Preparation method of SPECT/CT bimodal imaging contrast agent with FA targeting function and based on low-generation dendrimer

Preparation method of SPECT/CT bimodal imaging contrast agent with FA targeting function and based on low-generation dendrimer

  • CN 105,251,028 B
  • Filed: 11/05/2015
  • Issued: 12/18/2020
  • Est. Priority Date: 11/05/2015
  • Status: Active Grant
First Claim
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1. A preparation method of a SPECT/CT bimodal imaging contrast agent with FA targeting function based on low-generation dendrimers comprises the following steps:

  • (1) the second generation of polyamidoamine dendrimer G2.NH2Dissolving in water, adding a diethylenetriamine pentaacetic acid cyclic anhydride cDTPAA aqueous solution, and stirring at room temperature for 8-12 h to obtain G2-DTPA;

    wherein, G2.NH2And cDTPAA in a molar ratio of 1;

    3-5;

    (2) dissolving folic acid-polyethylene glycol FA-PEG-COOH in water, adding 1- (3-dimethylaminopropyl) -3-ethylcarbodiimide hydrochloride EDC for activation, then dropwise adding the solution into the G2-DTPA solution obtained in the step (1), stirring and reacting for 72-80h at room temperature, dialyzing, and freeze-drying to obtain dendrimer G2-DTPA-PEG-FA modified with diethyltriamine pentaacetic acid and folic acid-polyethylene glycol;

    wherein the molar ratio of FA-PEG-COOH to G2-DTPA is 10-15;

    1;

    (3) dissolving G2-DTPA-PEG-FA in the step (2) in water, adding chloroauric acid aqueous solution, stirring at room temperature, then adding sodium borohydride aqueous solution, stirring in ice water for reaction for 2-3h, dialyzing, freezing and drying to obtain gold nanoparticle-coated dendrimer G2-DTPA-PEG-FA @ Au modified with diethyltriamine pentaacetic acid and folic acid-polyethylene glycol;

    wherein the molar ratio of the chloroauric acid to the G2-DTPA-PEG-FA is 6-9;

    1;

    (4) dissolving G2-DTPA-PEG-FA @ Au in the step (3) in the radioactive pertechnetate solution, adding stannous chloride, and performing column chromatography analysis to obtain the encapsulated gold nanoparticles and the chelate nuclide99mTc low-generation dendrimer-based SPECT/CT bimodal imaging contrast agent G2-DTPA-PEG-FA @ Au-99mTc。

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