CN115919679A - Microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and reducing acne marks and preparation method and application thereof - Google Patents
Microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and reducing acne marks and preparation method and application thereof Download PDFInfo
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Abstract
The invention discloses a microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks, and a preparation method and application thereof, wherein the microemulsion preconcentration composition comprises the following components: functional components, emulsifier, auxiliary emulsifier and auxiliary components; wherein the effective components are composition of ascorbyl tetraisopalmitate, paeonol, caprylyl salicylic acid, peony seed oil and oat kernel extract. The functional components are oil-soluble acne-removing components, and compared with water-soluble components, the acne-removing cream has the advantages of stronger permeability, lower concentration and effect, and higher mildness and stability. The microemulsion preconcentrate composition is prepared from the composition by adopting a microemulsion technology, so that the stability is improved, the use is more convenient, and the microemulsion preconcentrate composition is suitable for any dosage form. The composition has effects of inhibiting growth and reproduction of harmful pox-causing bacteria, promoting wound healing, accelerating skin renewal, accelerating acne mark fading, reducing pigmentation or accelerating pigment metabolism, repairing and strengthening skin barrier, and solves the problem of incapability of taking effect and mildness into account.
Description
Technical Field
The invention relates to the technical field of acne-removing products, in particular to a microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks, and a preparation method and application thereof.
Background
Acne, known by the academic name of Acne vulgaris (Acne vugularis), is the most common chronic inflammatory disease of the pilosebaceous glands in dermatology, has skin lesions which are better developed on cheeks, forehead and mandible, and can also affect the trunk, such as the anterior chest, back and shoulder blade, is characterized by Acne, cattail rash, pustules, nodules, cysts and scars, is often accompanied by seborrhea, is better developed on young men and women, and is also commonly called as "whelk". Acne has a variety of causes, the main four of which are due to abnormal androgen levels, massive sebum secretion, parakeratosis of perifollicular cells and inflammatory responses (mainly caused by propionibacterium acnes). Besides the four main reasons, genetic, psychological stress, immunity and other factors can also influence.
Hyperseborrhea is the basic pathological basis for the development of acne. The development of sebaceous glands has great correlation with androgen level, and when the androgen content in a body is increased, the sebaceous gland functions vigorously to cause massive secretion of grease; parakeratosis of the perifollicular cells is another important factor in the development of acne. The follicular surrounding cell keratinization often causes the opening of a hair follicle to become small, narrow and blocked, so that sebum cannot be discharged, and visible acne or invisible microacne is formed; hyperproliferation of propionibacterium acnes. Propionibacterium acnes can promote the expression of Toll-like receptors of keratinocytes, sebaceous gland cells and monocytes, can hydrolyze triglyceride in sebum to generate free fatty acid, and the free fatty acid stimulates hair follicles and the periphery of the hair follicles to generate inflammatory reaction so as to locally generate papules, pustules, nodules and abscesses; inflammatory reaction. Because seborrhea leads to increased proliferation of propionibacterium acnes, which exacerbates various degrees of inflammation by modulating Toll-like receptor expression, a range of clinical symptoms occurs, ranging from inflammatory papules to cysts.
Acidic raw materials with high concentration, such as vitamin A acid, salicylic acid, azelaic acid and the like, are mostly used in more powerful acne removing products on the market. However, the topical retinoic acid drugs often have mild skin irritation reactions, such as local erythema and desquamation, and have tense and burning feeling; salicylic acid and azelaic acid are difficult, and are also easy to cause skin irritation reaction, local erythema, stabbing pain and the like. The mild acne removing products on the market are partially declared to have unobvious acne removing effect due to the defects of permeability, antibacterial strength, anti-inflammatory capacity, capacity of adjusting and improving abnormal cutin of cells around hair follicles and the like, and even partial deficiency of the acne inhibiting effect.
Disclosure of Invention
In order to overcome the defects of the prior art, one of the purposes of the invention is to provide a microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks, which contains various oil-soluble acne removing components, has stronger permeability compared with water-soluble components, has the characteristic of lower concentration for effect, and has higher mild performance; the invention also aims to provide a preparation method of the microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks, wherein the microemulsion preconcentration composition is prepared by using a microemulsion technology, is convenient to use and is suitable for any dosage form; the invention also aims to provide the application of the microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks, which can be used as the main component of an acne removing product, promote wound healing, accelerate wound repair, accelerate skin renewal and accelerate fading of acne marks.
One of the purposes of the invention is realized by adopting the following technical scheme:
a microemulsion preconcentrate composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks comprises the following components: functional components, emulsifier, auxiliary emulsifier and auxiliary components; wherein the effective components are composition of ascorbyl tetraisopalmitate, paeonol, caprylyl salicylic acid, peony seed oil and oat kernel extract.
Specifically, the material comprises the following raw materials in percentage by mass: 1 to 5 percent of ascorbyl tetraisopalmitate, 1 to 3 percent of paeonol, 1 to 3 percent of caprylyl salicylic acid, 2 to 8 percent of peony seed oil, 2 to 8 percent of oat kernel extract, 7 to 95 percent of emulsifier, 2 to 75 percent of auxiliary emulsifier and 0.01 to 0.05 percent of auxiliary component.
Further, the emulsifier is PEG-40 hydrogenated castor oil and/or polyglycerol-6 caprylate. Preferably, the emulsifier comprises the following raw materials in percentage by mass: 14 to 58 percent of PEG-40 hydrogenated castor oil and 7 to 29 percent of polyglycerol-6 caprylate.
Further, the coemulsifier is 1, 3-butanediol and/or 1, 3-propanediol. Preferably, the coemulsifier comprises the following raw materials in percentage by mass: 1 to 20 percent of 1, 3-butanediol and 1 to 52 percent of 1, 3-propanediol. The auxiliary component is tocopherol; the auxiliary component is 0.01-0.1% of tocopherol.
The second purpose of the invention is realized by adopting the following technical scheme:
the preparation method of the microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks comprises the following steps:
1) Heating the effective components, the emulsifier and the auxiliary emulsifier, and stirring for dissolving;
2) Adding the rest components, and stirring to obtain microemulsion preconcentration composition with effects of inhibiting bacteria, removing acne, promoting wound healing, and eliminating acne mark.
Further, in the step 1), the heating temperature is 70-80 ℃.
The third purpose of the invention is realized by adopting the following technical scheme:
the microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and removing acnes spots is used for preparing an acne removing product for preventing and repairing acnes and acne marks.
Further, the addition amount of the composition in the acne-removing product is 1-20%.
Compared with the prior art, the invention has the beneficial effects that:
(1) The invention relates to a microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks, which comprises the following components: functional components, emulsifier, auxiliary emulsifier and auxiliary components; wherein the effective components are ascorbyl tetraisopalmitate, paeonol, caprylyl salicylic acid, peony seed oil and oat kernel extract. The functional components are oil-soluble acne-removing components, and compared with water-soluble components, the acne-removing cream has the advantages of stronger permeability, lower concentration and effect, and higher mildness and stability. However, because the functional components are oil-soluble components, the application to aqueous products is troublesome, and the microemulsion technology is applied to prepare the composition into the microemulsion preconcentration composition, compared with the partial water-soluble functional components of the functional components, the stability is improved, the use is more convenient, and the microemulsion preconcentration composition is suitable for any dosage form. The composition is convenient to use, has the effects of inhibiting the growth and reproduction of harmful pox-causing bacteria, promoting wound healing, accelerating wound surface repair, accelerating skin renewal, accelerating acne mark fading, reducing pigmentation or accelerating pigment metabolism, repairing and strengthening skin barriers and the like, and solves the problem that the effect and the mildness cannot be considered at the same time.
(2) The microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks completely meets all indexes in the cosmetic hygiene Specification (2007 edition) issued by the state, and does not contain any toxic substance.
(3) The microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks is an effective component which can be added into cosmetics in various formulations in a proper amount.
Detailed Description
The present invention is further described below with reference to specific embodiments, and it should be noted that, without conflict, any combination between the embodiments or technical features described below may form a new embodiment.
A microemulsion preconcentrate composition for inhibiting bacteria, removing acne, promoting wound healing and fading acne marks comprises the following components: functional components, emulsifier, auxiliary emulsifier and auxiliary components; wherein the effective components are ascorbyl tetraisopalmitate, paeonol, caprylyl salicylic acid, peony seed oil and oat kernel extract.
Wherein the emulsifier is PEG-40 hydrogenated castor oil and/or polyglycerol-6 caprylate. The coemulsifier is 1, 3-butanediol and/or 1, 3-propanediol. The auxiliary component is tocopherol.
The paeonol in the invention is a component extracted from root bark of Chinese peony. Paeonol has effects of inhibiting generation of intracellular O2-free radical, whitening skin, reducing and discoloring pigment deposited in skin, removing blood stasis and speckle, relieving inflammation, relieving swelling and pain, resisting allergy and virus, etc. Has good treatment and health care effects on color spots, myalgia, skin pruritus, psoriasis, herpes zoster and eczema. The research shows that the in-vitro antibacterial performance of the paeonol reflects that the paeonol has obvious antibacterial action on bacteria such as Escherichia coli, proteus, typhoid bacillus, paratyphoid bacillus B, staphylococcus aureus, staphylococcus epidermidis and the like, and the antibacterial action is enhanced along with the increase of the concentration; the paeonol can reduce the generation and release of inflammatory mediators such as IL-6, IL-1 beta, TNF-alpha and the like by inhibiting inflammatory cell aggregation and infiltration in local inflammatory tissues, increase capillary permeability by reducing PGE2 release, relieve local edema and effectively control acute inflammatory reaction; the paeonol and the derivatives thereof have phenolic hydroxyl functional groups in chemical structures, and the hydroxyl can be combined with free radical active substances for initiating chain reaction in advance to generate stable compounds, so that the effect of removing oxygen free radicals is achieved; after percutaneous absorption, paeonol can enhance the oxidation resistance of organisms by increasing SOD activity, and inhibit oxidative stress reaction by reducing MDA generation, so that the generation and the removal of free radicals in vivo reach dynamic balance, the deposition of excessive oxygen free radicals is reduced, and the local tissue damage caused by oxidative stress reaction is alleviated. Paeonol has the effects of resisting inflammation, resisting bacteria, diminishing swelling, resisting oxidation and the like, and mainly plays the roles of inhibiting inflammation, diminishing swelling, relieving pain, inhibiting acne-causing bacteria, fading acne marks and the like in the composition.
The ascorbyl tetraisopalmitate in the invention is a fat-soluble ascorbic acid derivative and is commonly known as VC-IP. Ascorbyl tetraisopalmitate as a vitamin C derivative has better absorbability than vitamin C, excellent transdermal absorbability, better permeability than water-soluble vitamin C, less irritation, and stability to heat and oxidation. The ascorbyl tetraisopalmitate has excellent antioxidant effect and can effectively inhibit sebum oxidation; the ascorbyl tetraisopalmitate can promote the generation and activity of human fibroblasts, promote the synthesis of collagen and further promote the healing of wounds. Therefore, ascorbyl tetraisopalmitate has anti-inflammatory, collagen regeneration promoting, pox mark lightening, and the like effects in the composition of the present invention. The paeonol in the invention mainly has the functions of resisting inflammation, inhibiting bacteria and reducing swelling, and the ascorbyl tetraisopalmitate can improve the oxidation resistance of the material body per se and increase the stability, and the most important function is to inhibit the oxidative deterioration of redundant metabolic waste grease on the skin and promote the synthesis of collagen so as to promote the healing of wounds. The two have synergistic effect, and can effectively prevent early-stage acne by utilizing the antibacterial and antioxidant properties of the two; the effects of reducing swelling, relieving pain, resisting inflammation and promoting wound healing are utilized, so that the recovery time of mature pox can be accelerated; the characteristics of the ascorbyl tetraisopalmitate that the activity of tyrosinase is inhibited and the activity of cells is increased are utilized, which is beneficial to the repair of the acne marks.
The caprylyl salicylic acid in the invention can permeate into the deep layer of the pores along the sebaceous glands, dissolves the substances among cuticles, promotes the cuticles to fall off, prevents old cuticles which do not fall off normally from blocking the pores to form acne, can reduce the enlarged pores, promotes the epidermal cells to be updated quickly, and enables the skin to recover to be smooth and fine. The octanoyl salicylic acid can reorganize epidermal cell tissue, stimulate cell renewal, treat acne with dry skin, prevent skin aging, improve skin color, reduce wrinkle, and make face or body bright and clean.
The peony (Paeonia SUFFRUTICOSA) seed oil has the effect of promoting the generation of cathepsin, is used as an antioxidant in cosmetics and has the effect of resisting aging; has strong inhibiting effect on staphylococcus, proteus, pseudomonas aeruginosa, escherichia coli, bacillus subtilis and the like, so the antibacterial and anti-inflammatory effects are achieved; has contraction effect on collagen fiber gel, and can be used as pore astringing agent.
The oat (AVENA SATIVA) kernel extract of the present invention is a unique complex containing fatty acids capable of repairing, renewing and protecting the skin lipid barrier. The extract of the kernel of Avena SATIVA (Avena SATIVA) is helpful for increasing the content of ceramide and hyaluronic acid in skin; can promote the expression of genes activating proteins involved in the integrity of the epidermal structure and hyaluronic acid synthase, thereby improving the integrity of the skin; oat kernel extract is an excellent lipid source, and supplements the natural lipids of the skin, thereby improving the lipid barrier; the skin moistening property of the grease and the moisturizing performance brought by the repair barrier can improve the dry and itching condition brought by other acne removing components and improve the skin moisturizing; and research results show that the oat kernel extract has excellent film-forming protection effect and does not cause acne
The tocopherol (vitamin E) in the invention is a vitamin E which is naturally sourced and is an excellent antioxidant. The natural vitamin E is easy to be absorbed by the skin, can promote the metabolism of the skin, prevent pigmentation, improve the elasticity of the skin, moisten the skin, and play a role in beautifying, protecting the skin and resisting aging; it can also prevent the formation of nitrosamine carcinogens and prevent or delay the rancidity of oil therein.
The PEG-40 hydrogenated castor oil is a viscous liquid, is semisolid at low temperature, and is a simply used broad-spectrum solubilizer. Generally as a mild emulsifier or solubilizer.
The polyglycerol-6 caprylate is polyglycerol fatty acid ester and is an excellent polyhydroxy ester nonionic surfactant. The polyglycerol ester has the characteristics of hydrophile and lipophile, and has multiple performances of good emulsification, dispersion, wetting and stability. Has strong bactericidal effect on bacillus subtilis. Can be decomposed in the metabolic process of human body, thereby participating in metabolism and being utilized by human body, and is a high-efficiency safe additive. Meanwhile, the polyglycerol ester is quite stable in acid, alkaline and neutral environments, and has good emulsibility when the salt content is high.
Example 1
A microemulsion preconcentration composition for inhibiting bacteria, removing acne, promoting wound healing and reducing acne mark comprises the following components (by weight percent):
ascorbyl tetraisopalmitate: 1 percent of
Paeonol: 1 percent of
Caprylyl salicylic acid: 1 percent of
Peony (PAEONIA SUFFRUTICOSA) seed oil: 2 percent of
Oat (AVENA SATIVA) kernel extract: 2 percent of
PEG-40 hydrogenated castor oil: 21 percent of
Polyglyceryl-6 caprylate: 7 percent
1, 3-butanediol: 13 percent of
1, 3-propanediol: 51.95 percent
Tocopherol (vitamin E): 0.05 percent
The preparation method of the composition comprises the following steps:
1) Heating the effective components, the emulsifier and the co-emulsifier to about 75 ℃, and stirring for dissolving; 2) Adding the rest components, stirring, and cooling to below 40 deg.C to obtain composition 1.
Examples 2 to 5
The procedure of experimental example 1 was repeated according to the contents of ascorbyl tetraisopalmitate, paeonol, caprylylsalicylic acid, peony (PAEONIA SUFFRUTICOSA) seed oil, oat (AVENA SATIVA) kernel extract, PEG-40 hydrogenated castor oil, polyglycerin-6 caprylate, 1, 3-butylene glycol, 1, 3-propylene glycol, tocopherol (vitamin E) and the like specified in table 1 below to obtain a microemulsion preconcentrate composition for inhibiting bacteria, removing acne, promoting wound healing and lightening acne marks, respectively, as shown in table 1.
TABLE 1 formulation of the compositions of examples 2 to 5
The microemulsion preconcentrate compositions 1 to 5 for inhibiting bacteria, removing acnes, promoting wound healing and reducing acne marks, prepared in examples 1 to 5, were tested and investigated for the effect against propionibacterium acnes, oil control performance and acne mark reduction performance.
Test example 1 anti-Propionibacterium acnes Effect
Propionibacterium acnes is the primary pathogen that causes acne. In an antibacterial experiment, propionibacterium acnes is used as a bacterial model, and in order to verify the antibacterial effect of the composition, the composition disclosed in the embodiments 1-5 of the invention is subjected to antibacterial performance determination according to GB15979-2002 appendix C4 of hygienic Standard for Disposable sanitary articles, namely a test method for antibacterial performance of dissolution-type antibacterial (bacteriostatic) resistant products:
1) Test samples: the compositions described in examples 1-5 were each diluted to make a 2% aqueous solution.
2) Preparation of bacterial suspension: washing the Propionibacterium acnes 24h culture with 0.03mol/L phosphate buffer solution to obtain 104-106CFU/mL bacterial suspension.
3) Respectively taking 1g of test sample, adding 0.1mL of the bacterial suspension, uniformly coating and mixing, timing, adding 9mL of 0.03mol/L phosphate buffer solution after 20min, fully and uniformly mixing, taking 3 dilutions, respectively taking 1mL of the dilutions, placing the dilutions in two parallel plates, adding a corresponding culture medium, and culturing for 24 hours at 36 +/-1 ℃ under an anaerobic condition to count colonies. The above experiment was repeated 3 times, and the average number was taken to set a blank control group.
The calculation formula of the bacteriostatic rate is as follows: x = (A-B)/A X100%, wherein X is the bacteriostasis rate, A is the average recovered colony of a blank control sample, and B is the average recovered colony of a test sample.
The evaluation criteria for efficacy were: (1) the effect is obvious when the bacteriostasis rate is more than or equal to 90 percent; (2) the bacteriostasis rate is 40-90 percent, which is the general effect; (3) the bacteriostasis rate is less than 40 percent, and no effect is obtained. The results are given in the following table (table 2).
Table 2 results of the composition anti-propionibacterium acnes test for each group
Oil control test
Test samples: in 5 embodiments, 5% of the oil-controlling, acne-removing and acne-repairing gel is added into a basic formula respectively to prepare the oil-controlling, acne-removing and acne-repairing gel, and the components and the mass percentage are as follows (table 3):
table 3 formula of acne removing products of each group
The clinical test number is 80, the test part is the face, the skin is oily pox skin, and the main purpose is to eliminate the influence of the skin on the test result. The results are shown in Table 4:
table 4 oil control test results for each group of anti-acne products
Acne mark and scar removal test
The test method comprises the following steps: 120 volunteers with newly generated acne marks and scars (the acne marks and scars are generated within one month) are summoned and divided into 6 groups, each group comprises 20 persons, wherein each group comprises 1 test sample in the table 3 for controlling oil and removing acnes to repair acne scar condensation, and the other group comprises a blank control group (the basic formula of the test samples is used, the microemulsion preconcentration composition for inhibiting bacteria and removing acnes, promoting wound healing and fading acne marks is not added), the microemulsion preconcentration composition is used once in the morning and at night every day, the using amount is 0.2 g/time, and the blank control group is smeared on the face and gently massaged until the acne marks and scars are absorbed. The results of comparison of the acne marks and scars after the volunteers use the product for one month are shown in the following table (table 5).
TABLE 5 acne mark fading effect of acne removing products of each group
As can be seen from tables 2 to 5, the acne removing products containing the compositions of examples 1 to 5 have the effects of inhibiting the growth and reproduction of harmful acne-causing bacteria, promoting wound healing, accelerating wound repair, accelerating skin renewal, accelerating acne mark fading, reducing pigmentation or accelerating pigment metabolism, repairing and strengthening skin barriers, and can achieve the effects of removing and repairing acne marks.
The above embodiments are only preferred embodiments of the present invention, and the scope of the present invention should not be limited thereby, and any insubstantial changes and substitutions made by those skilled in the art based on the present invention are intended to be covered by the claims.
Claims (10)
1. The microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and fading acne marks is characterized by comprising the following components: functional components, emulsifier, auxiliary emulsifier and auxiliary components; wherein the effective components are ascorbyl tetraisopalmitate, paeonol, caprylyl salicylic acid, peony seed oil and oat kernel extract.
2. The microemulsion preconcentrate composition for inhibiting bacteria, removing acnes, promoting wound healing and lightening acne marks according to claim 1, which comprises the following raw materials in percentage by mass: 1 to 5 percent of ascorbyl tetraisopalmitate, 1 to 3 percent of paeonol, 1 to 3 percent of caprylyl salicylic acid, 2 to 8 percent of peony seed oil, 2 to 8 percent of oat kernel extract, 7 to 95 percent of emulsifier, 2 to 75 percent of auxiliary emulsifier and 0.01 to 0.05 percent of auxiliary component.
3. The microemulsion preconcentrate composition for bacteriostasis, acne removal, wound healing promotion and acne mark lightening according to claim 1 or 2, wherein the emulsifier is PEG-40 hydrogenated castor oil and/or polyglycerol-6 caprylate.
4. The microemulsion preconcentrate composition for inhibiting bacteria, removing acnes, promoting wound healing and lightening acne marks according to claim 3, wherein the emulsifier comprises the following raw materials in percentage by mass: 14 to 58 percent of PEG-40 hydrogenated castor oil and 7 to 29 percent of polyglycerol-6 caprylate.
5. The microemulsion preconcentrate composition for bacteriostasis, acne removal, wound healing promotion and acne mark reduction according to claim 1 or 2, wherein the co-emulsifier is 1, 3-butanediol and/or 1, 3-propanediol; the auxiliary component is tocopherol.
6. The microemulsion preconcentrate composition for inhibiting bacteria, removing acnes, promoting wound healing and lightening acne marks according to claim 5, wherein the co-emulsifier comprises the following raw materials in percentage by mass: 1 to 20 percent of 1, 3-butanediol and 1 to 52 percent of 1, 3-propanediol; the auxiliary component is 0.01 to 0.1 percent of tocopherol.
7. The method for preparing the microemulsion preconcentrate composition for inhibiting bacteria, removing acnes, promoting wound healing and lightening acne marks according to any one of claims 1 to 6, is characterized by comprising the following steps of:
1) Heating the effective components, the emulsifier and the auxiliary emulsifier, and stirring for dissolving;
2) Adding the rest components, and stirring to obtain microemulsion preconcentration composition with effects of inhibiting bacteria, removing acne, promoting wound healing, and eliminating acne mark.
8. The method for preparing the microemulsion preconcentrate composition for inhibiting bacteria, removing acnes, promoting wound healing and lightening acne marks according to claim 7, wherein the heating temperature in the step 1) is 70-80 ℃.
9. The use of the microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and removing acnes marks according to any one of claims 1 to 6, wherein the microemulsion preconcentration composition for inhibiting bacteria, removing acnes, promoting wound healing and removing acnes marks is used for preparing an acne removing product for preventing and repairing acnes and acne muscles.
10. The use of the microemulsion preconcentrate composition for inhibiting bacteria, removing acnes, promoting wound healing and reducing acne marks according to claim 9, wherein the composition is added in an amount of 1-20% in an acne removal product.
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