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Preparation of gold nanoparticle coated with folic acid-modified pegylated dendrimer

A dendrimer, PEGylation technology, used in the preparation of X-ray contrast agents, etc.

Inactive Publication Date: 2013-01-09
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Searching relevant patents and literature found that there has been no report on the use of folic acid-modified PEGylated dendrimer-wrapped gold nanoparticles for CT imaging contrast agents for targeted diagnosis of tumors

Method used

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  • Preparation of gold nanoparticle coated with folic acid-modified pegylated dendrimer
  • Preparation of gold nanoparticle coated with folic acid-modified pegylated dendrimer
  • Preparation of gold nanoparticle coated with folic acid-modified pegylated dendrimer

Examples

Experimental program
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Effect test

Embodiment 1

[0057] (1) Dilute 20 mg of folic acid with 20 mL of dimethyl sulfoxide solution and activate with 8.69 mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC·HCl) 3h, and then dropwise added polyethylene glycol (NH 2 -PEG-COOH), after reacting for 70~80h, the reaction product was dialyzed in the buffer solution with a dialysis membrane for 24h, and then dialyzed with ultrapure water for 48h, and finally the purified product was freeze-dried to obtain a folic acid-modified polyethylene glycol solid Product (FA-PEG-COOH).

[0058] (2) Dissolve dendrimer with a dry weight of 30 mg in 15 mL of DMSO solution, then take 22.49 mg of the solid obtained in (1), dissolve in 5 mL of DMSO solution and activate with EDC.HCl Afterwards, add the dendrimer solution dropwise, react for 72 hours, and then add polyethylene glycol monomethyl ether (mPEG-COOH) with a dry weight of 34.80 mg activated with EDC.HCl and one end of which is a carboxyl group. The dialysis membrane was d...

Embodiment 2

[0061] (1) Dilute 30 mg of folic acid with 20 mL of dimethyl sulfoxide solution and activate with 13.03 mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC·HCl) 3h, and then dropwise added polyethylene glycol (NH 2 -PEG-COOH), after reacting for 70~80h, the reaction product was dialyzed in the buffer solution with a dialysis membrane for 24h, and then dialyzed with ultrapure water for 48h, and finally the purified product was freeze-dried to obtain a folic acid-modified polyethylene glycol solid Product (FA-PEG-COOH).

[0062] (2) Dissolve dendrimer with a dry weight of 20 mg in 15 mL of DMSO solution, then take 14.99 mg of the solid obtained in (1), dissolve in 5 mL of DMSO solution and activate with EDC·HCl Afterwards, add the dendrimer solution dropwise, react for 72 hours, and then add polyethylene glycol monomethyl ether (mPEG-COOH) with a dry weight of 23.19 mg activated by EDC·HCl with a carboxyl group at one end, and react for 72 hours. The dialysis...

Embodiment 3

[0064] The G5.NH prepared by the embodiment 1 that got 2 -(PEG-FA)-mPEG, dissolve it with 20mL methanol or water, then add chloroauric acid solution (10mg / mL), stir at room temperature for 30min, then add ice NaBH 4 solution (43.88mg, CH 3 OH:H 2 O (volume ratio) = 2:1), stirred and reacted at room temperature for 2 hours, added 88.9 μL triethylamine to the reaction system, stirred and mixed for 30 minutes, then added 72.4 μL acetic anhydride to the reaction solution, stirred and reacted at room temperature for 24 hours , then the reaction product was dialyzed in PBS buffer solution and ultrapure water with a dialysis membrane, and finally the purified product was freeze-dried to obtain gold nanoparticles ({(Au 0 ) 300 -G5.NHAc-(PEG-FA)-mPEG}DENPs).

[0065] Described chloroauric acid solution is the HAuCl of 10mg / mL 4 Methanol solution or 10mg / mL HAuCl 4 aqueous solution; the NaBH 4 The solution is NaBH 4 H 2 O / CH 3 OH solution, H 2 O and CH 3 The volume ratio of ...

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Abstract

The invention relates to a preparation of a gold nanoparticle coated with a folic acid-modified pegylated dendrimer. The method comprises the following steps of: (1) preparing a folic acid-modified polyethylene glycol solid product FA-PEG-COOH; (2) modifying G5.NH2 with FA-PAG-COOH and mPEG-COOH in sequence to obtain solid G5.NH2-(PEG-FA)-mPEG; and (3) dissolving the solid G5.NH2-(PEG-FA)-mPEG obtained in the step (2), adding a chloroauric acid solution, stirring, adding a NaBH4 solution, reacting, adding triethylamine and acetic anhydride after reacting, dialyzing a reaction product after reacting, and performing freeze drying. The method disclosed by the invention has the advantages of easiness, mild reaction conditions, easiness in operating and industrial implementation prospect; and the gold nanoparticle prepared with the method has the advantages of high water solubility, high stability, high water dispersion and the application prospect in the field of early detection of tumors.

Description

technical field [0001] The invention belongs to the field of preparation of gold nanoparticles with tumor targeting, in particular to a preparation method of folic acid-modified PEGylated dendritic macromolecule-wrapped gold nanoparticles. Background technique [0002] Cancer has become one of the main killers that endanger human health all over the world, but if cancer can be detected at an early stage, the possibility of being cured is higher. Therefore, the development of early detection technology for cancer has become an urgent problem to be solved. CT imaging is currently one of the commonly used methods for clinical diagnosis of cancer, with high spatial and density resolution, so it has been extensively studied. In order to implement precise diagnosis of cancer cells, the development of suitable CT contrast agents is essential. [0003] Noble metal nanoparticles (NPs), such as Au NPs and Ag NPs, have attracted considerable scientific and technological attention in ...

Claims

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Application Information

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IPC IPC(8): A61K49/04
Inventor 史向阳彭琛
Owner DONGHUA UNIV
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