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Nuclear medicine and magnetic resonance bimodal development drug, drug precursor, preparation method and application

A technology of magnetic resonance and nuclear medicine, applied in the preparation of folic acid receptor-positive tumor imaging drugs, the field of nuclear medicine and magnetic resonance imaging dual-mode drug precursors

Pending Publication Date: 2017-08-29
HTA CO LTD
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0004] There have been some studies on MRI tumor contrast agents targeting folic acid receptors, and dual-modality imaging drugs for PET / MRI or SPECT / MRI are also being developed, but so far, there has been no official approval at home and abroad. Approved PET / MRI or SPECT / MRI dual-modal imaging drugs that can be used in clinical practice

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  • Nuclear medicine and magnetic resonance bimodal development drug, drug precursor, preparation method and application
  • Nuclear medicine and magnetic resonance bimodal development drug, drug precursor, preparation method and application
  • Nuclear medicine and magnetic resonance bimodal development drug, drug precursor, preparation method and application

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preparation example Construction

[0043] In another specific embodiment, a method for preparing a nuclear medicine and magnetic resonance imaging dual-modality imaging prodrug is provided, comprising the following steps:

[0044] (a) Using 3-aminopropyltriethoxysilane to modify the surface of superparamagnetic iron oxide nanoparticles to obtain SPIONs-APTES;

[0045] (b) coupling of folic acid and polyethylene glycol to obtain FA-PEG;

[0046] (c) SPIONs-APTES reacts with FA-PEG to obtain SPIONs-PEG-FA, which is then coupled with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid to obtain DOTA-SPIONs-PEG-FA, the nuclear medicine and magnetic resonance dual-modal imaging drug precursor.

[0047] Among them, FA-PEG is obtained through the following steps: coupling of folic acid and N-hydroxysuccinimide (NHS) to obtain FA-NHS; FA-NHS and NH 2 -PEG-COOH reaction yields FA-PEG.

[0048] Through the above synthesis method and labeling with radioactive metal nuclides, a PET / MRI dual-mode imaging drug with c...

Embodiment 1

[0054] Example 1 PET / MRI dual-modal imaging prodrug DOTA-SPIONs-PEG-FA and PET / MRI dual-modal imaging drug 64 Preparation of Cu-DOTA-SPIONs-PEG-FA

[0055] 1. Preparation of SPIONs

[0056] Synthesis reaction in N 2 under protection. 549mg FeCl 3 ·6H 2 O and 282mg FeSO 4 ·7H 2 O was dissolved in 40mL deoxygenated water, and stirred to dissolve. Aqueous ammonia was added dropwise to adjust the pH to 9. Then the temperature was raised to 50° C., and the reaction was continued for 1 h. After the reaction was completed, wash with 50 mL of deoxygenated water, and pour it by magnet adsorption to remove the ammonium salt, repeating 3 times. The product was vacuum-dried at 60°C to obtain 123 mg of black lumpy solid SPIONs with a yield of 53%, which was stored at 4°C.

[0057]

[0058] Product FT-IR (cm -1 ) (IRAffinity-1 Fourier Transform Infrared Spectrometer, Japan SHIMADAZU Company): 3419.7, 1623.0, 576.7. Magnetic measurement (BKT-4500Z vibrating sample magnetometer...

Embodiment 2

[0089] Embodiment 2 in vitro stability research

[0090] 100μL 64 Cu-DOTA-SPIONs-PEG-FA marker (~0.37MBq) was added to 200 μL phosphate buffered saline solution PBS (pH=7.4), incubated at 37°C, after incubation for 0h, 4h, and 12h, samples were taken and analyzed by rapid Determination of radiochemical purity by thin layer chromatography.

[0091] The results showed that when the marker was incubated in PBS for 4 hours, it still maintained good radiochemical purity stability, which was above 93%. After a half-life (12h), the radiochemical purity dropped to 85%. This shows that the marker is basically stable within 4h.

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Abstract

The invention discloses a nuclear medicine and magnetic resonance bimodal development drug precursor (DOTA-SPIONs-PEG-FA). The drug precursor takes superparamagnetic iron oxide nanoparticles as cores and is coated with a biocompatible material and a double functional chelating agent. Folic acid is connected to the superparamagnetic iron oxide nanoparticles through the biocompatible material. The bimodal development drug precursor is labeled by a radioactive metal nuclide, so that a brand-new nuclear medicine and magnetic resonance bimodal development drug (RM-DOTA-SPIONs-PEG-FA) is obtained for the first time. The drug is good in in-vitro stability, has very high initial uptake, a good tumor / blood ratio and a relatively long residence time in tumor if being applied to folate receptor positive tumor detection, moreover, the nanoparticles have obvious active targeting action on tumor, so that the drug precursor can be effectively suitable for MRI development and EPT or SPECT development.

Description

technical field [0001] The invention belongs to the technical fields of molecular imaging medicine, radiopharmaceutical and nuclear medicine. Specifically, it relates to a nuclear medicine and magnetic resonance dual-mode imaging drug precursor. In addition, the present invention also relates to a preparation method of a nuclear medicine and magnetic resonance dual-mode imaging drug precursor, a nuclear medicine and magnetic resonance dual-mode imaging drug and its application in the preparation of a folic acid receptor-positive tumor imaging drug. Background technique [0002] A recent research report pointed out that in 2012, there were 14 million new cancer patients worldwide and 8.2 million cancer patients died. Among them, there were 3.07 million new cancer patients and about 2.2 million deaths in China. Early diagnosis and effective treatment of cancer can reduce about 1 / 3 to 1 / 2 (ie 2.4 to 3.7 million) deaths of cancer patients every year. The early diagnosis of tu...

Claims

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Application Information

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IPC IPC(8): A61K51/06A61K51/04A61K49/12A61K49/18A61K103/00A61K103/10
Inventor 沈浪涛孙钰林申一鸣梁积新陈玉清
Owner HTA CO LTD
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