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Preparation and applications of mesoporous silica/insulin nanoparticles modified by phenylboronic acid

A technology of mesoporous silica and silica, which is applied in the field of medicine, can solve the problem of one-way release of drugs, achieve the effect of stabilizing blood sugar levels, avoiding blood sugar fluctuations, and reducing the number of administrations

Inactive Publication Date: 2016-12-21
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the above situation, in order to overcome the defects of the prior art, the purpose of the present invention is to provide the preparation and application of phenylboronic acid-modified mesoporous silica / insulin nanoparticles, which can effectively solve the problem of one-way drug release from traditional drug carriers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] In concrete implementation, the present invention can be realized by the following steps:

[0022] (1) Preparation of mesoporous silica nanoparticles: Mix 3.0mL of sodium hydroxide solution with a molar concentration of 2mol / L and 400mL of distilled water, stir and add 1.0g of cetyltrimethylammonium bromide at 75°C , and then dropwise added 5.0mL tetraethyl orthosilicate, stirred for 1.5h, filtered, dried in vacuum, and calcined at 500°C for 3.5h to obtain mesoporous silica nanoparticles;

[0023] (2) Amination of mesoporous silica nanoparticles: Disperse 400mg of mesoporous silica nanoparticles in 40mL of anhydrous toluene, stir at room temperature, add 1.0mL of 3-aminopropyltrimethylaminosilane dropwise, and stir for 25min , heated to 100°C, refluxed for 24 hours, and suction filtered to obtain aminated mesoporous silica nanoparticles;

[0024] (3) Dissolve 40 mg of aminated mesoporous silica nanoparticles and 20 mg of insulin in 40 mL of hydrochloric acid solution, ...

Embodiment 2

[0027] In concrete implementation, the present invention can be realized by the following steps:

[0028] (1) Preparation of mesoporous silica nanoparticles: Mix 4.0mL of sodium hydroxide solution with a molar concentration of 2mol / L and 500mL of distilled water, stir and add 1.2g of cetyltrimethylammonium bromide at 85°C , and then dropwise added 5.8mL tetraethyl orthosilicate, stirred for 2.5h, filtered, vacuum-dried, and calcined at 600°C for 4.5h to obtain mesoporous silica nanoparticles;

[0029] (2) Amination of mesoporous silica nanoparticles: Disperse 600mg of mesoporous silica nanoparticles in 60mL of anhydrous toluene, stir at room temperature, add 2.0mL of 3-aminopropyltrimethylaminosilane dropwise, and stir for 35min , heated to 120°C, refluxed for 24 hours, and suction filtered to obtain aminated mesoporous silica nanoparticles;

[0030] (3) Dissolve 60mg of aminated mesoporous silica nanoparticles and 30mg of insulin in 60mL hydrochloric acid solution, and stir ...

Embodiment 3

[0033] In concrete implementation, the present invention can be realized by the following steps:

[0034] (1) Preparation of mesoporous silica nanoparticles: Mix 3.5mL of sodium hydroxide solution with a molar concentration of 2mol / L and 450mL of distilled water, stir and add 1.1g of cetyltrimethylammonium bromide at 80°C , and then dropwise added 5.2mL tetraethyl orthosilicate, stirred for 2h, filtered, vacuum-dried, and calcined at 550°C for 4h to obtain mesoporous silica nanoparticles;

[0035] (2) Amination of mesoporous silica nanoparticles: Disperse 500mg of mesoporous silica nanoparticles in 45mL of anhydrous toluene, stir at room temperature, add 1.2mL of 3-aminopropyltrimethylaminosilane dropwise, and stir for 30min , heated to 110°C, refluxed for 24 hours, and suction filtered to obtain aminated mesoporous silica nanoparticles;

[0036](3) Dissolve 50 mg of aminated mesoporous silica nanoparticles and 25 mg of insulin in 45 mL of hydrochloric acid solution, and stir...

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Abstract

The invention relates to preparation and applications of mesoporous silica / insulin nanoparticles modified by phenylboronic acid, for effectively solving the problem that the traditional drug carriers release medicines unidirectionally. The technical scheme is as follows: the preparation comprises the following steps: firstly, synthesizing mesoporous silica nanoparticles, modifying amino groups on the surfaces of the mesoporous silica nanoparticles, loading medicine insulin in the mesoporous structure through physical absorption, and further modifying with phenylboronic acid and polysaccharide, thus obtaining the mesoporous silica / insulin nanoparticles modified by phenylboronic acid. The preparation and applications have the advantages that the synthesis process is simple, the prepared nanoparticles have the good biocompatibility, and the releasing valve of medicines can be repeatedly opened and closed, so that the sustained-release effect is achieved on the release of medicines; the mesoporous silica / insulin nanoparticles have a long-time circulation in the body, so that the administration times can be reduced, and thus the mesoporous silica / insulin nanoparticles belong to an innovation in diabetes treatment medicines.

Description

technical field [0001] The invention relates to medicine, especially the preparation and application of mesoporous silicon dioxide / insulin nanoparticles modified by phenylboronic acid. Background technique [0002] Diabetes Mellitus (DM) is a common endocrine and metabolic disease whose etiology and pathogenesis are not yet fully understood. Chronic hyperglycemia is a syndrome characterized by disorders of fat and protein metabolism caused by insufficient secretion or action of insulin. Insulin treatment of diabetes began in 1922, and it is still the first choice drug for the treatment of type 1 diabetes and has an irreplaceable role. The route of administration of insulin is subcutaneous injection, and daily insulin injections maintain blood sugar levels, which reflects the control of diabetes to a certain extent, but this is still far from the regulation and maintenance of blood sugar levels by the pancreas under normal physiological conditions, and may cause Cause cardi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K38/28A61K47/48A61K47/24A61K47/36A61P3/10
CPCA61K9/5115A61K9/0019A61K38/28
Inventor 侯琳张振中郑亚珍单晓宁郝丽莎张银玲冯倩华
Owner ZHENGZHOU UNIV
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