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Hydroxyapatite nanoparticle radionuclide marked product and preparation method thereof

A technology of hydroxyapatite and radionuclide, applied in the direction of radioactive carrier, can solve the problems of long degradation period, poor in vivo stability, label shedding, etc., to achieve the effect of strong penetrating power and stable labeling product

Inactive Publication Date: 2010-09-15
SHANGHAI NINTH PEOPLES HOSPITAL SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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Problems solved by technology

[0006] (1) Poor stability in vivo: In the existing labeling method, hydroxyapatite nanoparticles are labeled with radionuclides by adsorbing ligands. This adsorption binding has poor stability in vivo, and the markers are easy to fall off in vivo
In addition, some ligands have high specific binding ability to certain tissues in vivo, such as phosphonate has strong adsorption to bone tissue, which may affect the distribution of hydroxyapatite nanoparticles in vivo
[0007] (2) There is no suitable half-life: Since hydroxyapatite is a chemically stable inorganic substance with a long degradation cycle in vivo, it is necessary to study the biological distribution of hydroxyapatite nanoparticles in vivo, requiring labeled radioactive nuclei The prime has an appropriate half-life
Among the radionuclides that can ion-exchange with hydroxyapatite at present, most of the half-lives are too short, such as 153 The half-life of Sm is 46.3h, 90 The half-life of Y is 64.1h, 99m The half-life of Tc is 6.02h, and the half-life of these radionuclides is not suitable for studying the biological distribution of hydroxyapatite nanoparticles in vivo
[0008] (3) The inconvenience of radioactivity detection: In order to study the biological distribution of hydroxyapatite nanoparticles in vivo, it is necessary to perform quantitative detection of radioactivity in important organs in the body
When conducting biological distribution research in vivo, it is necessary to digest the organ tissue to make it into a liquid state before detecting the radioactive activity in the organ tissue. Correction, which will greatly increase the difficulty and cost of radioactivity measurement in organs and tissues

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  • Hydroxyapatite nanoparticle radionuclide marked product and preparation method thereof

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Embodiment Construction

[0024] The present invention will be further described in detail below in conjunction with specific experiments and analysis of their results and the corresponding accompanying drawings.

[0025] (1) Silane amination of hydroxyapatite nanoparticles

[0026] The hydroxyapatite nanoparticles were placed in an anhydrous ethanol solution, ultrasonicated at a frequency of 40KHz for 30min, washed repeatedly with anhydrous ethanol, and then set aside. In 90mL ethanol solvent, add 10mL aminopropyltriethoxysilane (molecular formula: (CH 3 CH 2 O) 3 SiCH 2 CH 2 CH 2 NH 2) of a diluted solution (coupling agent: ethanol = 1:5, V / V), sodium hydroxide solution was added dropwise to make the pH of the solution 8, and stirring was continued for 1 h at room temperature. Add 200mg of hydroxyapatite nanoparticles into the hydrolysis coupling agent solution, stir and react in a water bath at 50-60°C for 6 hours, after the reaction, place at room temperature for 2 days, filter, wash with et...

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Abstract

The invention discloses a hydroxyapatite nanoparticle radionuclide marked product and a preparation method thereof. The hydroxyapatite nanoparticle radionuclide marked product may be prepared by a method comprising: a, performing the amination surface modification of hydroxyapatite nanoparticles by using silane coupling agent; b, preparing a 125I-BH maker; and c, connecting the 125I-BH maker and the modified hydroxyapatite nanoparticles. In the invention, the 125I radionuclide with high chemical activity is used, and the 125I radionuclide has a proper radioactive half-life of 60 days. The 125I marked product obtained by the marking method is stable and can be used in researches on the in-vivo development and distribution of the hydroxyapatite nanoparticles.

Description

technical field [0001] The invention relates to a radionuclide-labeled product of hydroxyapatite nanoparticles and its labeling technology, specifically, a radionuclide-labeled product 125 Hydroxyapatite nanoparticles of I and methods for their preparation. Background technique [0002] Hydroxyapatite (HA) is a weakly alkaline calcium phosphate salt with the molecular formula Ca 10 (PO4) 6 (OH) 2 , is the main inorganic component of human and animal bones, teeth and other hard tissues. The natural hydroxyapatite in the hard tissue of the body is a needle-shaped hexagonal prism nanostructure with a length of 200-400nm and a thickness of 15-30nm. Synthetic hydroxyapatite has excellent biocompatibility and chemical stability, and is widely used in the repair of bone defects. Hydroxyapatite nanoparticles not only have good biocompatibility and bioactivity, but also have the unique small size effect and surface effect of nanomaterials. After nano-hydroxyapatite nanoparticle...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/02A61K101/02
Inventor 孙皎谢广平丁婷婷钟高仁
Owner SHANGHAI NINTH PEOPLES HOSPITAL SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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