Use of glycyrrhizin in the preparation of a medicament for the treatment of acne, and a medicament for the treatment of acne and a method of preparation thereof

By preparing LC/HP-β-CD/CS/β-GP hydrogel loaded with glycyrrhizin, the problems of toxicity and drug resistance in antibiotic treatment of acne were solved, and the effective loading and controlled release of glycyrrhizin were achieved, improving the safety and flexibility of acne treatment.

CN118903107BActive Publication Date: 2025-12-19BEIJING UNIV OF CHEM TECH
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Patent Information

Application Number
CN202410920926.6
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-07-10
Publication Date
2025-12-19
Estimated Expiration
2044-07-10

AI Technical Summary

Technical Problem

Existing antibiotic treatments for acne have issues with skin toxicity and drug resistance, and traditional hydrogel drug delivery methods have significant limitations, making it difficult to effectively load glycyrrhizin for acne treatment.

Method used

A hydrogel was prepared by combining glycyrrhizin with a hydroxypropyl-β-cyclodextrin inclusion complex, chitosan, and sodium β-glycerophosphate. Glycyrrhizin was then loaded into the hydrogel using a physical encapsulation technique to form an LC/HP-β-CD/CS/β-GP antibacterial hydrogel.

Benefits of technology

It improves the water solubility and biocompatibility of glycyrrhizin, achieves localized controlled release, reduces systemic side effects, enhances the safety and specificity of treatment, and adapts to the treatment needs of different conditions and individuals.

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Abstract

The application belongs to the technical field of biological medicine, and provides application of glycyrrhizin in preparation of a medicine for treating acne, the medicine for treating acne and a preparation method thereof. The glycyrrhizin is prepared into a clathrate, and then is loaded on a hydrogel to prepare the medicine for treating acne. Compared with other natural compounds, the glycyrrhizin has the lowest MIC, which indicates that the glycyrrhizin has a significant bacteriostatic effect on propionibacterium acnes. The glycyrrhizin is prepared into a clathrate, so that the dispersibility of the glycyrrhizin in water is improved, and the bacteriostatic effect of the glycyrrhizin in water is exerted. The application first discloses the significant bacteriostatic effect of the glycyrrhizin on propionibacterium acnes. The glycyrrhizin is used as a bacteriostatic component to prepare the hydrogel, compared with a chemically-synthesized antibacterial component, the glycyrrhizin has better biocompatibility and safety, and provides a new idea for treating diseases caused by propionibacterium acnes.
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Description

TECHNICAL FIELD

[0001] The present application relates to the technical field of biological medicine, and particularly relates to application of licoricidin in preparation of a medicine for treating acne and the medicine for treating acne and a preparation method thereof. BACKGROUND

[0002] Acne is a chronic inflammatory disease of the pilosebaceous unit, and its pathogenesis is rooted in excessive sebum secretion of facial skin, which leads to the obstruction of pilosebaceous duct. This obstruction creates an ideal environment for microorganisms, such as anaerobic Propionibacterium acnes and Staphylococcus, to breed in the pilosebaceous unit, thereby triggering bacterial infection and inflammatory response, and finally presenting typical symptoms such as skin redness. Propionibacterium acnes is one of the main pathogenic bacteria of acne, which is a gram-positive anaerobic bacterium widely distributed in human skin, hair, oropharynx and gastrointestinal tract. The current treatment plan for acne vulgaris mainly focuses on the use of antibiotics and anti-inflammatory drugs for intervention. However, long-term use of antibiotics has a series of potential problems, one of which is the occurrence of skin toxicity, and at the same time, it can stimulate Propionibacterium acnes to develop antibiotic resistance. This resistance has gradually emerged in antibiotics such as clindamycin, erythromycin and tetracycline, which has attracted widespread attention in the medical community. Therefore, it is of great clinical significance and demand to explore natural antibacterial drugs to treat acne.

[0003] Licoricidin is one of the active components of medicinal plant Glycyrrhiza glabra, which is an isoflavan with two isopentenyl groups, with a molecular formula of C 26 H 32 O5 and a molecular weight of 424.53, and its structural formula is as follows:

[0004]

[0005] Studies have shown that licoricidin has a wide range of biological effects, including antibacterial, anticancer, antioxidant, anti-UVA-induced photoaging and other biological activities. In terms of antibacterial effect, licoricidin shows good antibacterial effect on a variety of bacteria. These bacteria include oral pathogenic bacteria such as Streptococcus mutans, Porphyromonas gingivalis and Enterococcus faecalis, as well as Helicobacter pylori related to gastric diseases. These results show the potential application value of licoricidin in antibacterial aspect. Among them, the antibacterial activity of licoricidin may be related to its multiple isopentenyl and hydroxyl groups. It is worth noting that although licoricidin shows significant antibacterial effect on many bacteria, its effect on Propionibacterium acnes has not been reported.

[0006] Hydrogels are known for their complex three-dimensional network structure and hydrophilicity, and have high water absorption and shape retention properties, which have become an indispensable tool in the biomedical field. Chitosan (CS) is a positively charged natural polysaccharide derived from chitin n-deacetylation, and has become a hot spot in medical research due to its low cytotoxicity, biodegradability and broad-spectrum antibacterial properties. Despite the limitations of high viscosity and low solubility, composite hydrogels modified by chemical modification and integrated with nanomaterials have shown good performance, opening up new ways for drug delivery, antibacterial intervention and packaging. Chitosan / β-glycerophosphate (CS / β-GP) based hydrogels have many advantages and can be used as effective drug carriers. They can quickly gel on the surface of the skin and exhibit excellent biocompatibility and biodegradability, making them an ideal platform for cell and drug delivery applications. Hydrogels are usually used to load insoluble drugs through methods such as chemical coupling, emulsification and electrostatic interaction. However, these methods have certain limitations. Physical encapsulation provides flexibility and good biocompatibility, while providing positive protection for drugs. The use of encapsulation technology can solve the dispersion problem of glycowithanine in hydrogels. Hydroxypropyl-β-cyclodextrin (HP-β-CD) has a unique cavity structure, with internal hydrophobicity and external hydrophilicity, so it can effectively encapsulate hydrophobic molecules. Functionally, HP-β-CD can enhance the water solubility of natural bioactive ingredients, thereby enhancing their biological activity. In addition, HP-β-CD has very low toxicity, which further enhances its applicability in the pharmaceutical industry. Therefore, the use of hydrogels loaded with inclusion compounds to deliver glycowithanine is a novel strategy for treating acne. Therefore, how to load glycowithanine on hydrogels and apply it to the preparation of acne drugs has become a problem that needs to be solved by those skilled in the art. SUMMARY

[0007] Therefore, the application provides the use of glycowithanine in the preparation of a drug for treating acne, and the drug for treating acne and a preparation method thereof, and aims to provide a new way for the preparation of a drug for treating acne.

[0008] In order to achieve the above purpose, the application adopts the following technical solutions:

[0009] The application provides the use of glycowithanine in the preparation of a drug for treating acne, and the drug for treating acne and a preparation method thereof, and aims to provide a new way for the preparation of a drug for treating acne.

[0010] The application provides a drug for treating acne, and the active ingredient of the drug for treating acne comprises glycowithanine.

[0011] The application also provides a preparation method of the above-mentioned drug for treating acne, comprising the following steps:

[0012] S1, mixing the glycyrrhizin solution and the hydroxypropyl-β-cyclodextrin solution to obtain a mixed solution, and sequentially stirring, rotary evaporation, centrifugation and freeze-drying the mixed solution to obtain the LC / HP-β-CD inclusion compound;

[0013] S2, mixing the chitosan solution, the β-glycerophosphate sodium solution and the LC / HP-β-CD inclusion compound to obtain a sol, and inducing sol-gel transition of the sol to obtain the medicine for treating acne.

[0014] Further, in the step S1, the concentration of the glycyrrhizin solution is 30-120 μg / mL; and the concentration of the hydroxypropyl-β-cyclodextrin solution is 300-1200 μg / mL.

[0015] Further, in the step S1, the volume ratio of the glycyrrhizin solution to the hydroxypropyl-β-cyclodextrin solution is 1-3:1.

[0016] Further, in the step S1, the stirring temperature is 20-50℃, the stirring time is 2-5 h, and the stirring speed is 300-800 rpm.

[0017] Further, in the step S2, the concentration of the LC / HP-β-CD inclusion compound in the sol is 0.3-1.2 mg / mL.

[0018] Further, in the step S2, the concentration of the chitosan solution is 10-50 mg / mL; and the concentration of the β-glycerophosphate sodium solution is 40-60 mg / mL.

[0019] Further, in the step S2, the volume ratio of the chitosan solution to the β-glycerophosphate sodium solution and the LC / HP-β-CD inclusion compound solution is 6-8:2-4.

[0020] Further, in the step S2, the temperature for inducing the sol-gel transition is 30-40℃, and the time for inducing the sol-gel transition is 1-5 min.

[0021] According to the above technical solution, compared with the prior art, the present application has the following advantages:

[0022] 1. The present application first uses glycyrrhizin as an antibacterial component to prepare a hydrogel, which has good biocompatibility and safety compared with chemically synthesized antibacterial components, and provides a new idea for treating diseases caused by Propionibacterium acnes.

[0023] 2. The glycyrrhizin inclusion compound provided by the present application uses the inclusion technology, and selects hydroxypropyl-β-cyclodextrin with high biocompatibility as the wrapping material, thereby solving the problem of low solubility of glycyrrhizin in water.

[0024] 3. Compared with oral or injectable drug administration, the antibacterial hydrogel loaded with glycyrrhizin inclusion complex provided by this invention can reduce the distribution range of the drug in the body, reduce the incidence of systemic side effects, and enhance the safety of treatment by topical application.

[0025] 4. The antibacterial hydrogel loaded with glycyrrhizin inclusion complex provided by this invention can achieve controlled release and has a sustained antibacterial effect. The content of glycyrrhizin inclusion complex can be adjusted as needed to adapt to different conditions and individual treatment requirements. This customizability makes acne treatment plans more flexible and diverse, increasing the targeting and effectiveness of treatment.

[0026] 5. The preparation method of the present invention is simple, has good stability, and can be industrialized, and has broad prospects for promotion in the field of biomedicine. Attached Figure Description

[0027] Figure 1 The images show the appearance of the antibacterial hydrogel loaded with glycyrrhizin inclusion complex prepared in Example 1. In Figure A, the overall morphology is shown, and in Figure B, the word "BUCT" is written on the antibacterial hydrogel.

[0028] Figure 2 SEM image of the antibacterial hydrogel loaded with glycyrrhizin inclusion complex prepared in Example 3;

[0029] Figure 3 Growth curves of Propionibacterium acnes against different concentrations of LC / HP-β-CD inclusion complex solutions;

[0030] Figure 4 The image shows the effect of antibacterial hydrogels loaded with different concentrations of LC / HP-β-CD inclusion complex on the culture of Propionibacterium acnes. Detailed Implementation

[0031] This invention provides the use of glycyrrhizin in the preparation of a drug for treating acne, wherein the pathogens causing acne include Propionibacterium acnes.

[0032] The present invention provides a medicament for treating acne, wherein the active ingredient of the medicament for treating acne includes glycyrrhizin.

[0033] The present invention also provides a method for preparing the above-mentioned acne treatment drug, comprising the following steps:

[0034] S1. Glycyrrhizin solution and hydroxypropyl-β-cyclodextrin solution were mixed to obtain a mixed solution. The mixed solution was then stirred, rotary evaporated, centrifuged and freeze-dried in sequence to obtain LC / HP-β-CD inclusion complex.

[0035] S2, mixing the chitosan solution, the β-glycerophosphate sodium solution and the LC / HP-β-CD inclusion compound to obtain a sol, and inducing sol-gel transition of the sol to obtain the medicine for treating acne.

[0036] In the present application, in the step S1, the concentration of the glycyrrhizin solution is 30-120 μg / mL, preferably 40-100 μg / mL, and further preferably 60-80 μg / mL; the concentration of the hydroxypropyl-β-cyclodextrin solution is 300-1200 μg / mL, preferably 400-1000 μg / mL, and further preferably 600-800 μg / mL; and the solvents used in the glycyrrhizin solution and the hydroxypropyl-β-cyclodextrin solution are both preferably ethanol.

[0037] In the present application, in the step S1, the volume ratio of the glycyrrhizin solution to the hydroxypropyl-β-cyclodextrin solution is 1-3:1, and preferably 1:1.

[0038] In the present application, in the step S1, the stirring temperature is 20-50°C, preferably 25-45°C, and further preferably 30-40°C; the stirring time is 2-5 h, preferably 2.5-4.5 h, and further preferably 3-4 h; and the stirring speed is 300-800 rpm, preferably 400-700 rpm, and further preferably 500-600 rpm.

[0039] In the present application, in the step S2, the concentration of the LC / HP-β-CD inclusion compound in the sol is 0.3-1.2 mg / mL, preferably 0.4-1.0 mg / mL, and further preferably 0.5-0.8 mg / mL.

[0040] In the present application, in the step S2, the concentration of the chitosan solution is 10-50 mg / mL, preferably 20-40 mg / mL, and further preferably 30-35 mg / mL; the concentration of the β-glycerophosphate sodium solution is 40-60 mg / mL, preferably 45-55 mg / mL, and further preferably 50 mg / mL; the solvent used in the chitosan solution is preferably acetic acid, and the concentration of the acetic acid is preferably 0.05-0.5 mol / L, and further preferably 0.1 mol / L; and the solvent used in the β-glycerophosphate sodium solution is preferably water.

[0041] In the present application, in the step S2, the volume ratio of the chitosan solution, the β-glycerophosphate sodium solution and the LC / HP-β-CD inclusion compound solution is 6-8:2-4, and preferably 7:3.

[0042] In the present application, in the step S2, the mixing is performed under ice-bath conditions.

[0043] In the present application, the temperature for inducing sol-gel transition in step S2 is 30-40℃, preferably 32-38℃, and further preferably 34-36℃; and the time for inducing sol-gel transition is 1-5 min, preferably 2-4 min, and further preferably 3 min.

[0044] The technical solutions provided by the present application will be described in detail below in conjunction with examples, but they should not be understood as limiting the scope of protection of the present application.

[0045] Example 1

[0046] Licoricidin (LC) and hydroxypropyl-β-cyclodextrin (β-CD) were dissolved in ethanol to obtain a 30 μg / mL licoricidin solution and a 300 μg / mL hydroxypropyl-β-cyclodextrin solution, respectively; the same volume of licoricidin solution was added dropwise into the hydroxypropyl-β-cyclodextrin solution, and a mixed solution was obtained by stirring at 500 rpm for 2 h at 50℃; the ethanol was removed from the mixed solution on a rotary evaporator, and then water was added and centrifuged to remove the precipitate (i.e. licoricidin that was not wrapped); and the LC / HP-β-CD inclusion complex was obtained by freeze-drying.

[0047] Chitosan was dissolved in 0.1 mol / L acetic acid solution to obtain a 20 mg / mL chitosan solution; and β-glycerophosphate sodium (β-GP) was dissolved in water to obtain a 56 mg / mL β-glycerophosphate sodium solution, and the two solutions were stored at 4℃ for standby use.

[0048] The chitosan solution and the β-glycerophosphate sodium solution in a volume ratio of 7:3 were mixed under ice bath, and the LC / HP-β-CD inclusion complex was added to obtain a sol, so that the concentration of the LC / HP-β-CD inclusion complex in the sol was 0.3 mg / mL; the sol was placed in a water bath at 37℃ to induce sol-gel transition for 2 min to obtain an antibacterial hydrogel loaded with licoricidin inclusion complex (LC / HP-β-CD / CS / β-GP).

[0049] Figure 1 The appearance of the antibacterial hydrogel loaded with licoricidin inclusion complex prepared in the present example showed that it had good stability, ductility and flowability.

[0050] Example 2

[0051] Glycyrrhizin (LC) and hydroxypropyl-β-cyclodextrin (β-CD) were dissolved in ethanol to obtain glycyrrhizin solution of 60 μg / mL and hydroxypropyl-β-cyclodextrin solution of 600 μg / mL respectively; the same volume of glycyrrhizin solution was added dropwise into the hydroxypropyl-β-cyclodextrin solution, and mixed solution was obtained by stirring at 45 °C and 500 rpm for 3 h; the ethanol was removed from the mixed solution by rotary evaporator, and then water was added to centrifuge to remove the precipitate (the precipitate refers to glycyrrhizin not wrapped), and LC / HP-β-CD inclusion complex was obtained by freeze-drying.

[0052] Chitosan was dissolved in 0.1 mol / L acetic acid solution to obtain chitosan solution of 30 mg / mL; β-glycerophosphate sodium (β-GP) was dissolved in water to obtain β-glycerophosphate sodium solution of 50 mg / mL, and the two solutions were stored at 4 °C for standby.

[0053] The chitosan solution and the β-glycerophosphate sodium solution with a volume ratio of 7:3 were mixed under ice bath, and LC / HP-β-CD inclusion complex was added to obtain sol, and the concentration of LC / HP-β-CD inclusion complex in the sol was 0.6 mg / mL; the sol was placed in a water bath at 37 °C to induce sol-gel transition for 3 min to obtain antibacterial hydrogel loaded with glycyrrhizin inclusion complex (LC / HP-β-CD / CS / β-GP).

[0054] Example 3

[0055] Glycyrrhizin (LC) and hydroxypropyl-β-cyclodextrin (β-CD) were dissolved in ethanol to obtain glycyrrhizin solution of 120 μg / mL and hydroxypropyl-β-cyclodextrin solution of 1200 μg / mL respectively; the same volume of glycyrrhizin solution was added dropwise into the hydroxypropyl-β-cyclodextrin solution, and mixed solution was obtained by stirring at 40 °C and 500 rpm for 4 h; the ethanol was removed from the mixed solution by rotary evaporator, and then water was added to centrifuge to remove the precipitate (the precipitate refers to glycyrrhizin not wrapped), and LC / HP-β-CD inclusion complex was obtained by freeze-drying.

[0056] Chitosan was dissolved in 0.1 mol / L acetic acid solution to obtain chitosan solution of 40 mg / mL; β-glycerophosphate sodium (β-GP) was dissolved in water to obtain β-glycerophosphate sodium solution of 40 mg / mL, and the two solutions were stored at 4 °C for standby.

[0057] The chitosan solution and the β-glycerophosphate sodium solution with a volume ratio of 7:3 were mixed under ice bath, and the sol was obtained by adding the LC / HP-β-CD inclusion complex, so that the concentration of the LC / HP-β-CD inclusion complex in the sol was 1.2 mg / mL. The sol was placed in a water bath at 37°C to induce the sol-gel transition for 4 min to obtain the glycyrrhizin inclusion complex-loaded antibacterial hydrogel (LC / HP-β-CD / CS / β-GP).

[0058] After the glycyrrhizin inclusion complex-loaded antibacterial hydrogel prepared in this example was crushed by liquid nitrogen cryogenic, vacuum freeze-drying was performed, and then a conductive material (gold sputtering) was coated on the antibacterial hydrogel sample. The internal morphology of the sample was observed by scanning electron microscopy (SEM). Figure 2 The SEM image of the glycyrrhizin inclusion complex-loaded antibacterial hydrogel prepared in this example is shown in FIG. 1. Figure 2 It can be seen that the hydrogel has a porous three-dimensional network structure and has an open and interconnected pore structure, verifying the successful synthesis of the hydrogel. The pores of this structure are interconnected, which is helpful for the effective transport and release of the glycyrrhizin inclusion complex in the hydrogel.

[0059] Performance test

[0060] 1. Determination of the minimum inhibitory concentration (MIC) of glycyrrhizin and other 14 natural compounds on P. acnes:

[0061] Preparation of bacterial solution: P. acnes was inoculated in 5 mL of GYM liquid medium and cultured anaerobically at 37°C for 24 h, and the bacterial concentration was adjusted to 1×10 7 cfu / mL.

[0062] Glycyrrhizin was dissolved in sterile deionized water containing 1% DMSO to prepare a glycyrrhizin solution with an initial concentration of 0.4 mg / mL, which was stored in a refrigerator at 4°C in the dark for standby. The MIC of glycyrrhizin on P. acnes was obtained by microdilution method. First, 100 μL of medium was added to each well of a 96-well plate, and 100 μL of glycyrrhizin solution was added to the first column well, which was diluted by 2 times. Then, 100 μL of P. acnes bacterial solution with a concentration of 1×10 7 cfu / mL was inoculated in the well, and the plate was incubated in an anaerobic incubator at 37°C for 24 h. The MIC was defined as the lowest drug concentration at which no obvious growth was observed in the well.

[0063] The above steps were repeated for the remaining 13 natural compounds. The remaining 13 natural compounds were: quercetin, magnolol, resveratrol, rhein, tanshinone IIA, hesperetin, naringenin, kaempferol, curcumin, baicalein, chlorogenic acid, bacialin, and cryptotanshinone. The test results of the MIC are shown in Table 1.

[0064] Table 1 MIC data results of different natural extracts on P. acnes

[0065] Class MIC (mg / mL) Class MIC (mg / mL) Glycyrrihizin 0.0125 Naringenin >5 Quercetin 0.125 Kaempferol 5 Honokiol 0.03125 Curcumin >5 Resveratrol 0.25 Baicalein 2.5 Rhein 0.0625 Chlorogenic acid >0.5 Tanshinone IIA 0.25 Baicalin >0.5 Hesperetin >5 Cryptotanshinone >0.5

[0066] As shown in Table 1, glycyrrhizin has the lowest MIC compared with other thirteen natural compounds, which indicates that glycyrrhizin has a significant antibacterial effect on P. acnes. Further, it is indicated that glycyrrhizin can be used for preparing a medicament for treating acne.

[0067] 2. Determination of antibacterial effect of LC / HP-β-CD inclusion complex on P. acnes: LC / HP-β-CD inclusion complex prepared in Example 3 was dissolved in sterile deionized water to prepare a LC / HP-β-CD inclusion complex solution with an initial concentration of 0.5 mg / mL. Then, 100 μL of the culture medium was added to each well of a 96-well plate, 100 μL of the LC / HP-β-CD inclusion complex solution was added to the first column of wells, and 2-fold gradient dilution was performed. Subsequently, 100 μL of P. acnes bacterial solution with a concentration of 1 x 10 7 cfu / mL was inoculated into the wells, and the plate was incubated in an anaerobic incubator at 37°C for 24 h. The MIC was defined as the lowest drug concentration at which no obvious growth was observed in the wells. Further, the culture medium in the wells without growth was inoculated onto a fresh GAM agar plate, and the minimum concentration at which the number of colonies was less than 10 cfu was defined as the MBC. The positive control was erythromycin. Glycyrrhizin was used to replace the LC / HP-β-CD inclusion complex, and two groups of experiments were performed, one with 1% DMSO as a dissolving aid and the other without the dissolving aid. The above steps were repeated, and the test results are shown in Table 2.

[0068] Table 2 Antibacterial results of glycyrrhizin and LC / HP-β-CD inclusion complex

[0069]

[0070] As shown in Table 2, the solubility of glycyrrhizin in water is very low, so the antibacterial effect of the experimental group without the dissolving aid is poor. However, when glycyrrhizin is prepared into an inclusion complex, the MIC of the inclusion complex is 15.625 ug / mL, and the MBC is 31.25 ug / mL, both of which are the concentrations of glycyrrhizin in the inclusion complex. Therefore, it is indicated that the inclusion complex can improve the dispersibility of glycyrrhizin in water, thereby exerting the antibacterial effect of glycyrrhizin in water. Further, it is indicated that the inclusion complex can be used for preparing a medicament for treating acne.

[0071] 3. Determination of growth curve of P. acnes by LC / HP-β-CD inclusion complex: LC / HP-β-CD inclusion complex 0.3 mg of Example 1, LC / HP-β-CD inclusion complex 0.6 mg of Example 2, and LC / HP-β-CD inclusion complex 1.2 mg of Example 3 were respectively added to 1 mL of P. acnes bacterial solution with a concentration of 1 x 10 7A mixture of CFU / mL Propionibacterium acnes bacterial suspension was prepared and incubated in an anaerobic environment at 37°C. OD values ​​were measured at 1 mL intervals. 600 The measurement results are as follows Figure 3 As shown.

[0072] Depend on Figure 3 The results showed that the LC / HP-β-CD inclusion complex significantly delayed the onset of the exponential growth phase of *Propionibacterium acnes*, indicating its potential antibacterial activity in acne treatment. The slope of the growth curve gradually decreased with increasing LC / HP-β-CD concentration. Specifically, 0.3 mg / mL of the LC / HP-β-CD inclusion complex significantly inhibited the growth of *Propionibacterium acnes* within 24 hours. Both 0.6 mg / mL and 1.2 mg / mL of the LC / HP-β-CD inclusion complex showed good inhibitory effects within 72 hours, further confirming its inhibitory ability against *Propionibacterium acnes*. The antibacterial effect gradually increased with increasing LC / HP-β-CD concentration, exhibiting a concentration-dependent effect.

[0073] 4. Antibacterial effect of antibacterial hydrogel loaded with glycyrrhizin inclusion complex (LC / HP-β-CD / CS / β-GP):

[0074] Take 1 mL of each of the antibacterial hydrogels (LC / HP-β-CD / CS / β-GP) loaded with glycyrrhizin inclusion complexes from Examples 1-3, gel at 37°C, and then soak them in 1 mL of a solution with a concentration of 1×10⁻⁶ g / mL. 7 The bacteria were incubated in a CFU / mL solution of Propionibacterium acnes at 37°C for 24 hours. 100 μL of the incubator was then evenly spread onto GAM solid medium and incubated at 37°C for 72 hours. Colonies were observed and photographed. Results are shown below. Figure 4 ,in, Figure 4 The concentration in the figure represents the concentration of the LC / HP-β-CD inclusion complex in the antibacterial hydrogel.

[0075] Depend on Figure 4 As can be seen, the antibacterial hydrogel (LC / HP-β-CD / CS / β-GP) loaded with glycyrrhizin inclusion complex prepared in this invention showed a significant antibacterial effect against Propionibacterium acnes, and the effect was concentration-dependent. The antibacterial effect became more significant with the increase of the concentration of LC / HP-β-CD inclusion complex.

[0076] The above description is only a preferred embodiment of the present invention. It should be noted that for those skilled in the art, several improvements and modifications can be made without departing from the principle of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.

Claims

1. The use of glycyrrhizin for the preparation of a medicament for the treatment of acne, characterized in that, The pathogenic bacteria causing acne include Propionibacterium acnes.

2. A method of preparing a medicament for treating acne, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of claim 1. The active ingredient of the medicine for treating acne includes glycyrrhizin; The method comprises the following steps: S1, glycyrrhizin solution and hydroxypropyl β The mixed solution is sequentially subjected to stirring, rotary evaporation, centrifugation and freeze-drying to obtain LC / HP β CD inclusion compound; S2, dissolving chitosan solution, β sodium glycerophosphate solution and LC / HP β CD inclusion compound mixture to obtain sol, inducing sol to sol-gel transition gel transition to obtain a medicine for treating acne; In the step S2, LC / HP β The concentration of the CD inclusion complex in the sol was 0.3-1.2 mg / mL. The concentration of the chitosan solution in the step S2 is 20-50 mg / mL; β The concentration of the glycerophosphate sodium solution is 40-56 mg / mL; In the step S2, the chitosan solution and the β The volume ratio of the sodium glycerophosphate solution is 7:

3.

3. The preparation method according to claim 2, characterized in that, The concentration of glycyrrhizin solution in the step S1 is 30-120 μg / mL; the concentration of hydroxypropyl β The concentration of cyclodextrin solution is 300-1200 μg / mL.

4. The production method according to claim 3, characterized by, The volume ratio of the glycyrrhizin solution and the hydroxypropyl β The volume ratio of the cyclodextrin solution is 1-3:

1.

5. The method of any one of claims 2 to 4, wherein the method further comprises, In the step S1, the temperature of stirring is 20-50℃, the time of stirring is 2-5h, and the rotating speed of stirring is 300-800rpm.

6. The production method according to claim 5, characterized by, In the step S2, the sol is induced The temperature of the gel transition is 30-40°C, the sol is induced The time of the gel transition is 1-5 min.

Citation Information

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