Ursolic acid nanocapsule particles and preparation method thereof
By using thremella polysaccharide as a stabilizer, combined with surfactants and other auxiliary materials, stable ursolic acid nanocapsules particles are prepared, which solves the problem of low stability, improves the absorption and distribution of drugs, and enhances its health effect.
Patent Information
- Application Number
- CN202411650921.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-11-19
- Publication Date
- 2025-02-14
AI Technical Summary
Urso acid nanocapsule particles have low stability and are prone to adverse changes such as agglomeration and degradation during transportation or storage.
Using Tremella polysaccharide as a stabilizer, stable ursolic acid nanocapsule particles are prepared through steps such as tremella polysaccharide extraction, solution preparation, ursolic acid extraction and nanocapsule granules preparation, combined with surfactant, stabilizer and pH regulator.
It improves the stability of ursolic acid nanocapsule particles, reduces agglomeration and degradation during storage and transportation, and promotes the absorption and distribution of drugs, enhancing its health effects.
Abstract
Description
Technical Field
[0001] The invention relates to the technical field of ursolic acid nanocapsule particle preparation, in particular to ursolic acid nanocapsule particles and a preparation method thereof. Background Art
[0002] When choosing drugs for treatment, most people choose nanocapsule particles to improve their nutrition and flavor, increase the bioavailability of active ingredients, and promote digestion and absorption of active ingredients. Nanoparticles have the characteristics of simple synthesis, low cost, and biodegradability, and can be used as the most promising drug delivery system.
[0003] The existing ursolic acid nanocapsule particle formula is relatively fixed and single. Conventional ursolic acid nanocapsule particles have antioxidant, anti-inflammatory, antioxidant and anti-liver damage, immune regulation, anti-cancer and improved lipid metabolism disorder effects, but the stability of ursolic acid nanocapsule particles is low, and adverse changes such as agglomeration and degradation are prone to occur during their transportation or storage.
[0004] Therefore, in view of the low stability of the above-mentioned ursolic acid nanocapsule particles and the problem that they are prone to adverse changes such as agglomeration and degradation during transportation or storage, an ursolic acid nanocapsule particle and a preparation method thereof can be designed. Summary of the invention
[0005] In order to overcome the low stability of ursolic acid nanocapsule particles, they are prone to adverse changes such as agglomeration and degradation during transportation or storage.
[0006] The technical scheme of the present invention is: an ursolic acid nanocapsule particle, which is formulated as follows by weight: 30-50 parts of Tremella polysaccharide, 10-20 parts of ursolic acid and appropriate amounts of other auxiliary materials;
[0007] Other auxiliary materials include 2 to 5 parts of stabilizer, 1 to 3 parts of surfactant, 0.5 to 1.5 parts of pH regulator and an appropriate amount of solvent.
[0008] Preferably, Tremella polysaccharide is the wall material of the nanocapsule particles, ursolic acid is the core material of the nanocapsule particles, and the Tremella polysaccharide encapsulates the ursolic acid.
[0009] The method for preparing ursolic acid nanocapsule particles comprises the ursolic acid nanocapsule particles as described above, and the steps are as follows:
[0010] S1: Extraction of Tremella polysaccharide: fresh and uncontaminated Tremella is selected as raw material, the Tremella is put into a crusher and crushed into appropriate particle size, the crushed Tremella can be extracted by hot water leaching method, enzyme extraction method and microwave-assisted extraction method, and after the extraction is completed, the Tremella polysaccharide is filtered, concentrated and precipitated to obtain;
[0011] S2: Preparation of Tremella polysaccharide solution: The extracted Tremella polysaccharide is placed in a centrifuge for centrifugal filtration to remove impurities and obtain a relatively pure Tremella polysaccharide solution;
[0012] S3: Extraction of ursolic acid: select plants rich in ursolic acid as raw materials, and use ultrasonic-assisted ionic liquid method to extract; extract the crude ursolic acid extract obtained after the extraction to remove impurities, place the removed ursolic acid extract in an organic solvent, slowly add anti-solvent to make the solution reach a saturated state, and stir the solution to precipitate ursolic acid, and centrifuge the solution of the precipitated ursolic acid to obtain ursolic acid;
[0013] S4: Preparation of nanocapsule particles: Mix the purified Tremella polysaccharide and ursolic acid, and add appropriate amounts of surfactant and solvent; use a colloid mill to homogenize the mixed solution to obtain uniform nanoscale particles; the nanoscale particles are further refined by an ultrasonic processor; the nanoparticles are homogenized by a high-pressure homogenizer; the homogenized nanoparticle solution is freeze-dried to prepare the mixture into nanocapsule particles.
[0014] Preferably, hot water leaching is used to extract Tremella polysaccharide, and the crushed Tremella is placed in hot water and stirred and mixed.
[0015] Preferably, the water temperature of the hot water leaching method is 60-90° C., and the stirring time is 1-1.5 h.
[0016] Preferably, an enzyme extraction method is selected to extract Tremella polysaccharide, the crushed Tremella is placed in a reactor, and an enzyme preparation is added to react to extract Tremella polysaccharide.
[0017] Preferably, microwave-assisted extraction is used to extract Tremella polysaccharide, wherein the crushed Tremella is placed in a microwave reactor, and a suitable amount of solvent is added to perform microwave extraction to obtain Tremella polysaccharide.
[0018] The invention has the following beneficial effects: Tremella polysaccharide as a stabilizer is helpful to stabilize the structure of ursolic acid nanocapsule particles, reduce adverse changes such as agglomeration and degradation during storage and transportation, and Tremella polysaccharide promotes the absorption and distribution of ursolic acid by the human body, further improving its health effect; Tremella polysaccharide is a biological response modifier, has the effects of improving the body's immune function and increasing white blood cells; at the same time, it improves the phagocytic function of reticuloendothelial cells, promotes nonspecific immune effects, and increases the levels of immunoglobulins and serum total complement; Tremella polysaccharide also has multiple physiological functions such as regulating blood sugar and blood lipids, preventing thrombosis, resisting radiation, protecting gastric mucosa, etc. Ursolic acid has a significant effect on improving glucose and lipid metabolism disorders, and is suitable for occasional hyperglycemia and gestational hyperglycemia. Ursolic acid can regulate metabolism in the body and has certain antioxidant and anti-inflammatory effects. Through nano-preparation, it can penetrate the cell membrane and improve bioavailability. At the same time, it can slowly release drug ingredients, prolong the drug action time, reduce the frequency of medication, and improve the treatment effect. The combination of the three can activate immune cells, increase the expression of immune factors, build an immune barrier for the body, and improve the solubility and stability of the drug, increase the absorption and utilization rate of Tremella polysaccharides and ursolic acid in the body, and reduce drug damage and side effects to normal tissues. DETAILED DESCRIPTION
[0019] The present invention will be further described below in conjunction with the embodiments.
[0020] Example 1
[0021] Select fresh and unpolluted Tremella as raw material, put the Tremella into a crusher to crush it into appropriate particle size, put the crushed Tremella into 75°C hot water and stir for 1.3 hours, filter, concentrate and precipitate to obtain Tremella polysaccharide after extraction, put the extracted Tremella polysaccharide into a centrifuge for centrifugal filtration, remove impurities to obtain a relatively pure Tremella polysaccharide solution; select plants rich in ursolic acid as raw materials, and use ultrasonic assisted ionic liquid method for extraction; extract the ursolic acid crude extract obtained after extraction to remove impurities, place the removed ursolic acid extract in an organic solvent, and slowly add anti-solvent, The solution is made to reach a saturated state, and the solution is stirred at the same time to precipitate ursolic acid, and the solution of the precipitated ursolic acid is centrifuged to obtain ursolic acid; 30 parts of purified Tremella polysaccharide and 10 parts of ursolic acid are mixed, and 1 part of surfactant, 2 parts of stabilizer and 0.5 part of pH regulator are added; after mixing, the mixed solution is homogenized by using a colloid mill to obtain uniform nano-scale particles; the nano-scale particles are further refined by using an ultrasonic processor; the nano-particles are homogenized by a high-pressure homogenizer; and the homogenized nano-particle solution is freeze-dried to prepare the mixture into nano-capsule particles.
[0022] Example 2
[0023] Fresh and unpolluted Tremella fuciformis is selected as raw material, the Tremella fuciformis is put into a crusher and crushed into appropriate particle size, the crushed Tremella fuciformis is put into a reactor, an enzyme preparation is added for reaction, Tremella fuciformis polysaccharide is extracted, and after the extraction is completed, the Tremella fuciformis polysaccharide is filtered, concentrated and precipitated to obtain Tremella fuciformis polysaccharide, and the extracted Tremella fuciformis polysaccharide is put into a centrifuge for centrifugal filtration to remove impurities to obtain a relatively pure Tremella fuciformis polysaccharide solution; plants rich in ursolic acid are selected as raw materials, and ultrasonic-assisted ionic liquid method is used for extraction; the ursolic acid crude extract obtained after the extraction is extracted to remove impurities, and the removed ursolic acid extract is placed in an organic solvent, and slowly added The invention discloses a method for preparing a nanometer-sized particle-enhanced nanoparticle-containing nanoparticle by using an anti-solvent to make the solution reach a saturated state, and at the same time, stirring the solution to precipitate ursolic acid, and centrifuging the solution of the precipitated ursolic acid to obtain ursolic acid; mixing 40 parts of purified Tremella polysaccharide and 15 parts of ursolic acid, and adding 2 parts of surfactant, 3.5 parts of stabilizer and 1 part of pH regulator; homogenizing the mixed solution with a colloid mill to obtain uniform nano-sized particles; further refining the nano-sized particles with an ultrasonic processor; homogenizing the nano-sized particles with a high-pressure homogenizer; and preparing nano-capsule particles from the mixture of the homogenized nano-sized particle solution by freeze drying.
[0024] Example 3
[0025] Fresh and unpolluted Tremella fuciformis is selected as a raw material, the Tremella fuciformis is put into a crusher and crushed into a suitable particle size, the crushed Tremella fuciformis is placed in a microwave reactor, an appropriate amount of solvent is added, microwave extraction is performed to obtain Tremella fuciformis polysaccharide, and after the extraction is completed, the Tremella fuciformis polysaccharide is filtered, concentrated, and precipitated to obtain Tremella fuciformis polysaccharide, and the extracted Tremella fuciformis polysaccharide is placed in a centrifuge for centrifugal filtration to remove impurities to obtain a relatively pure Tremella fuciformis polysaccharide solution; plants rich in ursolic acid are selected as raw materials, and an ultrasonic-assisted ionic liquid method is used for extraction; the ursolic acid crude extract obtained after the extraction is extracted to remove impurities, and the removed ursolic acid extract is placed in an organic solvent and slowly The invention relates to a method for preparing nanocapsule-type nanoparticles by slowly adding an anti-solvent to make the solution reach a saturated state, stirring the solution to precipitate ursolic acid, and centrifuging the solution of the precipitated ursolic acid to obtain ursolic acid; mixing 50 parts of purified Tremella polysaccharide and 20 parts of ursolic acid, and adding 3 parts of a surfactant, 5 parts of a stabilizer and 1.5 parts of a pH regulator; homogenizing the mixed solution with a colloid mill to obtain uniform nano-scale particles; further refining the nano-scale particles with an ultrasonic processor; homogenizing the nano-particles with a high-pressure homogenizer; and preparing nanocapsule particles from the homogenized nano-particle solution by freeze-drying.
[0026] The preparation method of ursolic acid nanocapsule particles using Examples 1, 2, and 3 can activate immune cells, increase the expression of immune factors, build an immune barrier for the body, improve the solubility and stability of drugs, increase the absorption and utilization rate of Tremella polysaccharides and ursolic acid in the body, and reduce the damage and side effects of drugs to normal tissues.
[0027] The implementation modes of the present invention are described in detail above in conjunction with the embodiments, but the present invention is not limited to the above-mentioned implementation modes, and various changes can be made within the knowledge scope of those skilled in the art without departing from the purpose of the present invention.
Claims
1. An ursolic acid nanocapsule particle, the formula is as follows, by weight: 30-50 parts of Tremella polysaccharide, 10-20 parts of ursolic acid and appropriate amounts of other auxiliary materials; Other auxiliary materials include 2 to 5 parts of stabilizer, 1 to 3 parts of surfactant, 0.5 to 1.5 parts of pH regulator and an appropriate amount of solvent.
2. The ursolic acid nanocapsule particles according to claim 1, characterized in that: Tremella polysaccharide is the wall material of nanocapsule particles, ursolic acid is the core material of nanocapsule particles, and ursolic acid is wrapped by Tremella polysaccharide.
3. A method for preparing ursolic acid nanocapsule particles, characterized in that: The method comprises the ursolic acid nanocapsule particles according to claim 1-2, wherein the steps are as follows: S1: Extraction of Tremella polysaccharide: fresh and uncontaminated Tremella is selected as raw material, the Tremella is put into a crusher and crushed into appropriate particle size, the crushed Tremella can be extracted by hot water leaching method, enzyme extraction method and microwave-assisted extraction method, and after the extraction is completed, the Tremella polysaccharide is filtered, concentrated and precipitated to obtain; S2: Preparation of Tremella polysaccharide solution: The extracted Tremella polysaccharide is placed in a centrifuge for centrifugal filtration to remove impurities and obtain a relatively pure Tremella polysaccharide solution; S3: Extraction of ursolic acid: select plants rich in ursolic acid as raw materials, and use ultrasonic-assisted ionic liquid method or solvent extraction method to extract; extract the crude ursolic acid extract obtained after the extraction to remove impurities, place the removed ursolic acid extract in an organic solvent, slowly add anti-solvent to make the solution reach a saturated state, and stir the solution to precipitate ursolic acid, and centrifuge the solution of the precipitated ursolic acid to obtain ursolic acid; S4: Preparation of nanocapsule particles: Mix the purified Tremella polysaccharide and ursolic acid, and add appropriate amounts of surfactant and solvent; use a colloid mill to homogenize the mixed solution to obtain uniform nanoscale particles; the nanoscale particles are further refined by an ultrasonic processor; the nanoparticles are homogenized by a high-pressure homogenizer; the homogenized nanoparticle solution is freeze-dried to prepare the mixture into nanocapsule particles.
4. The method for preparing ursolic acid nanocapsule particles according to claim 3, characterized in that: The hot water leaching method is selected to extract Tremella polysaccharide, and the crushed Tremella is placed in hot water and stirred and mixed.
5. The method for preparing ursolic acid nanocapsule particles according to claim 4, characterized in that: The water temperature of the hot water leaching method is 60-90°C and the stirring time is 1-1.5h.
6. The method for preparing ursolic acid nanocapsule particles according to claim 3, characterized in that: The enzyme extraction method is selected to extract Tremella polysaccharide, the crushed Tremella is put into a reactor, and the enzyme preparation is added to react.
7. The method for preparing ursolic acid nanocapsule particles according to claim 3, characterized in that: The microwave-assisted extraction method is selected to extract Tremella polysaccharide. The crushed Tremella is placed in a microwave reactor, and an appropriate amount of solvent is added to perform microwave extraction to obtain Tremella polysaccharide.