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Icaritin nanoparticles as well as preparation method and application thereof

A technology of icariin and nanoparticles, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problems of low bioavailability, low biological potency, and limited applications, etc. problem, achieve the effect of improving water solubility and simple production process

Pending Publication Date: 2022-07-15
SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Like most flavonoids, icariin has poor water solubility, extremely low bioavailability, and is chemically unstable, which greatly limits its application as a functional factor in food and medicine
Therefore, it is necessary to find a way to solve the problems of poor water solubility, low biological potency and poor stability of icariin, so as to provide technical guidance for the development and utilization of icariin-related drugs and functional foods

Method used

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  • Icaritin nanoparticles as well as preparation method and application thereof
  • Icaritin nanoparticles as well as preparation method and application thereof
  • Icaritin nanoparticles as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation of icariin nanoparticles

[0035] (1) citrus pectin (Shanghai McLean Biochemical Technology Co., Ltd.) is added to the 0.0375mol / L aqueous hydrochloric acid solution according to a material-to-liquid ratio of 10g / L, and after high-speed shear dispersion, 50 ° C is heated to be completely dissolved to obtain a pectin solution;

[0036] (2) under stirring condition, add icariin (Sichuan Vikki Biotechnology Co., Ltd.) to 0.15mol / L sodium hydroxide aqueous solution according to the material-to-liquid ratio of 10g / L, and obtain icariin solution after completely dissolving;

[0037] (3) under stirring conditions (500rpm / min), add the icariin solution of step (2) to the pectin solution of step (1) according to the volume ratio of 1:4, and continue stirring for 2h at room temperature, 10000g Centrifuge, and take the upper layer solution as Icaritin-pectin nanoparticles (IPNPs).

[0038] The described IPNPs were characterized as follows:

[0039] (1) Ana...

Embodiment 2

[0073] Example 2: Preparation of icariin nanoparticles

[0074] (1) citrus pectin (Shanghai McLean Biochemical Technology Co., Ltd.) is added to the 0.02mol / L hydrochloric acid aqueous solution according to a material-to-liquid ratio of 5g / L, after high-speed shearing and dispersing, heating at 45°C to complete dissolution to obtain a pectin solution;

[0075] (2) under stirring condition, add icariin (Sichuan Vikki Biotechnology Co., Ltd.) to 0.4mol / L aqueous sodium hydroxide solution according to the material-to-liquid ratio 50g / L, and obtain icariin solution after completely dissolving;

[0076] (3) under stirring condition (500rpm / min), add the icariin sodium hydroxide aqueous solution of step (2) to the pectin solution of step (1) according to the volume ratio of 1:20, and continue stirring at room temperature for 1.5 After h, centrifuge at 10000g, and take the upper layer solution as icariin nanoparticles (IPNPs).

[0077] The average drug loading of the IPNPs obtained ...

Embodiment 3

[0078] Example 3: Preparation of icariin nanoparticles

[0079] (1) citrus pectin (Shanghai McLean Biochemical Technology Co., Ltd.) is added to the 0.0125mol / L hydrochloric acid aqueous solution according to a material-to-liquid ratio of 10g / L, and after high-speed shear dispersion, 45 ° C is heated to be completely dissolved to obtain a pectin solution;

[0080] (2) under stirring condition, add icariin (Sichuan Vikki Biotechnology Co., Ltd.) to 0.06mol / L sodium hydroxide aqueous solution according to the material-to-liquid ratio 5g / L, and obtain icariin solution after completely dissolving;

[0081] (3) under stirring condition (500rpm / min), add the icariin sodium hydroxide aqueous solution of step (2) to the pectin solution of step (1) according to the volume ratio of 1:4, and continue stirring for 3h at room temperature After centrifugation at 10000g, the upper layer solution was taken as icariin nanoparticles (IPNPs). The average drug loading of the IPNPs obtained in th...

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Abstract

The invention discloses an icaritin nanoparticle and a preparation method thereof. Comprising icaritin and pectin, and the icaritin is loaded on the pectin. The pectin is used for preparing the water-soluble icaritin nanoparticles, is a part of natural diet of human beings since ancient times, and is a safe and non-toxic natural food additive recommended by the FAO / WHO food additive combination committee; in addition, pectin is also a water-soluble dietary fiber and has various health effects, so that the prepared icaritin nanoparticles are safe and accord with the modern dietary recommendation of low fat and high dietary fiber. According to the invention, the combination of the pectin and the icaritin is promoted by utilizing the nano embedding property and acid-base combination of the pectin, so that the water solubility, the stability and the bioavailability of the icaritin are greatly improved, and the activity of the icaritin is not changed.

Description

Technical field: [0001] The invention belongs to the field of functional foods, in particular to an icariin nanoparticle and a preparation method and application thereof. Background technique: [0002] On January 10, 2022, the national first-class innovative anticancer drug icariin soft capsule was approved for marketing, filling the precision treatment plan for advanced hepatocellular carcinoma. As one of the innovative drugs of domestic traditional Chinese medicine, the core component of icariin soft capsule is icariin (formula I, the specific structure is as follows). Icariin is the monomer active ingredient of Chinese medicine Epimedium, which belongs to flavonoids. Icariin has various biological activities such as anti-inflammatory, anti-tumor, anti-aging, anti-oxidation, immune regulation and prevention of osteoporosis, and has broad application prospects. Like most flavonoids, icariin has poor water solubility, extremely low bioavailability, and is chemically unstab...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/352A61K47/36A61P35/00A23L33/105A23L29/231A23L33/21
CPCA61K9/5161A61K31/352A61P35/00A23L33/105A23L29/231A23L33/21A23V2002/00A23V2200/308A23V2200/32A23V2250/5072A23V2250/2116
Inventor 温玲蓉杨宝蒋跃明陈怡朋
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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