient, and the water-soluble whitening active ingredient and the water-insoluble whitening active ingredient are respectively dissolved by different solvents.

The liquid crystal emulsifier and the water-insoluble whitening active ingredients are dissolved by liquid lipid to obtain an oil phase for later use.

The invention dissolves the auxiliary emulsifier and the emulsifying thickener by part of water to obtain a water phase for later use.

The invention dissolves the water-soluble whitening active ingredient with the rest water to obtain the whitening active ingredient aqueous solution for standby.

The present invention is not particularly limited to the sequence of the above three steps.

The oil phase and the water phase prepared by the method are mixed and then dispersed to micron level, so that a liquid crystal carrier can be formed, and the liquid crystal carrier is encapsulated with the water-insoluble whitening active ingredient. Mixing the water solution of the whitening active ingredient with the micron-sized dispersoid, dispersing the mixture to the nanometer scale, and encapsulating the water-soluble whitening active ingredient into a liquid crystal carrier to obtain the whitening liquid crystal composition.

In the present invention, the micronization treatment preferably employs a shearing method, and more preferably, the conditions of the shearing treatment to micrometer scale are as follows: the shearing rotating speed is 5000-15000 rpm, preferably 6000-13000 rpm; the shearing time is 1-10 min, preferably 2-5 min.

In the present invention, the nanocrystallization treatment is preferably performed by shearing, high-pressure homogenization or high-pressure microfluidization.

When the shearing treatment is carried out to the nanometer level, the shearing rotating speed is preferably 5000-15000 rpm, and more preferably 6000-10000 rpm; the shearing time is preferably 1-10 min, and more preferably 2-8 min.

When high-pressure homogenization treatment is adopted to reach the nanometer level, the heating temperature is preferably 50-75 ℃, and more preferably 60-70 ℃; the homogenizing pressure is preferably 500-1000 bar, and more preferably 600-800 bar; the number of homogenization is preferably 1 to 3, and more preferably 2.

When the nano-scale treatment is carried out by adopting a high-speed microjet technology, the feeding temperature is preferably 50-70 ℃, and more preferably 60-65 ℃; the pressure is preferably 60-160 MPa, and more preferably 100-120 MPa; the number of homogenization is preferably 1 to 3, and more preferably 2.

In the invention, the particle size of the whitening liquid crystal composition prepared by the method is preferably 100-900 nm, and more preferably 300-700 nm.

The invention also provides application of the whitening liquid crystal composition in the technical scheme in preparation of cosmetics. Specifically, the whitening liquid crystal composition is used for preparing cosmetics with the effects of whitening, moisturizing, sun screening and the like.

In the present invention, the form of the cosmetic includes, but is not limited to, cream, milky lotion, cream, essence, pack.

In the invention, when the whitening liquid crystal composition is prepared into a cosmetic, the whitening liquid crystal composition accounts for 5-50% of the total mass of the cosmetic, and more preferably 10-30%.

In order to further illustrate the present invention, the following embodiments are described in detail, but they should not be construed as limiting the scope of the present invention.

Example 1

Melting 1.0% of soybean lecithin, 2.0% of cetearyl alcohol (and) coco glucoside, 4.0% of isopropyl palmitate, 2.0% of isopropyl myristate and 2% of glabridin in percentage by mass in a water bath at 70 ℃ to obtain an oil phase for later use;

mixing 0.1% ferulic acid, 0.1% arbutin, 1.0% nicotinamide, 0.1% VC and derivatives, 1.0% glycyrrhetinic acid, 5.0% tea polyphenols and 30% water, stirring at 35 deg.C water bath condition to obtain whitening active ingredient water solution;

dissolving 2.0% of polyethylene glycol, 3.0% of hexanediol and 0.01% of hydroxyethyl acrylate into 46.6% of water, and stirring in a water bath at 70 ℃ to obtain a water phase for later use;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 5min under the condition that the rotating speed is 5500rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 1min under the condition that the rotating speed is 5000rpm to obtain the whitening liquid crystal composition.

Example 2

According to the mass percentage, 0.5 percent of hydrogenated lecithin, 0.5 percent of hydroxystearyl alcohol and hydroxystearyl glucoside, 2.0 percent of caprylic/capric triglyceride, 2.0 percent of dioctyl/capric propylene glycol ester and 1.0 percent of VE are melted under the condition of water bath at 65 ℃ to obtain an oil phase for later use;

mixing 3.0% of alpha-arbutin, 3.0% of nicotinamide, 1.0% of vitamin C ethyl ether, 2.0% of silymarin and 35% of water, and stirring in a water bath at 40 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 2.0% stearyl alcohol, 3.0% hexanediol, 2.0% sodium acrylate/sodium acryloyldimethyl taurate copolymer (and) isohexadecane (and) polysorbate-80 and 3.0% carbomer in 35% water, and stirring in 65 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 1min under the condition that the rotating speed is 5000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with the aqueous solution of the whitening active ingredient, and homogenizing for 1 time at the temperature of 50 ℃ and the homogenizing pressure of 1000bar to obtain the whitening liquid crystal composition.

Example 3

Melting 2.0% of C14-22 alcohol (and) C12-20 alkyl glucoside, 3.0% of polyglycerol-3-methyl glucose distearate, 4.0% of cocoa butter octyldecanoate, 6.0% of glycerol laurate of polyethylene glycol, 4.0% of squalene and 1% of phenethyl resorcinol in percentage by mass under the condition of a water bath at 80 ℃ to obtain an oil phase for later use;

mixing 7.0% of alpha-arbutin, 6% of nicotinamide, 0.1% of mandelic acid, 5% of VC, 3% of tea polyphenol and 20% of water, and stirring in a water bath at 45 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 1.0% polyethylene glycol, 0.5% sodium carboxymethylcellulose and 0.05% guar gum in 38.35% water, and stirring in 80 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 7min under the condition that the rotating speed is 8000rpm to obtain a micron-sized dispersion;

mixing the micrometer-scale dispersion with the aqueous solution of whitening active ingredient, and homogenizing at 75 deg.C and 500bar for 5 times.

Example 4

Melting 3.5% of cetearyl glucoside, 5.0% of caprylic capric glyceride, 2.0% of vitamin E and 5.0% of polyethylene glycol glyceryl stearate in percentage by mass under the condition of water bath at 80 ℃ to obtain an oil phase for later use;

mixing 4.0% of alpha-arbutin, 3.0% of nicotinamide, 4.0% of vitamin C ethyl ether, 5.0% of hydroxytyrosol, 5.0% of phloretin and 23% of water, and stirring in a water bath at 40 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 1.0% of propylene glycol, 2.0% of 1, 3-butanediol, 0.5% of hydroxyethyl acrylate and 0.5% of polyvinylpyrrolidone into 36.5% of water, and stirring in a water bath at 75 ℃ to obtain a water phase for later use;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 3min under the condition that the rotating speed is 10000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 1min under the condition that the rotating speed is 12000rpm to obtain the whitening liquid crystal composition.

Example 5

According to the mass percentage, 2.0% tetradecyl glucoside, 3.0% cetearyl alcohol and cocoyl glucoside, 1.0% cetearyl alcohol and cetearyl glucoside, 4.0% caprylic/capric triglyceride, 2.0% macrogol lauric glyceride, 1.0% glycyrrhetinic acid, 4.0% dimethyl silicone oil and 1.0% glabridin are melted in a water bath condition at 85 ℃ to obtain an oil phase for later use;

mixing 10.0% alpha-arbutin, 3.0% nicotinamide, 2.0% quercetin and 28% water, and stirring in 35 deg.C water bath to obtain whitening active ingredient water solution;

dissolving 1.0% stearyl alcohol, 3.0% hexanediol, 1.5% polyacrylate-13 (and) polyisobutylene (and) polysorbate-20, and 0.5% polyvinylpyrrolidone in 33% water, and stirring in 85 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 4min under the condition that the rotating speed is 13000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersion with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 3min under the condition that the rotating speed is 11000rpm to obtain the whitening liquid crystal composition.

Example 6

According to the mass percentage, 3.0 percent of polyoxyethylene-polyoxypropylene segmented copolymer, 1.0 percent of polyoxyethylene (40) monostearate, 1.0 percent of cetearyl glucoside, 4.0 percent of isopropyl palmitate, 3.0 percent of propylene glycol monocaprylate, 4.0 percent of glyceryl triacetate, 5.0 percent of polyethylene glycol lauric glyceride, 2.0 percent of curcumin and 0.1 percent of glabridin are melted in a water bath condition at 85 ℃ to obtain an oil phase for later use;

dissolving 1.0% polyethylene glycol, 2.0% dipropylene glycol, 1.5% carbomer, 0.1% paeonol and 1.5% guar gum in 70.8% water, and stirring in 85 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and homogenizing for 5 times at 50 deg.C and 160Mpa by high-speed microfluidization technology to obtain whitening liquid crystal composition.

Example 7

According to the mass percentage, 2.3 percent of polyoxyethylated 4OE sorbitan monostearate, 3.2 percent of cetearyl glucoside, 3 percent of salicylic acid, 2.0 percent of caprylic/capric triglyceride and 4.0 percent of isopropyl myristate are melted in a water bath at the temperature of 70 ℃ to obtain an oil phase for later use;

mixing 0.1% of alpha-arbutin, 5.0% of vitamin C ethyl ether, 10.0% of nicotinamide, 0.5% of alpha-lipoic acid and 15% of water, and stirring in a water bath at 45 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 2.0% of propylene glycol and 0.1% of hydroxyethyl acrylate in 22.7% of water, and stirring in a water bath at 70 ℃ to obtain a water phase for later use;

mixing the water phase and the oil phase, and homogenizing for 1 time at 75 deg.C and 60Mpa by high-speed microfluidization technology to obtain whitening liquid crystal composition.

Example 8

According to the mass percentage, 1.0 percent of arachidyl alcohol, behenyl alcohol and arachidyl alcohol glucoside, 3.0 percent of tetradecyl glucoside, 5.0 percent of isopropyl octapalmitate, 5.0 percent of quercetin, 5.0 percent of polyethylene glycol glyceryl stearate, 5.0 percent of isononyl isononanoate and 3.0 percent of phenethyl resorcinol are melted under the condition of 80 ℃ water bath to obtain an oil phase for standby;

mixing 8.0% of alpha-arbutin, 8.0% of nicotinamide and 18% of water, and stirring in a water bath at 55 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 3.0% of dipropylene glycol, 8.0% of glycerol, 3.0% of guar gum and 0.2% of carbomer in 24.8% of water, and stirring in a water bath at the temperature of 80 ℃ to obtain a water phase for later use;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 10min under the condition that the rotating speed is 13000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 2min under the condition that the rotating speed is 12000rpm to obtain the whitening liquid crystal composition.

Example 9

According to the mass percentage, 3.0 percent of cetearyl glucoside, 5.0 percent of simethicone, 5.0 percent of squalene and 3.0 percent of vitamin E are melted under the condition of 80 ℃ water bath to obtain an oil phase for standby;

mixing 5.0% alpha-arbutin, 10.0% nicotinamide, 0.1% mandelic acid and 27% water, stirring at 40 deg.C water bath condition to obtain whitening active ingredient water solution;

dissolving 5.0% of glycerol, 10.0% of 1, 3-butanediol, 0.008% of sodium acrylate/sodium acryloyldimethyl taurate copolymer (and) isohexadecane (and) polysorbate-80 and 0.002% of hydroxypropyl methyl cellulose in 26.89% of water, and stirring in a water bath at 80 ℃ to obtain a water phase for later use;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 6min under the condition that the rotating speed is 14000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 5min under the condition that the rotating speed is 13000rpm to obtain the whitening liquid crystal composition.

Example 10

According to the mass percentage, 1.0 percent of polyglycerol-3 methyl glucose distearate, 1.0 percent of coco glucoside (and) coco alcohol, 4.0 percent of hydroxystearyl alcohol and hydroxystearyl glycoside, 5.0 percent of caprylic/capric triglyceride, 2.0 percent of vitamin E, 10.0 percent of polyethylene glycol glyceryl stearate, 3.0 percent of salicylic acid and 0.5 percent of glabridin are melted in a water bath condition at 80 ℃ to obtain an oil phase for later use;

mixing 5.0% of alpha-arbutin, 8.0% of nicotinamide, 1.0% of tea polyphenol and 20% of water, and stirring in a water bath at 55 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 5.0% glycerol, 5.0% 1, 2-pentanediol, 0.25% acacia and 0.25% polyacrylate-13 (and) polyisobutylene (and) polysorbate-20 in 29% water, and stirring in 80 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 5min under the condition that the rotating speed is 12000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 3min under the condition that the rotating speed is 12000rpm to obtain the whitening liquid crystal composition.

Example 11

According to the mass percentage, 2.0 percent of behenyl alcohol alkyl phosphate, 2.0 percent of cetearyl alcohol and cetearyl glucoside, 5.0 percent of vitamin E, 2.0 percent of dimethyl silicon oil, 15.0 percent of white oil, 1.0 percent of glycyrrhetinic acid and 1.0 percent of phenethyl resorcinol are melted under the condition of water bath at 75 ℃ to obtain an oil phase for later use;

mixing 8.0% of alpha-arbutin, 10.0% of nicotinamide, 2.0% of VC and 24% of water, and stirring in a water bath at 60 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 5.0% glycerol, 0.25% sodium carboxymethylcellulose and 0.25% polyacrylamide in 22.5% water, and stirring in 75 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 6min under the condition that the rotating speed is 13000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersion with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 2min under the condition that the rotating speed is 11000rpm to obtain the whitening liquid crystal composition.

Example 12

According to the mass percentage, 0.5 percent of behenyl alcohol alkyl phosphate, 2.5 percent of arachidyl alcohol and behenyl alcohol and arachidyl alcohol glucoside, 4.0 percent of sunflower seed oil, 5.0 percent of white oil, 1.0 percent of vitamin C ethyl ether and 8.0 percent of glabridin are melted under the condition of water bath at 80 ℃ to obtain an oil phase for later use;

mixing 10.0% of alpha-arbutin, 3.0% of nicotinamide, 1% of paeonol, 2% of hydroxytyrosol and 21% of water, and stirring in a water bath at 55 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 2.0% of hexanediol, 6.0% of 1, 3-butanediol, 1.0% of C22 alcohol alkyl phosphate, 0.2% of Arabic gum and 0.2% of hydroxyethyl acrylate into 32.6% of water, and stirring in a water bath at the temperature of 80 ℃ to obtain a water phase for later use;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 5min under the condition that the rotating speed is 14000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 6min under the condition that the rotating speed is 12000rpm to obtain the whitening liquid crystal composition.

Example 13

According to the mass percentage, 2.5 percent of hydroxystearyl alcohol and hydroxystearyl glycoside, 1.5 percent of behenyl alcohol alkyl phosphate, 4.0 percent of soybean oil, 3.0 percent of polyethylene glycol glyceryl stearate, 2.0 percent of phloretin, 5.0 percent of white oil and 2.0 percent of salicylic acid are melted under the condition of 75 ℃ water bath to obtain an oil phase for later use;

mixing 9.0% nicotinamide, 6.0% vitamin C ethyl ether and 22% water, and stirring in 40 deg.C water bath to obtain whitening active ingredient water solution;

dissolving 7.0% glycerol, 4.0% propylene glycol, 0.5% polyacrylate-13 (and) polyisobutylene (and) polysorbate-20 and 1.5% hydroxypropyl methylcellulose in 30% water, and stirring in 75 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 3min under the condition that the rotating speed is 13000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with the aqueous solution of the whitening active ingredients, and carrying out high-speed shearing emulsification for 1min under the condition that the rotating speed is 10000rpm to obtain the whitening liquid crystal composition.

Example 14

Melting 5.0% of polyglycerol-3-methylglucose distearate, 3.0% of behenyl alcohol alkyl phosphate, cetearyl alcohol and cetearyl glucoside, 2.0% of cetearyl alcohol and cetearyl glucoside, 5.0% of caprylic capric glyceride, 5.0% of polyethylene glycol glyceryl stearate, 2.0% of mandelic acid, 5.0% of silymarin and 5.0% of white oil by mass percent in a water bath condition at 75 ℃ to obtain an oil phase for later use;

mixing 2.0% of alpha-arbutin, 5.0% of nicotinamide, 0.1% of vitamin C ethyl ether and 20% of water, and stirring in a water bath at 35 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 7.0% of hexanediol, 12.0% of glycerol, 0.5% of polyacrylamide and 0.2% of hydroxypropyl methylcellulose into 21.2% of water, and stirring in a water bath at the temperature of 80 ℃ to obtain a water phase for later use;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 8min under the condition that the rotating speed is 14000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 4min under the condition that the rotating speed is 13000rpm to obtain the whitening liquid crystal composition.

Example 15

According to the mass percentage, 1.0 percent of hydroxystearyl alcohol and hydroxystearyl glycoside, 5.0 percent of cetearyl alcohol and coco glucoside, 8.0 percent of caprylic capric glyceride, 8.0 percent of linoleic glyceride, 8.0 percent of white oil, 8.0 percent of caprylic capric triglyceride, 3.0 percent of vitamin E, 0.5 percent of glabridin, 0.5 percent of salicylic acid and 1.5 percent of phenethyl resorcinol are melted under the condition of water bath at 85 ℃ to obtain an oil phase for standby;

mixing 3.0% of alpha-arbutin, 3.0% of nicotinamide and 17% of water, and stirring in a water bath at 55 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 3.0% of dipropylene glycol, 8.0% of glycerol, 2.0% of paeonol, 1.0% of tea polyphenol, 3.0% of guar gum and 0.2% of carbomer in 24.3% of water, and stirring in a water bath at the temperature of 80 ℃ to obtain a water phase for later use;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 10min under the condition that the rotating speed is 15000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 3min under the condition that the rotating speed is 14000rpm to obtain the whitening liquid crystal composition.

Example 16

Melting 1.0% of coco glucoside (and) coco alcohol, 3.0% of hydroxystearyl alcohol and hydroxystearyl glycoside, 5.0% of soybean lecithin, 5.0% of isononyl isononanoate and 4.0% of sunflower seed oil in terms of mass percentage under the condition of water bath at 90 ℃ to obtain an oil phase for later use;

mixing 10.0% of alpha-arbutin, 4.0% of nicotinamide and 22% of water, and stirring in a water bath at 55 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 10.0% stearyl alcohol, 3.0% dipropylene glycol, 12.0% glycerol, 0.2% polyacrylamide and 0.2% polyvinylpyrrolidone in 20.6% water, and stirring in 90 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 6min under the condition that the rotating speed is 15000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 6min under the condition that the rotating speed is 15000rpm to obtain the whitening liquid crystal composition.

Example 17

Melting 6.0% of arachidyl alcohol, behenyl alcohol and arachidyl alcohol glucoside, 10.0% of cocoa butter octadecanoate and 10.0% of squalene in terms of mass percent in a water bath at 85 ℃ to obtain an oil phase for later use;

mixing 5% of alpha-arbutin, 5.0% of nicotinamide and 24% of water, and stirring in a water bath at 30 ℃ to obtain a whitening active ingredient aqueous solution for later use;

dissolving 5.0% glycerol, 12.0% stearyl alcohol, 0.5% polyacrylamide and 0.5% polyvinylpyrrolidone in 22% water, and stirring in 85 deg.C water bath to obtain water phase;

mixing the water phase and the oil phase, and after mixing, carrying out high-speed shearing emulsification for 10min under the condition that the rotating speed is 14000rpm to obtain a micron-sized dispersion;

mixing the micron-sized dispersoid with a whitening active ingredient aqueous solution, and carrying out high-speed shearing emulsification for 7min under the condition that the rotating speed is 12000rpm to obtain the whitening liquid crystal composition.

Example 18

The whitening liquid crystal composition is respectively placed at 45 ℃, 4 ℃, illumination, room temperature and re-melting conditions for examining the stability, and the shape stability of the liquid crystal is observed in a polarizing microscope at 1 week, 3 weeks, 5 weeks, 7 weeks and 9 weeks. Table 1 shows the overall stability of the whitening liquid crystal compositions at 45 ℃, 4 ℃, under light, room temperature and under re-melting conditions:

table 1 stability of whitening liquid crystal compositions

As shown in fig. 1, the polarization microscope images of the whitening liquid crystal composition taken in the stability test at a magnification of 100 times were obtained, and the number of liquid crystals of the whitening liquid crystal composition after being left for 1 week, 3 weeks, 5 weeks, 7 weeks, and 9 weeks was the same as that of fig. 1 and was not significantly changed in the stability test.

The stability test result shows that: the whitening liquid crystal composition provided by the invention has no delamination and precipitation phenomenon after 1 week, 3 weeks, 5 weeks, 7 weeks and 9 weeks under the conditions of 45 ℃, 4 ℃, illumination, room temperature and re-melting. The liquid crystal is observed under a polarizing microscope, has a large number and uniform size, and meets the requirements of practical application (the liquid crystal is stable when placed at 45 ℃ for 3 months, and is considered to be stable when placed at normal temperature for 3 years in the field of cosmetics). Particularly, the whitening liquid crystal composition is still stable under the condition of containing higher whitening active ingredients, so that the whitening liquid crystal composition provided by the invention has good stability.

Example 19 whitening and moisturizing liquid crystal face cream

Melting 2.0% of PEC-10 polydimethylsiloxane, 1.0% of sucrose stearate, 1.0% of stearyl alcohol, 4.5% of glyceryl monostearate, 1.0% of hexadecanol and octadecanol, and 3.0% of jojoba oil in a water bath at 75 ℃ by mass percent to obtain an oil phase;

dissolving 5.0% glycerol, 5.0% propylene glycol, 0.3% triethanolamine, 0.2% carbomer 2020 and 77.0% purified water in 75 deg.C water bath to obtain water phase; mixing the oil phase and the water phase under stirring, and emulsifying to obtain common cream.

Mixing the common cream with the whitening liquid crystal composition in example 3 according to a ratio of 1:1 to obtain the cream with the mass fraction of 50.0% of the whitening liquid crystal composition, wherein the cream contains 3.5% of alpha-arbutin, 3% of nicotinamide, 0.05% of phenethyl resorcinol, 2.5% of VC and 0.05% of mandelic acid by mass percentage, and the total content of whitening active substances is 9.55%.

The prepared whitening and moisturizing liquid crystal cream is magnified by 100 times under a polarization microscope to obtain a polarization microscope image shown in fig. 2, as shown in fig. 2, the liquid crystal size of the whitening and moisturizing liquid crystal cream is uniform, and the effective components are coated in a liquid crystal structure.

Comparative example 1

Melting 0.05% of phenethyl resorcinol, 2.0% of PEC-10 polydimethylsiloxane, 1.0% of sucrose stearate, 1.0% of stearyl alcohol, 4.5% of glyceryl monostearate, 1.0% of hexadecadecyl alcohol and 3.0% of jojoba oil in a water bath at 75 ℃ by mass percent to obtain an oil phase;

mixing 3.5% of alpha-arbutin, 3% of nicotinamide, 0.05% of mandelic acid, 2.5% of VC, 5.0% of glycerol, 5.0% of propylene glycol, 0.3% of triethanolamine, 0.2% of carbomer 2020 and 67.9% of water, and stirring in a water bath at 45 ℃ to obtain a whitening active ingredient aqueous solution for later use;

mixing the oil phase and the water phase under stirring, and emulsifying to obtain a basic formula facial cream, wherein the basic formula facial cream contains 3.5% of alpha-arbutin, 3% of nicotinamide, 0.05% of phenethyl resorcinol, 2.5% of VC and 0.05% of mandelic acid by mass, and the total content of the whitening active substances is 9.1%.

The base formula cream prepared in comparative example 1 has the same content of the whitening active ingredient as that of example 19 except that the whitening active ingredient is not coated with a liquid crystal structure.

Comparative example 2O/W emulsion containing no liquid crystalline structure

According to the mass percentage, 2.0 percent of vitamin E, 4.0 percent of alpha-arbutin, 3.0 percent of nicotinamide, 4.0 percent of vitamin C ethyl ether, 5.0 percent of hydroxytyrosol, 5.0 percent of phloretin, 3.0 percent of stearic acid, 4.5 percent of glycerin monostearate, 5.0 percent of cetostearyl alcohol and 6.0 percent of polydimethylsiloxane are melted in a water bath at 75 ℃ to obtain an oil phase;

dissolving 10.0% glycerol, 5.0% propylene glycol, 0.3% triethanolamine and 63.2% purified water in 75 deg.C water bath to obtain O/W emulsion containing no liquid crystal structure, i.e. control group composite whitening composition.

The whitening active ingredient content of comparative example 2 is the same as that of the whitening liquid crystal composition prepared in example 4, except that the whitening active ingredient of comparative example 2 is coated with an O/W structure, and example 4 is coated with a liquid crystal structure.

Example 20

The test verifies the skin absorption and permeation performance of the whitening liquid crystal composition.

In-vitro transdermal experiments adopt an improved Franz diffusion cell and male SD rat abdominal skin with the weight of 160-220 g as a model. The diffusion cell parameters were: effective diffusion area 3.14cm²The volume of the receiving tank is 7.0mL, the receiving solution is physiological saline, and the magnetic stirring speed is 200 rpm.

The intact rat abdominal skin was secured between the receiving and feeding basins (inner skin layer facing the receiving basin); keeping the constant temperature of the receiving pool at 37.0 +/-0.5 ℃, sucking 0.35mL of receiving solution in 1h, 2h, 4h, 6h, 8h, 10h and 24h respectively, supplementing and releasing 0.35mL of substance to be detected, and filtering the receiving solution by using a 0.22 mu m organic filter membrane.

Since each of 2, 4, 5, 12 and 15 in the whitening liquid crystal composition examples contains 3% of nicotinamide, the concentration of nicotinamide in the receiving solution is measured by using high performance liquid chromatography, the cumulative transdermal permeation amount at each time point is calculated, and a transdermal absorption drug-time curve is drawn to know the in vitro transdermal permeation effect of nicotinamide.

The cumulative transdermal quantity per unit area of nicotinamide is calculated according to the following formula:

wherein: q_sCumulative transdermal mass; s is the effective diffusion area; v is the volume of the physiological saline in the receiving pool; c_iThe concentration of the drug in the receiving solution is from the 1 st to the last sampling; n is the nth sample volume; cn is the concentration of the drug in the receiving fluid at the time of the sampling.

In conclusion, the whitening liquid crystal composition has the advantages of low skin permeation and high retention, excellent skin care effect and long-acting whitening.

Example 21

The test verifies the water locking performance of the whitening liquid crystal composition.

The liquid crystal structure can form a structure the same as the real stratum corneum lipid, has higher affinity with the skin, and also has the same efficacy as the stratum corneum intercellular lipid. Due to its unique double-layer structure, it can be adsorbed on the stratum corneum of skin to form a protective layer, and has moisture keeping effect.

1. Determination of moisture content and moisture loss in the stratum corneum

The experimental method comprises the following steps: selecting 24 volunteers with healthy skin and no cosmetic allergy history and about 20-35 years old, and keeping the indoor temperature at 25 +/-1 ℃; and detecting under the environment with the humidity of 50% +/-5%. In the experiment, 0.5g of the corresponding product is smeared on the skin of 4cm multiplied by 4cm at the inner side of the arm as a test area.

Volunteers were randomly divided into two groups, one group was a test group with 12 persons each, and the whitening and moisturizing liquid crystal cream prepared in example 19 was applied, and the other group was a control group with the base formula cream prepared in comparative example 2.

Measurement: in a 4cm x 4cm test area on the inside of the arm, the test is carried out 15min after application of the product:

(1) the moisture content of the skin on the inner side of the arm was measured using a skin moisture detector. After using the corresponding product for 0h, 0.5h, 1h, 2h, 4h and 6h, testing the moisture content of the skin on the inner side of the arm, respectively measuring for 3 times, and taking an average value.

(2) Measuring the water loss value of skin with percutaneous water loss measuring instrument, measuring the skin loss amount of the inner side of arm after using corresponding products for 0h, 0.5h, 1h, 2h, 4h and 6h, respectively measuring for 3 times, and averaging.

The experimental results are as follows:

(1) determination of the moisture content of the stratum corneum

The change of the moisture content of the stratum corneum is measured by measuring the change of the capacitance of the stratum corneum of the skin before and after the product is used by a skin moisture tester, so that the evaluation of the moisturizing effect of the cosmetics is a common evaluation method at present. The effect of the inventive whitening liquid crystal composition-containing cream on the moisture content of the skin is shown in table 2.

Table 2 moisture content test value (%)

Group of	0h	0.5h	1h	2h	4h	6h
							Test group	57.43	50.24	44.69	44.23	43.73	43.13
Control group	54.12	40.27	36.94	30.21	27.12	28.43

As can be seen from table 2, compared with the control group, the moisture content of the cream containing the whitening liquid crystal composition applied to the test group is significantly different (p is less than 0.05), which indicates that the cream containing the whitening liquid crystal composition has a significant moisturizing effect, and the moisturizing time is longer than that of the base formula cream.

(2) Determination of the percutaneous loss of Water

The water dispersion loss of the skin can represent the water locking function of the cosmetic, the smaller the value of the water dispersion loss is, the less the water dispersion is, the stronger the water locking function is, and on the contrary, the weaker the water locking capacity is. The water loss values were measured using a skin water loss tester and the results are shown in table 3.

Table 3 moisture loss value (%)

Group of	0h	0.5h	1h	2h	4h	6h
							Test group	12.44	10.42	8.97	9.56	10.12	10.54
Control group	13.72	14.07	14.84	14.12	13.98	13.27

As can be seen from Table 3, compared with the control group, after the test group is smeared with the facial cream containing the whitening liquid crystal composition, the loss of skin moisture is effectively reduced within 2-6 h (p is less than 0.05), and the facial cream containing the whitening liquid crystal composition has a good water locking effect and long water locking time.

Comparative example 3

mixing 9.5% of alpha-arbutin, 5.0% of glycerol, 5.0% of propylene glycol, 0.3% of triethanolamine, 0.2% of carbomer 2020 and 67.5% of water, and stirring in a water bath at 45 ℃ to obtain a whitening active ingredient aqueous solution for later use;

mixing the oil phase and the water phase under stirring, and emulsifying to obtain alpha-arbutin facial cream containing whitening active substances containing 9.5% of alpha-arbutin by mass.

Comparative example 4

The procedure was the same as in comparative example 3 except that 9.5% of α -arbutin in comparative example 3 was replaced with 9.5% of niacinamide, to obtain a niacinamide cream.

Comparative example 5

The same procedure as in comparative example 3 was followed except that 9.5% of α -arbutin in comparative example 3 was replaced with 9.5% of VC, to obtain a VC cream.

Comparative example 6

According to mass percentage, 9.5% of phenethyl resorcinol, 2.0% of PEC-10 polydimethylsiloxane, 1.0% of sucrose stearate, 1.0% of stearyl alcohol, 4.5% of glyceryl monostearate, 1.0% of hexadecadecyl alcohol and 3.0% of jojoba oil are melted in a water bath at 75 ℃ to obtain an oil phase;

mixing 5.0% glycerol, 5.0% propylene glycol, 0.3% triethanolamine, 0.2% carbomer 2020 and 67.5% water, stirring in 45 deg.C water bath to obtain whitening active ingredient water solution;

and stirring and mixing the oil phase and the water phase, and emulsifying to obtain the phenethyl resorcinol facial cream which contains the whitening active substance containing 9.5 mass percent of alpha-arbutin.

Example 22

In order to further illustrate that the whitening liquid crystal composition can improve the whitening efficiency of the whitening active ingredients, a skin image analyzer MexametrMX 16 is selected to perform efficacy test on a sample.

30 volunteers are selected, the age is about 20-35 years old, the clinical grade of color spots is more than 3, the trial parts are two cheeks of the face, and the MI value of the skin melanin content in the same test area is collected by the same person through MexametrMX 16 before the test and after the product is continuously used for 4 weeks and 8 weeks.

Volunteers were randomly divided into 6 groups of 5 persons each, which were:

test groups: applying the whitening and moisturizing liquid crystal face cream prepared in example 19;

control group: applying the base formula cream prepared in comparative example 1;

9.5% of a-ursolic acid cream group: smearing the alpha-ursolic acid cream prepared in the comparative example 3;

9.5% niacinamide cream group: applying the niacinamide cream prepared in comparative example 4;

9.5% VC cream group: applying the VC face cream prepared in the comparative example 5;

9.5% phenethyl resorcinol cream group: the phenethyl resorcinol cream prepared in comparative example 6 was applied.

The test results for each group are shown in table 4:

TABLE 4 comparison of skin lightening values at different times

As can be seen from table 4, on the premise that the total quality of the whitening active substances is the same, the cream efficacy of the whitening liquid crystal composition is obviously higher than that of the control group, and also obviously higher than that of the 9.5% alpha-arbutin cream group, the 9.5% phenethyl resorcinol cream group, the 9.5% nicotinamide cream group and the 9.5% VC cream group, which indicates that the combination of the whitening active ingredients acting on different target spots has a synergistic effect, and the liquid crystal structure can increase the transdermal absorption of the whitening active ingredients, so that the whitening active ingredients can permeate into the deep layer of the skin more quickly, and the whitening efficacy is enhanced.

The test results show that the whitening liquid crystal composition provided by the invention can be well applied to the field of cosmetics, and due to the unique liquid crystal structure, the whitening liquid crystal composition has stable and slow-release effects on active ingredients, and the whitening and moisturizing effects of the whitening liquid crystal composition on human skin are improved.

The foregoing is only a preferred embodiment of the present invention, and it should be noted that, for those skilled in the art, various modifications and decorations can be made without departing from the principle of the present invention, and these modifications and decorations should also be regarded as the protection scope of the present invention.

Claims

1. A whitening liquid crystal composition comprises whitening active ingredient and liquid crystal carrier;

the whitening liquid crystal composition also comprises liquid lipid and water for dissolving whitening active ingredients and/or liquid crystal carrier raw materials;

based on the total mass of the whitening liquid crystal composition, the whitening active ingredients are 7.0% of alpha-arbutin, 6% of nicotinamide, 0.1% of mandelic acid, 5% of VC and 3% of tea polyphenol, or 5.0% of vitamin E, 1.0% of glycyrrhetinic acid, 1.0% of phenethyl resorcinol, 8.0% of alpha-arbutin, 10.0% of nicotinamide and 2.0% of VC.

2. The whitening liquid crystal composition according to claim 1, wherein, based on the total mass of the whitening liquid crystal composition:

3. The whitening liquid crystal composition according to claim 1, wherein the liquid lipid accounts for 2 to 35 percent of the total mass of the whitening liquid crystal composition, and the water accounts for 5 to 35 percent of the total mass of the whitening liquid crystal composition.

4. The whitening liquid crystal composition according to any one of claims 1 to 3, wherein,

the liquid crystal emulsifier is selected from one or more of polyoxyethylene-polyoxypropylene block copolymer, polyoxyethylene (40) monostearate, polyglycerol-3 methyl glucose distearate, soybean lecithin, hydrogenated lecithin, C14-22 alcohol (and) C12-20 alkyl glucoside, coco glucoside (and) coco alcohol, C22 alcohol alkyl phosphate, cetearyl glucoside, hydroxystearyl and hydroxystearyl glycosides, arachidyl and behenyl and arachidyl alcohol glucoside, behenyl alkyl phosphate, cetearyl alcohol and cetearyl glucoside, cetearyl alcohol and coco glucoside, and tetradecyl glucoside;

5. The whitening liquid crystal composition according to any one of claims 1 to 3, wherein the liquid lipid is selected from one or more of isopropyl myristate, isopropyl palmitate, caprylic capric acid glyceride, polyethylene glycol lauric acid glyceride, polyethylene glycol stearic acid glyceride, linoleic acid glyceride, propylene glycol monocaprylate, caprylic capric acid cocoa butter, isononyl isononanoate, glyceryl triacetate, dimethicone, white oil, squalene, sunflower seed oil and soybean oil.

6. A method for preparing a whitening liquid crystal composition according to any one of claims 1 to 5, comprising the steps of:

there is no restriction on the order between steps A, B and C.

7. The method for preparing a whitening liquid crystal composition according to claim 6, wherein in the step D, the micronization treatment is a shearing treatment to a micrometer scale;

8. Use of the whitening liquid crystal composition according to any one of claims 1 to 5 for the preparation of a cosmetic.