Preparation method of pH-responsive degradable hollow mesoporous organosilicon nanoparticle

A nanoparticle and organosilicon technology is applied in the field of preparation of pH-responsive degradable hollow mesoporous organosilicon nanoparticles, which can solve the problems of few types and limited applications, and achieve safe metabolism, increase loading, and avoid toxic and side effects. Effect

Active Publication Date: 2018-11-06
XUZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Redox and enzyme-responsive self-degradable silicone nanoparticles have been prepared by using alkoxysilane precursors containing disulfide bonds, but there are few types of such stimuli-responsive degradable silicone nanoparticles. Limit its application as an antitumor drug carrier

Method used

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  • Preparation method of pH-responsive degradable hollow mesoporous organosilicon nanoparticle
  • Preparation method of pH-responsive degradable hollow mesoporous organosilicon nanoparticle
  • Preparation method of pH-responsive degradable hollow mesoporous organosilicon nanoparticle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] (1) Dissolve 20.0g of terephthalaldehyde, 80.0g of dibromoneopentyl glycol and 0.5g of p-toluenesulfonic acid in 300ml of toluene, reflux at 100°C for 9 hours, cool to room temperature, and filter to obtain a white powder that is Aldehyde groups for pH-responsive small molecules.

[0025] (2) Add 1.0g of triethylamine, 1.5g of 3-aminopropyltriethoxysilane coupling agent, and 0.5g of pH-responsive small molecules into 20ml of tetrahydrofuran, react at 50°C for 5h, and add 30ml of n-hexane after the reaction , the ammonium salt was removed through a neutral alumina column, and the bridging alkoxysilane precursor containing a pH-responsive group was obtained by rotary evaporation and drying.

[0026] (3) Dissolve 2.0 g of cetyltrimethylammonium bromide in 20 ml of water, then add 1.0 g of triethylamine and 2.0 g of tetraethylorthosilicate, and react at 80° C. for 1 hour to obtain a silica template; Then add 4.0g mixed silicon source, mixed silicon source is made up of 2.0...

Embodiment 2

[0028] (1) Dissolve 25.0g of terephthalaldehyde, 90.0g of dibromoneopentyl glycol and 1.5g of p-toluenesulfonic acid in 1000ml of benzene, reflux at 120°C for 16h, cool to room temperature, and filter to obtain a white powder that is condensate Aldehyde groups for pH-responsive small molecules.

[0029] (2) Add 2.0g of triethylamine, 2.5g of 3-isocyanatopropyltrimethoxysilane coupling agent, and 1.5g of pH-responsive small molecules into 20ml of tetrahydrofuran, react at 80°C for 8h, and add 60ml of n-hexane after the reaction , the ammonium salt was removed through a neutral alumina column, and the bridging alkoxysilane precursor containing a pH-responsive group was obtained by rotary evaporation and drying.

[0030] (3) Dissolve 5.0g of cetyltrimethylammonium bromide in 50ml of water, then add 3.0g of triethylamine and 5.0g of tetraethyl orthosilicate, and react at 100°C for 1.5h to obtain a silica template ; Then add 7.0g mixed silicon source, mixed silicon source is compo...

Embodiment 3

[0032] (1) Dissolve 45.0g of terephthalaldehyde, 170.0g of dibromoneopentyl glycol and 2.0g of p-toluenesulfonic acid in 1200ml of toluene, reflux at 110°C for 12.5h, cool to room temperature, and filter to obtain a white powder. Acetal groups for pH-responsive small molecules.

[0033] (2) Add 1.5g of triethylamine, 2.0g of 3-aminopropyltriethoxysilane coupling agent, and 1.0g of pH-responsive small molecules into 10ml of dimethyl sulfoxide, and react at 65°C for 6.5h. After the reaction Add 30ml of n-hexane, remove the ammonium salt through a neutral alumina column, and dry by rotary evaporation to obtain a bridged alkoxysilane precursor containing a pH-responsive group.

[0034] (3) Dissolve 3.5g of cetyltrimethylammonium bromide in 35ml of water, then add 2.0g of triethylamine and 3.5g of tetraethylorthosilicate, and react at 90°C for 1 hour to obtain a silica template; Then add 5.0g mixed silicon source, mixed silicon source is made up of 1.5g tetraethyl orthosilicate an...

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Abstract

The invention discloses a preparation method of a pH-responsive degradable hollow mesoporous organosilicon nanoparticle. The preparation method comprises the following steps: at first, preparing a pH-sensitive micromolecule containing an acetal group; and then introducing the pH-sensitive micromolecule in a housing skeleton of the hollow mesoporous organosilicon nanoparticle to obtain the pH-responsive degradable hollow mesoporous organosilicon nanoparticle. A hollow mesoporous structure ensures that when being used as an anti-tumor drug carrier, the organosilicon nanoparticle has relatively high drug loading capacity; and under the weak acid condition, the organosilicon nanoparticle can be degraded, so that the loaded drug can be efficiently released, the degradation of the organosiliconnanoparticle ensures the safety metabolism of the carrier, the toxicity enrichment is avoided, and more selectivity is provided for preparing the anti-tumor drug carrier.

Description

technical field [0001] The invention belongs to the technical field of nanocomposite materials, in particular to a method for preparing pH-responsive degradable hollow mesoporous organic silicon nanoparticles. Background technique [0002] At present, chemotherapy is one of the main means of clinical treatment of cancer, but anti-tumor drugs have huge side effects, which will cause irreversible damage to the normal tissues of the human body during the treatment process, reduce the immune ability of the human body, and lead to a decrease in the utilization rate of the drug. delayed treatment. The reason is mainly due to the non-selectivity of anti-tumor drugs leading to their wide distribution in the human body. Therefore, designing safe and efficient drug carriers to improve the utilization efficiency of antitumor drugs and reduce their side effects has always been a research hotspot. [0003] As a drug carrier, mesoporous silica nanoparticles MSN have unique structural an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/24A61K31/704A61P35/00C07F7/18
CPCA61K31/704A61K47/24A61P35/00C07F7/1892
Inventor 杨舜范界王亚茹林诗婷
Owner XUZHOU NORMAL UNIVERSITY
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