A Folic Acid Modified Realgar-Mesoporous Silica Nanocomposite Drug

A technology of mesoporous silica and folic acid, applied in the directions of nano-drugs, drug combinations, nano-technology, etc., can solve the problems of normal cytotoxicity and side effects, and achieve the effects of easy modification, high yield and simple synthesis process

Inactive Publication Date: 2018-07-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the nano-realgar prepared by the above method also has certain toxic and side effects on normal cells while killing tumor cells.

Method used

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  • A Folic Acid Modified Realgar-Mesoporous Silica Nanocomposite Drug
  • A Folic Acid Modified Realgar-Mesoporous Silica Nanocomposite Drug
  • A Folic Acid Modified Realgar-Mesoporous Silica Nanocomposite Drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Synthesis of Mesoporous Silica Nanoparticles

[0041] At room temperature, weigh 0.7g of cetyltrimethylammonium bromide and place it in a 50mL round bottom flask, add 17.50mL of deionized water and heat and stir at 60°C. g, after stirring evenly, add 1.50mL tetraethyl orthosilicate dropwise, keep stirring at 60°C for 2 hours, centrifuge the reaction mixture, wash it with deionized water until neutral, wash it with absolute ethanol three times, and place it in a vacuum at 60°C Let dry overnight. Weigh 1.0 g of the above product in 200 mL of acidic ethanol (containing 20 mL of 36% concentrated hydrochloric acid), reflux at 60°C for 12 hours, centrifuge, wash with absolute ethanol three times, and then vacuum-dry at 60°C overnight to obtain mesoporous silica nanoparticles . The nanoparticles have a uniform particle size and a dispersed spherical shape, and the transmission electron microscope image is shown in figure 1 , it can be seen that the particle size distributio...

Embodiment 2

[0043] Synthesis of Aminated Mesoporous Silica Nanoparticles

[0044] At room temperature, weigh 0.7g of mesoporous silica nanoparticles into a 10mL round bottom flask, add 2.50mL of absolute ethanol to stir and disperse, measure 1.50mL of 3-aminopropyltriethoxysilane and dissolve it in 3.00mL of absolute ethanol , into the above-mentioned round-bottomed flask, stirred at room temperature for 48 hours, centrifuged, washed with absolute ethanol three times, and then vacuum-dried at 60°C overnight to obtain aminopropyl-modified mesoporous silica nanoparticles. The elemental analysis results of the nanoparticles show: N, 2.47%; C, 10.70%; H, 3.04%. Compared with the mesoporous silicon oxide nanoparticles, nitrogen element appears, and the infrared spectrum is shown in Figure 5 , 2936cm -1 (v C-H ) and 1473cm -1 (δ C-H ) absorption peak proves the existence of propyl group, which further illustrates the successful introduction of aminopropyl group by the post-grafting method....

Embodiment 3

[0046] Synthesis of Folic Acid Modified Mesoporous Silica Nanoparticles

[0047] At room temperature, weigh 0.2 g of folic acid in a round-bottomed flask, add 15.00 mL of dimethyl sulfoxide to dissolve it ultrasonically, add 0.1 g of N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3 -Ethylcarbodiimide hydrochloride 0.5g, stirred at room temperature for 1 hour in the dark, then added 50 mg of aminated mesoporous silica nanoparticles, continued to stir in the dark for 20 hours, centrifuged the reaction mixture, and washed with phosphoric acid with a pH of 7.00 After washing with salt buffer solution for three times, vacuum drying was performed to obtain folic acid-modified mesoporous silica nanoparticles. Its infrared spectrum is shown in Figure 5 , Curve a is the infrared spectrum of aminopropyl modified mesoporous silica nanoparticles, b is the infrared spectrum of folic acid modified mesoporous silica nanoparticles, and c is the infrared spectrum of folic acid, where 169...

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Abstract

Aiming at the defect that nano-realgar also has certain toxic and side effects on normal cells, the present invention modifies folic acid on the surface of mesoporous silica nanoparticles, and then loads realgar, aiming at improving its active targeting in vivo, and specifically relates to a folic acid-modified Realgar-mesoporous silicon oxide nanocomposite drug and preparation method thereof. In the present invention, by investigating the volume ratio of ethylenediamine to water, the concentration of realgar ethylenediamine solution, the carrier amount and the loading time, it is found that the folic acid-modified mesoporous silica nanoparticles have a certain loading capacity for realgar, forming a folic acid-modified Realgar-mesoporous silica nanocomposite drugs, and its morphology and structure have not changed significantly, but its targeting properties need to be further verified by in vitro cell experiments.

Description

technical field [0001] The patent of the present invention relates to the technical field of preparation of mesoporous materials and pharmaceutical preparations, in particular to a folic acid-modified realgar-mesoporous silica nanocomposite drug and a preparation method thereof. Background technique [0002] Realgar, a mineral medicine, is a traditional Chinese medicine with a long history of application in traditional Chinese medicine. It was first recorded in "Shen Nong's Materia Medica". 4 S 4 ), and mixed with a small amount of arsenic (As 2 o 3 ) and other heavy metal salts, used for detoxification, insecticide, dampness, phlegm, malaria, etc. Since the 1950s, many domestic scholars have used realgar-containing compound preparations or single realgar for clinical treatment of tumors in the blood system and other parts of the human body, and achieved good curative effects. And because its toxicity is lower than arsenic injection, realgar is recommended as a second-li...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/04A61K47/22A61K33/36B82Y5/00A61P35/00
Inventor 陈金龙沈玲玲刘忠莹狄斌
Owner CHINA PHARM UNIV
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