CN115737502A - BMR bionic repair co-delivery system and preparation method and application thereof - Google Patents

BMR bionic repair co-delivery system and preparation method and application thereof Download PDF

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CN115737502A
CN115737502A CN202211488399.3A CN202211488399A CN115737502A CN 115737502 A CN115737502 A CN 115737502A CN 202211488399 A CN202211488399 A CN 202211488399A CN 115737502 A CN115737502 A CN 115737502A
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ceramide
component
bmr
stirring
repair
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谢玲
任传鹏
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Shanghai Chuanmei Industry Co ltd
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Abstract

The invention relates to a BMR bionic repair co-delivery system and a preparation method thereof, wherein the BMR bionic repair co-delivery system comprises 0.1-10% of Scutellaria alpina, 0.1-10% of ceramide, 0.1-20% of fatty acid, 0.05-8% of sterol and the balance of water by mass percent; wherein, the mol ratio of ceramide, fatty acid and sterol is 0.8-1.2:0.8-1.2:0.8-1.2; the ceramide comprises one or more of ceramide 1, ceramide 3 and ceramide 6, and a ceramide-like compound; the sterol is one or more of cholesterol, ergosterol and phytosterol; the fatty acid is one or more of linolenic acid, linoleic acid and oleic acid; compared with the prior art, the invention has the advantages of immediate and long-term barrier repair capability, improvement of the tolerance of the skin to external irritants, reduction of susceptibility and maintenance of the healthy steady state of the skin.

Description

BMR bionic repair co-delivery system and preparation method and application thereof
[ technical field ]
The invention relates to the technical field of cosmetics, in particular to a BMR bionic repair co-delivery system and a preparation method and application thereof.
[ background art ]
The skin is the first barrier of the human body from the outside world and is an organ that prevents the invasion of foreign substances. However, with modern industrial culture, this defense system is increasingly being breached, including ultraviolet, pollution, blue-light equipment, and various types of endogenous and exogenous infections. These factors contribute to increased inflammatory response and sensitivity of the skin, a weakened skin barrier, and decreased resistance and defense.
Therefore, many products focusing on the prevention and treatment of skin inflammation have been developed and are receiving increasing attention. Chinese georges have rich plant resources, and natural plant extracts are favored nowadays when people pursue nature, pursue green and pursue enhancement of health and safety awareness. Taking scutellaria alpina (s.baicalensis) as an example, scutellaria alpina is a perennial plant, an herb belonging to the family labiatae, contains various flavonoid bioactive ingredients, and the root thereof has been used for the treatment of inflammation and allergic diseases, and is used as a medicinal material in traditional medicine. The major active ingredients of the scutellaria alpina are baicalin and glucuronide, and the scutellaria alpina has the capabilities of resisting oxidation, resisting inflammation and repairing. However, studies on the skin availability of scutellaria alpina have been very limited. The external-use scutellaria alpina is mainly used by the skin through a percutaneous delivery path, and the relation between the dosage and the bioavailability is not clearly researched.
The stratum corneum is the main barrier and consists of dense lipid mortar and protein bricks, which act to limit the skin permeability of the external ingredients. The physiological lipids present in the stratum corneum are ceramides, free fatty acids and cholesterol, and are present in a molar ratio close to 1. This near equimolar ratio is important for the dynamic balance of the epidermis, since inhibition of production of either component was found to delay repair after barrier damage.
Most skin penetration enhancers achieve penetration of the skin by reversibly reducing the diffusion resistance of the intercellular lipid bilayers of the stratum corneum. These components may not only dissolve intercellular lipids, but also interfere with the metabolic activity of the produced intercellular lipid components, causing structural changes in the stratum corneum and further causing adverse reactions such as irritation of inflammation. Therefore, the components and the content ratio of the simulated physiological lipid of the stratum corneum have higher affinity for the stratum corneum, and can supplement and store equivalent physiological lipid, increase the ordered arrangement of intercellular lipid, and be helpful for promoting lipid flow and creating a delivery path and repairing damaged skin barriers.
[ summary of the invention ]
The invention aims to solve the defects and provide a BMR bionic repair co-delivery system which has immediate and long-term barrier repair capability, can improve the tolerance of skin to external irritants, reduces the susceptibility and maintains the steady state of skin health.
In order to realize the aim, the BMR bionic repair co-delivery system is designed, and comprises the following raw materials in percentage by mass: 0.1-10% of scutellaria alpina, 0.1-10% of ceramide, 0.1-20% of fatty acid, 0.05-8% of sterol and the balance of water.
Further, the mole ratio of ceramide, fatty acid and sterol is 0.8-1.2:0.8-1.2:0.8-1.2.
Further, the ceramide is one or more of ceramide 1, ceramide 3, ceramide 6 and ceramide-like.
Further, the fatty acid is one or more of linolenic acid, linoleic acid and oleic acid.
Further, the sterol is one or more of cholesterol, ergosterol and phytosterol.
Further, the scutellaria alpina is replaced by one or more of ganoderma lucidum extract, centella asiatica extract, rosemary leaf extract, camellia extract, tea leaf extract, aloe extract, ginseng extract, jojoba extract and liquorice extract.
The invention also provides a preparation method of the BMR bionic repair co-delivery system, which comprises the following steps:
(1) Putting 50-80% of deionized water, 0.03-0.05% of EDTA disodium, 1-2% of component A, 3-5% of glycerol, 3-5% of 1, 3-propylene glycol and 0.1-0.2% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the stirring speed of 30 revolutions per minute, homogenizing at 1500rpm for 2min; the component A comprises hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, polysorbate-60 and sorbitan isostearate;
(2) 3-7% of component B, 0.05-1.5% of pentaerythritol distearate, 1-2% of component C, 1-8% of component E and 1-10% of fatty acid are put into an oil phase pot, heated to 75 ℃, stirred for 15 minutes and uniformly stirred; the component B comprises polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax ester and cetyl alcohol; the component C comprises dioctyl carbonate and tocopherol vitamin E; the component E comprises sterol, tocopherol, vitamin E and ascorbyl palmitate;
(3) Pumping the raw materials of the water phase pot into an emulsifying pot, pumping the raw materials of the oil phase pot into the emulsifying pot, starting homogenizing at 2000rpm for 8min, stirring for 15 min, and preserving the temperature at 75 ℃;
(4) Starting cooling water, cooling to 65 ℃, adding the component D with the mass percent of 1-10%, stirring for 30 revolutions/min, and stirring for 10min; the component D comprises ceramide and phytosphingosine;
(5) Mixing 0.5-0.8% of p-hydroxyacetophenone and 0.50-2% of 1, 2-hexanediol by mass percent, heating to 55 ℃, and stirring until the mixture is transparent for later use;
(6) Cooling to 45 deg.C, adding 1-10 wt% of component F, 0.5-0.8 wt% of pre-dissolved p-hydroxyacetophenone, and 0.5-2 wt% of 1, 2-hexanediol, and stirring; the component F comprises Scutellariae radix flower/leaf/stem extract, glycerol, water, and citric acid;
(7) When the temperature is reduced to 38 ℃, discharging and storing after the temperature is qualified through inspection.
Further, in the step (2), the fatty acid is one or more of linolenic acid, linoleic acid and oleic acid, and the sterol is one or more of cholesterol, ergosterol and phytosterol; in the step (4), the ceramide is one or more of ceramide 1, ceramide 3, ceramide 6 and ceramide-like substances.
The invention also provides an application of the BMR bionic repair co-delivery system in co-delivery of effective active ingredients, obviously enhancing the bioavailability of the active ingredients and repairing damaged barriers.
Compared with the prior art, the invention has the following advantages:
(1) The BMR co-delivery repair system has a structure imitating intercellular lipid of skin stratum corneum, is added according to the proportion of skin physiological lipid close to equimolar, has skin repair capacity, can create a transdermal delivery passage at the same time, and improves the bioavailability of active ingredients;
(2) The BMR bionic repair co-delivery system is evaluated and verified in multiple directions by creating a skin damage model, and the repair capability of the BMR bionic repair co-delivery system to external skin stimulation can be remarkably improved on the premise of not increasing the using amount of an active ingredient Scutellaria alpina;
(3) The invention discovers that the BMR containing the Scutellaria alpina not only realizes the instant repair of the barrier, but also promotes the stable state of the barrier health for a long time;
in conclusion, the BMR system containing the scutellaria alpina has the capability of immediate and long-term barrier repair, can improve the tolerance of the skin to external irritants, reduces the susceptibility, maintains the stable state of the skin health, and is worthy of popularization and application.
[ description of the drawings ]
FIG. 1 is a graph of the change in TEWL values from baseline in subjects 2 hours after use of each product in accordance with an embodiment of the present invention;
FIG. 2 is a graph of the change in TEWL values from baseline in subjects 24 hours after use of each product in accordance with an embodiment of the present invention;
FIG. 3 is a graph showing the change in TEWL value of a subject after 24h of patch removal compared to 30min of patch removal in accordance with an embodiment of the present invention;
FIG. 4 is a graph of the TEWL value of a subject at 48h removal versus 30min removal for patch removal in accordance with an embodiment of the present invention;
FIG. 5 is a graph showing the change in TEWL value of a subject after 72h of patch removal compared to 30min of patch removal in accordance with an embodiment of the present invention;
fig. 6a, 6b and 6c are graphs of lactic acid stinging 2.5min score, 5min score and total score for subjects using BMR mixtures according to an embodiment of the present invention compared to a blank control side;
FIGS. 7a, 7b and 7c are graphs of the score of 2.5min, the score of 5min and the total score of lactic acid stinging compared to a blank control side using Scutellaria alpina alone for subjects according to examples of the present invention;
FIGS. 8a, 8b and 8c are graphs of lactic acid stinging 2.5min score, 5min score and total score for subjects using BMR + Scutellaria alpina compared to placebo side in accordance with an embodiment of the present invention;
FIG. 9 is an analysis of TEWL values of a subject's skin over time (long-term) in accordance with an embodiment of the present invention.
[ detailed description of the invention ]
The invention provides a BMR (Bio Membrane Repair co-delivery system), in particular to a BMR bionic Repair system containing Scutellaria alpina, which comprises 0.1-10% of Scutellaria alpina, 0.1-10% of ceramide, 0.1-20% of fatty acid, 0.05-8% of sterol and the balance of water according to mass percentage. Wherein, ceramide, fatty acid and sterol are added in nearly equimolar proportion; the ceramide comprises one or more of ceramide 1, ceramide 3 and ceramide 6, and ceramide-like; the sterol is one or more of cholesterol, ergosterol and phytosterol; the fatty acid is one or more of linolenic acid, linoleic acid and oleic acid; the co-delivered active component is plant anti-inflammatory repair active component radix scutellariae alpina, the plant anti-inflammatory repair active component can also be one or a combination of more of ganoderma lucidum extract, centella asiatica extract, rosemary leaf extract, camellia extract, tea leaf extract, aloe extract, ginseng extract, jojoba extract, liquorice extract and the like. Meanwhile, the invention provides an application of the BMR bionic repair system, namely, the BMR bionic repair system is used for co-delivering effective active ingredients, obviously enhancing the bioavailability of the active ingredients and repairing damaged barriers.
The present invention will be further described below with reference to specific examples and comparative examples:
example 1 BMR + Scutellaria alpina, this example provides a BMR biomimetic repair co-delivery system comprising Scutellaria alpina and a method for preparing the same
Figure BDA0003963728890000061
The preparation method comprises the following steps:
(1) Putting raw materials of 50-80% of deionized water, 0.03-0.05% of EDTA disodium, 1-2% of component A, 3-5% of glycerol, 3-5% of 1, 3-propylene glycol and 0.1-0.2% of sodium stearyl glutamate into a water phase pot by mass percent, heating to 75 ℃, uniformly stirring at the stirring speed of 30 r/min, homogenizing at 1500rpm and 2min; the component A comprises hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, polysorbate-60 and sorbitan isostearate;
(2) 3-7% of component B, 0.05-1.5% of pentaerythritol distearate, 1-2% of component C, 1-8% of component E and 1-10% of fatty acid are put into an oil phase pot, heated to 75 ℃, stirred for 15 minutes and uniformly stirred; the component B comprises polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax ester and cetyl alcohol; the component C comprises dioctyl carbonate and tocopherol vitamin E; the component E comprises sterol, tocopherol, vitamin E and ascorbyl palmitate;
(3) Pumping the raw materials in the water phase pot into an emulsifying pot, pumping the raw materials in the oil phase pot into the emulsifying pot, starting homogenization at 2000rpm for 8min, stirring for 15 min, and preserving the temperature for 75 ℃;
(4) Starting cooling water, cooling to 65 ℃, adding the component D with the mass percent of 1-10%, stirring for 30 revolutions per minute, and stirring for 10 minutes; the component D comprises ceramide and phytosphingosine;
(5) Mixing 0.5-0.8% of p-hydroxyacetophenone and 0.50-2% of 1, 2-hexanediol by mass percent, heating to 55 ℃, and stirring until the mixture is transparent for later use;
(6) Cooling to 45 deg.C, adding 1-10 wt% of component F, 0.5-0.8 wt% of pre-dissolved p-hydroxyacetophenone, and 0.5-2 wt% of 1, 2-hexanediol, and stirring; the component F comprises Scutellariae radix flower/leaf/stem extract, glycerol, water, and citric acid;
(7) When the temperature is reduced to 38 ℃, discharging and storing after the temperature is qualified through inspection.
In the case of the example 2, the following examples are given,
(1) Putting raw materials of 58% of deionized water, 0.04% of EDTA disodium, 1.5% of component A (hydroxyethyl acrylate/acryloyl dimethyl sodium taurate copolymer, polysorbate-60 and sorbitan isostearate), 4% of glycerol, 4% of 1, 3-propylene glycol and 0.15% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the speed of 30 r/min; homogenizing at 1500rpm; and 2min.
(2) 5% of component B (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax and cetyl alcohol), 1% of pentaerythritol distearate, 1.5% of component C (dioctyl carbonate, tocopherol (vitamin E)), 5% of component E (phytosterol, tocopherol (vitamin E) and ascorbyl palmitate), and 5% of linolenic acid raw material are put into an oil phase pot, heated to 75 ℃, stirred for 15 minutes and stirred uniformly.
(3) Pumping the raw materials of the water phase pot into an emulsifying pot, pumping the raw materials of the oil phase pot into the emulsifying pot, starting homogenizing at 2000rpm for 8min, stirring for 15 min, and preserving the temperature at 75 ℃.
(4) Cooling with cooling water, cooling to 65 deg.C, adding 10% of component D (ceramide 1, phytosphingosine, and hexadecyl glucoside), stirring for 30 r/min, and stirring for 10min.
(5) Mixing 0.66% of p-hydroxyacetophenone and 1.15% of 1, 2-hexanediol, heating to 55 ℃, and stirring until the mixture is transparent for later use.
(6) Cooling to 45 deg.C, adding 3% of component F (Scutellariae radix extract, glycerol, water, and citric acid) and pre-dissolved p-hydroxyacetophenone and 1, 2-hexanediol, and stirring.
(7) When the temperature is reduced to 38 ℃, discharging and storing after the temperature is qualified through inspection.
In the case of the embodiment 3, the following examples,
(1) Putting raw materials of 55.2% of deionized water, 0.05% of EDTA disodium, 1% of component A (hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, polysorbate-60 and sorbitan isostearate), 5% of glycerol, 5% of 1, 3-propylene glycol and 0.2% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the stirring speed of 30 r/min; homogenizing at 1500rpm; and 2min.
(2) 3% of component B (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax and cetyl alcohol), 0.05% of pentaerythritol distearate, 1% of component C (dioctyl carbonate, tocopherol (vitamin E)), 4% of component E (ergosterol, tocopherol (vitamin E) and ascorbyl palmitate), and 4% of linoleic acid raw material are put into an oil phase pot, heated to 75 ℃, stirred for 15 minutes and uniformly stirred.
(3) Pumping the raw materials of the water phase pot into an emulsifying pot, pumping the raw materials of the oil phase pot into the emulsifying pot, starting homogenizing at 2000rpm for 8min, stirring for 15 min, and preserving the temperature at 75 ℃.
(4) Cooling with cooling water, cooling to 65 deg.C, adding 9% of component D (ceramide 3, phytosphingosine, octyl glucoside), stirring for 30 r/min and 10min.
(5) Mixing 0.5% of p-hydroxyacetophenone and 2% of 1, 2-hexanediol, heating to 55 ℃, and stirring until the mixture is transparent for later use.
(6) Cooling to 45 deg.C, adding 10% of component F (radix Scutellariae extract, glycerol, water, and citric acid) and pre-dissolved p-hydroxyacetophenone and 1, 2-hexanediol, and stirring.
(7) When the temperature is reduced to 38 ℃, discharging and storing after the temperature is qualified through inspection.
In the case of the example 4, it is preferred,
(1) Putting 50% of deionized water, 0.03% of EDTA disodium, 2% of component A (hydroxyethyl acrylate/acryloyl dimethyl sodium taurate copolymer, polysorbate-60 and sorbitan isostearate), 3% of glycerol, 3% of 1, 3-propylene glycol and 0.1% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the stirring speed of 30 r/min; homogenizing at 1500rpm; and 2min.
(2) Adding 7% of component B (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax and cetyl alcohol), 1.5% of pentaerythritol distearate, 2% of component C (dioctyl carbonate, tocopherol (vitamin E)), 8% of component E (cholesterol) and 10% of oleic acid raw material into an oil phase pot, heating to 75 ℃, stirring for 15 minutes, and uniformly stirring.
(3) Pumping the raw materials of the water phase pot into an emulsifying pot, pumping the raw materials of the oil phase pot into the emulsifying pot, starting homogenizing at 2000rpm for 8min, stirring for 15 min, and preserving the temperature at 75 ℃.
(4) Cooling with cooling water, cooling to 65 deg.C, adding 10% of component D (ceramide 6, phytosphingosine, polyoxyethylene hydrogenated castor oil), stirring for 30 r/min, and stirring for 10min.
(5) Mixing 0.8% of p-hydroxyacetophenone and 0.5% of 1, 2-hexanediol, heating to 55 ℃, and stirring until the mixture is transparent for later use.
(6) Cooling to 45 deg.C, adding 2.07% of component F (stem extract of Scutellaria alpina Georgi, glycerol, water, citric acid) and pre-dissolved p-hydroxyacetophenone and 1, 2-hexanediol, and stirring.
(7) When the temperature is reduced to 38 ℃, discharging and storing after the temperature is qualified through inspection.
In the case of the example 5, the following examples were conducted,
(1) Putting 80% of deionized water, 0.03% of EDTA disodium, 1% of component A (hydroxyethyl acrylate/acryloyl dimethyl sodium taurate copolymer, polysorbate-60 and sorbitan isostearate), 3% of glycerol, 3% of 1, 3-propylene glycol and 0.1% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the stirring speed of 30 r/min; homogenizing at 1500rpm; and 2min.
(2) 3% of component B (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax ester and cetyl alcohol), 0.05% of pentaerythritol distearate, 1% of component C (dioctyl carbonate, tocopherol (vitamin E)), 2% of component E (cholesterol, tocopherol (vitamin E) and ascorbyl palmitate), 2% of linolenic acid and linoleic acid raw materials are put into an oil phase pot, heated to 75 ℃, stirred for 15 minutes and stirred uniformly.
(3) Pumping the raw materials in the water phase pot into an emulsifying pot, pumping the raw materials in the oil phase pot into the emulsifying pot, starting homogenization at 2000rpm for 8min, stirring for 15 min, and preserving the temperature for 75 ℃.
(4) Cooling with cooling water, cooling to 65 deg.C, adding 2% of component D (ceramide, phytosphingosine, PEG-10 glycine max), stirring for 30 r/min and 10min.
(5) Mixing 0.5% of p-hydroxyacetophenone and 0.5% of 1, 2-hexanediol, heating to 55 ℃, and stirring until the mixture is transparent for later use.
(6) Cooling to 45 deg.C, adding 1.82% of component F (Ganoderma extract, glycerol, water, citric acid) and pre-dissolved p-hydroxyacetophenone and 1, 2-hexanediol, and stirring.
(7) When the temperature is reduced to 38 ℃, discharging and storing after passing the inspection.
In the case of the example 6, it is shown,
(1) Putting raw materials of 56.3% of deionized water, 0.04% of EDTA disodium, 1.45% of component A (hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, polysorbate-60 and sorbitan isostearate), 4.05% of glycerol, 4.07% of 1, 3-propylene glycol and 0.18% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the stirring speed of 30 r/min; homogenizing at 1500rpm; and 2min.
(2) 4.5 percent of component B (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax ester and cetyl alcohol), 0.06 percent of pentaerythritol distearate, 1.2 percent of component C (dioctyl carbonate, tocopherol (vitamin E)), 1.5 percent of component E (ergosterol, tocopherol (vitamin E) and ascorbyl palmitate), 20 percent of linoleic acid and oleic acid raw materials are put into an oil phase pot, heated to 75 ℃, stirred for 15 minutes and stirred uniformly.
(3) Pumping the raw materials of the water phase pot into an emulsifying pot, pumping the raw materials of the oil phase pot into the emulsifying pot, starting homogenizing at 2000rpm for 8min, stirring for 15 min, and preserving the temperature at 75 ℃.
(4) Cooling with cooling water, cooling to 65 deg.C, adding 1.5% of component D (ceramide 1, ceramide E, phytosphingosine, polyoxyethylene sorbitan fatty acid ester), stirring for 30 r/min, and stirring for 10min.
(5) Mixing 0.55% of p-hydroxyacetophenone and 0.6% of 1, 2-hexanediol, heating to 55 ℃, and stirring until the mixture is transparent for later use.
(6) Cooling to 45 deg.C, adding 4% of component F (herba Centellae extract, glycerol, water, and citric acid) and pre-dissolved p-hydroxyacetophenone and 1, 2-hexanediol, and stirring.
(7) When the temperature is reduced to 38 ℃, discharging and storing after passing the inspection.
In the case of the embodiment 7, the following examples,
(1) Putting 54.6% of deionized water, 0.05% of EDTA disodium, 1.5% of component A (hydroxyethyl acrylate/acryloyl dimethyl sodium taurate copolymer, polysorbate-60 and sorbitan isostearate), 3.5% of glycerol, 3.5% of 1, 3-propylene glycol and 0.2% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the stirring speed of 30 r/min; homogenizing at 1500rpm; and 2min.
(2) Putting 6% of component B (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax and cetyl alcohol), 1.1% of pentaerythritol distearate, 1.5% of component C (dioctyl carbonate, tocopherol (vitamin E)), 0.05% of component E (ergosterol) and 0.1% of linolenic acid raw material into an oil phase pot, heating to 75 ℃, stirring for 15 minutes, and uniformly stirring.
(3) Pumping the raw materials of the water phase pot into an emulsifying pot, pumping the raw materials of the oil phase pot into the emulsifying pot, starting homogenizing at 2000rpm for 8min, stirring for 15 min, and preserving the temperature at 75 ℃.
(4) Cooling with cooling water, cooling to 65 deg.C, adding 20% of component D (ceramide 1/3, polyglycerol-10 oleate), stirring at 30 rpm for 10min.
(5) Mixing 0.7% of p-hydroxyacetophenone and 1.2% of 1, 2-hexanediol, heating to 55 ℃, and stirring until the mixture is transparent for later use.
(6) Cooling to 45 deg.C, adding 6% of component F (flos Camelliae Japonicae extract, glycerol, water, citric acid) and pre-dissolved p-hydroxyacetophenone and 1, 2-hexanediol, and stirring.
(7) When the temperature is reduced to 38 ℃, discharging and storing after passing the inspection.
In the case of the example 8, the following examples are given,
(1) Putting raw materials of 78.2% of deionized water, 0.03% of EDTA disodium, 1% of component A (hydroxyethyl acrylate/acryloyl dimethyl sodium taurate copolymer, polysorbate-60 and sorbitan isostearate), 3% of glycerol, 3% of 1, 3-propylene glycol and 0.15% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the speed of 30 r/min; homogenizing at 1500rpm; and 2min.
(2) 3.5% of component B (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax and cetyl alcohol), 0.07% of pentaerythritol distearate, 1.8% of component C (dioctyl carbonate, tocopherol (vitamin E)), 1% of component E (phytosterol, tocopherol (vitamin E) and ascorbyl palmitate), and 1% of linoleic acid raw material are put into an oil phase pot, heated to 75 ℃, stirred for 15 minutes and stirred uniformly.
(3) Pumping the raw materials of the water phase pot into an emulsifying pot, pumping the raw materials of the oil phase pot into the emulsifying pot, starting homogenizing at 2000rpm for 8min, stirring for 15 min, and preserving the temperature at 75 ℃.
(4) Cooling with cooling water, cooling to 65 deg.C, adding 1.2% of component D (ceramide 1, phytosphingosine, octyl glucoside), stirring for 30 r/min, and stirring for 10min.
(5) Mixing 0.5% of p-hydroxyacetophenone and 0.55% of 1, 2-hexanediol, heating to 55 ℃, and stirring until the mixture is transparent for later use.
(6) Cooling to 45 deg.C, adding 5% of component F (Glycyrrhrizae radix extract, glycerol, water, citric acid) and pre-dissolved p-hydroxyacetophenone and 1, 2-hexanediol, and stirring.
(7) When the temperature is reduced to 38 ℃, discharging and storing after passing the inspection.
Comparative example 1 BMR blank
Figure BDA0003963728890000131
Figure BDA0003963728890000141
As shown in the above table, the preparation process is:
(1) Putting raw materials of 1 (deionized water), 2 (disodium EDTA), 3 (hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, polysorbate-60, sorbitan isostearate, 4 (glycerol), 5 (1, 3-propylene glycol) and 6 (sodium stearyl glutamate) into a water phase pot, heating to 75 ℃, uniformly stirring at the stirring speed of 30 revolutions per minute; homogenizing at 1500rpm; and 2min.
(2) Adding 7 (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax, cetyl alcohol), 8 (pentaerythritol distearate), 9 (dioctyl carbonate, tocopherol (vitamin E)), 11 (phytosterol oleate, tocopherol (vitamin E), ascorbyl palmitate, phytosterol), 12 (linolenic acid, linoleic acid, oleic acid) into an oil phase pot, heating to 75 deg.C, stirring for 15 min, and stirring.
(3) Pumping the raw materials of the water phase pot into an emulsifying pot, pumping the raw materials of the oil phase pot into the emulsifying pot, starting homogenizing at 2000rpm for 8min, stirring for 15 min, and preserving the temperature at 75 ℃.
(4) Cooling with cooling water, cooling to 65 deg.C, adding 10 (ceramide NP \ AP \ EOP, phytosphingosine, and lauroyl lactyl sodium lactate), stirring for 30 r/min and 10min.
(5) Mixing 13 (p-hydroxyacetophenone) and 14 (1, 2-hexanediol), heating to 55 deg.C, and stirring to transparent.
(6) Cooling to 45 deg.C, adding dissolved 13 (p-hydroxyacetophenone) and 14 (1, 2-hexanediol), and stirring.
(7) When the temperature is reduced to 38 ℃, discharging and storing after passing the inspection.
Comparative example 2, scutellaria alpina Franch alone
Figure BDA0003963728890000151
As shown in the above table, the preparation process is:
(1) Putting raw materials of No. 1 (deionized water), 2 (disodium EDTA), 3 (hydroxyethyl acrylate/acryloyl dimethyl sodium taurate copolymer, polysorbate-60, sorbitan isostearate, 4 (glycerin), 5 (1, 3-propylene glycol) and 6 (sodium stearyl glutamate) into a water phase pot, heating to 75 ℃, uniformly stirring at the speed of 30 revolutions per minute; homogenizing at 1500rpm; and 2min.
(2) Adding No. 7 (polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax, and cetyl alcohol), no. 8 (pentaerythritol distearate), and No. 9 (dioctyl carbonate, and tocopherol (vitamin E)) into an oil phase pot, heating to 75 deg.C, stirring for 15 min, and stirring.
(3) Pumping the raw materials in the water phase pot into an emulsifying pot, pumping the raw materials in the oil phase pot into the emulsifying pot, starting homogenization at 2000rpm for 8min, stirring for 15 min, and preserving the temperature for 75 ℃.
(4) Mixing raw materials of No. 11 (p-hydroxyacetophenone) and No. 12 (1, 2-hexanediol), heating to 55 ℃, and stirring until the mixture is transparent for later use.
(5) Cooling with cooling water, cooling to 45 deg.C, adding 10 (Scutellaria ALPINA) flower/leaf/stem extract, glycerol, water, citric acid) and pre-dissolved 11 (p-hydroxyacetophenone) and 12 (1, 2-hexanediol), and stirring.
(6) When the temperature is reduced to 38 ℃, discharging and storing after the temperature is qualified through inspection.
Test example 1 short-term repair efficacy test of barrier failure model using tape stripping method
The BMR bionic restoration system containing the scutellaria alpina has a synergistic effect in barrier restoration, a skin barrier damage model is established by using a cuticle peeling method, and comparative tests are respectively carried out by using example 1 (BMR + scutellaria alpina), comparative example 1 (BMR) and comparative example 2 (single scutellaria alpina). All of the compositions prepared in the examples and comparative examples above were subjected to a transepidermal water loss (TEWL) experiment.
The transepidermal water loss rate (TEWL) was accurately measured using a non-invasive measuring device (Tewameter TM 300). The testing principle is that a pair of relative temperature/humidity sensors are arranged in a Tewameter TM300 probe, and the evaporation amount of water in a body passing through the skin is tested according to the Fick diffusion law. The TEWL is obviously reduced before and after the test product is used, so that the skin barrier is restored, and the product has the repairing efficacy.
20 healthy people are selected, male and female are not limited, and the age is 18-60 years. Randomly selecting one side arm, selecting four 1.5cm × 1.5cm forearm flexor skin, positioning and marking the part to be tested, and measuring TEWL of the four areas. Multiple peels of each area were made using hypoallergenic tape, and the skin barrier physical damage model was considered successful when the TEWL value increased above 50% of the basal value.
And performing blank control treatment and smearing three types of test products on each area respectively, and measuring each index of each area again after using the products for 2 hours. The subjects visit again the same time the day after, and each index of each area after using the product for 24h was measured.
The repair ability of each test product to restore skin barrier function over time was evaluated by comparing the skin TEWL value after 2h with the amount of change immediately after molding completion for each product, and the amount of change from baseline level for 24h with each product.
As can be seen from FIG. 1, the TEWL values after 2h using the three products were all reduced more than the blank control group than immediately after the completion of the molding. Wherein the TEWL value of the blank control group is averagely reduced by 6.69g/hm 2 Mean reduction in TEWL values of 7.91g/hm for BMR blend groups 2 The TEWL value of a single alpine scutellaria group is averagely reduced by 9.00g/hm 2 The TEWL value of BMR + alpine scutellaria group is averagely reduced by 11.94g/hm 2 . Wherein the change of the TEWL value of the BMR + alpine radix scutellariae group is significant compared with that of a blank control group.
As can be seen from figure 2, the TEWL values for each treatment group were slightly above baseline levels after 24h with the three products. The blank control group TEWL values averaged 5.43g/hm above baseline 2 The BMR mixture group TEWL values averaged 6.03g/hm above baseline 2 The single alpine scutellaria group TEWL value is averagely higher than the baseline by 5.02g/hm 2 The TEWL value of BMR + alpine scutellaria is averagely higher than the baseline by 2.98g/hm 2 . Wherein the TEWL value of the BMR + Scutellaria alpina group is closer to the baseline level before damage, and the difference is significant compared with the blank control group. The results indicate that under the test condition, the BMR and the scutellaria alpina test product can obviously reduce the transdermal water loss of the skin and has the repairing effect.
Test example 2 short-term repair efficacy test for SLS irritant patch model
SLS is a common positive control substance in a human skin irritant model patch test, and can induce epidermal inflammatory cell infiltration, destroy skin barriers and generate a skin erythema reaction after SLS stimulation. The soothing ability of each test product to improve the skin irritation state in a short time was evaluated by inclusion of 20 healthy subjects, closed patch application of 0.5% sls solution to each area for 24 hours, and by observing TEWL and patch change amounts at 30min for each area 24 hours, 48 hours, and 72 hours after patch removal. Thus reflecting the short-term repair efficacy of the three test products on skin barrier damage caused by chemical irritants.
2.1 TEWL values for each group at 24h patch removal
Average reduction of TEWL value of blank control group by 3.36g/hm 2 Mean reduction in TEWL value of 3.06g/hm for BMR blend groups 2 The TEWL value of a single scutellaria alpina group is averagely reduced by 2.18g/hm 2 The mean reduction of TEWL value of BMR + Scutellaria alpina group is 5.22g/hm 2 . There was no significant difference in the variation between each product group and the blank control group, as shown in fig. 3.
2.2 TEWL values for each group at 48h patch removal
Average reduction of TEWL value of blank control group by 4.16g/hm 2 Mean reduction in TEWL values for BMR blend groups of 4.84g/hm 2 The TEWL value of the single alpine scutellaria group is averagely reduced by 5.09g/hm 2 The TEWL value of the BMR + alpine radix scutellariae group is averagely reduced by 8.14g/hm 2 . The TEWL values of the three test products are all reduced more than that of the blank control group, the TEWL values of the BMR + Scutellaria alpina group are reduced more, and the variation is obviously different from that of the blank control group, as shown in figure 4.
2.3 TEWL values for each patch removal 72
Average reduction of TEWL value of blank control group by 5.37g/hm 2 Mean reduction in TEWL values of 6.84g/hm for BMR blend groups 2 The average TEWL value of a single alpine scutellaria group is reduced by 7.12g/hm 2 The mean reduction of TEWL value of BMR + Scutellaria alpina group is 10.16g/hm 2 . The reduction of TEWL values was most significant in the BMR + Scutellaria alpina group, as shown in FIG. 5.
TABLE 1 TEWL values and 30min changes from patch removal compared to subject at 24h, 48h, 72h, respectively
Figure BDA0003963728890000181
The data show that the short-term repair efficacy test of the SLS stimulant patch model of 20 subjects shows that the TEWL value of the skin of each region of the subjects is reduced after the three products are used, and the reduction amount is obviously higher than that of a blank control group (P < 0.05), which indicates that the three products have certain repair efficacy. The skin reaction score of the BMR + alpine radix scutellariae group is reduced most, and the variation difference with the blank control group is most obvious. Through BMR, the relieving and repairing effect of the scutellaria alpina on external stimulation can be more obviously improved on the premise of not increasing the using amount of the scutellaria alpina.
Test example 3 immediate relief efficacy test of lactic acid stimulant
Lactic acid can induce sensitive symptoms such as stabbing pain, pruritus and redness of skin, and can be used as a common chemical probe for semi-subjective test of the relieving efficacy of skin with damaged barrier. By inclusion of 60 sensitive skin subjects, 20 persons per product group, self-half-face control by lactic acid sting test, immediate soothing efficacy of three products on the stimulating substance was evaluated based on the difference in sting scores on both sides after lactic acid stimulation.
3.1 test found that by subjecting 60 sensitive skin subjects to their own half-face control lactic prick test, subjects experienced a reduction in lactic prick by 44.44%, 28.00% and 34.88%, respectively, immediately upon use of the BMR mixture product, compared to the blank control side, 5min score and total score (see fig. 6a, 6b and 6 c); however, these differences are not yet statistically significant.
3.2 subjects had a 2.5min score, a 5min score and a total score reduction of 52.38% (P < 0.05), 33.33% (P < 0.05) and 40.70% (P < 0.05) in lactic acid stinging, respectively, as compared to the placebo side, immediately with single alpine scutellaria product (see fig. 7a, 7b and 7 c); the single alpine scutellaria has the effect of relieving.
3.3 immediately after the subject uses the BMR + Scutellaria alpina product, the lactic acid stinging score of 2.5min, the 5min score and the total score were decreased by 62.07% (P < 0.05), 51.43% (P < 0.05) and 56.25% (P < 0.05), respectively, compared to the blank control side (see FIG. 8a, FIG. 8b and FIG. 8c. From the data, it was found that Scutellaria alpina could be better promoted to exert its effect of soothing and repairing by BMR without increasing the concentration of Scutellaria alpina.
Test example 4 evaluation of Long-lasting skin repair Using BMR + Scutellaria alpina
The effect of the BMR and scutellaria alpina containing product of example 1 on the long-lasting repair of skin after use by the subject was evaluated by a human efficacy evaluation test. The evaluation standard of the efficacy is based on QB/T4256-2011 'guidelines for evaluating moisturizing efficacy of cosmetics'. The test was conducted on 35 enrolled women aged 20-55 years who were self-rated to have sensitive skin. The face was associated with symptoms of slight redness, erythema, dryness (desquamation, tightness), etc., and the lactic acid challenge test screened scores: the score is more than or equal to 3. The follow-up time was 1 week, 3 weeks, and 4 weeks (W0, W1, W3, W4) before use, respectively, and the TEWL of the skin was observed with time to evaluate the long-lasting repair effect on the skin after the use of the subject.
As in fig. 9, the subject's skin TEWL value increased by 2.42% after 1 week of product use; the TEWL value of the skin is reduced by 11.73 percent after the product is used for 3 weeks, and the TEWL value of the skin is reduced by 17.25 percent after the product is used for 4 weeks. The results suggest that under the test conditions, the test product can obviously reduce the transdermal water loss of the skin and has the efficacy of long-acting repair.
The present invention is not limited to the above embodiments, and any other changes, modifications, substitutions, combinations, and simplifications which do not depart from the spirit and principle of the present invention should be construed as equivalents and are included in the scope of the present invention.

Claims (9)

1. A BMR bionic repair co-delivery system is characterized by comprising the following raw materials in percentage by mass: 0.1 to 10 percent of alpine radix scutellariae, 0.1 to 10 percent of ceramide, 0.1 to 20 percent of fatty acid, 0.05 to 8 percent of sterol and the balance of water.
2. The BMR biomimetic repair co-delivery system according to claim 1, wherein: the mole ratio of the ceramide to the fatty acid to the sterol is 0.8-1.2:0.8-1.2:0.8-1.2.
3. The BMR biomimetic repair co-delivery system according to claim 1, wherein: the ceramide is one or more of ceramide 1, ceramide 3, ceramide 6 and ceramide-like.
4. The BMR biomimetic repair co-delivery system according to claim 1, wherein: the fatty acid is one or more of linolenic acid, linoleic acid and oleic acid.
5. The BMR biomimetic repair co-delivery system according to claim 1, wherein: the sterol is one or more of cholesterol, ergosterol and phytosterol.
6. The BMR biomimetic repair co-delivery system according to claim 1, wherein: the Scutellaria alpina is replaced by one or more of a ganoderma lucidum extract, a centella asiatica extract, a rosemary leaf extract, a camellia extract, a tea leaf extract, an aloe extract, a ginseng extract, a jojoba extract and a licorice root extract.
7. A preparation method of a BMR bionic repair co-delivery system is characterized by comprising the following steps:
(1) Putting 50-80% of deionized water, 0.03-0.05% of EDTA disodium, 1-2% of component A, 3-5% of glycerol, 3-5% of 1, 3-propylene glycol and 0.1-0.2% of sodium stearyl glutamate into a water phase pot, heating to 75 ℃, uniformly stirring at the stirring speed of 30 revolutions per minute, homogenizing at 1500rpm for 2min; the component A comprises hydroxyethyl acrylate/sodium acryloyldimethyl taurate copolymer, polysorbate-60 and sorbitan isostearate;
(2) 3-7% of component B, 0.05-1.5% of pentaerythritol distearate, 1-2% of component C, 1-8% of component E and 1-10% of fatty acid are put into an oil phase pot, heated to 75 ℃, stirred for 15 minutes and uniformly stirred; the component B comprises polyglycerol-6 distearate, jojoba esters, polyglycerol-3 beeswax ester, and cetyl alcohol; the component C comprises dioctyl carbonate and tocopherol vitamin E; the component E comprises sterol, tocopherol, vitamin E and ascorbyl palmitate;
(3) Pumping the raw materials in the water phase pot into an emulsifying pot, pumping the raw materials in the oil phase pot into the emulsifying pot, starting homogenization at 2000rpm for 8min, stirring for 15 min, and preserving the temperature for 75 ℃;
(4) Starting cooling water, cooling to 65 ℃, adding the component D with the mass percent of 1-10%, stirring for 30 revolutions per minute, and stirring for 10 minutes; the component D comprises ceramide and phytosphingosine;
(5) Mixing 0.5-0.8% of p-hydroxyacetophenone and 0.50-2% of 1, 2-hexanediol by mass percent, heating to 55 ℃, and stirring until the mixture is transparent for later use;
(6) Cooling to 45 deg.C, adding 1-10 wt% of component F, 0.5-0.8 wt% of pre-dissolved p-hydroxyacetophenone, 0.5-2 wt% of 1, 2-hexanediol, and stirring; the component F comprises Scutellariae radix flower/leaf/stem extract, glycerol, water, and citric acid;
(7) When the temperature is reduced to 38 ℃, discharging and storing after the temperature is qualified through inspection.
8. The method of claim 8, wherein: in the step (2), the fatty acid is one or more of linolenic acid, linoleic acid and oleic acid, and the sterol is one or more of cholesterol, ergosterol and phytosterol; in the step (4), the ceramide is one or more of ceramide 1, ceramide 3, ceramide 6 and ceramide-like.
9. A BMR biomimetic repair co-delivery system for co-delivery of an active ingredient with efficacy, significantly enhancing the bioavailability of the active ingredient, and repairing damaged barriers.
CN202211488399.3A 2022-11-25 2022-11-25 BMR bionic repair co-delivery system and preparation method and application thereof Pending CN115737502A (en)

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