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A preparation method of a dqa-encapsulated mesoporous silica-carried small-molecule drug targeting mitochondrial carrier

A technology of mesoporous silica and mitochondria, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem of the reduction of the function of cells to remove metabolic waste and the reduction of the viability of living organisms , excessive accumulation of damaged proteins and organelles

Active Publication Date: 2021-05-14
广州智园生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Aging is the decrease in the function of cells to remove metabolic waste, resulting in the excessive accumulation of damaged proteins and organelles, thereby reducing the viability of living organisms

Method used

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  • A preparation method of a dqa-encapsulated mesoporous silica-carried small-molecule drug targeting mitochondrial carrier
  • A preparation method of a dqa-encapsulated mesoporous silica-carried small-molecule drug targeting mitochondrial carrier
  • A preparation method of a dqa-encapsulated mesoporous silica-carried small-molecule drug targeting mitochondrial carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] (1) Add 30ml of CTAC solution and 1.8g of TEA into 50ml of deionized water, and gently stir at 65°C for 2 h in a 100mL round bottom flask; then add 20ml of TEA into the water-CTAC-TEA solution 10 v / v % TEOS in 1-octadecene and kept in an oil bath at 60 °C under magnetic stirring. The stirring rate was set at ~150 rpm, then the reactant was kept at constant temperature and stirred continuously for 12 h to obtain the first-dimensional product; then, the upper phase 1-octadecene solution was completely removed and washed with 10 v / v% TEOS Hydronaphthalene solution was replaced to maintain the same reaction conditions for the second dimension growth for another 12 h; for the third dimension, the upper oil layer was changed to TEOS-cyclohexane solution while the reaction conditions were kept at the same conditions for 12 h.

[0027] (2) Mix the carrier with 5-HMF at a ratio of 0.5:1 (m / m), disperse the carrier evenly by ultrasound, then rotate in vacuum for 30 min, add an eq...

Embodiment 2

[0031] (1) Add 20ml of CTAC solution and 1.5g of TEA into 36ml of deionized water, and gently stir at 65°C for 1.5h in a 100mL round bottom flask; then add 18ml of TEA into the water-CTAC-TEA solution 10 v / v % TEOS in 1-octadecene and kept in an oil bath at 60 °C under magnetic stirring. The stirring rate was set at ~150 rpm, then the reactants were kept at constant temperature and stirred continuously for 24 h to obtain the first-dimensional product; then, the upper phase 1-octadecene solution was completely removed and washed with 10 v / v% TEOS Hydronaphthalene solution was replaced to maintain the same reaction conditions for the second dimension growth for another 24 h; for the third dimension, the upper oil layer was changed to TEOS-cyclohexane solution while the reaction conditions were kept at the same conditions for 24 h;

[0032] (2) Mix the carrier and curcumin (Curcumin) at a ratio of 0.75:1 (m / m), disperse the carrier evenly by ultrasound, then rotate in vacuum for ...

Embodiment 3

[0035] (1) Add 40ml CTAC solution and 2.0 g TEA to 450 ml deionized water, and stir gently at 65 °C for 1 h in a 100 mL round bottom flask; then add 15 ml of TEA to the water-CTAC-TEA solution 10 v / v % TEOS in 1-octadecene and kept in an oil bath at 60 °C with magnetic stirring. The stirring rate was set at ~150 rpm, and then the reactants were kept at a constant temperature and continuously stirred for 6 h to obtain the first-dimensional product; then, the upper phase 1-octadecene solution was completely removed and washed with 10 v / v% TEOS Hydronaphthalene solution was replaced to maintain the same reaction conditions for the second dimension growth for another 6 h; for the third dimension, the upper oil layer was changed to TEOS-cyclohexane solution while keeping the reaction conditions at the same conditions for 6 h;

[0036] (2) Mix the carrier with doxorubicin (DOX) at a ratio of 0.8:1 (m / m), disperse the carrier evenly by ultrasound, then rotate in vacuum for 30 min, ad...

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Abstract

The invention discloses a preparation method of a DQA-encapsulated mesoporous silicon dioxide-carried small-molecule drug targeting mitochondrial carrier. The method is as follows: first prepare three-dimensional dendritic mesoporous silica nanoparticles, load the drug in the pores by means of ultrasound, vacuum rotation and recrystallization, and then react with DQA single molecule through the ultrasonic probe to make DQA successfully Mesoporous silica coating. Mesoporous silica is a kind of hydrophilic substance, has good biocompatibility, and can effectively deliver drugs to the lesion site. DQA has a natural affinity for mitochondria, which can help deliver drugs to mitochondria and effectively treat diseases related to mitochondria. Using DQA to wrap the drug-loaded mesoporous silica, first, can effectively prevent the drug in the pores from leaking in advance and reduce the loss of the drug; second, the drug can be effectively brought into the mitochondria to improve the efficacy of the drug.

Description

technical field [0001] The invention belongs to the technical field of biological materials, and in particular relates to a preparation method of a DQA-loaded mesoporous silica-loaded small-molecule drug targeting mitochondrial carrier. Background technique [0002] Mitochondria are the main place for energy synthesis in cells and play an important role in maintaining normal physiological functions of cells. Mitochondria are not only the main energy output in the body, but also related to the generation of oxygen free radicals and the regulation of cell death process. [0003] Aging is the reduction of the function of cells to remove metabolic waste, resulting in the excessive accumulation of damaged proteins and organelles, thereby reducing the viability of living organisms. Aging is not only caused by loose skin and various skin problems, but also causes many related diseases, such as: cardiovascular and cerebrovascular diseases, neurological diseases (Parkinson), diabete...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K31/12A61K31/341A61K31/704A61K47/69A61K47/22
CPCA61K9/5123A61K31/12A61K31/341A61K31/704A61K47/6949
Inventor 魏坤牛雪明万淑倩罗逍
Owner 广州智园生物科技有限公司
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