Preparation method of mitochondria-targeting carrier containing small-molecule-drug-loading mesoporous silica encapsulated with DQA

A technology of mesoporous silica and small molecules, which is used in medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas. It can prevent the leakage of drugs in advance, improve the efficacy of drugs, and reduce the amount of losses.

Active Publication Date: 2018-11-30
广州智焜生物科技有限公司
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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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  • Preparation method of mitochondria-targeting carrier containing small-molecule-drug-loading mesoporous silica encapsulated with DQA
  • Preparation method of mitochondria-targeting carrier containing small-molecule-drug-loading mesoporous silica encapsulated with DQA
  • Preparation method of mitochondria-targeting carrier containing small-molecule-drug-loading mesoporous silica encapsulated with DQA

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] (1) Add 30ml of CTAC solution and 1.8g of TEA to 50ml of deionized water, and gently stir at 65°C for 2 h in a 100mL round bottom flask; then add 20ml of TEA to 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 ~150rpm, 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 decahydrogenated with 10 v / v% TEOS Naphthalene solution was replaced to maintain the same reaction conditions for the growth of the second dimension 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, ad...

Embodiment 2

[0031] (1) Add 20ml of CTAC solution and 1.5g of TEA to 36ml of deionized water, and gently stir at 65°C for 1.5h in a 100mL round bottom flask; then add 18ml of TEA to 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 30 mi...

Embodiment 3

[0035] (1) Add 40ml CTAC solution and 2.0g TEA to 450ml deionized water, and stir gently at 65°C for 1 h in a 100mL round bottom flask; then add 15ml of TEA to 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, 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, add an...

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Abstract

The invention discloses a preparation method of a mitochondria-targeting carrier containing small-molecule-drug-loading mesoporous silica encapsulated with DQA. The preparation method comprises: preparing three-dimensional dendritic silica nanoparticles; loading a drug into the pores through ultrasound, vacuum rotation and re-crystallization; and carrying out a reaction on the obtained material and a DQA single molecule through an ultrasonic probe so as to successfully coat the mesoporous silica with the DQA. According to the present invention, mesoporous silica is a hydrophilic substance, hasgood biocompatibility, and can efficiently deliver the drugs to the lesion; DQA has natural affinity to mitochondria, and can help deliver the drug to the mitochondria so as to effectively treat mitochondria-related diseases; and with the application of the DQA to coat the drug-loading mesoporous silica, the drug in the pore channel can be effectively prevented from the leakage in advance so as to reduce the drug loss, and the drug can be effectively introduced into the mitochondria so as to improve the efficacy.

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 Applications(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 广州智焜生物科技有限公司
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