CN115531237B - Acne-removing repairing composition, acne-removing repairing microneedle patch, and preparation method and application thereof - Google Patents
Acne-removing repairing composition, acne-removing repairing microneedle patch, and preparation method and application thereof Download PDFInfo
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- CN115531237B CN115531237B CN202211247336.9A CN202211247336A CN115531237B CN 115531237 B CN115531237 B CN 115531237B CN 202211247336 A CN202211247336 A CN 202211247336A CN 115531237 B CN115531237 B CN 115531237B
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- acne
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- drug
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- A61M37/00—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
- A61M37/0015—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin by using microneedles
- A61M2037/0023—Drug applicators using microneedles
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- A—HUMAN NECESSITIES
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- A61M37/00—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
- A61M37/0015—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin by using microneedles
- A61M2037/0046—Solid microneedles
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- A—HUMAN NECESSITIES
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- A61M37/00—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
- A61M37/0015—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin by using microneedles
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- A61M37/00—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
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Abstract
The invention discloses an acne-removing repairing composition, an acne-removing repairing microneedle patch and a preparation method and application thereof, wherein the acne-removing repairing composition comprises the following components in parts by weight as 100 parts: 0.012-0.07 part of antibacterial drug, 0.07-0.72 part of anti-inflammatory drug and 0.01-0.06 part of repair drug. The acne-removing and repairing microneedle patch comprises the composition. The hexapeptide-5 and the quaternary ammonium salt-73 are selected as antibacterial medicines, the palmitoyl tripeptide-8 and the chitosan are anti-inflammatory medicines, and the hexapeptide-9 is a repair medicine, so that the composition can remove acne caused by bacteria and inflammation, can not be peeled or stimulated after being used, and has the effect of repairing acne marks. And the synergistic effect can be exerted when the mass ratio of the palmitoyl tripeptide-8 to the chitosan is 0.2:1-0.4:1, so that the acne-removing and repairing effects are obviously improved.
Description
Technical Field
The invention belongs to the field of skin care products, and particularly relates to an acne-removing repairing composition, an acne-removing repairing microneedle patch, a preparation method and application thereof.
Background
Acne is commonly called acne or whelk, and is a common chronic inflammatory skin disease of pilosebaceous glands, which is good in puberty, and is slightly more serious than female, but the female is older than male by 1-2 years. Acne is mainly related to excessive sebum secretion, obstruction of pilosebaceous ducts, bacterial infection, inflammation, immune response and other factors; clinically, the lesion degree according to acne is summarized as "grade three and grade four", namely mild (grade 1): acne only, moderate (grade 2): inflammatory papules, moderate (grade 3): pus cell, severe (grade 4): nodules & cysts. Acne can lead to reduced patient confidence, reduced quality of life, depression, and even mental disturbance.
Common methods for treating acne in daily life are: 1. external medicine treatment, such as medicines of tretinoin, adapalene and the like are smeared on acne, main adverse reactions are manifested by local skin dryness, desquamation and irritation symptoms, and 2, on antibiotics such as erythromycin, gram Lin Dusu and the like for external use, the curative effect is poor due to the gradual serious drug resistance problem, and the medicines are rarely used; 3. the skin cells can be flaked and shed by high-concentration acid, and too thick cutin can also be shed, including micro acne and cells with excessive proliferation of hair follicle, and common acids are salicylic acid, glycolic acid, lactobionic acid and the like; early use requires the establishment of skin tolerance and frequency of use, otherwise the disruption of skin barrier function becomes sensitive and fragile. 4. The acne is removed by laser, radio frequency and physics by going to the beauty parlor, and the treatment process is accompanied by stronger pain and more expensive.
Most of acne-removing cosmetics sold in the market at present can not well penetrate the epidermis to be absorbed by directly smearing the acne parts, and the effective acne-removing components are mainly biased to inhibit the propionibacterium acnes and the cuticles from falling off in the formula design, so that the acne-removing effect is poor or repeated acne growth is caused, and the patient loses confidence on the acne-removing cosmetics.
Disclosure of Invention
In order to solve the technical problems, the invention provides an acne removing and repairing composition, an acne removing and repairing microneedle patch, a preparation method and application thereof, and the effective acne removing components are directly conveyed to the periphery of hair follicles by breaking through a stratum corneum barrier through a soluble transdermal microneedle technology, and the composition is not singly used for inhibiting propionibacterium acnes and exfoliating cutin to serve as central links of acne morbidity in the formula design, and is combined with anti-inflammation and repairing to serve as new directions of acne treatment, so that the effects of effectively improving acne and preventing acne are achieved.
In order to achieve the above purpose, the present invention adopts the following technical scheme:
the acne-removing repairing composition comprises the following components in parts by weight based on 100 parts: 0.012-0.07 part of antibacterial drug, 0.07-0.72 part of anti-inflammatory drug and 0.01-0.06 part of repair drug.
Preferably, the antibacterial agent comprises hexapeptide-5 and/or quaternary ammonium salt-73.
Preferably, the anti-inflammatory drug comprises chitosan and/or palmitoyl tripeptide-8.
Preferably, the repair drug comprises hexapeptide-9.
The acne-removing and repairing composition disclosed by the invention can remove acnes caused by bacteria and inflammation, can be used without peeling or stimulating, and has the effect of repairing acne marks.
The technical effects described in the present invention can be achieved by the above technical solutions, but in some preferred embodiments, the technical effects achieved are superior to other solutions.
For example: the mass ratio of the palmitoyl tripeptide-8 to the chitosan is 0.2:1-0.4:1.
The mass ratio of the hexapeptide-5 to the quaternary ammonium salt-73 is 7.5:1-2:1.
The invention also provides a preparation method of the acne-removing repairing composition, which comprises the following steps of; mixing and stirring the antibacterial drug, the anti-inflammatory drug, the repair drug and the solvent according to the formula amount to dissolve the antibacterial drug, the anti-inflammatory drug, the repair drug and the solvent, thereby obtaining the acne-removing repair composition.
Preferably, the solvent is alcohol and/or water, when the antibacterial drug contains quaternary ammonium salt-73, alcohol is used as the solvent of quaternary ammonium salt-73, and other drugs use water as the solvent.
Further preferably, the alcohol is used in an amount of 2.995 to 2.9970 parts by weight, the balance being water.
Further preferably, the alcohol is at least one of ethanol, propylene glycol and butylene glycol.
The invention also provides application of the acne-removing and repairing composition in preparation of an acne-removing and repairing cosmetic.
Preferably, the cosmetic comprises a microneedle patch.
The invention also provides an acne-removing repair microneedle patch, which comprises microneedles containing the acne-removing repair composition.
Preferably, the skeleton matrix of the microneedle is at least one of gelatin, trehalose, hyaluronic acid, polyvinylpyrrolidone, polyethylene glycol, polylactic acid, polyvinyl alcohol, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose and chondroitin sulfate; further preferably at least one of gelatin, trehalose and hyaluronic acid.
Preferably, the mass ratio of the acne-removing repairing composition to the skeleton matrix is 1:12-17; most preferably 1:15.
According to the invention, the micro-needle prepared by taking the soluble component as the skeleton matrix is selected to pierce the skin, so that a micron-sized channel is generated in the skin, the active component is rapidly dissolved and permeated in different skin layers, meanwhile, no needle point waste is generated, and painless autonomous administration is realized.
Preferably, the microneedle comprises a three-layer structure, and a first layer, a second layer and a third layer are sequentially arranged from the substrate to the direction of the needle tip and correspond to a nipple layer, a sebaceous gland layer and a matrix layer of the skin structure respectively.
Further preferably, the first layer is an anti-inflammatory drug layer, the second layer is an antibacterial drug layer, and the third layer is a repair drug layer.
Specifically, the anti-inflammatory drug layer acts on the dermal papilla layer of the skin at a depth of 50-200 μm from the epidermis, preferably, the first layer has a microneedle length of 50-200 μm and is located at a distance of 50-200 μm from the substrate;
the antibacterial drug layer acts on the dermal sebaceous gland layer of the skin, and is located at a depth of 200-600 μm from the epidermis, preferably the microneedle length of the second layer is about 110-550 μm; is positioned at a distance of 200-600 mu m from the substrate;
the repair drug layer acts on the dermal matrix layer of the skin at a depth of 600-1000 microns from the epidermis, preferably the microneedle length of the third layer is about 180-650 microns; located at a distance of 600-1000 μm from the substrate
According to the invention, the corresponding medicine layers are arranged at different heights of the micro-needle, and the functional components are released in different skin layers (the nipple layer, the sebaceous gland layer and the matrix layer) in a targeted manner by utilizing the different medicine layers, so that the acne removing and repairing effects are realized.
Preferably, the tips of the microneedles are bullet-shaped. Compared with the micro needle with conical tip, the micro needle has more medicine carrying content, smaller puncture force and easier penetration through the skin surface layer.
Further preferably, the anti-inflammatory drug layer comprises chitosan and/or palmitoyl tripeptide-8; the antibacterial drug layer comprises hexapeptide-5 and/or quaternary ammonium salt-73; the repair drug layer comprises hexapeptide-9.
Preferably, the substrate of the microneedle patch is selected from a nonwoven fabric, a hydrocolloid patch, a medical grade adhesive tape, or a printed cloth.
The invention also provides a preparation method of the acne-removing and repairing microneedle patch, which comprises the following steps:
(1) Fully dissolving the acne-removing repairing composition with the formula amount and a framework matrix by using a solvent to prepare an acne-removing repairing composition solution;
(2) Filling the acne-removing repairing composition solution prepared in the step (1) on a microneedle mould plate, and drying and curing;
(3) Transferring and fixing the microneedle obtained by demolding in the step (2) onto a substrate to obtain a microneedle patch;
or (b)
(1) Respectively dissolving the functional components in the first layer, the second layer and the third layer and the skeleton matrix by using solvents to prepare corresponding medicine mixed solution;
(2) filling the medicine mixed liquid prepared in the step (1) on a microneedle mould plate, filling one medicine mixed liquid, and then refilling the other medicine mixed liquid, wherein the medicine mixed liquid needs to be dried and solidified after each filling;
(3) transferring and fixing the microneedle obtained by demolding in the step (2) on a substrate to obtain the microneedle patch.
Preferably, the mass ratio of the acne-removing repairing composition to the skeleton matrix in the step (1) is 1:12-17; the mass ratio of the components in the first layer, the second layer and the third layer to the skeleton matrix is 1:12-17.
Preferably, in step (1), different matrix materials of the skeleton may be selected for different layers to control the dissolution rate and thus the drug release rate.
Preferably, the filling method in step (2) is a spray method, self-leveling or centrifugation.
Preferably, the temperature of drying and curing in the step (2) is 20-45 ℃, and the time of drying and curing is 10-90min.
The cause of acne is that sebum secretion is increased by external or internal factors, but the keratosis of the pilosebaceous canal is abnormal, so that sebum is difficult to be discharged, i.e. a slight acne is formed. The massive proliferation of a variety of microorganisms in hair follicles, particularly propionibacterium acnes, breaks down sebum to produce free fatty acids, while chemotactic inflammatory cells and mediators, ultimately inducing and aggravating the inflammatory response. The antibacterial drug layer provided by the invention has the main functional components of hexapeptide-5 and quaternary ammonium salt-73 by pertinently acting on the facial sebaceous gland layer, wherein hexapeptide-5 is mainly a small molecular peptide targeting the cell membrane of bacteria, so that the direct initial contact and interaction of the hexapeptide-5 and the small molecular peptide are driven, and propionibacterium acnes and staphylococcus aureus are effectively inhibited to relieve inflammation; the quaternary ammonium salt-73 has the effects of inhibiting the generation of propionibacterium acnes and staphylococcus aureus, relieving inflammation and preventing inflammatory acne from forming by destroying bacterial cell membranes and promoting the degradation of bacterial cells.
When acne is treated improperly, it will result in concave acne after healing on skin, and the appearance is poor, seriously affecting the psychological, physiological and social interaction of patients. The anti-inflammatory drug layer can pertinently act the anti-inflammatory component on the dermal papilla layer of the skin, and the main efficacy components of the anti-inflammatory drug layer comprise palmitoyl tripeptide-8 and chitosan, so that the anti-inflammatory drug layer can effectively improve inflammation. Palmitoyl tripeptide-8 endogenous anti-inflammatory substances, inhibiting the release of inflammatory factors IL-8 and TNF-alpha, and preventing and improving acne marks; chitosan has the effects of reducing the levels of interleukin-6 and TNF-alpha, thereby achieving the effects of relieving skin inflammation, accelerating the repair of damaged horny layer and promoting the repair of skin barrier.
The repair type medicine layer can pertinently act repair components on the dermis layer part, the main efficacy component of the repair type medicine layer is hexapeptide-9, the main efficacy of the repair type medicine layer is to induce the synthesis of collagen type I and collagen type III of the dermis layer matrix layer, the formation and reinforcement of the dermis connective tissue are promoted, and the repair type medicine layer has good effect on acne mark repair.
Compared with the prior art, the invention has the beneficial effects that:
(1) The acne-removing and repairing composition disclosed by the invention is prepared by carefully selecting hexapeptide-5 and quaternary ammonium salt-73 as antibacterial drugs, palmitoyl tripeptide-8 and chitosan as anti-inflammatory drugs, and hexapeptide-9 as repairing drugs. The composition can remove acne caused by bacteria and inflammation, can not be peeled or stimulated after being used, has the effect of repairing acne marks, and can exert synergistic effect when the mass ratio of palmitoyl tripeptide-8 to chitosan is 0.2:1-0.4:1, so that the acne removing and repairing effects are remarkably improved.
(2) The microneedle patch provided by the invention adopts the soluble microneedles, and has the characteristics of good safety of the used functional components, no obvious side effect, small irritation, no allergy, peeling, safety and reliability.
(3) According to the invention, the effects of the components are analyzed, the layering microneedles are designed, the effects of the components are in one-to-one correspondence with the problems of different skin layers (papilla layers, sebaceous gland layers and matrix layers), the administration is accurate, the using effect is further enhanced, the effects of improving and repairing inflammatory acnes and recessed acnes are good, and the acne problems can be solved in an all-around and multiple-effect manner.
Drawings
Fig. 1 is a graph showing the effect of use of example 1 and comparative example 4.
Fig. 2 is a graph showing the effect of use of example 2 and comparative example 5.
Fig. 3 is a graph showing the effect of use of example 7 and comparative example 6.
Fig. 4 is a graph showing the effect of use of example 8 and comparative example 7.
Detailed Description
Other advantages and effects of the present invention will become apparent to those skilled in the art from the following disclosure, which describes the embodiments of the present invention with reference to specific examples. The invention may be practiced or carried out in other embodiments that depart from the specific details, and the details of the present description may be modified or varied from the spirit and scope of the present invention.
Before the embodiments of the invention are explained in further detail, it is to be understood that the invention is not limited in its scope to the particular embodiments described below; it is also to be understood that the terminology used in the examples of the invention is for the purpose of describing particular embodiments only, and is not intended to limit the scope of the invention.
Where numerical ranges are provided in the examples, it is understood that unless otherwise stated herein, both endpoints of each numerical range and any number between the two endpoints are significant both in the numerical range. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs.
The invention does not limit the sources of the adopted raw materials, and if no special description exists, the adopted raw materials are all common commercial products in the technical field.
Example 1A microneedle patch for acne removal and repair
The acne-removing repair microneedle patch comprises, by weight, 0.173% of an acne-removing repair composition, 2.076% of a skeleton matrix, 2.996% of alcohol and the balance of water,
the acne-removing repairing composition comprises the following components in percentage by weight: antibacterial drugs: hexapeptide-5.02%, quaternary ammonium salt-73.003%; anti-inflammatory drugs: palmitoyl tripeptide-8.03%, chitosan 0.1%; repair type medicine: hexapeptide-9.02%;
the skeleton matrix is gelatin;
the alcohol is ethanol.
Example 2 an acne-removing repair microneedle patch
The acne-removing repair microneedle patch comprises, by weight, 0.705% of an acne-removing repair composition, 9.9% of a skeleton matrix, 2.995% of alcohol and the balance of water,
the acne-removing repairing composition comprises the following components in percentage by weight: antibacterial drugs: hexapeptide-5.05%, quaternary ammonium salt-73.005%; anti-inflammatory drugs: palmitoyl tripeptide-8.1% chitosan 0.5%; repair type medicine: hexapeptide-9.05%;
the skeleton matrix is trehalose;
the alcohol is ethanol.
Example 3 an acne-removing repair microneedle patch
The acne-removing repair microneedle patch comprises, by weight, 0.673% of an acne-removing repair composition, 11.441% of a skeleton matrix, 2.997% of alcohol and the balance of water,
the acne-removing repairing composition comprises the following components in percentage by weight: antibacterial drugs: hexapeptide-5.02%, quaternary ammonium salt-73.003%; anti-inflammatory drugs: palmitoyl tripeptide-8.1% chitosan 0.5%; repair type medicine: hexapeptide-9.05%;
the skeleton matrix is hyaluronic acid;
the alcohol is ethanol.
Example 4 an acne-removing repair microneedle patch
The acne-removing repair microneedle patch comprises, by weight, 0.792% of an acne-removing repair composition, 10.296% of a skeleton matrix, 2.9965% of alcohol and the balance of water,
the acne-removing repairing composition comprises the following components in percentage by weight: antibacterial drugs: hexapeptide-5.01%, quaternary ammonium salt-73.002%; anti-inflammatory drugs: palmitoyl tripeptide-8.12% chitosan 0.6%; repair type medicine: hexapeptide-9.06%;
the skeleton matrix is polyvinylpyrrolidone and polydiethanol with the mass ratio of 1:1;
the alcohol is propylene glycol.
Example 5 an acne-removing repair microneedle patch
The acne-removing repair microneedle patch comprises 0.15% of acne-removing repair composition, 2.1% of skeleton matrix, 2.996% of alcohol and the balance of water in percentage by weight,
the acne-removing repairing composition comprises the following components in percentage by weight: antibacterial drugs: hexapeptide-5.06%, quaternary ammonium salt-73.01%; anti-inflammatory drugs: palmitoyl tripeptide-8.02% chitosan 0.05%; repair type medicine: hexapeptide-9.01%;
the skeleton matrix is polylactic acid, polyvinyl alcohol and hydroxymethyl cellulose with the mass ratio of 1:1:1;
the alcohol is butanediol.
Example 6 an acne-removing repair microneedle patch
The acne-removing repair microneedle patch comprises, by weight, 0.429% of an acne-removing repair composition, 6.864% of a skeleton matrix, 2.997% of alcohol and the balance of water,
the acne-removing repairing composition comprises the following components in percentage by weight: antibacterial drugs: hexapeptide-5.03%, quaternary ammonium salt-73.004%; anti-inflammatory drugs: palmitoyl tripeptide-8.06%, chitosan 0.3%; repair type medicine: hexapeptide-9.035%;
the skeleton matrix is hydroxyethyl cellulose, hydroxypropyl methylcellulose and chondroitin sulfate in a mass ratio of 1:1:1;
the alcohol is ethanol.
The preparation method of the acne-removing and repairing microneedle patch in the above examples 1-6 comprises the following steps:
(1) Dissolving quaternary ammonium salt-73 in the acne-removing repairing composition by using alcohol, dissolving other components and skeleton matrix in the acne-removing repairing composition by using water, and then mixing the components to prepare the medicine mixture.
(2) Filling the drug mixed solution prepared in the step (1) on a microneedle mould plate, and drying and solidifying;
(3) Transferring and fixing the microneedle obtained by demolding in the step (2) on a substrate to obtain the microneedle patch.
The microneedles of the acne removal repair microneedle patches prepared in examples 1-6 above were not layered, in order to further verify the technical effect of the layered microneedles. The acne-removing repair microneedle patches of examples 1-6 were prepared as layered microneedles (the radius of the bottom of the microneedle was 150 μm, the number of microneedles was 1000/cm) according to the following preparation method 2 ) Layered anti-acne repair microneedle patch examples 7-12 were obtained, respectively.
The specific preparation method of the layered microneedle patch comprises the following steps:
(1) Respectively dissolving the functional components in the first layer, the second layer and the third layer and the skeleton matrix by using a solvent to prepare corresponding first-layer medicine mixed solution, second-layer medicine mixed solution and third-layer medicine mixed solution;
(2) And filling the microneedle mould plate with a drug mixed solution, filling one drug mixed solution, and then refilling the other drug mixed solution, wherein the drug mixed solution is required to be dried and solidified after each filling.
(3) Transferring and fixing the microneedle obtained by demolding in the step (2) on a substrate to obtain the microneedle patch.
Example 7A layered acne repair microneedle patch
The first layer is anti-inflammatory medicine: palmitoyl tripeptide-8.03%, chitosan 0.1%; is positioned at a position of 0-50 mu m away from the substrate by the micro needle;
the second layer is antibacterial medicine: hexapeptide-5.02%, quaternary ammonium salt-73.003%; the micro-needles are positioned 50-600 μm away from the substrate;
the third layer is repair type medicine: hexapeptide-9.02%; is positioned at the position of the microneedle which is 600-780 mu m away from the substrate;
a skeletal matrix: 2.076% of gelatin;
ethanol: 2.996%;
the balance being water.
Example 8
The first layer is anti-inflammatory medicine: palmitoyl tripeptide-8.1% chitosan 0.5%; is positioned at a position of 0-200 mu m away from the substrate by the micro needle;
the second layer is antibacterial medicine: hexapeptide-5.05%, quaternary ammonium salt-73.005%; is positioned at a distance of 200-400 mu m from the substrate;
the third layer is repair type medicine: hexapeptide-9.05%; is positioned at the position of the microneedle which is 400-800 mu m away from the substrate;
a skeletal matrix: trehalose 9.9%;
ethanol: 2.995%;
the balance being water.
Example 9
The first layer is anti-inflammatory medicine: palmitoyl tripeptide-8.1% chitosan 0.5%; is positioned at a position of 0-110 mu m away from the substrate by the micro needle;
the second layer is antibacterial medicine: hexapeptide-5.02%, quaternary ammonium salt-73.003%; is positioned at a distance of 110-300 mu m from the substrate;
the third layer is repair type medicine: hexapeptide-9.05%; the micro-needles are positioned at a distance of 300-700 mu m from the substrate;
a skeletal matrix: 11.441% of hyaluronic acid;
ethanol: 2.997%;
the balance being water.
Example 10
The first layer is anti-inflammatory medicine: palmitoyl tripeptide-8.12% chitosan 0.6%; is positioned at a position of 0-140 mu m away from the substrate by the micro needle;
the second layer is antibacterial medicine: hexapeptide-5.01%, quaternary ammonium salt-73.002%; is positioned at a distance of 140-350 mu m from the substrate;
the third layer is repair type medicine: hexapeptide-9.06%; is positioned at the position of the microneedle which is 350-1000 mu m away from the substrate;
a skeletal matrix: mass ratio 1: polyvinylpyrrolidone and polyethylene glycol 10.296% of 1;
propylene glycol: 2.9965%;
the balance being water.
Example 11
The first layer is anti-inflammatory medicine: palmitoyl tripeptide-8.02% chitosan 0.05%; is positioned at a position of 0-90 mu m away from the substrate by the micro needle;
the second layer is antibacterial medicine: hexapeptide-5.06%, quaternary ammonium salt-73.01%; is positioned at the position of the microneedle 90-200 mu m away from the substrate;
the third layer is repair type medicine: hexapeptide-9.01%; is positioned at a distance of 200-680 mu m from the substrate;
a skeletal matrix: mass ratio 1:1:1, polylactic acid, polyvinyl alcohol and hydroxymethyl cellulose 2.1%;
butanediol: 2.996%;
the balance being water.
Example 12
The first layer is anti-inflammatory medicine: palmitoyl tripeptide-8.06%, chitosan 0.3%; is positioned at a position of 0-150 mu m away from the substrate by the micro needle;
the second layer is antibacterial medicine: hexapeptide-5.03%, quaternary ammonium salt-73.004%; is positioned at a position 150-500 mu m away from the substrate by the micro needle;
the third layer is repair type medicine: hexapeptide-9.035%; the micro-needle is positioned at a distance of 500-850 mu m from the substrate;
a skeletal matrix: mass ratio 1:1:1, hydroxyethyl cellulose, hydroxypropyl methylcellulose and chondroitin sulfate 6.864%;
ethanol alcohol: 2.997%;
the balance being water.
Comparative example 1
The difference between this comparative example and example 1 is that: the repair type drug hexapeptide-9 is absent.
Comparative example 2
The difference between this comparative example and example 2 is that: antibacterial agents are lacking.
Comparative example 3
The difference between this comparative example and example 3 is that: lack of anti-inflammatory drugs.
Comparative example 4
The difference between this comparative example and example 1 is that: 0.01% of palmitoyl tripeptide-8 and 0.09% of chitosan, i.e. the mass ratio of palmitoyl tripeptide-8 to chitosan is 0.11:1.
Comparative example 5
The difference between this comparative example and example 2 is that: hexapeptide-5.059%, quaternary ammonium salt-73.006%; that is, the mass ratio of hexapeptide-5 to quaternary ammonium salt-73 is 9.83:1.
Comparative example 6
The difference between this comparative example and example 7 is that: in the anti-inflammatory drug of the first layer, the mass ratio of the palmitoyl tripeptide-8 to the chitosan is 0.625:1, namely, the palmitoyl tripeptide-8 and the chitosan are 0.05 percent and 0.08 percent.
Comparative example 7
The difference between this comparative example and example 8 is that: in the antibacterial medicine of the second layer, hexapeptide-5.049% and quaternary ammonium salt-730.006%; that is, the mass ratio of hexapeptide-5 to quaternary ammonium salt-73 is 8.2:1.
Product effect test
95 volunteers with similar acne size and area were selected for testing, the microneedle patches prepared in examples 1-12 and comparative examples 1-7 (wherein 5 volunteers in examples 1-12 and comparative examples 1-7 were each tried), the initial redness index and acne status of the facial skin of the above 95 volunteers were measured by photographing with a VISIA instrument, and the improvement degree of facial acne of the volunteers was measured 2 days after recording the related products for testing, and the specific test results are shown in table 1.
TABLE 1
From the data in the table and the actual observation of volunteers, the volunteers using the microneedle patches prepared in examples 1-12 have significantly reduced acne indexes of facial skin, and the excellent proportions of the drug layered structure and the efficacy components adopted in the microneedle patches in examples 1-12 are proved to be effective in eliminating and improving acne symptoms. The effective components used in the microneedle patches of examples 1-6 and examples 7-12 are the same, but the significant reduction rate of the acne index of the facial skin of the volunteer is different, because the microneedle patches prepared in the examples have better acne treatment and repair effects by arranging different drug layers in the microneedles to improve the acne problems corresponding to different skin layers.
Meanwhile, comparative example 4 was different in that the mass ratio of palmitoyl tripeptide-8 to chitosan was different from that of example 1, resulting in a significantly reduced acne treatment effect of the microneedle patch prepared in comparative example 4, as shown in fig. 1. Comparative example 5 was different in that hexapeptide-5 was different from quaternary ammonium salt-73 in terms of mass ratio, compared to example 2, resulting in a remarkable decrease in the anti-acne effect of the microneedle patch prepared in comparative example 5, as shown in fig. 2. Comparative example 6 was different from example 7 in that the mass ratio of palmitoyl tripeptide-8 to chitosan in the anti-inflammatory drug of the first layer was different, resulting in a significant decrease in the anti-acne effect of the microneedle patch prepared in comparative example 6, as shown in fig. 3. Comparative example 7 was different in that the mass ratio of hexapeptide-5 to quaternary ammonium salt-73 in the second layer of antibacterial agent was different from that of example 8, resulting in a significant decrease in the anti-acne effect of the microneedle patch prepared in comparative example 7, as shown in fig. 4.
The invention has been further described above in connection with specific embodiments, which are exemplary only and do not limit the scope of the invention in any way. It will be understood by those skilled in the art that various changes and substitutions of details and forms of the technical solution of the present invention may be made without departing from the spirit and scope of the present invention, but these changes and substitutions fall within the scope of the present invention.
Claims (9)
1. The acne-removing repairing composition is characterized by comprising the following components in parts by weight based on 100 parts: 0.012-0.07 part of antibacterial drug, 0.07-0.72 part of anti-inflammatory drug and 0.01-0.06 part of repair drug;
the antibacterial drug comprises hexapeptide-5 and quaternary ammonium salt-73, wherein the mass ratio of the hexapeptide-5 to the quaternary ammonium salt-73 is 7.5:1-2:1;
the anti-inflammatory drug comprises chitosan and palmitoyl tripeptide-8, wherein the mass ratio of the palmitoyl tripeptide-8 to the chitosan is 0.2:1-0.4:1;
the repair type medicine comprises hexapeptide-9.
2. A method of preparing the anti-acne repair composition of claim 1, comprising the steps of: mixing and stirring the antibacterial drug, the anti-inflammatory drug, the repair drug and the solvent according to the formula amount to dissolve the antibacterial drug, the anti-inflammatory drug, the repair drug and the solvent, thereby obtaining the acne-removing repair composition.
3. The preparation method according to claim 2, wherein the solvent is alcohol and water, the quaternary ammonium salt-73 uses alcohol as the solvent, and the other drugs use water as the solvent.
4. Use of the anti-acne repair composition of claim 1 in the preparation of an anti-acne repair cosmetic.
5. An anti-acne repair microneedle patch comprising a microneedle comprising the anti-acne repair composition of claim 1.
6. The acne-removing and repair microneedle patch of claim 5, wherein the matrix of the microneedle is at least one of gelatin, trehalose, hyaluronic acid, polyvinylpyrrolidone, polyethylene glycol, polylactic acid, polyvinyl alcohol, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose, and chondroitin sulfate.
7. The acne-removing and repair microneedle patch according to claim 6, wherein the mass ratio of the acne-removing and repair composition to the skeleton matrix is 1:12-17.
8. The acne-removing and repair microneedle patch according to claim 5, wherein the microneedle comprises a three-layer structure, a first layer, a second layer and a third layer are sequentially arranged in the direction from a substrate to a needle tip, the first layer is an anti-inflammatory drug layer, the second layer is an antibacterial drug layer, and the third layer is a repair drug layer.
9. A method for preparing the acne-removing and repairing microneedle patch according to claim 8, which is characterized by comprising the following steps:
(1) Fully dissolving the acne-removing repairing composition with the formula amount and a framework matrix by using a solvent to prepare an acne-removing repairing composition solution;
(2) Filling the acne-removing repairing composition solution prepared in the step (1) on a microneedle mould plate, and drying and curing;
(3) Transferring and fixing the microneedle obtained by demolding in the step (2) onto a substrate to obtain a microneedle patch; or (b)
(1) Respectively dissolving the components in the first layer, the second layer and the third layer and the skeleton matrix by using a solvent to prepare corresponding medicine mixed solution;
(2) filling the medicine mixed liquid prepared in the step (1) on a microneedle mould plate, filling one medicine mixed liquid, and then refilling the other medicine mixed liquid, wherein the medicine mixed liquid needs to be dried and solidified after each filling;
(3) transferring and fixing the microneedle obtained by demolding in the step (2) on a substrate to obtain the microneedle patch.
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