A kind of mesoporous silica nanoparticles of disulfiram monomer and its preparation method and application

A technology of mesoporous silica and nanoparticles, which is applied in the field of medicine, can solve the problems of increasing patient tolerance, low bioavailability, and poor drug effectiveness, and achieve the effects of reducing treatment costs, low preparation costs, and uniform distribution

Active Publication Date: 2021-04-30
武汉格迪泰健康科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the current disulfiram anticancer drugs generally have the problem of low bioavailability, which leads to high application costs, increased patient tolerance, poor therapeutic effect, and poor drug effectiveness.

Method used

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  • A kind of mesoporous silica nanoparticles of disulfiram monomer and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] 1. Preparation of mercapto mesoporous silica nanoparticles (MSNs-SH)

[0023] Mix 2.35ml (70.5mmol) ethanol, 0.56g (1.755mmol) cetyltrimethylammonium chloride (CTAC), 16ml (0.9mol) ultrapure water, add 2.6ml (0.0192mol) triethanolamine, stir To dissolve, raise the temperature to 60°C, pass nitrogen gas at a speed of 130mL / min, add 1.454ml (6.5mmol) tetraethyl orthosilicate (TEOS) and 0.32ml (1.3mmol) MPTES dropwise at a certain speed (1mL / min) (Mercaptopropyltriethoxysilane) mixed solution, react for 2h, end the reaction, cool to room temperature, centrifuge (10000r / min, 15min), wash with ethanol five times, centrifuge, vacuum dry (65°C, 12h ), to obtain thiol-modified mesoporous silica nanoparticles MSNs-SH without template removal.

[0024] 2. Preparation of mesoporous silica nanoparticles of disulfiram monomer (diethylcarbamate)

[0025] The prepared thiol-modified mesoporous silica nanoparticles MSNs-SH (100mg) without template removal were dispersed in PBS (100ml...

Embodiment 2

[0027] 1. Preparation of mercapto mesoporous silica nanoparticles (MSNs-SH)

[0028] Mix 80mmol of ethanol, 2mmol of cetyltrimethylammonium chloride (CTAC) and 0.75mol of ultrapure water, add 0.021mol of triethanolamine, stir until dissolved, heat up to 80°C, and use 100mL / min Nitrogen was passed at a speed of 1mL / min, and a mixture of 7.8mmol tetraethyl orthosilicate (TEOS) and 1.5mmol mercaptopropyltrimethoxysilane was added dropwise at a speed of 1mL / min, reacted for 2h, and the reaction was terminated, cooled to room temperature, and centrifuged (10000r / min, 15min), washed five times with ethanol, centrifuged, and vacuum dried (65°C, 12h) to obtain mercapto-modified mesoporous silica nanoparticles MSNs-SH without template removal.

[0029] 2. Preparation of mesoporous silica nanoparticles of disulfiram monomer (diethylcarbamate)

[0030] The prepared thiol-modified mesoporous silica nanoparticles MSNs-SH (100mg) without template removal were dispersed in PBS (100ml, pH7.4...

Embodiment 3

[0032] 1. Preparation of mercapto mesoporous silica nanoparticles (MSNs-SH)

[0033] Mix 60mmol of ethanol, 1.4mmol of cetyltrimethylammonium chloride (CTAC) and 1.1mol of ultrapure water, add 0.014mol of triethanolamine, stir until dissolved, heat up to 45°C, and Nitrogen at a speed of 1 mL / min, dropwise add a mixture of 4.5 mmol tetraethyl orthosilicate (TEOS) and 1.2 mmol mercaptopropyltrimethoxysilane at a speed of 1 mL / min, react for 2 h, end the reaction, cool to room temperature, centrifuge Separation (10000r / min, 15min), washing with ethanol five times, centrifugal separation, and vacuum drying (65°C, 12h) to obtain thiol-modified mesoporous silica nanoparticles MSNs-SH without template removal.

[0034] 2. Preparation of mesoporous silica nanoparticles of disulfiram monomer (diethylcarbamate)

[0035] The prepared thiol-modified mesoporous silica nanoparticles MSNs-SH (100mg) without template removal were dispersed in PBS (100ml, pH7.4), and then dispersed in 30ml et...

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Abstract

The present invention relates to a kind of mesoporous silicon dioxide nano-particle of disulfiram monomer and its preparation method and application. The preparation method is as follows: (1) preparation of mesoporous silicon dioxide nano-particle; Mesoporous silica nanoparticles of disulfiram monomers (diethylcarbamodithiocarbamate) with disulfide bonds were prepared. The average particle diameter of the nanoparticles is 50-300nm, and the nanoparticles are uniformly distributed and have good dispersibility. The mesoporous silica nanoparticles of the disulfiram monomer are beneficial to improve the targeting of drugs, improve the bioavailability of drugs, and the preparation cost of drugs is low, which can greatly reduce the treatment cost of patients, and has potential market value and profound social significance.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a mesoporous silicon dioxide nanoparticle of disulfiram monomer and its preparation method and application. Background technique [0002] Nano-mesoporous materials have a series of advantages such as highly ordered pores, uniform and adjustable pore size, high specific surface area, large pore area, narrow particle size distribution, controllable morphology characteristics and surface-modified functional groups. It shows great advantages in terms of drug performance. Mesoporous silica nanoparticles (MSN) are biocompatible inorganic mesoporous materials with a series of remarkable characteristics, such as high surface area (>800m 2 / g), large pore volume (>1XXZSZXcm 3 / g), adjustable pore size (2-10nm), controllable morphology and modifiable surface, can load various drugs in the mesoporous channel or on the mesoporous surface, and can control the drug loading of the drug...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/52A61K9/16A61K31/145A61P25/32A61P35/00
CPCA61K9/1611A61K31/145A61P25/32A61P35/00
Inventor 刘明星王友运
Owner 武汉格迪泰健康科技有限公司
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