CN113893197B - Skin whitening and anti-saccharification soluble beautifying microneedle patch composition and preparation method thereof - Google Patents

Skin whitening and anti-saccharification soluble beautifying microneedle patch composition and preparation method thereof Download PDF

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CN113893197B
CN113893197B CN202111273771.4A CN202111273771A CN113893197B CN 113893197 B CN113893197 B CN 113893197B CN 202111273771 A CN202111273771 A CN 202111273771A CN 113893197 B CN113893197 B CN 113893197B
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soluble
skin whitening
skin
saccharification
composition
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CN113893197A (en
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龚婷
王蕾
郭苗
何珂
郭阳
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Hubei Maishite Biotechnology Co Ltd
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Hubei Maishite Biotechnology Co Ltd
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    • 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
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0208Tissues; Wipes; Patches
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61K8/494Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4946Imidazoles or their condensed derivatives, e.g. benzimidazoles
    • 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
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • 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
    • A61K8/73Polysaccharides
    • A61K8/735Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M37/00Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
    • A61M37/0015Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin by using microneedles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
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    • A61M37/00Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
    • A61M37/0015Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin by using microneedles
    • A61M2037/0046Solid microneedles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M37/00Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
    • A61M37/0015Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin by using microneedles
    • A61M2037/0053Methods for producing microneedles

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Abstract

The invention discloses a skin whitening, anti-saccharification and soluble beautifying microneedle patch composition and a preparation method thereof. The microneedle patch composition comprises a base, a needle body positioned on the base and a hydrogel patch for relieving and fixing the needle body, wherein the needle body is internally embedded with a skin whitening and anti-saccharification composition: 0.1-3% of licorice root extract, 0.1-2% of 4-butylresorcinol, 0.1-3% of nonapeptide and 0.1-5% of carnosine. The composition provided by the invention not only inhibits tyrosinase activity in three processes of pre-synthesis, during-synthesis and post-synthesis of melanin, but also has multiple effects of whitening; meanwhile, the active saccharide compounds are removed, saccharide toxins are removed, AGEs are prevented from generating multiple anti-saccharification and multi-path synergistic effects, and finally, the skin is white and transparent. The whitening and anti-saccharification composition is embedded in the hyaluronic acid soluble microneedle needle body, so that the composition can be directly supplied to deep skin through the stratum corneum of the skin, the percutaneous absorption efficiency is improved, and meanwhile, the skin is relieved to keep moisture, so that the effects of high-efficiency whitening, brightening and uniform skin color are achieved.

Description

Skin whitening and anti-saccharification soluble beautifying microneedle patch composition and preparation method thereof
Technical Field
The invention relates to a skin care product and a preparation method thereof, belongs to the technical field of daily chemicals, and particularly relates to a skin whitening and anti-saccharification soluble beautifying microneedle patch composition and a preparation method thereof.
Background
Both baked bread and braised pork in daily life are "saccharification phenomenon", which refers to physiological reactions generated by combination of protein in our body and sugar ingested in diet. The carbohydrate taken every day is decomposed into glucose and fructose through the digestive system and then is transported to cells, and under the action of enzyme, complex chemical reaction occurs, and energy is released to meet the requirements of human bodies.
In young age, the activity is high, metabolism is normal, most of ingested sugar is metabolized, and the sugar cannot be accumulated in the body. However, with the age, the pressure of life and work is increased, and irregular life and eating habits are added, metabolism is disturbed, and ingested sugar is not metabolized immediately and can be accumulated in the body.
The free sugar reacts with collagen in dermis without enzyme action to form some reversible primary glycosylation products, and then irreversible advanced glycosylation end products (AGEs) are formed, and the whole process is saccharification. The saccharified collagen turns yellow and crisp in texture, and the skin turns yellow gradually with the accumulation of AGEs. In addition, AGEs can promote melanin production by stimulating AGEs receptors.
Healthy and fair skin is a hot spot pursued by all people loving beauty, but the whitening skin care products on the market generally have the following problems:
(1) the whitening mechanism is single: most whitening products are only researched aiming at inhibiting the activity of tyrosinase, and full-effect whitening cannot be realized;
(2) the product stability is poor: the whitening components in most whitening products are directly added into the formula, so that the problems of color change, smell change, layering, coarseness and the like of the products are easily caused;
(3) the whitening efficiency is low: because of the natural skin barrier of the skin, the whitening active ingredients are difficult to permeate into the muscle bottom, the absorption rate of the active ingredients is low, and the whitening effect is poor;
(4) skin irritation is easily caused: such as niacinamide, when added to skin care products at too high a concentration, skin irritation and even inflammation can easily occur.
Disclosure of Invention
In order to overcome the problems in the prior art, the invention aims to provide the skin whitening and anti-saccharification soluble beautifying microneedle film composition, which is embedded in a hyaluronic acid soluble microneedle needle body, so that the composition is beneficial to directly supplying deep skin through the stratum corneum of the skin, the percutaneous absorption efficiency is improved, and meanwhile, the skin is relieved to keep moisture continuously, so that the effects of high-efficiency whitening, brightening and uniform skin color are brought.
The invention also aims to provide a preparation method of the skin whitening and anti-saccharification soluble beautifying microneedle film composition, which is simple, low in energy consumption and low in production cost, and is easy to realize continuous mass production.
The invention is realized by adopting the following technical scheme.
A skin whitening and anti-saccharification soluble beautifying microneedle patch composition comprises a base, a needle body positioned on the base and a hydrogel patch for relieving and fixing the needle body; the skin whitening and anti-saccharification composition is embedded in the needle body, and comprises the following components in percentage by weight:
0.1-3% of licorice root extract, 0.1-2% of 4-butylresorcinol, 0.1-3% of nonapeptide-1 and 0.1-5% of carnosine.
Preferably, the skin whitening and anti-saccharification composition comprises the following components in percentage by weight, based on the total weight of the microneedle:
0.1-1% of licorice root extract, 0.1-0.5% of 4-butylresorcinol, 0.1-1% of nonapeptide and 0.1-2% of carnosine.
Preferably, the skin whitening and anti-saccharification composition further comprises the following components in percentage by weight:
5-15% of glycerol, 1-3% of low molecular weight sodium hyaluronate and 7-9% of high molecular weight sodium hyaluronate.
Preferably, the soluble beauty micro-needles are conical, the main component is hyaluronic acid, the length of the needle head is 150-450 mu m, the distance between the micro-needles is 400-700 mu m, and the whole dry sheet comprises 1500-4500 hyaluronic acid microcrystal struts.
Preferably, the hydrogel adhesive film has 4 layers and 10-20 components.
The hydrogel film comprises non-woven fabrics, hydrogel body, active component layer and protective film from top to bottom.
The non-woven fabric is non-woven fabric and is formed by solidifying high polymer slices, short fibers or filaments.
The hydrogel body comprises the following specific components in percentage by weight: 5-15% of glycerin, 1-2% of sodium polyacrylate, 1-3% of dihydroxyglycine aluminum, 0.5-2% of cellulose gum, 1-5% of tartaric acid, 5-15% of butanediol and 50-80% of water.
The active component layer comprises the following specific components in percentage by weight:
0.1-3% of centella asiatica extract, 0.2-2% of polygonum cuspidatum root extract, 0.2-3% of scutellaria baicalensis root extract, 0.1-2% of tea leaf extract, 0.2-3% of glycyrrhiza glabra root extract, 0.3-1% of chamomile flower extract and 0.1-2% of rosemary leaf extract.
The protective film is in particular a white plastic film.
In another aspect, the invention provides a method for preparing a skin whitening, anti-saccharification and soluble cosmetic microneedle patch composition, comprising the following steps:
1) Preparation of viscous liquid:
adding skin whitening and anti-saccharification composition into the rest water, stirring for dissolving, adding 5-15% of glycerol, 1-3% of sodium hyaluronate (low molecular weight) and 7-9% of sodium hyaluronate (high molecular weight), continuously stirring to make it swell uniformly, centrifuging and removing air bubbles to obtain viscous liquid.
2) Preparation of soluble cosmetic microneedles:
and (3) injecting the viscous liquid into a microneedle mould, drying and demoulding to obtain the soluble beauty microneedle.
3) Preparation of hydrogel adhesive film:
uniformly mixing 1-2% of sodium polyacrylate and 1-3% of dihydroxyglycine aluminum, adding 5-15% of glycerol and 5-15% of butanediol, and fully stirring to obtain a phase A solution;
adding 0.5-2% cellulose gum into water, stirring, adding 1-5% tartaric acid, adding active component layer, stirring to dissolve completely to obtain phase B solution;
adding the B phase solution into the A phase solution, stirring in vacuum to obtain hydrogel paste, and finally coating with non-woven fabrics and protective films on a coating machine to obtain the hydrogel film.
Preferably, in step 1), the molecular weight of the low molecular weight sodium hyaluronate is 2000 to 10000 daltons; the molecular weight of the high molecular weight sodium hyaluronate is 40-100 ten thousand daltons.
The mass ratio of the high molecular weight sodium hyaluronate to the low molecular weight sodium hyaluronate is 1:3.0-5.0.
Preferably, in step 2), the microneedle mould comprises a square, a rectangle or an arc shape, and can also be made into a mask type with higher cost.
Preferably, the drying temperature is room temperature, the humidity is 15-25%, and the drying time is 12-24h.
Preferably, in the step 3), the stirring speed of the vacuum stirring is 50-120r/min, and the stirring time is 5-15min.
By means of the technical scheme, the invention has the following beneficial technical effects:
1) The invention discloses a skin whitening, anti-saccharification and soluble beautifying microneedle patch composition and a preparation method thereof. The microneedle patch composition comprises a base, a needle body positioned on the base and a hydrogel patch for relieving and fixing the needle body, wherein the needle body is internally embedded with a skin whitening and anti-saccharification composition: 0.1-3% of licorice root extract, 0.1-2% of 4-butylresorcinol, 0.1-3% of nonapeptide and 0.1-5% of carnosine.
2) The composition provided by the invention not only inhibits tyrosinase activity in three processes of pre-synthesis, during-synthesis and post-synthesis of melanin, but also has multiple effects of whitening; meanwhile, the active saccharide compounds are removed, saccharide toxins are removed, AGEs are prevented from generating multiple anti-saccharification and multi-path synergistic effects, and finally, the skin is white and transparent.
3) The whitening and anti-saccharification composition is embedded in the hyaluronic acid soluble microneedle needle body, so that the composition can be directly supplied to deep skin through the stratum corneum of the skin, the percutaneous absorption efficiency is improved, and meanwhile, the skin is relieved to keep moisture, so that the effects of high-efficiency whitening, brightening and uniform skin color are achieved.
Drawings
Fig. 1 is a block diagram of a skin whitening, anti-glycation and soluble beauty microneedle provided by the invention.
FIG. 2 is a graph showing a comparison of the permeability results of the active ingredients of the soluble cosmetic microneedle and the external skin care product.
Detailed Description
The technical scheme of the invention is further specifically described through specific examples. It should be understood that the specific embodiments described herein are for purposes of illustration only and are not intended to limit the scope of the invention.
As shown in the structure diagram of the soluble beauty micro-needle in fig. 1, the invention discloses a skin whitening and anti-saccharification soluble beauty micro-needle film composition and a preparation method thereof. The microneedle patch composition comprises a base, a needle body positioned on the base and a hydrogel patch for relieving and fixing the action of the needle body, wherein the needle body is internally embedded with a skin whitening and anti-saccharification composition, and the composition comprises the following components:
0.1-3% of licorice root extract, 0.1-2% of 4-butylresorcinol, 0.1-3% of nonapeptide-1 and 0.1-5% of carnosine.
The invention relates to a skin whitening and anti-saccharification soluble beautifying microneedle patch composition, which comprises a base, a needle body positioned on the base and a hydrogel patch. The base is composed of hyaluronic acid; the microneedle needle body contains viscous liquid; the hydrogel film comprises non-woven fabrics, hydrogel body, active component layer and protective film from top to bottom. The function of the non-woven fabric is to improve the air permeability of the film, the function of the hydrogel body is to lock water for a long time, the function of the active component layer is to slowly release water, assist in moisturizing and relieving irritation resistance, and the function of the protective film is to prevent the loss of gel nutrition and water.
As shown in the comparative graph of the permeability results of the active ingredients of the soluble beauty microneedle and the external skin care product in fig. 2, the permeability of the active ingredients of the soluble microneedle technology is 4-6 times that of the common smearing type skin care product in 90 minutes.
The following focuses on the efficacy of the ingredients of the compositions.
(1) Glycyrrhiza glabra root extract
The Glycyrrhiza glabra root extract can penetrate into the skin and keep high activity, can inhibit tyrosinase activity, can inhibit dopachrome interconversion and DHICA oxidase activity, has the capability of scavenging oxygen free radicals similar to SOD (superoxide dismutase), has the capability of resisting oxygen free radicals similar to vitamin E, and also has the effects of preventing rough skin, resisting inflammation and resisting bacteria, and the Glycyrrhiza glabra extract used as a natural whitening agent is the only component which directly plays a role in 3 stages in 5 stages of melanin formation so far.
(2) 4-butylresorcinol
4-butyl resorcinol is a high-efficiency skin whitening agent, can inhibit tyrosinase with high efficiency, reduce melanin formation, interfere synthesis and glycosylation of tyrosinase, improve degradation of tyrosinase, inhibit conversion of melanin into keratinocytes, and has the advantages of oxidation resistance, ultraviolet resistance, rapid permeation, low sensitization and the like.
(3) Nonapeptide-1
The nonapeptide-1 and the MC1 receptor on the melanocyte have very good matching property, can be used as an antagonist for promoting melanocyte hormone, competitively combined with the MC1 receptor, prevents tyrosinase from being further activated to generate melanin, reduces the generation amount of the melanin, and can obviously lighten the skin color.
(4) Carnosine (carnosine)
Studies prove that carnosine has good anti-glycation effect. Carbonylated proteins and glycation end products (AGEs) are signals of cell senescence. They accumulate abnormally in the cell, accelerating cross-linking with other proteins. Carnosine can replace in vivo proteins to react with sugar in a form of reacting with sugar before the sugar erodes the skin, thereby helping to protect the proteins from glycosylation and achieving the anti-glycation effect.
Therefore, the composition formed by combining the four components not only inhibits tyrosinase activity and has multiple effects of whitening in three processes of before, during and after melanin synthesis; meanwhile, the active saccharide compounds are removed, saccharide toxins are removed, AGEs are prevented from generating multiple anti-saccharification and multi-path synergistic effects, and finally, the skin is white and transparent.
The skin whitening and anti-saccharification composition is embedded in the hyaluronic acid soluble microneedle needle body, so that the composition can be directly supplied to deep skin through the stratum corneum of the skin, the percutaneous absorption efficiency is improved, and meanwhile, the skin is relieved to keep moisture, so that the effects of high-efficiency whitening, brightening and uniform skin color are achieved.
The following percentages are by weight. All raw material components of the invention are commercial products.
The Glycyrrhiza glabra root extract is prepared by cleaning Glycyrrhiza glabra root, drying, and pulverizing to obtain Glycyrrhiza glabra root powder; mixing the powder, crushed materials for fine bubble crushing and deionized water, reacting for 4-8 hours at 70-80 ℃ to obtain a mixed solution, and performing ultrasonic treatment to obtain an extracting solution; and finally, passing the extract through macroporous adsorption resin, eluting with water and 70% ethanol water solution respectively, and drying to obtain the glycyrrhiza glabra root extract.
The Glycyrrhiza glabra root extract is purchased from the pill preparation; 4-butylresorcinol and carnosine were purchased from delphinidin; nonapeptide-1 was purchased from Zhejiang surge peptide. Centella asiatica extract, polygonum cuspidatum root extract, scutellaria baicalensis root extract, tea extract, glycyrrhiza glabra root extract, chamomile flower extract and rosemary leaf extract are all purchased from Beijing university or Galois leaf biotechnology limited.
Example 1
A preparation method of a skin whitening and anti-saccharification soluble beautifying microneedle patch composition comprises the following steps:
1) Preparation of viscous liquid:
adding 0.6% of Glycyrrhiza glabra root extract, 0.4% of 4-butylresorcinol, 0.8% of nonapeptide-1 and 1.2% of carnosine into the rest water, stirring to dissolve, adding 10% of glycerol, 2% of sodium hyaluronate (molecular weight is 5000 dalton) and 8% of sodium hyaluronate (molecular weight is 60 kilodalton), continuing stirring to make it swell uniformly, centrifuging to remove air bubbles, and obtaining viscous liquid.
2) Preparation of soluble cosmetic microneedles:
and (3) injecting the viscous liquid into a square microneedle mould, drying for 20 hours at room temperature and humidity of 20%, and demoulding to obtain the soluble beauty microneedle.
3) Preparation of hydrogel adhesive film:
uniformly mixing 1.5% of sodium polyacrylate and 2% of dihydroxyglycine aluminum, adding 10% of glycerol and 10% of butanediol, and fully stirring to obtain a phase A solution;
adding 1% cellulose gum into water, stirring, adding 3% tartaric acid, adding 0.5% herba Centellae extract, 0.6% rhizoma Polygoni Cuspidati extract, 0.4% radix Scutellariae extract, 0.5% folium Camelliae sinensis extract, 0.6% radix Glycyrrhiza glabra extract, 0.8% flos Matricariae Chamomillae extract and 0.6% herba Rosmarini officinalis leaf extract, stirring to dissolve completely to obtain phase B solution;
adding the B phase solution into the A phase solution, stirring in vacuum to obtain hydrogel paste, wherein the stirring speed is 80r/min, the stirring time is 10min, and finally coating the hydrogel paste with non-woven fabrics and a protective film on a coating machine to obtain the hydrogel film.
Example 2
A preparation method of a skin whitening and anti-saccharification soluble beautifying microneedle patch composition comprises the following steps:
1) Preparation of viscous liquid:
adding 0.4% Glycyrrhiza glabra root extract, 0.3% 4-butylresorcinol, 0.5% nonapeptide-1 and 1% carnosine into the rest water, stirring to dissolve, adding 10% glycerol, 2% sodium hyaluronate (molecular weight is 5000 dalton) and 8% sodium hyaluronate (molecular weight is 60 kilodalton), continuing stirring to swell uniformly, centrifuging and removing air bubbles to obtain viscous liquid.
2) Preparation of soluble cosmetic microneedles: as in example 1.
3) Preparation of hydrogel adhesive film: as in example 1.
Example 3
A preparation method of a skin whitening and anti-saccharification soluble beautifying microneedle patch composition comprises the following steps:
1) Preparation of viscous liquid:
adding 0.2% of Glycyrrhiza glabra root extract, 0.1% of 4-butylresorcinol, 0.3% of nonapeptide-1 and 0.5% of carnosine into the rest water, stirring to dissolve, adding 10% of glycerol, 2% of sodium hyaluronate (molecular weight is 5000 dalton) and 8% of sodium hyaluronate (molecular weight is 60 kilodalton), continuing stirring to make it swell uniformly, centrifuging to remove air bubbles, and obtaining viscous liquid.
2) Preparation of soluble cosmetic microneedles: as in example 1.
3) Preparation of hydrogel adhesive film: as in example 1.
Blank example 1
A method for preparing a soluble cosmetic microneedle patch composition, comprising the steps of:
1) Preparation of viscous liquid:
adding 10% glycerol, 2% sodium hyaluronate (molecular weight of 5000 dalton) and 8% sodium hyaluronate (molecular weight of 60 kilodalton) into the rest water, stirring to swell uniformly, centrifuging to remove air bubbles, and obtaining viscous liquid.
2) Preparation of soluble cosmetic microneedles: as in example 1.
3) Preparation of hydrogel adhesive film: as in example 1.
Effect verification test example
1. Anti-glycation efficacy analysis experiment
Inhibition of non-enzymatic glycosylation reaction studies:
enzymatic glycosylation is a complex series of non-enzymatic reactions, in which proteins and glucose react in vivo, ultimately forming "murder" AGEs of skin glycation. The ability of skin whitening, anti-glycation compositions to resist glycation can be reflected by studies on non-enzymatic glycation reactions.
Under aseptic conditions, 20.00g/L bovine serum albumin solution and 5.00mL of 0.50mol/L glucose solution each after sterilization with 0.2 μm sterilization film are added to a sterile cell culture flask, and 1% NaN is added 3 10.00mL of phosphate buffer solution with the pH of 7.4 at the concentration of 0.20mol/L, and establishing a complete glycosylation system control group a; meanwhile, a control group b without glucose solution and without the viscous liquid containing the skin whitening and anti-saccharification composition is established; adding a control group c containing a skin whitening and anti-saccharification composition and containing no protein in the viscous liquid; and d, adding a control group d containing a viscous liquid of the skin whitening and anti-saccharification composition and not containing a glucose solution.
The viscous liquid containing the skin whitening and anti-glycation composition of examples 1-3 in solution and the intervention group of blank example 1 were set and incubated at 37℃for 28 days. Tests were performed on days 0, 2, 4, 8, 12, 16, 20, 24, 26, 28, respectively.
And taking out 0.5mL of culture solution, diluting to 10mL, measuring the fluorescence value F of the glycosylation end product at the excitation wavelength of 370nm and the emission wavelength of 440nm, and calculating the inhibition rate IE of non-enzymatic glycosylation.
Calculation formula of inhibition rate IE of non-enzymatic glycosylation: IE (%) = [1- (drug F-control cF-control dF)/(control aF-control bF) ]x100%.
Wherein, the drug F is the fluorescence value of the sample to be detected, the contrast cF is the fluorescence value of the contrast group c, the contrast dF is the fluorescence value of the contrast group d, the contrast aF is the fluorescence value of the contrast group a, and the contrast bF is the fluorescence value of the contrast group b. After the end of the glycosylation product incubation, the fluorescence intensity was measured at 370nm/440nm and the inhibition was calculated, and the specific test results are shown in Table 1:
table 1 test results
Project Inhibition rate%
Example 1 39.1
Example 2 35.2
Example 3 33.9
Blank example 1 0.4
As can be seen from Table 1, the viscous liquid containing the skin-whitening and anti-glycation composition obtained in examples 1 to 3 of the present invention can well inhibit non-enzymatic glycosylation, and the inhibition rate IE for non-enzymatic glycosylation is 33% or more, whereas the viscous liquid containing no skin-whitening and anti-glycation composition obtained in blank example 1 is very weak in inhibition ability. The skin whitening and anti-glycation composition has an anti-glycation effect.
2. Experimental example of synergistic effect
Comparative examples 1 to 14
A soluble skin care microneedle patch composition comprises the following viscous liquid components in proportions shown in tables 2-3.
TABLE 2 viscous liquid composition (wt.%)
TABLE 3 viscous liquid composition (wt.%)
The preparation process was as described in example 1.
Whitening effect test was performed on example 1, comparative examples 1 to 14 and blank example 1.
1. The tester: 160 healthy females (25-45 years old) are divided into 16 groups of 10 individuals each; the same formulation was used for each group.
2. Test area: face (left face blank example 1 sample, right face example, comparative example sample).
3. The method comprises the following steps: once daily, each time lasts for 1-2 hours, and the use lasts for 4 weeks.
4. Test instrument: delfinSkinColorPatch (Finland).
5. The effect index is as follows: the change in color brightness (Δl), ITA degree, and the L value (brightness), ITA degree (individual color type angle) in the present invention are measured and mainly used as indicators.
Equation (1): Δl = [ L + (after 1 month of testing of the comparative or example product) -L + (before starting the test) ] -L + (after 1 month of testing of the blank product) -L + (before starting the test).
(2): ITA degree (representing the overall change in chromaticity), the greater the ITA degree value, the lighter the skin tone.
TABLE 4 skin color Classification for different ITA ranges
Average value of each group。
Average value of each group.
The test results are shown in table 5 below.
Table 5 test results
As can be seen from the test data in table 5, the whitening effect is ranked as example 1> comparative examples 11, 12, 13, 14> comparative examples 5, 6, 7, 8, 9, 10> comparative examples 1, 2, 3, 4, which demonstrates that the skin whitening and anti-glycation composition has better whitening effect through the synergistic effect between the components than the single one, two or three component combination.
3. Human trial evaluation experiment
The experimental method comprises the following steps: the skin whitening and anti-glycation soluble cosmetic microneedle patch compositions prepared in examples 1, 2, and 3 and blank 1 were selected as experimental samples, and were individually subjected to trial evaluation for volunteers. 80 dark-colored volunteers were selected, 40 men and women were randomly grouped into 4 groups of 10 men and 10 women each.
The skin whitening, anti-glycation soluble cosmetic microneedle patch composition samples prepared in examples 1, 2, 3 and blank 1 were used by 4 groups of volunteers, respectively. The using method comprises the following steps: after the face is cleaned, the face is used once a day for 1-2 hours, and is continuously used for 4 weeks, and sensory evaluation is carried out according to the improvement condition of the skin color.
The scoring standard is 1 minute-no effect, 2 minutes-effective, very weak, 3 minutes-effective, obvious in effect, 4 minutes-effective, better in effect, 5 minutes-effective, very good in effect.
The score of more than or equal to 3 is judged to be obvious in effect, and the proportion of more than or equal to 3 in each group is counted.
The results obtained are shown in Table 6:
TABLE 6 test results
Evaluation results Obvious whitening effect Has the effects of Has no effect
Example 1 85% 10% 5%
Example 2 65% 25% 10%
Example 3 45% 45% 10%
Blank example 1 0 5% 95%
As can be seen from Table 6, the skin whitening and anti-glycation soluble cosmetic microneedle patch compositions obtained in examples 1 to 3 of the present invention are effective in whitening skin, and the effect is superior to that of the soluble cosmetic microneedle patch composition of blank example 1, which does not contain the skin whitening and anti-glycation composition.
In conclusion, the skin whitening and anti-saccharification composition provided by the invention not only inhibits tyrosinase activity in three processes of pre-synthesis, during-synthesis and post-synthesis of melanin, but also has multiple effects of whitening; meanwhile, the active saccharide compounds are removed, saccharide toxins are removed, AGEs are prevented from generating multiple anti-saccharification and multi-path synergistic effects, and finally, the skin is white and transparent.
The whitening and anti-saccharification composition is embedded in the hyaluronic acid soluble microneedle needle body, so that the composition can be directly supplied to deep skin through the stratum corneum of the skin, the percutaneous absorption efficiency is improved, and meanwhile, the skin is relieved to keep moisture, so that the effects of high-efficiency whitening, brightening and uniform skin color are achieved.
The hydrogel film is matched with the soluble micro-needles to be used, can release the water of the hydrogel film when the water is deficient, has self-adhesive property and low sensitization, can cover the soluble beauty micro-needles on the skin and is not easy to fall off, and ensures the stable exertion of the whitening and anti-saccharification effects of the micro-needles.
The above description is only of the preferred embodiments of the present invention, and is not intended to limit the invention in any way, but other variations and modifications are possible without departing from the technical solution described in the claims.

Claims (10)

1. A skin whitening and anti-saccharification soluble beautifying microneedle patch composition is characterized in that: comprises a base, a needle body positioned on the base and a hydrogel film for relieving and fixing the action of the needle body;
the skin whitening and anti-saccharification composition is embedded in the needle body, and comprises the following components in percentage by weight:
0.1-3% of licorice root extract, 0.1-2% of 4-butylresorcinol, 0.1-3% of nonapeptide-1 and 0.1-5% of carnosine;
the hydrogel film has 4 layers and 10-20 components;
the hydrogel film consists of non-woven fabrics, hydrogel body, an active component layer and a protective film from top to bottom;
the active component layer comprises the following specific components in percentage by weight:
0.1-3% of centella asiatica extract, 0.2-2% of polygonum cuspidatum root extract, 0.2-3% of scutellaria baicalensis root extract, 0.1-2% of tea leaf extract, 0.2-3% of glycyrrhiza glabra root extract, 0.3-1% of chamomile flower extract and 0.1-2% of rosemary leaf extract.
2. The skin whitening, anti-glycation soluble cosmetic microneedle patch composition of claim 1, wherein: the skin whitening and anti-saccharification composition comprises the following components in percentage by weight, based on the total weight of the microneedle:
0.1-1% of licorice root extract, 0.1-0.5% of 4-butylresorcinol, 0.1-1% of nonapeptide and 0.1-2% of carnosine.
3. The skin whitening, anti-glycation soluble cosmetic microneedle patch composition of claim 1, wherein: the skin whitening and anti-saccharification composition also comprises the following components in percentage by weight:
5-15% glycerol, 1-3% low molecular weight sodium hyaluronate having a molecular weight of 2000-10000 daltons, and 7-9% high molecular weight sodium hyaluronate; the molecular weight of the high molecular weight sodium hyaluronate is 40-100 ten thousand daltons.
4. The skin whitening, anti-glycation soluble cosmetic microneedle patch composition of claim 1, wherein: the soluble beauty micro-needle is conical, the main component is hyaluronic acid, the length of the needle head is 150-450 mu m, the distance between the micro-needles is 400-700 mu m, and the whole dry sheet comprises 1500-4500 hyaluronic acid microcrystal struts.
5. The skin whitening, anti-glycation soluble cosmetic microneedle patch composition of claim 1, wherein: the non-woven fabric is non-woven fabric and is formed by solidifying high polymer slices, short fibers or filaments;
the hydrogel body comprises the following specific components in percentage by weight: 5-15% of glycerol, 1-2% of sodium polyacrylate, 1-3% of dihydroxyglycine aluminum, 0.5-2% of cellulose gum, 1-5% of tartaric acid, 5-15% of butanediol and 50-80% of water;
the protective film is specifically a white plastic film.
6. The method for preparing the skin whitening and anti-glycation soluble cosmetic microneedle patch composition according to any one of claims 1 to 5, comprising the following steps:
1) Preparation of viscous liquid:
adding the skin whitening and anti-saccharification composition into the rest water, stirring and dissolving, adding 5-15% of glycerol, 1-3% of low molecular weight sodium hyaluronate and 7-9% of high molecular weight sodium hyaluronate, continuously stirring to make the skin whitening and anti-saccharification composition swell uniformly, centrifuging and removing bubbles to obtain viscous liquid;
2) Preparation of soluble cosmetic microneedles:
injecting the viscous liquid into a microneedle mould, drying and demoulding to obtain a soluble beauty microneedle;
3) Preparation of hydrogel adhesive film:
uniformly mixing 1-2% of sodium polyacrylate and 1-3% of dihydroxyglycine aluminum, adding 5-15% of glycerol and 5-15% of butanediol, and fully stirring to obtain a phase A solution;
adding 0.5-2% cellulose gum into water, stirring, adding 1-5% tartaric acid, adding active component layer, stirring to dissolve completely to obtain phase B solution;
adding the B phase solution into the A phase solution, stirring in vacuum to obtain hydrogel paste, and finally coating with non-woven fabrics and protective films on a coating machine to obtain the hydrogel film.
7. The method for preparing the skin whitening, anti-glycation and soluble beautifying microneedle patch composition according to claim 6, wherein the method comprises the following steps: in the step (1) of the process,
the mass ratio of the high molecular weight sodium hyaluronate to the low molecular weight sodium hyaluronate is 1:3.0-5.0.
8. The method for preparing the skin whitening, anti-glycation and soluble beautifying microneedle patch composition according to claim 6, wherein the method comprises the following steps: in the step 2), the microneedle mould comprises a square, a rectangle or an arc shape, or a mask shape.
9. The method for preparing the skin whitening, anti-glycation and soluble beautifying microneedle patch composition according to claim 6, wherein the method comprises the following steps: in the step 2), the drying temperature is room temperature, the humidity is 15-25%, and the drying time is 12-24h.
10. The method for preparing the skin whitening, anti-glycation and soluble beautifying microneedle patch composition according to claim 6, wherein the method comprises the following steps: in the step 3), the stirring speed of the vacuum stirring is 50-120r/min, and the stirring time is 5-15min.
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