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Mesoporous silica nanoparticles having disulfiram monomer and preparation method and application thereof

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

Active Publication Date: 2018-09-18
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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0028] Mix 2.35ml (70.5mmol) ethanol, 0.56g (1.755mmol) cetyltrimethylammonium chloride (CTAC) and 16ml (0.9mol) ultrapure water, add 2.6ml (0.0192mol) triethanolamine, stir To dissolve, heat up to 60°C, blow nitrogen, add 1.454ml (6.5mmol) tetraethyl orthosilicate (TEOS) dropwise at a certain speed (1mL / min), react for 2h, end the reaction, cool to room temperature, centrifuge ( 10000r / min, 15min), washed with water and ethanol respectively and centrifuged, dispersed in 90ml ethanol and 10ml hydrochloric acid (37%) mixed solution system, refluxed twice at 60°C for 2h each time. After reflux, wash with water and ethanol respectively, centrifuge and dry in vacuum (65°C, 12h).

[0029] 2. Preparation of mercapto mesoporous silica nanoparticles (MSNs-SH)

[0030]Mix 2.35ml (70.5mmol) ethanol, 0.56g (1.755mmol) cetyltrimethylammonium chloride (CTAC), 16ml (0.9mol) ultrapure water, add 2.6ml (0.0192mol) triethanola...

Embodiment 2

[0034] 1. Preparation of mesoporous silica nanoparticles (MSNs)

[0035] Mix 80mmol of ethanol, 1.850mmol of trioctylmethylammonium chloride and 1mol of ultrapure water, then add 0.0225mol of sodium hydroxide, stir until dissolved, heat up to 80°C, blow nitrogen, and use 1mL / min Add 7mmol of tetraethyl orthosilicate dropwise at a high speed, react for 2h, end the reaction, cool to room temperature, centrifuge (10000r / min, 15min), wash with water and ethanol, and then disperse in 90ml of ethanol and 10ml of hydrochloric acid (37%) after centrifugation In the mixed solution system, reflux twice at 60° C. for 2 hours each time; after reflux, wash with water and ethanol respectively, centrifuge and dry in vacuum (65° C., 12 hours).

[0036] 2. Preparation of mercapto mesoporous silica nanoparticles (MSNs-SH)

[0037] 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...

Embodiment 3

[0041] 1. Preparation of mesoporous silica nanoparticles (MSNs)

[0042] Mix 90mmol of ethanol, 1.65mmol of dodecyltrimethylammonium chloride and 0.75mol of ultrapure water, then add 0.0155mol of ammonia water, stir until dissolved, raise the temperature to 45°C, and blow nitrogen gas at 1mL / min Add 7mmol of tetrabutyl orthosilicate dropwise at a high speed, react for 2h, end the reaction, cool to room temperature, centrifuge (10000r / min, 15min), wash and centrifuge with water and ethanol respectively and disperse in 90ml ethanol and 10ml hydrochloric acid (37% ) in the mixed solution system, reflux twice at 60°C, each time for 2h; after the reflux, wash with water and ethanol respectively, centrifuge, and vacuum dry (65°C, 12h).

[0043] 2. Preparation of mercapto mesoporous silica nanoparticles (MSNs-SH)

[0044] 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...

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Abstract

The invention relates to mesoporous silica nanoparticles having a disulfiram monomer and a preparation method and application thereof. The method includes (1) preparing mesoporous silica nanoparticles; and (2) by utilizing disulfide bonds of disulfiram, preparing mesoporous silica nanoparticles having a disulfide-bond-containing disulfiram monomer (diethyldithiocarbamate), with the average particle size of the nanoparticles being 50-300 nm. The prepared nanoparticles having the disulfiram monomer are uniform in distribution and good in dispersibility, facilitate improvement on medicine targeting properties, increase medicine bioavailability, make drug preparation costs low, greatly reduce the treatment cost of patients and have potential market value and far-reaching 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 (>800m2 / g), large pore volume (>1XXZSZXcm3 / 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 and Drug relea...

Claims

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Application Information

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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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