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Tumor microenvironment reduction responsive nano-drug and preparation method thereof

A tumor microenvironment and nano-drug technology, which is applied in the field of preparation of reduction-responsive anti-cancer nano-drugs, can solve toxicity and other problems, and achieve the effects of low biological toxicity, easy degradation, and convenient operation

Pending Publication Date: 2021-02-26
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although monomethoxypolyethylene glycol-racemic polylactic acid block copolymer pharmaceutical polymer excipients are low-toxic substances, it is generally believed that they have certain toxic effects when used in large quantities

Method used

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  • Tumor microenvironment reduction responsive nano-drug and preparation method thereof
  • Tumor microenvironment reduction responsive nano-drug and preparation method thereof
  • Tumor microenvironment reduction responsive nano-drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 (This part of the operation is protected from light during the whole process)

[0025] 1) Accurately weigh monomethoxy polyethylene glycol-succinimide carbonate (MPEG 2K -SC) 10.00g and cystamine dihydrochloride 3.36g were dissolved in 200ml of dichloromethane / methanol (100ml / 100ml) mixed solvent, after complete dissolution, 3.54g of triethylamine was added and reacted at room temperature for 12 hours.

[0026] 2) The solution after the reaction is saturated with 100ml NH 4 The Cl solution was washed twice, the organic phase was dried with anhydrous sodium sulfate and concentrated under reduced pressure, and the residue was slurried with 200 ml of methyl tert-butyl ether. MPEG can be obtained after vacuum drying at 50℃ 2k -SS-NH 2 .

Embodiment 2

[0027] Example 2 (This part of the operation is protected from light during the whole process)

[0028] 1) Accurately weigh tripterine 135mg, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) 172.5mg, 1-hydroxybenzotriazole (HOBT) 121.5mg, dissolved in 3ml of anhydrous DMF, completely dissolved, protected from light, and reacted at zero degrees Celsius for 2 hours.

[0029] 2) Accurately weigh MPEG 2k -SS-NH 2 210 mg, added to the reaction system in 1), protected from light, and continued to react at room temperature for 24 hours.

[0030]3) After the reaction, transfer the above organic solution to a cellulose dialysis membrane with a molecular weight cut-off of 2000, dialyze in 2L DMF for 24 hours (change the dialysate every 4 hours), and then transfer it to distilled water for dialysis for 24 hours (every 2 hours). Change distilled water once).

[0031] 4) After dialysis, transfer the aqueous solution in the dialysis bag to a glass petri dish, cover the ...

Embodiment 3

[0034] 1) Accurately weigh 10 mg of monomethoxypolyethylene glycol-SS-tripterine prodrug and dissolve it in 1.5 ml of tetrahydrofuran, and ultrasonically oscillate for 2 min to fully dissolve it.

[0035] 2) Then, under the condition of vigorous stirring, the solution was added to 10 ml of distilled water, and stirred at room temperature for 30 min.

[0036] 3) Remove tetrahydrofuran in the system by rotary evaporation under reduced pressure.

[0037] 4) Pass the solution treated by rotary evaporation through a 0.22 μm filter membrane to obtain MPEG with a particle size of 130-150nm 2K -SS-Cel micellar aqueous solution

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Abstract

The invention relates to a tumor microenvironment reduction responsive nano-drug and a preparation method thereof. The nano-drug is a nano-scale monomethoxypolyethylene glycol and celastrol compound (MPEG2k-SS-Cel) drug which takes safe and non-toxic monomethoxypolyethylene glycol (MPEG2k) with the molecular weight of about 2000 as a hydrophilic material, hydrophobic natural antitumor drug celastrol is chemically bonded through-SS-, MPEG2k-SS-Cel can be self-assembled into a nano-micelle with the particle size of about 140 nm, and the monomethoxypolyethylene glycol is used as a hydrophilic segment to embed the celastrol outside the micelle. The drug is bonded with the celastrol through the hydrophilic monomethoxypolyethylene glycol so as to overcome the defect that celastrol is difficult to effectively utilize in vivo due to hydrophobicity of the celastrol, and the nano-micelle has the characteristic that the micelle disintegrates and releases the drug in a tumor microenvironment due to fracture response under the condition of high-concentration glutathione (GSH) through the -SS- in the middle. Cell experiments detect that the nano-drug has efficient treatment effects.

Description

technical field [0001] The invention relates to a tumor microenvironment reduction-responsive nano-medicine and a preparation method thereof, which is a preparation method of a reduction-responsive anti-cancer nano-medicine. Background technique [0002] According to statistics, nearly 4.3 million people are diagnosed with cancer every year, that is to say, more than 8 people are diagnosed with cancer every minute in China. In addition, cancer is also a disease with a very high mortality rate. More than 2.8 million people die of cancer every year, and an average of 5 people die of cancer every minute. The main means of cancer treatment are surgical resection, chemotherapy and radiation therapy. Although these treatments have played an important therapeutic effect clinically, they cannot completely cure cancer. For example, although surgery can remove most of the tumor tissue, a small part of the tumor tissue that has not been removed may still recur. While chemotherapy dr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/60A61K47/69A61K31/56A61P35/00
CPCA61K47/60A61K47/6907A61K31/56A61P35/00
Inventor 于奡王永健黄晓龙郑佳
Owner NANKAI UNIV
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