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    STIMULI-RESPONSIVE CARRIERS FOR MPI-GUIDED DRUG DELIVERY
    1.
    发明申请
    STIMULI-RESPONSIVE CARRIERS FOR MPI-GUIDED DRUG DELIVERY 审中-公开
    用于MPI指导药物递送的STIMULI-RESPONSIVE CARRIERS

    公开(公告)号：US20120100079A1

    公开(公告)日：2012-04-26

    申请号：US13379056

    申请日：2010-06-25

    申请人： Dirk Burdinski ,  Jeroen A. Pikkemaat ,  Bertrand Schmitt ,  Holger Gruell ,  Sander Langereis

    发明人： Dirk Burdinski ,  Jeroen A. Pikkemaat ,  Bertrand Schmitt ,  Holger Gruell ,  Sander Langereis

    IPC分类号： A61K49/18 ,  A61P41/00

    CPC分类号： A61K9/0009

    摘要： The present invention relates to a composition comprising a shell structure forming a cavity, wherein said shell structure comprises a drug and wherein said composition is associated with at least one contrast agent; wherein said shell structure is capable of releasing its contents into the exterior upon the application of an external stimulus and wherein said contrast agent comprises magnetic particles which are capable of being detected by Magnetic Particle Imaging (MPI), wherein at least more than 5% (w/w) of the magnetic particles comprised in said contrast agent have a magnetic moment of at least −18 m 2 A, 10 wherein said magnetic particles are preferably composed of Fe, Co, Ni, Zn or Mn or alloys thereof or oxides of any of these. The present invention further relates to the use of such a composition or a composition comprising a shell structure forming a cavity, wherein said shell structure comprises a drug and wherein said composition is associated with at least one contrast agent, wherein said contrast agent is capable of being detected by MPI and wherein said shell structure is capable of releasing its contents into the exterior upon the application of an external stimulus as a carrier for a controlled delivery of a drug, as well as to a method of data acquisition for the control of a drug delivery process comprising the detection or localization via MPI of such compositions. In a further aspect the present invention relates to such compositions for treating a pathological condition, wherein the treatment comprises the release of the drug by the application of a stimulus.

    摘要翻译： 本发明涉及包含形成空腔的壳结构的组合物，其中所述壳结构包含药物，并且其中所述组合物与至少一种造影剂相关联; 其中所述壳结构能够在施加外部刺激时将其内容物释放到外部，并且其中所述造影剂包括能够通过磁性粒子成像（MPI）检测的磁性颗粒，其中至少大于5％ w / w）包含在所述造影剂中的磁性颗粒具有至少-18m 2 A，10的磁矩，其中所述磁性颗粒优选由Fe，Co，Ni，Zn或Mn组成或其合金或其合金或 任何这些。 本发明还涉及这样的组合物或组合物在组合物中的用途，所述组合物或组合物包含形成空腔的壳结构，其中所述壳结构包含药物，并且其中所述组合物与至少一种造影剂缔合，其中所述造影剂能够 被MPI检测到，并且其中所述外壳结构能够在外部刺激作为用于控制药物递送的载体的情况下将其内容释放到外部，以及用于控制药物的数据采集方法 药物递送过程包括通过这种组合物的MPI的检测或定位。 在另一方面，本发明涉及用于治疗病理状况的这种组合物，其中所述治疗包括通过施用刺激物释放药物。

    DRUG CARRIER PROVIDING MRI CONTRAST ENHANCEMENT
    3.
    发明申请
    DRUG CARRIER PROVIDING MRI CONTRAST ENHANCEMENT 有权
    药物载体提供MRI对比增强

    公开(公告)号：US20110177009A1

    公开(公告)日：2011-07-21

    申请号：US13062550

    申请日：2009-09-03

    申请人： Sander Langereis ,  Jochen Keupp ,  Holger Gruell ,  Dirk Burdinski ,  Danielle Beelen

    发明人： Sander Langereis ,  Jochen Keupp ,  Holger Gruell ,  Dirk Burdinski ,  Danielle Beelen

    IPC分类号： A61K49/18 ,  A61P35/00 ,  A61P9/00 ,  A61P43/00 ,  B82Y5/00

    CPC分类号： A61K49/08 ,  A61K9/127 ,  A61K9/1271 ,  A61K9/1273 ,  A61K41/0028 ,  A61K49/10 ,  A61K49/12 ,  A61K49/1812

    摘要： Described are drug carriers useful in magnetic resonance imaging (MRI)-guided drug release comprising a shell capable of releasing an enclosed biologically active agent as a result of a local stimulus, e.g. energy input, such as heat, wherein the shell encloses a 19F MR contrast agent. Preferably, the carrier also acts as a contrast enhancement agent for MRI based on the principle of Chemical Exchange-dependent Saturation Transfer (CEST). To this end the shell encloses a cavity that comprises a paramagnetic chemical shift reagent, a pool of proton analytes, and the 19F contrast agent, and wherein the shell allows diffusion of the proton analytes.

    摘要翻译： 描述了可用于磁共振成像（MRI）指导的药物释放的药物载体，其包含能够释放作为局部刺激的结果的封闭的生物活性剂的壳，例如， 能量输入，例如热量，其中壳体包围19F MR造影剂。 优选地，基于化学交换依赖性饱和转移（CEST）的原理，载体也用作MRI的对比度增强剂。 为此，壳体包围包含顺磁化学位移试剂，质子分析物池和19F造影剂的空腔，并且其中壳允许质子分析物的扩散。

    MR IMAGING WITH CEST CONTRAST ENHANCEMENT
    4.
    发明申请
    MR IMAGING WITH CEST CONTRAST ENHANCEMENT 审中-公开
    成像与CEST对比增强

    公开(公告)号：US20110288402A1

    公开(公告)日：2011-11-24

    申请号：US13139518

    申请日：2009-12-15

    申请人： Jeroen Alphons Pikkemaat ,  Sander Langereis ,  Holger Gruell ,  Dirk Burdinski ,  Rudolf Mathias Johannes Nicolaas Lamerichs ,  Jochen Keupp

    发明人： Jeroen Alphons Pikkemaat ,  Sander Langereis ,  Holger Gruell ,  Dirk Burdinski ,  Rudolf Mathias Johannes Nicolaas Lamerichs ,  Jochen Keupp

    IPC分类号： A61B5/055

    CPC分类号： G01R33/5601 ,  G01R33/5616

    摘要： The invention relates to a method of MR imaging of at least a portion of a body of a patient placed in an examination volume of an MR device. The object of the invention is to improve CEST contrast enhanced imaging. The method of the invention comprises the following steps: a) saturation of nuclear magnetization of exchangeable protons of a CEST contrast agent administered to the patient by subjecting the portion of the body to at least one frequency-selective saturation RF pulse matched to the MR frequency of exchangeable protons of the CEST contrast agent, wherein the saturation period, i.e. the duration of the frequency-selective saturation RF pulse, is shorter than the time required for saturation to build up a full CEST contrast enhancement effect when starting from zero saturation; b) generating at least one MR signal of water protons of the body by subjecting the portion of the body to an MR imaging sequence comprising at least one RF pulse and switched magnetic field gradients; c) acquiring sampling the at least one MR signal from the body; d) repeating steps a) to c) a number of times under variation of parameters of the MR imaging sequence, wherein MR signals are acquired and sampled during a saturation build-up period, i.e. before a steady state of the CEST effect is achieved; e) reconstructing a proton-density weighted, CEST contrast-enhanced MR image from the acquired and sampled MR signals.

    摘要翻译： 本发明涉及放置在MR装置检查体积中的患者身体的至少一部分的MR成像方法。 本发明的目的是改善CEST对比度增强成像。 本发明的方法包括以下步骤：a）通过使身体的一部分经受与MR频率匹配的至少一个频率选择性饱和RF脉冲，使给予患者的CEST造影剂的可交换质子的核磁化饱和 的CEST造影剂的可交换质子，其中饱和周期，即频率选择性饱和RF脉冲的持续时间比从零饱和开始时建立饱和CEST对比度增强效果所需的时间短; b）通过使身体的一部分经受包括至少一个RF脉冲和切换的磁场梯度的MR成像序列来产生身体的水质子的至少一个MR信号; c）从身体采集至少一个MR信号; d）在MR成像序列的参数变化下重复步骤a）至c）多次，其中在饱和建立期间，即在实现CEST效应的稳定状态之前获取和采样MR信号; e）从获取和采样的MR信号重构质子密度加权的CEST对比度增强的MR图像。

    CARRIERS FOR THE LOCAL RELEASE OF HYDROPHILIC PRODRUGS
    9.
    发明申请
    CARRIERS FOR THE LOCAL RELEASE OF HYDROPHILIC PRODRUGS 审中-公开
    当地发布水力发电机的承运人

    公开(公告)号：US20130302253A1

    公开(公告)日：2013-11-14

    申请号：US13981438

    申请日：2012-01-25

    申请人： Holger Gruell ,  Sander Langereis ,  Charles Sio

    发明人： Holger Gruell ,  Sander Langereis ,  Charles Sio

    IPC分类号： A61K9/127 ,  A61K9/00

    CPC分类号： A61K9/0087 ,  A61K9/0004 ,  A61K9/0019 ,  A61K9/127 ,  C07D305/14

    摘要： Disclosed is a carrier for the local, targeted administration of a hydrophobic drug. The hydrophobic drug is rendered in to a hydrophilic prodrug thereof, and is contained in the lumen of a thermosensitive liposome or polymersome. Upon administration of the carrier, heat can be applied at the locus where the drug is to be released. After release of the prodrug, it will be activated so as to turn into the active drug.

    摘要翻译： 公开了用于局部，有针对性地施用疏水性药物的载体。 将疏水性药物置于其亲水性前体药物中，并且包含在热敏脂质体或聚合物体的内腔中。 在施用载体时，可以在药物要释放的地方施加热量。 释放前药后，其将被活化以变成活性药物。