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    • 7. 发明申请
    • ULTRAFINE NANOPARTICLES COMPRISING A FUNCTIONALIZED POLYORGANOSILOXANE MATRIX AND INCLUDING METAL COMPLEXES; METHOD FOR OBTAINING SAME AND USES THEREOF IN MEDICAL IMAGING AND/OR THERAPY
    • 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
    • WO2011135101A3
    • 2012-05-31
    • PCT/EP2011056972
    • 2011-05-02
    • NANOHUNIV LYON 1 CLAUDE BERNARDINST NAT SCIENCES APPLIQLUX FRANCOISTILLEMENT OLIVIERSAINT JEAN MAXIMEMOWAT PIERREPERRIAT PASCALROUX STEPHANEMIGNOT ANNA
    • LUX FRANCOISTILLEMENT OLIVIERSAINT JEAN MAXIMEMOWAT PIERREPERRIAT PASCALROUX STEPHANEMIGNOT ANNA
    • A61K49/18B82Y5/00B82Y15/00
    • A61K49/1824A61K9/0019A61K9/14A61K41/0038A61K49/0002A61K49/0093A61K49/1857A61K49/1881B82Y5/00B82Y15/00Y10T428/2982
    • The invention relates to novel biocompatible hybrid nanoparticles of very small size that are of use in particular for diagnosis and/or therapy. The objective of the invention is to provide novel nanoparticles which are of use in particular as contrast agents in imaging (e.g. MRI) and/or in other diagnostic techniques and/or as therapeutic agents, which are more effective than the known nanoparticles of the same type and which combine both a small size (for example less than 20 nm) and a high metal (e.g. rare earth) loading rate, in particular so as to have, in imaging (e.g. MRI), a strong enhancement and a correct response (increased relaxivity) at high frequencies. Thus, the nanoparticles according to the invention, of diameter d1 between 1 and 20 nm, each comprise a polyorganosiloxane (POS) matrix including gadolinium cations, optionally associated with doping cations; a DTPABA (diethylenetriaminepentaacetic acid bisanhydride) chelating C1 graft bonded to the POS matrix via -Si-C- covalent bonding, and present in sufficient amount to be able to complex all the gadolinium cations; and optionally an other functionalization graft Gf* bonded to the POS matrix via -Si-C- covalent bonding (it being possible for Gf* to result from a hydrophilic compound (PEG); from a compound comprising an active ingredient PA1; from a targeting compound; from a luminescent compound (fluorescein)). The method for obtaining these nanoparticles and the uses thereof in imaging and in therapy are also part of the invention.
    • 本发明涉及特别用于诊断和/或治疗的非常小尺寸的新型生物相容性杂合纳米颗粒。 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,其比其相同的已知纳米颗粒更有效 类型,并且其结合了小尺寸(例如小于20nm)和高金属(例如稀土)加载速率,特别是在成像(例如MRI)中具有强增强和正确响应( 增加弛豫力)。 因此,根据本发明的直径为d1至1nm的纳米颗粒各自包含任选与掺杂阳离子相关的包含钆阳离子的聚有机硅氧烷(POS)基质; 通过-Si-C-共价键合键合到POS基质上的DTPABA(二亚乙基三胺五乙酸双酐)螯合C1,并且存在足以使所有钆阳离子复合的量; 和任选的通过-Si-C-共价结合到POS基质上的其它官能化移植物Gf *(Gf *可以由亲水性化合物(PEG)产生);来自包含活性成分PA1的化合物;来自靶向 化合物;由发光化合物(荧光素))。 获得这些纳米颗粒的方法及其在成像和治疗中的用途也是本发明的一部分。