CN110876693A

CN110876693A - Natural skin repair emulsion for psoriasis and preparation method thereof

Info

Publication number: CN110876693A
Application number: CN201911249080.3A
Authority: CN
Inventors: 单士军
Original assignee: Nanjing Yiliao Biotechnology Co Ltd
Current assignee: Nanjing Yiliao Biotechnology Co Ltd
Priority date: 2019-12-09
Filing date: 2019-12-09
Publication date: 2020-03-13

Abstract

The invention discloses a natural skin repair emulsion for psoriasis, which consists of the following raw materials: caprylic/capric triglyceride, cetostearyl alcohol, silicone oil, synthetic squalane, glyceryl stearate, glycerol, pearl barley oil and the balance of deionized water, wherein the emulsion is prepared from the following raw materials in proportion: 3-5% of caprylic/capric triglyceride, 3-5% of cetostearyl alcohol, 0.5-3% of silicone oil, 3-5% of synthetic squalane, 1-3.5% of glyceryl stearate, 4-8% of glycerol, 1.5-4.5% of coix seed oil and the balance of deionized water.

Description

Natural skin repair emulsion for psoriasis and preparation method thereof

Technical Field

The invention relates to the technical field of dermatosis treatment, in particular to natural skin repair emulsion for psoriasis and a preparation method thereof.

Background

Psoriasis, which is a common chronic easily-relapsed inflammatory skin disease with characteristic skin damage, is initially an inflammatory red papule, is about chestnut grains to mung bean in size, is gradually enlarged or fused into a brownish red plaque, is clear in boundary, has inflammatory halos around the periphery, is obviously infiltrated into a substrate, is covered with multiple layers of dry grey-white or silvery-white scales on the surface, slightly scrapes off the scales on the surface, gradually exposes a layer of pale red and shiny semi-transparent film, is called a film phenomenon, and then scrapes off the film, so that small bleeding points appear, is called a punctate bleeding phenomenon, and the white scales, the shiny films and the punctate bleeding are important characteristics for diagnosing psoriasis, and are called triad signs;

psoriasis is an upgraded version of atopic dermatitis, and the two have a lot of coincidence in pathogenesis and the like, the treatment of the psoriasis is mainly implemented by using external hormones at present, the long-term use of the hormones can cause a large number of side effects, such as skin capillary vessel expansion, skin atrophy and thinning, pigment change, hair aggravation, blood pressure, blood sugar and electrolyte disorder, local induction or aggravation infection, disease hormone resistance, relapse aggravation after drug withdrawal, erythroderma and other serious consequences, and the actual, safe and effective non-hormonal medicaments or skin repair products are not available in the market at present for controlling the disease.

Disclosure of Invention

The invention provides a natural skin repair emulsion for psoriasis and a preparation method thereof, which can effectively solve the problem that the prior market lacks a reliable, safe and effective non-hormone medicament or skin repair product for controlling the psoriasis.

In order to achieve the purpose, the invention provides the following technical scheme: a natural skin repair emulsion for psoriasis, the emulsion consisting of: caprylic/capric triglyceride, cetostearyl alcohol, silicone oil, synthetic squalane, glyceryl stearate, glycerol, Coicis semen oil, and the balance of deionized water.

According to the technical scheme, the emulsion is prepared from the following raw materials in proportion range: 3-5% of caprylic/capric triglyceride, 3-5% of cetostearyl alcohol, 0.5-3% of silicone oil, 3-5% of synthetic squalane, 1-3.5% of glyceryl stearate, 4-8% of glycerol, 1.5-4.5% of coix seed oil and the balance of deionized water.

According to the technical scheme, the emulsion is prepared from the following raw materials in parts by weight: caprylic/capric triglyceride 5%, cetostearyl alcohol 4%, silicone oil 2.2%, synthetic squalane 4%, glyceryl stearate 3%, glycerin 5%, coix seed oil 3.5%, deionized water 73.3%.

A preparation method of natural skin repair emulsion for psoriasis comprises the following steps:

a1, weighing 50.00g of crushed coix seeds, and putting into a filter paper cylinder;

a2, then putting into a Soxhlet extractor, adding 250ml of diethyl ether, and introducing condensed water;

a3, refluxing and extracting for 8 hours on a water bath at 45 ℃;

a4, and removing ether by rotary evaporator to obtain Coicis semen oil as oily mixture.

According to the technical scheme, the average yield of the coix seed oil is 4.86% after multiple parallel tests.

According to the technical scheme, the emulsion is prepared in the following way:

s1, putting the raw materials into a reaction kettle, heating to 85 ℃, and slowly stirring in the heating process until the solid of the mixture is completely melted;

s2, after melting, the contents in the reaction kettle are clear and transparent, and the oil phase and the water phase are layered clearly and then homogenized and emulsified by a homogenizer;

s3, stopping heating cold water after homogenizing, slowly cooling, and defoaming in a water bath;

s4, cleaning the storage tank, spraying alcohol, drying, irradiating under an ultraviolet lamp, and storing the emulsion for subsequent experiments.

According to the technical scheme, the homogenizing speed in the homogenizing emulsification of the homogenizer is 2200-3000rpm, and the homogenizing time is 3-6 min.

According to the technical scheme, the alcohol concentration in the step S4 is 75%, and the ultraviolet lamp irradiates for 15-30 minutes.

Compared with the prior art, the invention has the beneficial effects that: the emulsion has a scientific and reasonable structure, is safe and convenient to use, can effectively repair a damaged skin barrier of a mouse model, reduces the transdermal water loss of the mouse when the skin barrier is damaged by regulating the expression position and the change of the expression quantity of the aquaporin 3 of the skin cells of the mouse, preserves moisture and locks water, inhibits the immune inflammatory reaction of the skin by inhibiting the overexpression of a TOLL-like receptor 2/4 of the skin cells of the mouse, plays a role in treating psoriasis, can effectively relieve the severity of the rash of a psoriasis patient, reduces the PASI score, relieves pruritus, improves the clinical manifestations of pachynsis, desquamation and the like of the skin, and provides a new method for the clinical skin repair and protection of the psoriasis.

Drawings

The accompanying drawings, which are included to provide a further understanding of the invention and are incorporated in and constitute a part of this specification, illustrate embodiments of the invention and together with the description serve to explain the principles of the invention and not to limit the invention. In the drawings:

FIG. 1 is a schematic view of the process for preparing Job's tears seed oil of the present invention;

FIG. 2 is a schematic of the emulsion preparation scheme of the present invention;

FIG. 3 is a schematic representation of the comparison of skin lesion expression and pathological expression in mice of the present invention;

FIG. 4 is a schematic representation of the changes in mouse skin aquaporin 3 and Toll-like receptor 2.4 expression at 28 days of treatment according to the invention;

FIG. 5 is a schematic representation of the degree of skin itching before and after treatment according to the invention;

FIG. 6 is a schematic representation of the degree of skin dryness before and after treatment according to the present invention;

FIG. 7 is a graphical representation of the PASI score before and after treatment according to the present invention;

FIG. 8 is a graph showing a comparison of the effect of the present invention on facial psoriasis patients before and after 2 and 3 weeks of treatment;

fig. 9 is a comparison of the effect of the facial psoriasis patients of the invention three weeks after treatment, with the patients taking a photograph of the comparison structure on a daily basis.

Detailed Description

The preferred embodiments of the present invention will be described in conjunction with the accompanying drawings, and it will be understood that they are described herein for the purpose of illustration and explanation and not limitation.

Example (b): as shown in fig. 1-2, the present invention provides a technical solution, a natural skin repair emulsion for psoriasis, which is composed of the following raw materials: caprylic/capric triglyceride, cetostearyl alcohol, silicone oil, synthetic squalane, glyceryl stearate, glycerol, Coicis semen oil, and the balance of deionized water.

a3, refluxing and extracting for 8 hours on a water bath at 45 ℃;

According to the technical scheme, the homogenizing speed in homogenizing and emulsifying of the homogenizer is 2500rpm, and the homogenizing time is 4 min.

According to the above technical solution, the alcohol concentration in the step S4 is 75%, and the irradiation time of the ultraviolet lamp is 20 minutes.

As shown in fig. 3: randomly dividing 40 SPF-grade female pure line BALB/c mice into a blank group (8 mice) and a model group (32 mice), wherein the model group adopts 2, 4-Dinitrochlorobenzene (DNCB), acetone and olive oil solution to construct a skin barrier damage mouse model, after the model is made, 8 mice in the blank group and 8 mice in the model group are killed immediately, and the other 24 mice in the model group are randomly divided into a model control group, a coix seed oil emulsion group and a matrix group 3;

the model control group is not treated, the back and ear of the coix seed oil group and the matrix group are respectively coated with the coix seed oil and the matrix for 1 time every day for 28 days, and the change of skin lesions is observed by naked eyes every day; the thickness meter detects the skin damage thickness of the left ear of the mouse before the model building, when the model building is completed and 12 hours after the last drug administration; killing 3 groups of mice 12 hours after the last administration, taking blood from eyeballs, separating serum, and taking a tissue sample at a back skin lesion;

carrying out HE staining and toluidine blue staining after the tissue is sliced to observe the infiltration condition of inflammatory cells of the skin lesion; detecting the expression changes of aquaporin 3(AQP3) and Toll-like receptors (TLR)2 and 4 by an immunohistochemical method; ELISA method for detecting serum IgE, interleukin 4(IL-4) and interferon gamma (IFN-gamma) level.

As shown in fig. 4, after 28 days of treatment, the skin lesions of mice with coix seed oil improved, and the clinical symptom score (1.50 ± 0.58) was lower than that of the model control group (2.50 ± 0.58) P < 0.05);

immunohistochemistry shows that the expression levels of coix seed oil aquaporin 3(AQP3), TLR2 and TLR4 are lower than those of a model control group, and the expression of AQP3 stratum spinosum is reduced;

IL-4 level in blood of mouse with coix seed oil is lower than that of model control group, IFN-gamma level is higher than that of model control group, and the difference has statistical significance (P <0.05)

The external coix seed oil has an obvious treatment effect on skin damage of a mouse model with skin barrier damage, the skin inflammation is relieved by adjusting the levels of IL-4 and IFN-gamma in serum, transdermal water loss and moisture retention of the mouse with the skin barrier damage are reduced by adjusting the expression position and the expression quantity change of aquaporin 3 in skin cells of the mouse, the important effect on improving dryness and desquamation of psoriasis is achieved, the immune inflammatory response of the skin is inhibited by inhibiting the overexpression of TOLL-like receptor 2/4 in the skin cells of the mouse, and the important effect is played in the pathogenesis of the psoriasis.

As shown in FIGS. 5 to 9, chronic hypertrophic dry skin lesions of psoriasis patients were selected and observed for clinical efficacy and safety, the number of clinical trial cases was designed to be 20, a typical skin lesion was selected as a target skin lesion for each patient, subjects cleaned the target site and then administered externally 2 times a day for 3 weeks, and the repeated diagnosis was recorded and photographed 1, 2, and 3 weeks after the treatment, while observing and recording side effects in the trial.

Firstly, referring to PASI (psoriasis area and severity index) standard, selecting typical part skin damage, calculating severity score, and combining pruritus and skin dryness severity to judge curative effect.

We selected typical skin lesion sites in patients, each site scored according to the following 3 clinical characteristics of skin lesion: erythema (erythema, E): red or dark red inflammatory plaques, fading of pressure;

infiltration (I): the skin damage has the tendency of spreading and spreading to the periphery, the boundary is fuzzy, and the pressure has the substantial feeling;

desquamation/scaling (D): the exfoliated epidermal cells are exfoliated;

each feature was evaluated on a 0-4 point scale: 0 ═ none; 1 is mild; 2 is moderate; 3-severe; 4-very severe.

Plaque thickening degree I: 0-skin lesions level with normal skin;

1-skin lesions are slightly elevated above normal skin surface;

2-moderate elevation, the edge of the plaque is round or slope type;

3-the skin is damaged and thickened and the bulge is obvious;

4-the skin lesions were highly thickened and the ridges were very pronounced.

Erythema E: 0-no erythema visible; 1-is light red; 2-red; 3-deep red; 4-extremely deep red.

Scale D: 0-no visible scale on the surface; 1-scale is covered on the surface of part of the skin damage, and the fine scale is taken as the main part;

2-most of the skin damage surfaces are completely or incompletely covered with scales which are flaky;

3-almost all the surface of the skin damage is covered with scale which is thicker and layered;

4-all the damaged surfaces are covered with scales, and the scales are thick and layered.

Skin lesion area scoring: taking 5 as a base point, 99-75% of disappearance is 4, 74-50% of disappearance is 3, 49-25% of disappearance is 2, 24-1% of disappearance is 1, and all the disappearance is 0.

PASI specific scoring formula: PASI score (E + I + D) × skin lesion area score

Recording PASI scores before and after treatment according to the psoriasis skin damage area and severity index (PASI) score standard, and judging the curative effect according to the PASI score reduction rate;

the reduction rate of PASI score was two (pre-treatment PASI score-post-treatment PASI score)/x 100% pre-treatment PASI score.

Healing, the reduction rate of PASI score is more than 90%;

the effect is obvious, the reduction rate of the PASI score is 60 percent to 89 percent;

effective, the reduction rate of PASI score is 20% -59%;

no effect, PASI score reduction rate < 20%.

The total effective rate (number of cure cases + number of obvious cases + number of effective cases)/, the total number of cases is 100%.

Second, evaluation of itching

Scoring the pruritus according to the severity degree of the pruritus by 0-3, wherein 0 is no pruritus, 1 is mild pruritus, scratching is not needed, and rest sleep is not affected; 2, scratching is needed for moderate pruritus, and rest and sleep are not affected; when the patient feels severe itching, scratching is required, which affects rest and sleep.

Third, dry skin score

Scoring the skin for severity of dryness by 0-3 points, 0 points being smooth and no signs of dryness; 1, the skin is slightly dry and is scattered with fine scales; 2, the skin is moderately dry, scales are widely distributed on the skin, the edges of the scales are tilted, and the surface of the skin is whitish; with 3 points being severe dryness, the skin has a wide distribution of scales, separated from the skin, with chapped skin.

Subjects were scored 3 times 0, 2 and 4 weeks before the start of the trial, with analysis of variance with one repeat measure of quantitative data for each score before and after treatment, and SAS9.2 for statistical analysis software.

Data descriptions are expressed in x ± s, statistical analysis is performed using analysis of variance with repeated measures, significance level is 0.05, and statistical analysis software is performed using SAS 9.4.

Fourthly, the result

(I) grading change of skin pruritus degree before and after treatment

Skin itch degree score changes before and after treatment:

time of day

N

Mean

Min

Max

F

P

0 week

20

2.2±0.8

0.5

3.0

35.5

<0.0001

1 week

20

1.3±0.5

0.5

2.0

2 weeks

20

0.9±0.6

0.0

2.0

Time of day

N

Mean

Min

Max

F

P

The grading difference of the skin pruritus degrees at different time points has statistical significance (F is 35.6P is less than 0.0001), and the difference between the time points is found to have statistical significance by comparing two times;

the natural repair emulsion can obviously relieve the pruritus of chronic hypertrophic dry skin lesions of psoriasis patients.

Skin dryness score changes before and after treatment:

time of day	N	Mean	Min	Max	F	P
							0 week	20	2.2±0.8	0.5	3.0	44.2	<0.0001
1 week	20	1.4±0.8	0.0	2.5
							2 weeks	20	1.0±0.8	0.0	2.5
3 weeks	20	0.8±0.7	0.0	2.0

The difference in dryness scores at different time points was statistically significant (F44.2P < 0.0001);

the difference between the time points is statistically significant, and the natural repair emulsion can remarkably relieve the dryness of chronic hypertrophic dry skin lesions of psoriasis patients.

PASI score changes before and after treatment:

time of day	N	Mean	Min	Max	F	P
							0 week	20	7.4±2.7	3.0	11.5	81.9	<0.0001
1 week	20	4.7±2.0	1.5	8.0
							2 weeks	20	3.1±1.4	1.0	6.0

Finally, it should be noted that: although the present invention has been described in detail with reference to the foregoing embodiments, it will be apparent to those skilled in the art that changes may be made in the embodiments and/or equivalents thereof without departing from the spirit and scope of the invention. Any modification, equivalent replacement, or improvement made within the spirit and principle of the present invention should be included in the protection scope of the present invention.

Claims

1. A natural skin repair emulsion for psoriasis characterized by: the emulsion consists of the following raw materials: caprylic/capric triglyceride, cetostearyl alcohol, silicone oil, synthetic squalane, glyceryl stearate, glycerol, Coicis semen oil, and the balance of deionized water.

2. The natural skin repair emulsion for psoriasis according to claim 1, which consists of the following raw materials in proportion range: 3-5% of caprylic/capric triglyceride, 3-5% of cetostearyl alcohol, 0.5-3% of silicone oil, 3-5% of synthetic squalane, 1-3.5% of glyceryl stearate, 4-8% of glycerol, 1.5-4.5% of coix seed oil and the balance of deionized water.

3. The natural skin repair emulsion for psoriasis according to claim 1, which is prepared from the following raw materials in parts by weight: caprylic/capric triglyceride 5%, cetostearyl alcohol 4%, silicone oil 2.2%, synthetic squalane 4%, glyceryl stearate 3%, glycerin 5%, coix seed oil 3.5%, deionized water 73.3%.

4. A method for preparing a natural skin repair emulsion for psoriasis according to any of claims 1 to 3, wherein the Job's tears oil is prepared by:

a3, refluxing and extracting for 8 hours on a water bath at 45 ℃;

5. The method of claim 4, wherein the average yield of the Job's tears oil after multiple parallel tests is 4.86%.

6. The method of claim 4, wherein the natural skin rejuvenating emulsion is prepared by:

7. The method for preparing a natural skin repair emulsion for psoriasis as claimed in claim 6, wherein the homogenizing speed in the homogenizing and emulsifying by the homogenizer is 2200-3000rpm, and the homogenizing time is 3-6 min.

8. The method of claim 6, wherein the alcohol concentration of step S4 is 75%, and the UV light irradiation is 15-30 min.