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Mesoporous silica drug-loaded nanoparticles coated with a ph-responsive Schiff base copolymer and its preparation method and application

A kind of mesoporous silica, drug-loaded nanotechnology

Active Publication Date: 2020-08-18
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the drug-loading system that uses polymers to block mesoporous silica usually initiates polymerization on the surface of mesoporous silica, and uses different stimuli to induce the change of the hydrophilicity and hydrophobicity of the polymer to trigger the exposure of mesoporous pores, but the polymer does not Falling off from the surface of mesoporous silica, thus hindering the diffusion of drugs, resulting in low drug release efficiency

Method used

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  • Mesoporous silica drug-loaded nanoparticles coated with a ph-responsive Schiff base copolymer and its preparation method and application
  • Mesoporous silica drug-loaded nanoparticles coated with a ph-responsive Schiff base copolymer and its preparation method and application
  • Mesoporous silica drug-loaded nanoparticles coated with a ph-responsive Schiff base copolymer and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] (1) Preparation of mesoporous silica containing surfactant: Take 0.2 parts by mass of CTAB, 0.7 parts by volume of NaOH solution (2M) and 96 parts by volume of water and mechanically stir for 0.5h, then quickly add 1.0 parts by volume of ethyl orthosilicate Esters, the temperature was raised to 80°C, and the reaction was continued for 2h. After the reaction was completed, it was naturally cooled to room temperature, centrifuged at 10,000 rpm, washed with water several times, and vacuum-dried at 30°C for 24 hours to obtain a white powder (MSN@CTAB).

[0070] The parts by weight of the reactants in the step (1) are as follows: 0.20 parts of CTAB; 0.06 parts of sodium hydroxide; 0.96 parts of TEOS; 98.78 parts of water.

[0071] (2) Preparation of surface aminated mesoporous silica: disperse 0.5 parts by mass of MSN@CTAB in 20 parts by volume of anhydrous toluene, N 2 Reflux at 80°C for 2 hours, add 0.75 parts by volume of silane coupling agent APTES dropwise with a syrin...

Embodiment 2

[0087] (1) Preparation of mesoporous silica containing surfactant: after mechanically stirring 0.15 parts by mass of CTAB, 3.75 parts by volume of TEOA solution and 96 parts by volume of water for 0.5 h, quickly add 1.0 parts by volume of ethyl orthosilicate, and heat up To 80 ℃, continue to react for 2h. After the reaction was completed, it was naturally cooled to room temperature, centrifuged at 10,000 rpm, washed with water several times, and vacuum-dried at 30°C for 24 hours to obtain a white powder (MSN@CTAB).

[0088] The parts by weight of the reactants in the step (1) are as follows: 0.15 parts of CTAB; 0.06 parts of TEOA; 0.95 parts of TEOS; 98.78 parts of water.

[0089] (2) Preparation of surface aminated mesoporous silica: disperse 0.6 parts by mass of MSN@CTAB in 20 parts by volume of anhydrous toluene, N 2 Reflux at 80°C for 2 hours, add 0.5 parts by volume of silane coupling agent APS dropwise with a syringe, N 2 Reflux at 80°C for 24h. After the reaction was...

Embodiment 3

[0096] (1) Preparation of mesoporous silica containing surfactant: after mechanically stirring 0.25 parts by mass of CTAB, 2.5 parts by volume of ammonia and 96 parts by volume of water for 0.5 h, quickly add 1.0 parts by volume of ethyl orthosilicate, and heat up to 80°C, continue to react for 2h. After the reaction was completed, it was naturally cooled to room temperature, centrifuged at 10,000 rpm, washed with water several times, and vacuum-dried at 30°C for 24 hours to obtain a white powder (MSN@CTAB).

[0097] The parts by weight of the reactants in the step (1) are as follows: 0.15 parts of CTAB; 0.06 parts of TEOA; 0.95 parts of TEOS; 98.78 parts of water.

[0098] (2) Preparation of surface aminated mesoporous silica: disperse 0.5 parts by mass of MSN@CTAB in 20 parts by volume of anhydrous toluene, N 2 Reflux at 80°C for 2 hours, add 1.0 volume parts of silane coupling agent APTES dropwise with a syringe, N 2 Reflux at 80°C for 24h. After the reaction was complet...

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Abstract

The invention belongs to the technical field of biomedical nanomaterials, and discloses a pH-responsive schiff base copolymer-coated mesoporous silica drug-loaded nanoparticle as well as a preparationmethod and application thereof. The nanoparticle provided by the invention comprises a mesoporous silica nanoparticle, a drug loaded inside the mesoporous silica nanoparticle, and a polymer modifiedon a surface of the mesoporous silica nanoparticle; and the polymer modified on a surface of the mesoporous silica nanoparticle is specifically P (PEGMA-co-MAEBA) modified on the surface of the mesoporous silica nanoparticle by an imine bond. The nanoparticle material provided by the invention has good biocompatibility, and realizes controlled release of the drug by utilizing an acid-sensitive imine bond; the drug is hardly released around normal cells, but the imine bond is broken in a slightly acidic environment of tumor cells, and the polymer falls off to rapidly release the drug, thereby realizing targeted therapy for the tumors; and the nanoparticle material is applicable to the field of controlled release of drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedical nanomaterials, and in particular relates to a pH-responsive Schiff-base copolymer-coated mesoporous silicon dioxide drug-loaded nanoparticle and a preparation method and application thereof. Background technique [0002] Cancer is one of the most complex and challenging diseases, which seriously threatens human life and health. Therefore, many anti-cancer drug delivery systems have been researched and developed, among which mesoporous silica nanoparticles (MSN) have large specific surface area and internal pore volume, adjustable pore size, highly ordered structure, and rich active hydroxyl groups on the surface. Modification, as well as good biocompatibility, low cost and other advantages, are particularly suitable for use as drug delivery materials. In addition, the effect of "zero leakage" can be achieved by blocking mesopores, which shows good application prospects in the field of anticanc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/32A61K9/51A61K31/337A61K31/4745A61K31/704A61P35/00
CPCA61K9/5146A61K31/337A61K31/4745A61K31/704A61K47/6925A61K47/6949A61P35/00
Inventor 章莉娟彭诗元袁晓哲
Owner SOUTH CHINA UNIV OF TECH
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