首页> 外国专利> ULTRAFINE NANOPARTICLES INCLUDING A FUNCTIONALIZED POLYORGANOSILOXANMATRIX AND COMPREHENSIVE METAL COMPLEX; PROCEDURE FOR MANUFACTURE THEREOF AND USES THEREOF IN MEDICAL IMAGE

ULTRAFINE NANOPARTICLES INCLUDING A FUNCTIONALIZED POLYORGANOSILOXANMATRIX AND COMPREHENSIVE METAL COMPLEX; PROCEDURE FOR MANUFACTURE THEREOF AND USES THEREOF IN MEDICAL IMAGE

机译:超细纳米颗粒,包括功能化的聚有机硅氧杂化物和全面的金属络合物;制造图像的方法及其在医学图像中的使用

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.
机译:本发明涉及非常小尺寸的新型生物相容性杂化纳米颗粒,其特别用于诊断和/或治疗。本发明的目的是提供新颖的纳米颗粒,其特别是在成像(例如MRI)和/或其他诊断技术中用作造影剂和/或作为治疗剂,其比已知的相同类型的纳米颗粒具有更好的性能。并结合了小尺寸(例如小于20 nm)和金属(例如稀土)的高负荷,尤其是在成像(例如MRI)中具有较强的强度和正确的响应(增强的弛豫度) )。因此,根据本发明的纳米颗粒,其直径d1在1至20nm之间,各自包含聚有机硅氧烷(POS)基质,所述聚有机硅氧烷(POS)基质包含任选地与掺杂阳离子缔合的g阳离子。通过-Si-C-共价键与POS基体结合的螯合接枝C1 DTPABA(二亚乙基三胺五乙酸二氢二酐),并以足以络合所有all阳离子的量存在;任选地,另一种通过-Si-C-共价键结合到POS基质上的官能化接枝物Gf *(其中Gf *可以衍生自亲水化合物(PEG);具有活性成分PA1的化合物;目标化合物;这些纳米粒子的生产方法及其在成像和治疗中的应用也构成了本发明的一部分。

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