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Targeting nano diamond carrier and targeted drug, and preparation method and application thereof

A nano-diamond and carrier technology, which is applied in the direction of drug combination, pharmaceutical formula, anti-infective drugs, etc., can solve the problems of application limitations, toxic and side effects of nanoparticles, etc., and achieve the effects of improving lethality, reducing toxic and side effects, and stabilizing chemical properties

Inactive Publication Date: 2013-07-17
SHANXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these nanoparticles have varying degrees of toxic side effects, so their clinical applications are limited

Method used

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  • Targeting nano diamond carrier and targeted drug, and preparation method and application thereof
  • Targeting nano diamond carrier and targeted drug, and preparation method and application thereof
  • Targeting nano diamond carrier and targeted drug, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] (1) Preparation of carrier nanodiamond-polyethylene glycol (ND-PEG-OH)

[0024] Dry 50.26mg of carboxylated nano-diamonds in a vacuum oven at 70°C overnight, place them in 3mL of anhydrous DMF solution, disperse ultrasonically to form a suspension, and then immediately add the suspension to 25mL of SOCl 2 , Refluxed at 70°C for 24h. After the reaction was completed, the above mixed solution was evaporated with a rotary evaporator at 40°C to remove excess SOCl 2 . Next, 30 mL of anhydrous DMF solution, 150.78 mg of PEG and 6 mL of triethylamine were added to the product obtained in (2), and refluxed at 90° C. for 24 h. Finally, the product was centrifuged at 15,000 rpm for 5 minutes, washed 5 times with redistilled water, and the supernatant was removed to obtain nanodiamond-polyethylene glycol and vacuum-dried.

[0025] (2) Preparation of targeting carrier nanodiamond-polyethylene glycol-transferrin (ND-PEG-Tf)

[0026] Disperse 10.8 mg of dry ND-PEG-OH in 20 mL of ...

Embodiment 2

[0032] (1) The preparation of the carrier nano diamond-polyethylene glycol (ND-PEG-OH) is the same as in Example 1;

[0033] (2) Preparation of targeting carrier nanodiamond-polyethylene glycol-transferrin (ND-PEG-Tf)

[0034] Disperse 10.8 mg of dry ND-PEG-OH in 20 mL of DMF solution, ultrasonically disperse for 30 min to form a suspension, then add 25.6 mg of SA and 24.4 mg of DMAP, and reflux at 90°C for 24 h. After the reaction is completed, centrifuge at 15000 rpm, wash with double distilled water for 5 times, remove the supernatant, and obtain ND-PEG-COOH precipitate. Disperse 1.0 mg of dry ND-PEG-COOH in 1.0 mL of boric acid (pH 8.0) buffer solution, ultrasonically disperse for 30 min to form a suspension, then add 2.0 mg of EDC to the suspension, and react for 30 min. Then, 500 μg Tf was placed in the suspension and shaken overnight on a shaker. Finally, the product was centrifuged at 15,000 rpm for 5 minutes, washed 5 times with double-distilled water, the supernata...

Embodiment 3

[0040] (1) The preparation of the carrier nano diamond-polyethylene glycol (ND-PEG-OH) is the same as in Example 1;

[0041] (2) Preparation of targeting carrier nanodiamond-polyethylene glycol-transferrin (ND-PEG-Tf)

[0042] Disperse 10.8 mg of dry ND-PEG-OH in 20 mL of DMF solution, ultrasonically disperse for 30 min to form a suspension, then add 25.6 mg of SA and 24.4 mg of DMAP, and reflux at 90°C for 24 h. After the reaction is completed, centrifuge at 15000 rpm, wash with double distilled water for 5 times, remove the supernatant, and obtain ND-PEG-COOH precipitate. Disperse 1.0mg of dry ND-PEG-COOH in 1.0mL boric acid (pH8.0) buffer solution, ultrasonically disperse for 30min to form a suspension, then add 2mg of EDC to this suspension, and react for 30min. Then, 1.0 mg Tf was placed in the suspension and shaken overnight on a shaker. Finally, the product was centrifuged at 15,000 rpm for 5 minutes, washed 5 times with double-distilled water, the supernatant was rem...

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Abstract

The invention provides a targeting nano diamond carrier ND-PEG-Tf and a preparation method, and a targeted nano-drug ND-PEG-Tf-DOX prepared by loading chemotherapeutic adriamycin through physical absorption. The carrier interacts with a human liver cancer cell (HepG2) and a normal liver cell (L-02) and free transferrin is taken as a competitor, and the result indicates that the ND-PEG-Tf carrier is mediated by a transferrin receptor into the cells; MTT testing of interaction of ND-PEG-Tf-DOX with the two cells indicates that the nano-drug has targeted anti-tumor effect on cancer cells; and compared with the cell damage force of independent adriamycin, ND-PEG-Tf-DOX has the characteristics of a slow-release drug. Therefore, ND-PEG-Tf-DOX is capable of either reducing toxic and side effects of chemotherapeutics on normal cells or improving the damage force of the chemotherapeutics on tumor cells. In addition, the targeting nano diamond carrier can be applied to preparing targeted anti-tumor drugs.

Description

technical field [0001] The present invention relates to a drug carrier, in particular to a targeted nano-diamond carrier, a targeted drug and its preparation method and application. More specifically, nano-diamonds are used as raw materials, polyethylene glycol is used as a bridge, and transferrin is covalently coupled Linking nanodiamonds, preparing nanodiamond-polyethylene glycol-transferrin (ND-PEG-Tf) targeting carrier, using physical adsorption to load chemotherapy drug doxorubicin to prepare targeted drug-loaded nano-drug ND-PEG-Tf- DOX, the nano-medicine can be used in anti-tumor drugs. Background technique [0002] The application of nanotechnology to cancer therapy and drug delivery has attracted much attention, opening the way for an emerging field with potential nanomedicines. In recent years, although the application of carbon nanomaterials, such as fullerenes and carbon nanotubes, in the biological field has made progress, the biocompatibility of these nanomate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K31/704A61P35/00A61P31/00
Inventor 李英奇王东新杨斌盛
Owner SHANXI UNIV
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