Gold and iodine element-supported arborescent macromolecular computed tomography (CT) targeted contrast medium and preparation thereof

A technology of dendritic macromolecules and targeting contrast agents, which is applied in the direction of nuclear magnetic resonance/magnetic resonance imaging contrast agents, preparations for in vivo experiments, and pharmaceutical formulations, and can solve the problem of high toxicity of CT contrast agents, short circulation time in vivo, Poor imaging effect and other problems, to effectively identify the lesion, reduce the dosage and its harm to the human body, and achieve the effect of high contrast

Inactive Publication Date: 2011-02-23
DONGHUA UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The technical problem to be solved by the present invention is to provide a dendrimer CT targeting contrast agent loaded with gold and iodine elements and its preparation, which overcomes the high toxicity, poor imaging effect, short circulation time in the body and no defects in targeting

Method used

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  • Gold and iodine element-supported arborescent macromolecular computed tomography (CT) targeted contrast medium and preparation thereof
  • Gold and iodine element-supported arborescent macromolecular computed tomography (CT) targeted contrast medium and preparation thereof
  • Gold and iodine element-supported arborescent macromolecular computed tomography (CT) targeted contrast medium and preparation thereof

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Experimental program
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Effect test

Embodiment 1

[0029] (1) Weigh 1.70 mg of folic acid (FA) and dissolve it in 3 mL of dimethylsulfoxide (DMSO), then weigh 1-[3-(dimethylamino)propyl]-3-ethyl-carbodiimide Dissolve 7.38mg of hydrochloric acid (EDC) in 3mL of DMSO, add 3mL of FA solution dropwise into the EDC solution and react for 4h, then slowly add the above solution dropwise into 10mL of PAMAM dendrimer DMSO solution (2mg / mL) , under stirring conditions for 2 days. After dialysis and freeze-drying, a dendrimer carrier modified with targeting molecule folic acid is obtained.

[0030] (2) the 1wt% chloroaurate aqueous solution that takes 3.96ml is slowly added dropwise in the aqueous solution of (1) and stirs, and in the mixed solution, add the 1wt% sodium borohydride aqueous solution of reducing agent 1.85ml, the chloride gold The acid salt is completely reduced under the protection of the dendrimer to form a dendrimer loaded with gold nanoparticles; and freeze-dried to obtain a targeted dendrimer material loaded with gol...

Embodiment 2

[0033](1) Weigh 2.75mg of lactobionic acid and dissolve it in 3mL of water, then weigh 11.80mg of 1-[3-(dimethylamino)propyl]-3-ethyl-carbodiimide hydrochloride (EDC) and N- 7.08 mg of hydroxysuccinimide (NHS) was dissolved in 5 mL of water, and 3 mL of lactobionic acid solution was added dropwise to the above solution to react for 4 hours. The activated lactobionic acid solution was slowly added dropwise to 20 mL of an aqueous solution (2 mg / mL) of PAMAM dendrimers, and reacted for 2 days under stirring conditions. After dialysis and freeze-drying, the modified dendrimer carrier with liver targeting function is obtained.

[0034] (2) Get the 1wt% chloroaurate aqueous solution of 7.92ml and slowly drop in the dendrimer aqueous solution of (1) and stir evenly, add the 1wt% sodium borohydride aqueous solution of reducing agent 3.70ml in the mixed solution, The chloroauric acid salt is completely reduced under the protection of the dendrimers, and freeze-dried to obtain the targ...

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Abstract

The invention relates to a gold and iodine element-supported arborescent macromolecular computed tomography (CT) targeted contrast medium and preparation thereof. The CT targeted contrast medium comprises the following components of arborescent macromolecules, targeted molecules, a gold nanoparticle and iodine-containing micromolecules. The preparation method comprises the following steps of: (1)connecting the targeted molecules and amino groups on the surfaces of the PAMAM arborescent macromolecules in a chemical bonding way to prepare a target arborescent macromolecule carrier; (2) dissolving the carrier into water, adding dropwise the aqueous solution of chloroauric acid and adding sodium borohydride to form a gold nanoparticle-supported targeted arborescent macromolecular material; and (3) dissolving the material into the solution of dimethyl sulfoxide, and connecting the iodine-containing micromolecules and the amino groups on the surfaces of the arborescent macromolecules to obtain the CT targeted contrast medium. The contrast medium of the invention has the advantages of high contrast ratio, high biocompatibility, long in-vivo circulation time, high stability and the like,and can be applied to X-ray computed tomography examination.

Description

technical field [0001] The invention belongs to the field of CT targeting contrast agent and its preparation, in particular to a dendrimer CT targeting contrast agent loaded with gold and iodine elements and its preparation. Background technique [0002] X-ray computed tomography (CT) is a large-scale medical imaging method that has developed rapidly in recent decades. Due to its clear image, excellent tissue density display and no overlapping structure, CT examination has been widely used in various clinical medical fields such as the central nervous system, respiratory system, digestive system, genitourinary system, and bone and joint system. Clinically, the diagnosis of some diseases, especially the early diagnosis of tumors, requires enhanced scans to be qualitative, which requires the use of contrast agents. The currently used contrast agents are mainly iodine-containing small molecule contrast agents. However, since small molecule iodides are likely to cause allergic...

Claims

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Application Information

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IPC IPC(8): A61K49/14A61K49/06A61K49/12A61K49/16
Inventor 史向阳郭睿
Owner DONGHUA UNIV
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