Nano preparation of porous material coated alkynyl modified sorafenib derivative and silver, preparation method and application thereof

A technology of sorafenib and nano-preparation, applied in the directions of nanotechnology, nanotechnology, nanomedicine, etc., can solve problems such as increasing the survival time of patients, and achieve a good synergistic anti-tumor effect

Active Publication Date: 2022-07-22
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, previous studies have shown that Sorafenib can only show a good tumor inhibitory effect on about 1 / 3 of patients with liver cancer, and it does not significantly increase the survival time of patients.

Method used

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  • Nano preparation of porous material coated alkynyl modified sorafenib derivative and silver, preparation method and application thereof
  • Nano preparation of porous material coated alkynyl modified sorafenib derivative and silver, preparation method and application thereof
  • Nano preparation of porous material coated alkynyl modified sorafenib derivative and silver, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Synthesis of Alkynyl Modified Sorafenib Derivatives:

[0033] (1) Preparation of carboxylic acid intermediates

[0034] Sorafenib (3 g) and NaOH (3.87 g) were dissolved in 20 mL absolute ethanol solution, N 2 protection, and the reaction was refluxed at 80 °C for 8 h. After the reaction was completed, the organic solvent was removed by low pressure rotation, dilute hydrochloric acid (2 mol / L) was added to neutralize the excess alkali, the pH was adjusted to about 5, the color of the reaction solution changed from blue to light pink, and a gray solid was precipitated after continuing the reaction for 5h, Suction filtration with a Buchner funnel, washed with a small amount of distilled water, and dried in a vacuum drying oven at 40 o Dry at C overnight to obtain 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)picolinic acid (referred to as carboxylic acid intermediate) as a grey solid powder. .

[0035] (2) Preparation of acid chloride intermediates

[003...

Embodiment 2

[0042] Example 2 Preparation method of ZIF-8-encapsulated alkynyl-modified sorafenib derivatives (ASOR@ZIF-8 for short)

[0043] The preparation method of described ASOR@ZIF-8 is as follows:

[0044] With zinc nitrate and 2-methylimidazole, deionized water molar ratio 1: 25: 700, stir at room temperature to obtain white emulsion; In the obtained emulsion, add the alkynyl group prepared in Example 1 The modified sorafenib derivative was continuously stirred until uniform to obtain a suspension; the obtained suspension was transferred to a hydrothermal synthesis reactor, and the hydrothermal reaction was carried out at 130 °C for 1.5 h. After cooling, centrifugation, washing with ethanol solution, and drying, a white solid was obtained, which was ASOR@ZIF-8. Elemental analysis showed that the mass percentage of ASOR was 12.6%.

[0045] The molar ratio of the alkynyl-modified sorafenib derivative to the sum of the molar numbers of zinc nitrate, 2-methylimidazole and deionized wa...

Embodiment 3

[0047] Example 3 ZIF-8 encapsulated alkynyl-modified sorafenib derivatives and silver nanoformulations (ASOR-Ag for short) x @ZIF-8) preparation method

[0048] The ASOR-Ag x The preparation method of @ZIF-8 is as follows: Disperse 50 mg of the ASOR@ZIF-8 nanomaterial prepared in the above Example 2 in 10 mL of methanol solution with a concentration of 0.025 mol / L silver nitrate, stir and react for 6 h (stirring speed 400 rpm), centrifuged (10,000 rpm), washed with ethanol solution, and dried to obtain a white powder, which is ASOR-Ag x @ZIF-8, elemental analysis showed an ASOR mass percentage of 7.5%.

[0049] ASOR-Ag x TEM image of @ZIF-8 ( Figure 5 ) analysis showed that ASOR-Ag x Although @ZIF-8 maintains the approximate configuration of ZIF-8, the edges and corners of the polyhedral structure are completely blurred, and the size is comparable to that of ASOR@ZIF-8 (80~120 nm), and Ag can be clearly observed inside the ZIF-8 framework. presence of nanoparticles.

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Abstract

The invention relates to a nano preparation of porous material coated alkynyl modified sorafenib derivative and silver as well as a preparation method and application of the nano preparation. The size of the nano preparation is 80-120 nm; the porous material is ZIF-8; the nano preparation is prepared from a ZIF-8 porous material, an alkynyl modified sorafenib derivative and nano silver, in the nano preparation, the mass percentage content of the alkynyl modified sorafenib derivative is 7.3 to 7.7 percent. The nano preparation prepared by the invention has a good acid response targeted release function; the nano preparation prepared by the invention contains the alkynyl-modified sorafenib derivative and the silver ions, and has a good synergistic anti-tumor effect.

Description

technical field [0001] The invention relates to a composite nano-formulation, in particular to a nano-formulation in which alkynyl-modified sorafenib derivatives and silver are wrapped by a porous material, a preparation method and an application thereof, and belongs to the technical field of nano-formulations. Background technique [0002] Liver cancer is one of the most common clinical malignant tumors. Surgical removal of tumor tissue is the most effective way to treat early-stage liver cancer. However, most patients with liver cancer are already in the middle and advanced stages when diagnosed, and surgery is no longer available. Therefore, chemotherapy is the first choice for most patients with liver cancer. Although traditional chemotherapeutics can kill tumor cells to a certain extent, significant drug side effects will bring great pain to patients. Since chemotherapeutics also kill normal liver cells, in most cases, the life cycle of patients cannot be significantl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/38A61K31/44A61K47/69A61P35/00B82Y5/00B82Y40/00
CPCA61K33/38A61K31/44A61K47/6949A61P35/00B82Y5/00B82Y40/00A61K2300/00
Inventor 高广刚司呈帅亓永杰刘红张春晖
Owner UNIV OF JINAN
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