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A kind of ester bond coupled nano diamond doxorubicin drug and its preparation method and application

A diamond doxorubicin and nanodiamond technology, which can be used in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve problems such as toxic side effects and strong drug resistance of tumor cells, and achieve stable chemical properties, low immunogenicity, good biocompatibility

Inactive Publication Date: 2017-10-17
SHANXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Doxorubicin is one of the most widely used small-molecule chemotherapy drugs, but due to defects such as non-selective drug distribution, doxorubicin has very serious side effects on normal tissues after entering the body
At the same time, if doxorubicin is used for a long time, it will also induce tumor cells to develop strong drug resistance.

Method used

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  • A kind of ester bond coupled nano diamond doxorubicin drug and its preparation method and application
  • A kind of ester bond coupled nano diamond doxorubicin drug and its preparation method and application
  • A kind of ester bond coupled nano diamond doxorubicin drug and its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0030] (1) Preparation of nanodiamond-polyethylene glycol (ND-PEG) nanoparticles

[0031] Accurately weigh 10 mg of carboxylated nano-diamonds, pass through dimethyl sulfoxide (DMSO), absolute ethanol (C 2 h 5 OH), sterile water (H 2 O) After washing, place in 10mL MES (0.1M, pH5.8) buffer solution, ultrasonically disperse for 30min to form a suspension, then add 2mg of EDC, 2.5mg of NHS, and stir at room temperature for 6h. Centrifuge for 5 minutes, remove the supernatant, and obtain nano-diamond precipitates with activated carboxyl groups;

[0032] Quickly disperse the nano-diamond precipitate with activated carboxyl group into 10mL BBS (0.1M, pH8.4) buffer solution, ultrasonically disperse for 10min to form a suspension, then add 3mg polyethylene glycol (H 2 N-PEG-COOH), continue to stir and react at room temperature for 12 hours. After the reaction is completed, collect the supernatant by high-speed centrifugation at 15,000 rpm for 5 minutes, and continue to wash with d...

Embodiment 2

[0038] (1)~(2) are prepared with embodiment 1

[0039] (3) Accurately weigh 10 mg of vacuum-dried nano-diamond-polyethylene glycol (ND-PEG-COOH), then add 10 mL of sterilized double-distilled water, ultrasonically disperse for 30 minutes to form a suspension, and then drop by drop into the dissolved 2 mg of doxorubicin-glycidol (DOX-GLY) in sterilized double distilled water, then add 2.0 mg of EDC, 2.5 mg of NHS, and then add a few drops of triethylamine to make the system pH about 8, then place in a water bath at 37 °C The pot was protected from light and stirred for 24 hours. After the reaction was completed, the supernatant was collected by high-speed centrifugation at 15,000 rpm for 5 minutes, washed 5 times with sterilized double-distilled water, and then washed with acetone until the supernatant was colorless. Ethylene glycol-glycidyl-doxorubicin (NPGD) nanomedicine, vacuum-dried and stored in the dark. All supernatants were collected and the volume was recorded for det...

Embodiment 3

[0041] Infrared spectroscopic characterization of nanoparticles

[0042] In order to confirm whether an ester bond is formed between nano-diamond-polyethylene glycol (ND-PEG-COOH) and glycidol-doxorubicin (GLY-DOX), respectively take a small amount of nano-particles and potassium bromide in a mass ratio of 1: 100 were mixed and ground into tablets, and their infrared spectra were measured.

[0043] figure 2 Infrared spectra of the prepared nanoparticles. Doxorubicin (DOX) is compared with the absorption peak of glycidyl-doxorubicin (GLY-DOX), by 3422cm -1 Red shifted to 3339cm -1 , and the absorption peak broadened, indicating that glycidol was successfully connected to the surface of doxorubicin. Compared with nanodiamond (ND), nanodiamond-polyethylene glycol (ND-PEG-COOH) appeared 1621cm -1 and 1656cm -1 double peaks, and this is the characteristic absorption peak of the amide bond, indicating that polyethylene glycol is connected to the diamond surface with an amide b...

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Abstract

The invention provides an ester bond-coupled nano-diamond doxorubicin drug, a preparation method and application thereof. The present invention first uses H2N‑PEG‑COOH to modify nano-diamonds, synthesizes ND‑PEG‑COOH carriers, and then makes the surface of adriamycin rich in hydroxyl groups through the ring-opening reaction of glycidol and doxorubicin, and finally utilizes ND‑PEG‑COOH The carboxyl group on the surface of the carrier reacts with the hydroxyl group on the surface of doxorubicin to produce the target drug nano-diamond-polyethylene glycol-glycidyl-doxorubicin (ND-PEG-GLY-DOX). The formation of ester bonds was confirmed by infrared spectrum characterization and in vitro drug release experiments. Cell cycle and apoptosis experiments were measured by MTT assay and flow cytometry, indicating that ND‑PEG‑GLY‑DOX can induce tumor cell apoptosis, which can It is used in the preparation of antitumor drugs.

Description

technical field [0001] The present invention relates to nano-medicines, in particular to nano-medicines prepared by covalently coupling doxorubicin to the modified nano-diamonds through ester bonds after surface modification of nano-diamonds, and the use of the drug in anti-tumor drugs Applications. Background technique [0002] The diet, environmental pollution, sedentary, smoking and other bad living habits in modern life make the incidence of tumors increase year by year. Adriamycin is one of the most widely used small molecule chemotherapeutic drugs, but due to defects such as non-selectivity of drug distribution, Adriamycin has very serious toxic side effects on normal tissues after entering the body. At the same time, if doxorubicin is used for a long time, it will also induce tumor cells to develop strong drug resistance. How to improve the specificity of doxorubicin distribution in vivo, enhance its chemotherapy efficacy, and minimize its toxic and side effects has...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/52A61K47/60C08G65/00A61K31/704A61P35/00
Inventor 李林李英奇杨斌盛
Owner SHANXI UNIV