A kind of drug-loaded silicon dioxide nanoparticles and its preparation method and application

A silicon dioxide and nanoparticle technology, used in pharmaceutical formulations, drug combinations, medical preparations with inactive ingredients, etc., can solve the problems of low free drug concentration, cell oxidative damage, weak heavy metal binding ability, etc., to avoid blood The effect of high concentration, uniform particle size distribution and excellent monodispersity

Active Publication Date: 2020-09-11
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, heavy metals can also generate free radicals through the free radical reaction of the human body, causing oxidative damage to cells, which is extremely toxic
[0004] Dimercaptosuccinic acid is a heavy metal detoxification drug commonly used clinically, but its heavy metal binding ability is weak, and the absorption rate of the drug after oral administration is only 20%, and it is easy to cause intestinal disorders, and the plasma protein binding rate is as high as 95%. Low free drug concentration
In addition, dimercaptosuccinic acid is insoluble in water and cannot purify heavy metals in sewage

Method used

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  • A kind of drug-loaded silicon dioxide nanoparticles and its preparation method and application
  • A kind of drug-loaded silicon dioxide nanoparticles and its preparation method and application
  • A kind of drug-loaded silicon dioxide nanoparticles and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] (1) Weigh 0.45g of CTAB and 0.47g of Brij58, add 120ml of PB buffer solution with a pH of 7.0, dissolve in a water bath at 60°C, and slowly add 2.14ml of TEOS dropwise after the temperature of the reaction system is stable, and continue magnetic stirring for 45min Afterwards, 180 μL of 3-mercaptopropyltriethoxysilane was slowly added dropwise, reacted for 8 hours, filtered, and the filter cake was washed twice with deionized water. Then, wash twice with absolute ethanol, disperse in 150ml of absolute ethanol (containing 2ml of concentrated hydrochloric acid), heat and reflux in a water bath at 78°C for 8h, and repeat the operation of washing with absolute ethanol and refluxing in absolute ethanol containing concentrated hydrochloric acid for 3 times, and then washed 3 times with absolute ethanol to prepare mercaptolated mesoporous silica nanoparticles, and the obtained mercaptolated mesoporous silica nanoparticles (MSN-SH) were dispersed in ethanol for storage.

[0062]...

Embodiment 2

[0077] Ultrasonic dispersion of 100 mg of thiolated mesoporous silica nanoparticles prepared in step (1) of Example 1 above was dispersed in 20 ml of methanol, 80 mg of dimercaptosuccinic acid was added thereto, stirred for 24 hours at room temperature in the dark, and centrifuged (15000 rpm , 10 min), the nanoparticles were collected and washed 6 times with methanol to obtain the adsorption-type silica nanoparticles (MSN-SH adsorbed DMSA).

[0078] After MSN-SH absorbs DMSA, adopt the method in embodiment 1 to carry out Raman spectrum detection, by Figure 6 It can be seen that at 2560cm -1 There are sulfhydryl peaks, indicating the existence of sulfhydryl and DMSA sulfhydryl on the material, and at 510cm -1 There is no absorption peak of the disulfide bond, which shows that the two are not coupled.

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Abstract

The invention provides a drug-loaded silica nanoparticle, and a preparation method and application thereof. The drug-loaded silica nanoparticle contains dimercaptosuccinic acid and a sulfhydrylated mesoporous silica nanoparticle, wherein dimercaptosuccinic acid is optionally coupled with the sulfhydrylated mesoporous silica nanoparticle. The drug-loaded silica nanoparticle provided by the invention is uniform in particle size distribution, excellent in monodispersity and applicable to environmental purification (e.g., sewage treatment). Moreover, the drug-loaded silica nanoparticle can perfectly load cells with a heavy-metal detoxifying drug, so toxic and side effect caused by too high blood concentration of the drug is avoided, and accumulation of the heavy-metal detoxifying drug in the cells is substantially increased; and the drug-loaded silica nanoparticle is high in capability of binding with heavy metals, has the characteristics of environment responsiveness and intelligent release, and can be applied to detoxifcation of heavy metals in the body and to biomedicine and the like.

Description

technical field [0001] The invention relates to a drug-loaded silicon dioxide nanoparticle, a preparation method and application thereof. Background technique [0002] With the rapid development of modern industry and the wide application of heavy metals in industry and agriculture, while people are enjoying the convenience of life, food and environmental pollution caused by human activities are also intensifying. One of the most serious hazards is heavy metal pollution, which seriously endangers human health. [0003] Heavy metal refers to the density greater than 4.5Kg / cm 3 metals, such as Au, Ag, Hg, Cu, Pb, Cd, etc. Many heavy metals can enter the human body through food, destroying the normal physiological functions of the human body and damaging human health. Heavy metals chelate with the active site of the enzyme, causing the conformation of the protein to change, thereby inactivating the enzyme and disrupting the normal physiological metabolism of the cell. In ad...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/52A61K33/00A61K31/191A61P39/02
CPCA61K31/191A61K33/00A61K2300/00
Inventor 吴强王玉丽李桂玲翟宏强侯冠华陈艳君于菲菲高春生
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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