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1. 发明申请

US20130195766A1 ULTRAFINE NANOPARTICLES COMPRISING A FUNCTIONALIZED POLYORGANOSILOXANE MATRIX AND INCLUDING METAL COMPLEXES; METHOD FOR OBTAINING SAME AND USES THEREOF IN MEDICAL IMAGING AND/OR THERAPY 审中-公开
标题翻译：包含官能化聚硅氧烷基质并包括金属络合物的超纳米纳米粒子; 用于获得其的方法及其在医学成像和/或治疗中的用途
公开(公告)号：US20130195766A1
公开(公告)日：2013-08-01
申请号：US13695090
申请日：2011-05-02
申请人： François Lux , Olivier Tillement , Maxime Saint Jean , Pierre Mowat , Pascal Perriat , Stéphane Roux , Anna Mignot
发明人： François Lux , Olivier Tillement , Maxime Saint Jean , Pierre Mowat , Pascal Perriat , Stéphane Roux , Anna Mignot
IPC分类号： A61K49/18 , A61K9/14
摘要： The invention relates to novel biocompatible hybrid nanoparticles of very small size, useful in particular for diagnostics and/or therapy.The purpose of the invention is to offer novel nanoparticles which are useful in particular as contrast agents in imaging (e.g. MRI) and/or in other diagnostic techniques and/or as therapeutic agents, which give better performance than the known nanoparticles of the same type and which combine both a small size (for example less than 20 nm) and a high loading with metals (e.g. rare earths), in particular so as to have, in imaging (e.g. MRI), strong intensification and a correct response (increased relaxivity) at high frequencies.Thus, the nanoparticles according to the invention, with diameter d1 between 1 and 20 nm, each comprise a polyorganosiloxane (POS) matrix including gadolinium cations optionally associated with doping cations; a chelating graft C1 DTPABA (diethylenetriaminepentaacetic acid bisanhydride) bound to the POS matrix by an —Si—C— covalent bond, and present in sufficient quantity to be able to complex all the gadolinium cations; and optionally another functionalizing graft Gf* bound to the POS matrix by an —Si—C— covalent bond (where Gf* can be derived from a hydrophilic compound (PEG); from a compound having an active ingredient PA1; from a targeting compound; from a luminescent compound (fluorescein).The method for the production of these nanoparticles and the applications thereof in imaging and in therapy also form part of the invention.
摘要翻译：本发明涉及非常小尺寸的新型生物相容性杂合纳米粒子，特别适用于诊断和/或治疗。本发明的目的是提供新颖的纳米颗粒，其特别用作成像（例如MRI）和/或其它诊断技术和/或作为治疗剂的造影剂，其比具有相同类型的已知纳米颗粒更好的性能并且其结合了小尺寸（例如小于20nm）和高负载金属（例如稀土），特别是在成像（例如MRI）中，具有强烈的强化和正确的响应（增加的弛豫性）在高频率。因此，直径d1在1和20nm之间的根据本发明的纳米颗粒各自包含聚有机硅氧烷（POS）基质，其包含任选与掺杂阳离子相关的钆阳离子; 通过-Si-C-共价键与POS基质结合的螯合接枝C1DTPABA（二亚乙基三胺五乙酸双酐），并且以足够的量存在以能够使所有的钆阳离子复合; 和任选的通过-Si-C-共价键（其中Gf *可以衍生自亲水性化合物（PEG））与POS基质结合的另一个官能化移植物Gf *;具有活性成分PA1的化合物;来自靶向化合物; 来自发光化合物（荧光素）的方法。用于制备这些纳米颗粒的方法及其在成像和治疗中的应用也构成本发明的一部分。

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