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Nanocomposite applicable to tumor diagnosis and targeted therapy and preparation method thereof

A nano-composite, targeted therapy technology, applied in the preparations for in vivo experiments, anti-tumor drugs, medical preparations with inactive ingredients, etc., can solve problems such as dilution, reduce aggregation, improve therapeutic effects, and The effect of cycle time

Inactive Publication Date: 2018-08-24
FUZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, HA nanoparticles have a disadvantage after systemic administration, that is, after the nanoparticles enter the blood circulation, the concentration is greatly diluted, and they are easily transported to the liver and kidneys for metabolism, and only a very small amount of nanoparticles remain in the blood

Method used

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  • Nanocomposite applicable to tumor diagnosis and targeted therapy and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0012] 1) Weigh 1.000 g of formylated hyaluronic acid, dissolve in 100 mL of double-distilled water, and stir magnetically until completely dissolved;

[0013] 2) Weigh 0.504 g and 0.303 g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide respectively and add to the solution obtained in step 1) to avoid light Reaction for 4 h;

[0014] 3) Weigh 0.25 g of Cy5.5-labeled polyethylene glycol and add it to the solution obtained in step 2) to react for 8 h;

[0015] 4) Place the solution obtained in step 3) in a dialysis bag of MWCO 3500 for dialysis at room temperature for 3 days, during which the water was changed every 8 hours, and freeze-dried for 3 days to obtain Cy5.5-labeled polyethylene glycol grafted aldehyde groups hyaluronic acid;

[0016] 5) Weigh 1.000 g of Cy5.5-labeled polyethylene glycol-grafted hyaluronic acid, dissolve it in double-distilled water at 37°C, and prepare 10 mg / mL of Cy5.5-labeled polyethylene glycol-grafted Ald...

Embodiment 2

[0022] 1) Weigh 1.000 g of formylated hyaluronic acid, dissolve in 100 mL of double-distilled water, and stir magnetically until completely dissolved;

[0023] 2) Weigh 0.504 g and 0.303 g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide respectively and add to the solution obtained in step 1) to avoid light Reaction for 4 h;

[0024] 3) Weigh 0.25 g of Cy5.5-labeled polyethylene glycol and add it to the solution obtained in step 2) to react for 8 h;

[0025] 4) Place the solution obtained in step 3) in a dialysis bag of MWCO 3500 for dialysis at room temperature for 3 days, during which the water was changed every 8 hours, and freeze-dried for 3 days to obtain Cy5.5-labeled polyethylene glycol grafted aldehyde groups hyaluronic acid;

[0026] 5) Weigh 1.000 g of Cy5.5-labeled polyethylene glycol-grafted hyaluronic acid, dissolve it in double-distilled water at 37°C, and prepare 10 mg / mL of Cy5.5-labeled polyethylene glycol-grafted Ald...

Embodiment 3

[0032] 1) Weigh 1.000 g of aldehyde-based hyaluronic acid, dissolve it in 100 mL of double-distilled water, and stir magnetically until it is completely dissolved;

[0033] 2) Weigh 0.504 g and 0.303 g of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide, respectively, and add them to the solution obtained in step 1) to protect from light. reaction for 4 hours;

[0034] 3) Weigh 0.25 g of Cy5.5 labeled polyethylene glycol and add it to the solution obtained in step 2) to react for 8 h;

[0035] 4) The solution obtained in step 3) was placed in a dialysis bag of MWCO 3500 for 3 d at room temperature, during which the water was changed every 8 h, and freeze-dried for 3 d to obtain Cy5.5-labeled polyethylene glycol grafted aldehyde group. hyaluronic acid;

[0036] 5) Weigh 1.000 g of Cy5.5-labeled polyethylene glycol grafted aldehyde-ylated hyaluronic acid, dissolve it in double distilled water at 37 °C, and prepare 10 mg / mL of Cy5.5-labeled p...

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Abstract

The invention discloses a nanocomposite applicable to tumor diagnosis and targeted therapy and a preparation method thereof. The preparation method comprises the following steps: firstly grafting Cy5.5-labeled polyethylene glycol amine onto the aldehyde hyaluronic acid through an amidation reaction to obtain Cy5.5-labeled polyethylene glycol grafted aldehyde hyaluronic acid, then compounding withcisplatin through ion coordination and a Schiff base reaction to obtain a cisplatin-Cy5.5-labeled polyethylene glycol grafted aldehyde hyaluronic acid nanocomposite. By the preparation method, neededraw materials are simple, the preparation technology is skilful and easy to operate, and the prepared nanocomposite has a moderate size, good biocompatibility and moderate medicine loading amount; thenanocomposite has good tumor active / passive targeting and controlled medicine release effects, so that medicine accumulation on a tumor site is improved, the circulating time of a medicine in blood is prolonged and the medicine toxicity is reduced; the nanocomposite further has a fluorescent imaging property, so that the diagnosis of the tumor site is facilitated.

Description

technical field [0001] The invention belongs to the field of polymer drug carriers, and in particular relates to a nanocomposite that can be used for tumor diagnosis and targeted therapy and a preparation method thereof. Background technique [0002] Cisplatin is one of the most commonly used anti-tumor drugs in clinical practice. It has the characteristics of strong anti-cancer effect, high anti-cancer activity, compatibility with various anti-tumor drugs to produce synergistic effects, and no cross-resistance. It is indispensable in chemotherapy. drug. Cisplatin is mostly used as an injection clinically, but it quickly binds to proteins in the body and becomes ineffective, and is easily taken up by all fast-metabolizing cells in the body and excreted by the kidneys, resulting in dose-limiting toxicity. Therefore, finding a way to increase the circulation time of cisplatin in the body and reduce the toxicity of the drug to normal cells has become the key. For this reason,...

Claims

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Application Information

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IPC IPC(8): A61K47/60A61K47/61A61K33/24A61K9/14A61K49/00A61P35/00
CPCA61K9/146A61K33/24A61K47/60A61K47/61A61K49/0032A61K49/0093A61P35/00
Inventor 程翠孟亚彬章志鸿李亚张其清
Owner FUZHOU UNIVERSITY
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