CN116036046A - Solid lipid nanoparticle containing schisandra lignan compound, and preparation method and application thereof - Google Patents

Abstract

The invention provides solid lipid nano particles containing schisandra lignan compounds, and a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The preparation method of the solid lipid nanoparticle provided by the invention comprises the following steps: (1) Mixing the schisandra lignan compound and a lipid carrier to obtain an oil phase; (2) adding an emulsifier into water to obtain a water phase; (3) Dropwise adding the oil phase into the water phase, and stirring and ultrasonic treatment to obtain colostrum; (4) Homogenizing the colostrum to obtain the solid lipid nanoparticle containing the schisandra lignans. The solid lipid nanoparticle containing the schisandra lignan compound has higher drug encapsulation efficiency and drug effect, can effectively prevent and treat obesity, controls the weight increase of obese people, changes the biochemical value of serum and the fat index, and provides a new treatment way for obese people.

Description

A kind of solid lipid nanoparticle containing schisandra lignans and its preparation method and application

technical field

The invention relates to the technical field of pharmaceutical preparations, in particular to a solid lipid nanoparticle containing schisandra lignan compounds, a preparation method and application thereof.

Background technique

Obesity refers to a certain degree of obvious overweight and thick fat layer, which is a state caused by excessive accumulation of body fat, especially triglycerides. Excessive body fat accumulation due to excessive food intake or changes in body metabolism results in excessive weight gain and causes human pathology, physiological changes or latency. Because obesity can lead to metabolic disorders in the human body, metabolic syndrome will appear, resulting in hyperlipidemia. Obesity will lead to fat accumulation in the human body, abnormal lipid metabolism, and finally lead to increased blood lipids, resulting in arteriosclerosis and plaque formation in blood vessels Obesity can lead to elevated blood sugar, leading to diabetes, and obesity is also an important incentive and risk factor for hypertension; obesity is also an important risk factor for coronary heart disease and vascular disease, so obesity can bring a series of diseases related to blood vessels; It leads to bone and joint abnormalities, especially the compression of knee joints, ankle joints, and lumbar joints, leading to premature degeneration of weight-bearing joints. Many elderly obese patients will be accompanied by knee arthritis, ankle joint and lumbar spine lesions. Weight loss is very important for these people. Obesity will also lead to abnormal secretion of hormones, resulting in irregular menstruation in some patients and irregular menstruation in some men. Fertility, female infertility, etc. At present, the common weight loss methods are: enema weight loss method, osmotic pressure weight loss method, sauna weight loss method, milk powder weight loss method, rope skipping weight loss method, Pu'er tea weight loss method, etc.

The genus Schisandra belongs to the Schisandra family. The plants of the genus Schisandra have the functions of astringent and astringent, nourishing qi and promoting body fluid, nourishing the kidney and calming the heart, etc. It mainly contains chemical components such as lignans, triterpenes, polysaccharides and volatile oils. Treatment of diseases such as hepatitis, liver and kidney transplants, Alzheimer's disease and insomnia. Modern studies have shown that lignans in Schisandra genus are the main active ingredients of this genus, and have pharmacological effects such as liver protection, anti-tumor, anti-virus, anti-oxidation and neuroprotection. At present, there are as many as 200 kinds of lignans isolated from plants of the genus Schisandra, but most of the lignans are hydrophobic and have low bioavailability. They are wasteful because they cannot be absorbed and excreted, resulting in Application is limited.

Solid Lipid Nanoparticles (SLN) is a general term for new nanoparticle preparations under research and development in recent years. This new drug delivery carrier uses non-biologically toxic lipids as a matrix and has the physical stability of nanoparticles. High, controllable drug release and good targeting, and has the advantages of low toxicity and large-scale production of liposomes and emulsions. It is a new type of drug delivery carrier with great development prospects. It has the advantages of good biocompatibility, controlled drug release, avoiding drug degradation and leakage, and easy large-scale industrial production. The use of SLNs can effectively improve the bioavailability of Schisandra lignans. However, in this field, there is no relevant research on solid lipid nanoparticles of schisandra lignans.

Contents of the invention

The object of the present invention is to provide a solid lipid nanoparticle containing schisandra lignans and its preparation method and application. The solid lipid nanoparticles containing schisandra lignan compounds prepared by the present invention have higher drug encapsulation efficiency and drug efficacy, can effectively prevent and treat the occurrence of obesity, control the weight increase of obese people, and the changes of serum biochemical values and fat index , to provide a new therapeutic approach for obese people.

In order to achieve the above object, the present invention provides the following technical solutions:

The invention provides a method for preparing solid lipid nanoparticles comprising schisandra lignans, comprising the following steps:

(1) mixing Schizandra lignans with a lipid carrier to obtain an oil phase;

(2) adding the emulsifier into water to obtain an aqueous phase;

(3) adding the oil phase dropwise into the water phase, stirring and sonicating to obtain colostrum;

(4) After the colostrum is homogenized, the solid lipid nanoparticles containing schisandra lignans are obtained.

Preferably, the schisandra lignans include gomisin B, gomisin D, gomisin E, gomisin G, gomisin H, gomisin J, gomisin N, schisandrin, Any one or more of schisandrin and d-epigabaxin.

Preferably, the lipid carrier includes any one or more of stearic acid, glyceryl monostearate, palmitic acid and glyceryl trimyristate.

Preferably, the emulsifier includes any one or more of Tween 40, Tween 80 and sodium cholate.

Preferably, the mass ratio of the Schizandra lignans to the lipid carrier is 1: (35-50); the mass ratio of the lipid carrier to the emulsifier is 10: (1-4) ; The mass volume ratio of the emulsifier to the water is (1-6) mg: (50-100) mL.

Preferably, the mixing temperature is 70-85°C; the temperature of the water is the same as that of the oil phase.

Preferably, the rotation speed of the stirring is 2000-3200rpm, the stirring time is 0.5-1h; the ultrasonication time is 2-6min, and the ultrasonic frequency is 3s with an interval of 2s.

Preferably, the homogenization pressure is 150-180 MPa, the homogenization time is 2-4 minutes, and the homogenization times are 4-5 times.

The present invention also provides a solid lipid nanoparticle obtained by the above preparation method.

The present invention also provides an application of the above-mentioned solid lipid nanoparticles in the preparation of medicines for preventing and treating obesity.

The invention provides a solid lipid nanoparticle containing schisandra lignan compounds, a preparation method and application thereof. In the present invention, the schisandra lignans are wrapped into solid lipid nanoparticles (SLN), and the emulsification of the oil phase and the water phase is more uniform by adjusting the ratio of the drug to the carrier, technical parameters, etc., thereby improving the schisandra lignans. The high encapsulation rate makes it have good stability and improves the medicinal effect of schisandra lignans. The solid lipid nanoparticles containing schisandra lignans provided by the present invention can effectively prevent and treat obesity, control or reduce body weight and fat accumulation, control changes in serum biochemical values and fat index, and provide a new treatment approach for obese people .

Detailed ways

The technical solutions provided by the present invention will be described in detail below in conjunction with the examples, but they should not be interpreted as limiting the protection scope of the present invention.

Example 1

Taking gomisin B as an example, the present invention provides a solid lipid nanoparticle containing gomisin B, the specific preparation process is as follows:

Mix 2mg of gomisin B and 80mg of glyceryl monostearate at 85°C to a molten state to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain a water phase; Slowly add it dropwise into the water phase, continuously stir at 3000rpm for 45min, and then use a sonicator to sonicate for 4min at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized under a pressure of 160 MPa for 3 minutes, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Example 2

Taking gomisin B as an example, the present invention provides a solid lipid nanoparticle containing gomisin B, the specific preparation process is as follows:

Mix 2mg of gomisin B and 70mg of stearic acid at 80°C until it melts to obtain an oil phase; add 28mg of Tween 40 into 350ml of water at 80°C and dissolve to obtain a water phase; slowly add the oil phase to In the water phase, the mixture was continuously stirred at 2000 rpm for 60 minutes, and then ultrasonicated at a frequency of 3 s and 2 s intermittently for 2 min with a sonicator to obtain colostrum. The colostrum was homogenized for 2 minutes under a pressure of 150 MPa, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Example 3

Taking gomisin B as an example, the present invention provides a solid lipid nanoparticle containing gomisin B, the specific preparation process is as follows:

Mix 2mg of gomisin B and 100mg of palmitic acid at 70°C until it melts to obtain an oil phase; add 10mg of sodium cholate to 200ml of water at 70°C and dissolve to obtain a water phase; slowly drop the oil phase into water Stir continuously at 3200rpm for 30min in the phase, and then ultrasonicate for 6min with a sonicator at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized for 4 minutes under a pressure of 180 MPa, and homogenized 5 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Comparative example 1

Mix 2mg of gomisin B and 60mg of glyceryl monostearate at 85°C to a molten state to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain a water phase; Slowly add it dropwise into the water phase, continuously stir at 3000rpm for 45min, and then use a sonicator to sonicate for 4min at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized under a pressure of 160 MPa for 3 minutes, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Comparative example 2

Mix 2mg of gomisin B and 110mg of glyceryl monostearate at 85°C to a molten state to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain a water phase; Slowly add it dropwise into the water phase, continuously stir at 3000rpm for 45min, and then use a sonicator to sonicate for 4min at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized under a pressure of 160 MPa for 3 minutes, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Comparative example 3

Mix 2mg of gomisin B and 80mg of glyceryl monostearate at 85°C to a molten state to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain a water phase; Slowly add it dropwise into the water phase, continuously stir at 500 rpm for 45 min, and then use a sonicator to sonicate for 4 min at a frequency of 3 s and 2 s intermittently to obtain colostrum. The colostrum was homogenized under a pressure of 160 MPa for 3 minutes, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Comparative example 4

Mix 2mg of gomisin B and 80mg of glyceryl monostearate at 85°C until it melts to obtain an oil phase; add 24g of Tween 80 into 300ml of water at 85°C and dissolve to obtain a water phase; Slowly add it dropwise into the water phase, continuously stir at 5000rpm for 45min, and then use a sonicator to sonicate for 4min at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized under a pressure of 160 MPa for 3 minutes, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Comparative example 5

Mix 2mg of gomisin B and 80mg of glyceryl monostearate at 85°C to a molten state to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain a water phase; Slowly add it dropwise into the water phase, continuously stir at 3000rpm for 45min, and then use a sonicator to sonicate for 10min at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized under a pressure of 160 MPa for 3 minutes, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Comparative example 6

Mix 2mg of gomisin B and 80mg of glyceryl monostearate at 85°C to a molten state to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain a water phase; Slowly add it dropwise into the water phase, continuously stir at 3000rpm for 45min, and then use a sonicator to sonicate for 4min at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized for 3 minutes under a pressure of 160 MPa, and homogenized twice in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing gomisin B.

Test example 1

The drug encapsulation efficiency of the solid lipid nanoparticles prepared in Examples 1-3 and Comparative Examples 1-6 was determined, and the specific process was as follows:

1. Detect the average particle diameter of the solid lipid nanoparticles prepared in Examples 1-3 and Comparative Examples 1-6 (measured by Nano-ZS nano laser particle size analyzer), and the test results are shown in Table 1.

The average particle diameter of the solid lipid nanoparticles prepared by table 1 embodiment 1～3 and comparative examples 1～6

sample average particle size Example 1 261nm Example 2 298nm Example 3 254nm Comparative example 1 315nm Comparative example 2 306nm Comparative example 3 254nm Comparative example 4 287nm Comparative example 5 312nm Comparative example 6 281nm

2. The drug encapsulation efficiency of the solid lipid nanoparticles prepared in Examples 1-3 and Comparative Examples 1-6 was detected by HPLC method, and the detection results are shown in Table 2.

Table 2 The drug encapsulation efficiency of the solid lipid nanoparticles prepared by Examples 1 to 3 and Comparative Examples 1 to 6

As can be seen from Table 2, the drug encapsulation efficiency of Comparative Examples 1 to 6 is lower than that of Examples 1 to 3, indicating that adjusting parameters such as the ratio of drug to lipid carrier, stirring speed, ultrasonic time, homogenization times, etc. It has a great influence on the encapsulation efficiency of Schisandra lignans.

Example 4

According to the preparation method of Example 1, taking schisandrin as an example, the present invention provides a solid lipid nanoparticle containing schisandrin, the specific preparation process is as follows:

Mix 2mg of schisandrin and 80mg of glyceryl monostearate at 85°C until it melts to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain a water phase; slowly drop the oil phase Add it into the water phase, continue to stir at 3000rpm for 45min, and then use a sonicator to sonicate for 4min at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized under a pressure of 160 MPa for 3 minutes, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing schisandrin.

Example 5

According to the preparation method of Example 1, taking schisandrin as an example, the present invention provides a solid lipid nanoparticle containing schisandrin, the specific preparation process is as follows:

Mix 2mg of schisandrin and 80mg of glyceryl monostearate at 85°C to a molten state to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain a water phase; slowly dissolve the oil phase Add it dropwise into the water phase, continue to stir at 3000rpm for 45min, and then use a sonicator to sonicate for 4min at a frequency of 3s and 2s intermittently to obtain colostrum. The colostrum was homogenized for 3 minutes under a pressure of 160 MPa, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing schisandrin.

Example 6

According to the preparation method of Example 1, taking d-epigabaxin as an example, the invention provides a solid lipid nanoparticle comprising d-epigabaxin, the specific preparation process is as follows:

Mix 2mg of d-epigabaxin and 80mg of glyceryl monostearate at 85°C to a molten state to obtain an oil phase; add 24mg of Tween 80 to 300ml of water at 85°C and dissolve to obtain an aqueous phase; The oil phase was slowly added dropwise into the water phase, continuously stirred at 3000 rpm for 45 min, and then ultrasonicated for 4 min at a frequency of 3 s and 2 s intermittently with a sonicator to obtain colostrum. The colostrum was homogenized for 3 minutes under a pressure of 160 MPa, and homogenized 4 times in total. After cooling at room temperature, the precipitate was collected by centrifugation at 1200 rpm for 5 minutes to obtain solid lipid nanoparticles containing d-epigabaxin.

Test example 2

The preventive effect of the solid lipid nanoparticles (SLN) prepared in Examples 1, 4-6 and Comparative Examples 1-6 on obesity induced by high-fat diet was verified. The specific process is as follows:

Select 60 C57BL/6J mice (body weight 22 ± 2g), and randomly divide them into 12 groups, which are respectively blank group, control group, embodiment 1 group, embodiment 4 group, embodiment 5 group, embodiment 6 group, Comparative Example 1 Group, Comparative Example 2 Group, Comparative Example 3 Group, Comparative Example 4 Group, Comparative Example 5 Group, Comparative Example 6 Group.

Except the blank group, all the other groups of mice were fed high-fat feed (common feed 78.8%, cholesterol 1%, ox bile salt 0.2%, egg yolk powder 10%, lard 10%), wherein, embodiment 1, 4, Groups 5 and 6, Comparative Example 1-6 Groups of mice were given the corresponding solid lipid nanoparticle emulsion at a dose of 2 mg (SLN)/10 g (body weight) per day while feeding the feed for 4 consecutive weeks.

1. Record the average body weight of mice in each group before the experiment, 1 week of the experiment, 2 weeks of the experiment, 3 weeks of the experiment, and 4 weeks of the experiment. The results are shown in Table 3.

Table 3 Changes in body weight of mice in each group

As can be seen from Table 3, compared with the blank group, after feeding high-fat feed, the body weight of the mice in the control group increased significantly, and the body weight of the mice in the drug groups increased slowly compared with the control group. The body weight of the mice was lower than that of the control group. It was shown that the use of solid lipid nanoparticles containing schisandra lignans can effectively control the increase in body weight of mice induced by high-fat diet. Among them, the solid lipid nanoparticles of Examples 1, 4, 5, and 6 have a better control effect on the body weight of mice, and the solid lipid nanoparticles of Comparative Examples 1 to 6 have the second best control effect on the body weight of mice; and , the weight gain of mice in the control group 4 was similar to that of the control group mice in the 1st week of the experiment, and the body weight began to increase slowly in the 2nd week of the experiment, indicating that the schisandra lignans in the solid lipid nanoparticles of the comparative example 4 Compounds are slow to act.

2. After the experiment, blood was collected from the eyeballs of the mice, centrifuged after standing for 10 minutes, and the serum was separated to detect the serum biochemical values (TC, TG, LDL-C, HDL-C) of the mice in each group. The test results are shown in Table 4.

Table 4 Serum biochemical values of mice in each group

As can be seen from Table 4, compared with the blank group, after feeding the high-fat diet, the contents of TC, TG, and LDL-C in the serum of the mice in the control group were significantly increased, and the mice in each group of medication were lower than those in the control group; Compared with the control group, after feeding the high-fat diet, the HDL-C content in the serum of the mice in the control group was significantly reduced, and the levels of the mice in the medication groups were higher than those in the control group. It is shown that the use of solid lipid nanoparticles containing schisandra lignans can effectively control the changes in serum biochemical values of mice induced by high-fat diet. Among them, the solid lipid nanoparticles of Examples 1, 4, 5, and 6 have a better control effect on the serum biochemical values of mice, and the solid lipid nanoparticles of Comparative Examples 1 to 6 have a better control effect on the serum biochemical values of mice. The effect is second.

3. The mice in each group were killed, dissected, and the white fat around the mouse gonads, heart, and kidneys was peeled off, and the fat weight was measured. According to the formula of (fat index=fat weight/body weight*100%), the average fat of the mice in each group was calculated. index. The test results are shown in Table 5.

Table 5 Fat index of mice in each group

group fat index blank group 3.12% control group 7.34% Example 1 group 3.62% Embodiment 4 groups 4.52% Embodiment 5 groups 4.98% Embodiment 6 groups 4.13% Comparative example 1 group 6.11% Comparative example 2 groups 5.75% Comparative example 3 groups 6.23% Comparative example 4 groups 6.54% Comparative example 5 groups 5.87% Comparative example 6 groups 5.63%

It can be seen from Table 5 that compared with the blank group, the fat index of the mice in the control group was significantly increased after feeding the high-fat diet, and the mice in the medication groups were lower than those in the control group. It was shown that the use of solid lipid nanoparticles containing schisandra lignans can effectively control the accumulation of fat content in mice induced by high-fat diet. Among them, the solid lipid nanoparticles of Examples 1, 4, 5, and 6 have a better control effect on the accumulation of fat content in mice, and the solid lipid nanoparticles of Comparative Examples 1 to 6 have a better control effect on the accumulation of fat content in mice. The effect is second.

Test example 3

The therapeutic effect of the solid lipid nanoparticles (SLN) prepared in Examples 1, 4-6 and Comparative Examples 1-2 on the obesity mouse model induced by high-fat diet was verified. The specific process is as follows:

Select 60 C57BL/6J mice (body weight 22 ± 2g), and randomly divide them into 12 groups, which are respectively blank group, control group, embodiment 1 group, embodiment 4 group, embodiment 5 group, embodiment 6 group, Comparative Example 1 Group, Comparative Example 2 Group, Comparative Example 3 Group, Comparative Example 4 Group, Comparative Example 5 Group, Comparative Example 6 Group.

Except for the blank group, mice in other groups were fed with high-fat diet (common diet 78.8%, cholesterol 1%, ox bile salt 0.2%, egg yolk powder 10%, lard 10%) for 4 consecutive weeks, and the obese mice were constructed. mouse model. Blank group and control group are fed normal saline according to the dosage of 2ml/10g every day, embodiment 1,4,5,6 groups, the obese mice of comparative example 1～6 groups are according to the dosage of 2mg (SLN)/10g (body weight) every day , given the corresponding solid lipid nanoparticle emulsion for 2 consecutive weeks.

1. Record the average body weight of mice in each group before and after administration. The results are shown in Table 6.

Table 6 Changes in body weight of mice in each group

group Before medication (g) After medication (g) blank group 24.98 25.03 control group 35.62 36.44 Example 1 group 35.69 26.54 Embodiment 4 groups 35.12 27.45 Embodiment 5 groups 35.49 26.97 Embodiment 6 groups 36.24 28.11 Comparative example 1 group 34.95 30.44 Comparative example 2 groups 36.51 31.07 Comparative example 3 groups 36.84 31.51 Comparative example 4 groups 36.95 31.54 Comparative example 5 groups 37.10 32.25 Comparative example 6 groups 35.64 30.67

It can be seen from Table 6 that compared with the blank group and the control group, the body weight of the obese mice in each medication group decreased. It is shown that the use of solid lipid nanoparticles containing schisandra lignans can effectively reduce the body weight of obese mice and achieve weight loss. Among them, the weight loss effect of the solid lipid nanoparticles in the groups of Examples 1, 4, 5 and 6 is better, and the weight loss effect of the solid lipid nanoparticles in the groups of Comparative Examples 1 to 6 is second.

2. The mice in each group were killed, dissected, and the white fat around the mouse gonads, heart, and kidneys was peeled off, and the fat weight was measured. According to the formula of (fat index=fat weight/body weight*100%), the average fat of the mice in each group was calculated index. The test results are shown in Table 7.

Table 7 Fat index of mice in each group before and after treatment

group Before medication after medication blank group 3.51% 3.64% control group 6.94% 7.23% Example 1 group 6.96% 4.32% Embodiment 4 groups 7.36% 4.58% Embodiment 5 groups 7.35% 4.69% Embodiment 6 groups 7.26% 4.55% Comparative example 1 group 6.57% 5.98% Comparative example 2 groups 6.99% 6.01% Comparative example 3 groups 7.23% 6.24% Comparative example 4 groups 7.12% 6.10% Comparative example 5 groups 7.36% 6.85% Comparative example 6 groups 6.75% 5.87%

It can be seen from Table 7 that compared with the blank group and the control group, the fat index of the obese mice in each medication group decreased. It is shown that the use of solid lipid nanoparticles containing schisandra lignans can effectively reduce the fat content of obese mice and achieve the effect of reducing fat. Among them, the fat-reducing effects of the solid lipid nanoparticles in the groups of Examples 1, 4, 5, and 6 are better, and the fat-reducing effects of the solid lipid nanoparticles in the groups of Comparative Examples 1-6 are second.

The above is only a preferred embodiment of the present invention, it should be pointed out that, for those of ordinary skill in the art, without departing from the principle of the present invention, some improvements and modifications can also be made, and these improvements and modifications can also be made. It should be regarded as the protection scope of the present invention.

Claims (10)

1. A method for preparing solid lipid nanoparticles containing schisandra lignan compounds, which is characterized by comprising the following steps:

(1) Mixing the schisandra lignan compound and a lipid carrier to obtain an oil phase;

(2) Adding an emulsifier into water to obtain a water phase;

(3) Dropwise adding the oil phase into the water phase, and stirring and ultrasonic treatment to obtain colostrum;

(4) Homogenizing the colostrum to obtain the solid lipid nanoparticle containing the schisandra lignans.

2. The preparation method according to claim 1, wherein the schisandrin lignan compound comprises any one or more of gomisin B, gomisin D, gomisin E, gomisin G, gomisin H, gomisin J, gomisin N, schizandrin, and D-epigabaxin.

3. The method of claim 2, wherein the lipid carrier comprises any one or more of stearic acid, glycerol monostearate, and palmitic acid.

4. The method according to claim 3, wherein the emulsifier comprises one or more of tween 40, tween 80 and sodium cholate.

5. The preparation method according to claim 4, wherein the mass ratio of the schisandra lignan compound to the lipid carrier is 1: (35-50); the mass ratio of the lipid carrier to the emulsifier is 10: (1-4); the mass volume ratio of the emulsifier to the water is (1-6) mg: (50-100) mL.

6. The method of claim 5, wherein the temperature of the mixing is 70-85 ℃; the temperature of the water is the same as the temperature of the oil phase.

7. The method according to claim 6, wherein the stirring speed is 2000-3200rpm and the stirring time is 0.5-1h; the ultrasonic time is 2-6min, and the ultrasonic frequency is 3s and intermittent 2s.

8. The method according to claim 7, wherein the homogenizing pressure is 150 to 180MPa, the homogenizing time is 2 to 4min, and the homogenizing times are 4 to 5 times.

9. A solid lipid nanoparticle obtained by the method of any one of claims 1 to 8.

10. Use of the solid lipid nanoparticle of claim 9 in the preparation of a medicament for preventing and treating obesity.