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A kind of preparation method of zeolite imidazole frame nanoparticle material loaded with zoledronic acid

A technology of zoledronic acid and zeolite imidazole, which is applied in the field of preparation of zeolite imidazole framework nanoparticle materials, can solve the problems of affecting the overall performance of nanomaterials, limiting the pharmacological activity of zoledronic acid, and being unable to uniformly load zoledronic acid, etc. , to achieve good drug loading capacity, good biological safety, and improve the therapeutic effect

Active Publication Date: 2022-03-11
XIANGYA HOSPITAL CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The usual preparation method of ZIF-8 is completed in the methanol system, and the solubility of zoledronic acid in methanol is extremely low, and complex chemical modification of zoledronic acid is often required to be loaded into ZIF-8 nanoparticles, but this This method changes the structure of zoledronic acid and then changes its ability to inhibit osteoclasts, which limits the pharmacological activity of zoledronic acid itself, and the preparation process is cumbersome and the production efficiency is low
If ZIF-8 is prepared in the methanol system first, and then transferred to the water system to compound with zoledronic acid, ZIF-8 will form obvious agglomeration in the process of transferring to the water system, so that the zoledronic acid cannot be evenly encapsulated. load, seriously affecting the overall performance of the final nanomaterial

Method used

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  • A kind of preparation method of zeolite imidazole frame nanoparticle material loaded with zoledronic acid
  • A kind of preparation method of zeolite imidazole frame nanoparticle material loaded with zoledronic acid
  • A kind of preparation method of zeolite imidazole frame nanoparticle material loaded with zoledronic acid

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Embodiment 1

[0039] A method for preparing a zoledronic acid-loaded zeolite imidazole framework nanoparticle material specifically targeting bone tissue, comprising the following steps:

[0040] (1) Prepare 9mL of 2-methylimidazole aqueous solution (pH=8.5) with a concentration of 0.04mol / L, and slowly add Zn(NO 3 ) 2 Aqueous solution (pH = 7) 1mL, continue to stir for 30min, until the reaction system is white colloid, this time is ZIF-8 nanoparticle colloid;

[0041] (2) In the zeolite imidazole framework-8 colloid obtained in step (1), add dropwise 0.6 mL of zoledronic acid aqueous solution (pH=7) with a concentration of 0.05 mol / L while stirring, and continue stirring for 30 min, 10000 g / 10 min Centrifugation and deionized water washing were repeated three times, and the obtained white precipitate was the zeolitic imidazole framework nanoparticle material (ZIF-8@ZA nanoparticles) loaded with zoledronic acid. After freeze-drying, the yield was weighed to 10 mg.

[0042] 1. Characteriza...

Embodiment 2

[0056] A method for preparing a zoledronic acid-loaded zeolite imidazole framework nanoparticle material specifically targeting bone tissue, comprising the following steps:

[0057] (1) Prepare 9mL of 2-methylimidazole aqueous solution (pH=8.5) with a concentration of 0.05mol / L, and slowly add Zn(NO 3 ) 2 Aqueous solution (pH = 7) 1mL, continue to stir for 30min, until the reaction system is white colloid, this time is ZIF-8 nanoparticle colloid;

[0058] (2) In the zeolite imidazole framework-8 colloid obtained in step (1), add dropwise 0.6 mL of zoledronic acid aqueous solution (pH=7) with a concentration of 0.05 mol / L while stirring, and continue stirring for 30 min, 10000 g / 10 min Centrifugation and deionized water washing were repeated three times, and the obtained white precipitate was the zeolite imidazole framework nanoparticle material (ZIF-8@ZA nanoparticles) loaded with zoledronic acid. After freeze-drying, the yield was 8 mg.

Embodiment 3

[0060] A method for preparing a zoledronic acid-loaded zeolite imidazole framework nanoparticle material specifically targeting bone tissue, comprising the following steps:

[0061] (1) Prepare 9mL of 2-methylimidazole aqueous solution (pH=8.5) with a concentration of 0.03mol / L, and slowly add Zn(NO 3 ) 2 Aqueous solution (pH = 7) 1mL, continue to stir for 30min, until the reaction system is white colloid, this time is ZIF-8 nanoparticle colloid;

[0062] (2) Add 0.6 mL of zoledronic acid aqueous solution (pH=7) with a concentration of 0.06 mol / L dropwise to the zeolite imidazole framework-8 colloid obtained in step (1), and continue stirring for 30 min, 10000 g / 10 min Centrifugation and deionized water washing were repeated three times, and the obtained white precipitate was the zeolite imidazole framework nanoparticle material (ZIF-8@ZA nanoparticles) loaded with zoledronic acid. After freeze-drying, the yield was 8 mg.

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Abstract

The invention discloses a preparation method of a zeolite imidazole framework nanoparticle material loaded with zoledronic acid, which comprises the following steps: preparing an aqueous solution of 2-methylimidazole, and then adding Zn(NO 3 ) 2 Aqueous solution, continue to stir until the reaction system is white colloid, in the obtained zeolite imidazole framework-8 colloid, dropwise add zoledronic acid aqueous solution while stirring, continue to stir, centrifuge, and the white precipitate obtained after washing is the described Zeolite imidazole framework nanoparticle material loaded with zoledronic acid. The present invention uses a one-step method to synthesize the zeolite imidazole framework nanoparticle material (ZIF-8@ZA) loaded with zoledronic acid in the water system, and the zoledronic acid can be loaded into the ZIF-8@ZA without modifying the zoledronic acid. 8 nanometer particles, not only preserves the pharmacological activity of zoledronic acid itself, but also simplifies the process, simple operation and high production efficiency.

Description

technical field [0001] The invention belongs to the technical field of targeting materials, and in particular relates to a preparation method of a zoledronic acid-loaded zeolite imidazole framework nanoparticle material specifically targeting bone tissue. Background technique [0002] The particularity of the anatomical structure of human bone tissue leads to poor blood circulation in some parts (such as subchondral bone, skull, etc.). Intravenous administration is often difficult to form an effective blood concentration in the lesion; although local injection can overcome this obstacle to a certain extent, the hard bone tissue makes local injection impossible most of the time, and repeated local injection will not only aggravate the The pain of the patient increases the risk of infection significantly. Therefore, how to increase the blood concentration of therapeutic drugs in the bone tissue of the lesion and improve the therapeutic effect is an important scientific proble...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/22A61K47/02A61K31/675A61P19/10A61P35/04A61P19/08
CPCA61K9/5123A61K9/5115A61K31/675A61P19/10A61P35/04A61P19/08
Inventor 胡懿郃潘依潇汪龙
Owner XIANGYA HOSPITAL CENT SOUTH UNIV
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