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Quercetin drug-loading system based on copper sulphide-metal organic frame material

A metal-organic framework and drug-carrying system technology, applied in the field of medicine, to achieve the effects of low cytotoxicity, improved anti-cancer effect, and good curative effect

Active Publication Date: 2018-09-14
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, no quercetin-targeted drug delivery system entrapped by MOF materials has been disclosed.

Method used

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  • Quercetin drug-loading system based on copper sulphide-metal organic frame material
  • Quercetin drug-loading system based on copper sulphide-metal organic frame material
  • Quercetin drug-loading system based on copper sulphide-metal organic frame material

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of FA-BSA / CuS@ZIF-8-QT

[0049] 1) A certain amount of PVP is dissolved in water, and copper chloride pentahydrate is added. After stirring at room temperature for 30 minutes, sodium sulfide was added, followed by reaction in an oil bath at 90°C for 15 minutes. After cooling to room temperature, CuS NPs were collected by centrifugation and dispersed in methanol. 2-Methylimidazole was dissolved in methanol, mixed with the above-mentioned CuS methanol solution, after stirring for a period of time, zinc nitrate was added, and the stirring was continued for 1 hour. The gray-black precipitate was collected by centrifugation and dispersed into methanol. Quercetin was dissolved in methanol, mixed with a certain amount of CuS@ZIF-8 dispersion and stirred at room temperature for one day. CuS@ZIF-8-QT was collected by centrifugation, washed twice with methanol, then twice with deionized water, and finally freeze-dried to obtain a yellow-brown powder.

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Embodiment 2

[0051] Example 2 Morphological observation of FA-BSA / CuS@ZIF-8-QT nanoaggregates

[0052] Take about 20 μL of CuS@ZIF-8 and FA-BSA / CuS@ZIF-8-QT methanol suspension respectively, drop them on the carbon-coated copper mesh, absorb the excess liquid with filter paper, dry them under infrared light and place them under the transmission electron microscope Observe the morphology of FA-BSA / CuS@ZIF-8-QT nanoaggregate. Electron microscope photos such as figure 2 As shown, FA-BSA / CuS@ZIF-8-QT is a spherical shape with uniform particle size, good dispersion, and a particle size of about 40nm, which meets the particle size requirements for intravenous injection and passive targeting.

Embodiment 3

[0053] Embodiment 3 quercetin stability change research

[0054] Accurately weigh a certain amount of quercetin with an analytical balance, dilute with distilled water to prepare a suspension of 500 μg / mL, take a certain amount of CuS@ZIF-8-QT and FA-BSA / CuS@ZIF-8-QT, and configure suspension in distilled water with the same concentration of quercetin. Then take 1 mL of the above suspension, add 0.5 mL of 0.1 M hydrochloric acid, and dissolve with 8.5 mL of methanol. Measure their UV absorbance. In the following 5 hours, repeat the above operation every half hour, measure and record the corresponding ultraviolet absorption. The changes in the relative intensity of ultraviolet absorption in each group are as follows: image 3 shown. The results showed that after dispersing in water for 5 h, the relative UV absorption intensity of free quercetin decreased by about 75%, indicating that it decomposed rapidly; while the relative UV absorption of CuS@ZIF-8-QT NP group decreased ...

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Abstract

The invention discloses a quercetin drug-loading system based on a copper sulphide-metal organic frame material. A metal organic frame zeolite imidazolate framework material (ZIF-8) is generated on the surfaces of copper sulphide nano-particles (CuS NPs) as a photothermal preparation to obtain a CuS@ZIF-8 carrier, quercetin is adsorbed into a carrier, and then is modified by a stabilizer and a targeting agent FA-BSA, and thus, a nano delivery system (FA-BSA / CuS@ ZIF-8) with a targeting active effect and pH response can be formed. The water solubility and the chemical stability of the quercetinare improved, good curative effect of treating tumors by combination of phototherapy and chemotherapy can further be played, meanwhile, drug can be rapidly released under the condition of low pH in atumor microenvironment, the tumor cell intake of a pharmaceutic preparation is further enhanced, and the quercetin drug-loading system based on the copper sulphide-metal organic frame material has low toxicity to normal cells, and is good in biological compatibility.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the preparation, characterization and in vitro evaluation of the anti-tumor effect of a quercetin drug-loading system based on copper sulfide nanoparticles metal-organic framework materials. Background technique [0002] Cancer is a major killer that threatens human life and health in today's society, and its morbidity and mortality have increased year by year in recent years. Among various treatment methods, chemotherapy is one of the most effective ways to inhibit tumor cell proliferation and promote tumor cell apoptosis by using chemical drugs through different mechanisms of action, such as interfering with DNA replication. However, most anticancer drugs have severe side effects in clinical practice, such as skin and mucous membrane reactions, hair loss, and side effects on various organs. Therefore, there is an urgent need to find and develop new anticancer drugs. [0003]...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K31/352A61K9/19A61K47/22A61P35/00
CPCA61K9/19A61K31/352A61K41/0052A61K47/22A61P35/00A61K2300/00
Inventor 栾玉霞蒋伟李钟号
Owner SHANDONG UNIV
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