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Title:
ORGANIC GADOLINIUM NANOPARTICLES, PREPARATION METHOD THEREFOR, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/247142
Kind Code:
A1
Abstract:
Disclosed in the present invention are organic gadolinium nanoparticles, a preparation method therefor, and the use thereof. The organic gadolinium nanoparticles are particles of hydrophilic macromolecules bound with gadolinium ions. The preparation method therefor comprises firstly subjecting hydrophilic macromolecules and gadolinium ions to a coordination reaction; and then adding an alkali liquor and reacting same to obtain the organic gadolinium nanoparticles. Hydrophilic macromolecules and gadolinium ions are subjected to a coordination reaction and free gadolinium ions in a reaction system are depleted to form particles of hydrophilic macromolecules bound with gadolinium ions; after the coordination reaction is performed for a period of time, particle growth is accelerated under the action of an alkali liquor to obtain organic gadolinium nanoparticles with a good T1 imaging effect, wherein the obtained organic gadolinium nanoparticles have r1 ≥ 30 mM-1s-1 and r2/r1 ≤ 1.3 at 1.5 T and are not prone to dissociation, such that the present invention overcomes the defects of gadolinium oxide nanoparticles easily releasing toxic gadolinium ions in an acidic environment of endosome or lysosome after being endocytosed by cells.

Inventors:
SHEN ZHEYU (CN)
LU YUDIE (CN)
LU XUANYI (CN)
Application Number:
PCT/CN2021/127912
Publication Date:
December 01, 2022
Filing Date:
November 01, 2021
Export Citation:
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Assignee:
SOUTH MEDICAL UNIV (CN)
International Classes:
A61K49/12; A61K49/18
Foreign References:
CN113318243A2021-08-31
CN112940157A2021-06-11
CN108392642A2018-08-14
CN1994472A2007-07-11
CN109939246A2019-06-28
CN103992792A2014-08-20
Other References:
RATCHAPOL, J. ET AL.: "Enhanced Conjugation Stability and Blood Circulation Time of Macromolecular Gadolinium-DTPA Contrast Agent", MATERIALS SCIENCE AND ENGINEERING C, vol. 61, 7 January 2016 (2016-01-07), XP029403094, DOI: 10.1016/j.msec.2016.01.008
DARRAS VINCENT, NELEA MONICA, WINNIK FRANÇOISE M., BUSCHMANN MICHAEL D.: "Chitosan modified with gadolinium diethylenetriaminepentaacetic acid for magnetic resonance imaging of DNA/chitosan nanoparticles", CARBOHYDRATE POLYMERS, APPLIED SCIENCE PUBLISHERS , LTD BARKING, GB, vol. 80, no. 4, 22 January 2010 (2010-01-22), GB , pages 1137 - 1146, XP093006753, ISSN: 0144-8617, DOI: 10.1016/j.carbpol.2010.01.035
Attorney, Agent or Firm:
JIAQUAN IP LAW (CN)
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