Method for preparing PH response amino-modified three-dimensional dendritic silica nanoparticle carrier carrying hydrophilic small molecule drug

An amino-modified, silicon dioxide technology, applied in pharmaceutical formulations, drug combinations, drug delivery, etc., can solve problems such as adverse reactions, and achieve the effects of preventing drug leakage, reducing pressure, and degrading quickly.

Inactive Publication Date: 2018-12-18
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, due to the very active nature of 5-HMF, the drug is easy to change due to the stimulation of the external environment before reaching the lesion site, and its good hydrophilicity makes it easy for the drug to be released suddenly in the cell. The release of a large amount of drugs in the body will suddenly increase the blood drug level and cause adverse reactions in the body, thus limiting the promotion of 5-HMF

Method used

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  • Method for preparing PH response amino-modified three-dimensional dendritic silica nanoparticle carrier carrying hydrophilic small molecule drug
  • Method for preparing PH response amino-modified three-dimensional dendritic silica nanoparticle carrier carrying hydrophilic small molecule drug
  • Method for preparing PH response amino-modified three-dimensional dendritic silica nanoparticle carrier carrying hydrophilic small molecule drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1) Add 20 ml of CTAC solution and 0.2 g of TEA to 40 ml of deionized water, and gently stir at 60 °C for 1 h in a 100 mL round bottom flask;

[0030] (2) Then add 15 ml of 30 v / v % TEOS in 1-octadecene solution to the water-CTAC-TEA solution and keep it in an oil bath at 60 °C under magnetic stirring. The stirring rate was set at ~150 rpm, and then the reactant was kept at a constant temperature and stirred continuously for 24 h to obtain the first-dimensional product;

[0031] (3) Then, the upper phase 1-octadecene solution was completely removed and replaced with 20 v / v% TEOS in decahydronaphthalene to maintain the same reaction conditions for second-dimensional growth for another 24 h;

[0032] (4) For the third dimension, change the upper oil layer to 20 v / v% TEOS-cyclohexane solution, while keeping the reaction conditions under the same conditions for 24 h;

[0033] (5) Mix the carrier with 5-HMF at a ratio of 0.5:1 (m / m), disperse the carrier evenly by ultrasoun...

Embodiment 2

[0036] (1) Add 30ml of CTAC solution and 0.15g of TEA to 35ml of deionized water, and gently stir at 60°C for 1.5h in a 100mL round bottom flask;

[0037] (2) Then add 25ml of 30 v / v % TEOS in 1-octadecene solution to the water-CTAC-TEA solution and keep it in an oil bath at 60 °C under magnetic stirring. The stirring rate was set at ~150 rpm, and then the reactant was kept at a constant temperature and stirred continuously for 24 h to obtain the first-dimensional product;

[0038] (3) Then, the upper phase 1-octadecene solution was completely removed and replaced with 20 v / v% TEOS in decahydronaphthalene to maintain the same reaction conditions for second-dimensional growth for another 12 h;

[0039](4) For the third dimension, change the upper oil layer to 20 v / v% TEOS-cyclohexane solution, while keeping the reaction conditions at the same condition for 12 h;

[0040] (5) Mix the carrier and curcumin at a ratio of 0.75:1 (m / m), disperse the carrier evenly by ultrasound, the...

Embodiment 3

[0042] (1) Add 40 ml of CTAC solution and 0.1 g of TEA to 30 ml of deionized water, and gently stir at 60 °C for 2 h in a 100 mL round bottom flask;

[0043] (2) Then add 30 ml of 15 v / v % TEOS in 1-octadecene solution to the water-CTAC-TEA solution and keep it in an oil bath at 60 °C under magnetic stirring. The stirring rate was set at ~150 rpm, and then the reactant was kept at a constant temperature and stirred continuously for 24 h to obtain the first-dimensional product;

[0044] (3) Then, the upper phase 1-octadecene solution was completely removed and replaced with 20 v / v% TEOS in decahydronaphthalene to maintain the same reaction conditions for second-dimensional growth for another 48 h;

[0045] (4) For the third dimension, change the upper oil layer to 20 v / v% TEOS-cyclohexane solution, while keeping the reaction conditions at the same condition for 48 h;

[0046] (5) Mix the carrier and DOX at a ratio of 1:1 (m / m), disperse the carrier evenly by ultrasound, then r...

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Abstract

The invention discloses a method for preparing a PH response amino-modified three-dimensional dendritic silica nanoparticle carrier carrying a hydrophilic small molecule drug. The method comprises thefollowing steps: firstly, the drug is loaded into pores of a mesoporous nanocarrier by stirring with a magnetic force, the mesoporous nanocarrier is added into KH-550 for amino group modification ofthe surface of silicon spheres, by the amino group modification of the surface of the silicon spheres, the pores are blocked to prevent drug spillage, and after the drug is loaded into the pores, thePH response amino-modified three-dimensional dendritic silica nanoparticle carrier carrying the hydrophilic small molecule drug is obtained by dehydration condensation of hydroxyl groups on the KH-550and silicon hydroxyl groups on the surface of the silicon spheres. The pore diameter of the PH response amino-modified three-dimensional dendritic silica nanospheres gradually decreases from outsideto inside, the outermost pore diameter is the largest, the wall is thin and easy to degrade, and the drug is released with the degradation of the carrier, and a three-dimensional dendritic structure allows the nanoparticles to have a low degree of crosslinking and accelerate degradation.

Description

technical field [0001] The invention belongs to the technical field of biomaterials, and relates to an antioxidant drug silicon dioxide porous material with a slow-release pH response effect. Background technique [0002] Pentahydroxymethylfurfural (5-HMF) is a common Maillard reaction product and an important fine chemical raw material. It can be obtained by dehydrating glucose and fructose in fruits and plants such as garlic and algae. 5-HMF is a hydrophilic small molecular substance with very active chemical properties and has a furan ring, an aldehyde group and a hydroxymethyl group. Excessive 5-HMF has obvious biological toxicity, and only a small amount will show good anti-oxidation and anti-inflammatory effects. [0003] However, due to the very active nature of 5-HMF, the drug is easy to change due to the stimulation of the external environment before reaching the lesion site, and its good hydrophilicity makes it easy for the drug to be released suddenly in the cell...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/04A61K47/24A61K31/341A61P39/06A61P29/00
CPCA61K9/501A61K9/5015A61K31/341A61P29/00A61P39/06
Inventor 魏坤牛雪明罗逍万淑倩严柳柳
Owner SOUTH CHINA UNIV OF TECH
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