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公开(公告)号：US07737108B1
公开(公告)日：2010-06-15
申请号：US09755701
申请日：2001-01-05
CPC分类号： A61K47/6883 , A61K47/56 , A61K47/62
摘要： Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes (at physiologic pH, but can become active toward cell membranes if the environment is acidified below ca. pH 6.8), coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof. The compounds can be coupled by ionic, covalent or H bonds to an agent to be delivered or to a ligand which forms a complex with the agent to be delivered. Agents to be delivered can be therapeutic and/or diagnostic agents. Treatments which enhance delivery such as ultrasound, iontopheresis, and/or electrophereis can also be used with the disrupting agents.
摘要翻译： 描述了用于从细胞，细胞内的细胞室或通过细胞层或屏障转运或释放治疗和诊断试剂或代谢物或其它分析物的组合物和方法。 组合物包括膜屏障转运增强剂，并且通常与增强剂和/或暴露于刺激物一起施用以实现破坏或改变渗透性，运输或释放。 在优选的实施方案中，组合物包括响应于内体中的低pH而破坏内体膜的化合物，但是对于细胞膜（在生理pH下）相对无活性的化合物，但是如果环境被酸化至低于约5℃，则可以变得对细胞膜有活性。 pH 6.8），直接或间接地与治疗剂或诊断剂偶联。 还可以使用其它破坏剂，对除了pH之外的刺激和/或增强剂如光，电刺激，电磁刺激，超声，温度或其组合都有反应。 这些化合物可以通过离子，共价键或H键连接到待递送的试剂上，或者与配制剂形成配合物。 待递送的药剂可以是治疗和/或诊断剂。 还可以与破坏剂一起使用增强交付如超声，离子层析和/或电穿孔的处理。
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公开(公告)号：US20080220531A1
公开(公告)日：2008-09-11
申请号：US11683889
申请日：2007-03-08
CPC分类号： G01N33/54326 , B82Y25/00 , C01G49/02 , H01F1/0054
摘要： Stimuli-responsive magnetic nanoparticles, methods of making the nanoparticles, and methods of using the nanoparticles.
摘要翻译： 刺激响应磁性纳米颗粒，制备纳米颗粒的方法和使用纳米颗粒的方法。
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公开(公告)号：US09211250B2
公开(公告)日：2015-12-15
申请号：US13059946
申请日：2009-05-13
申请人： Paul Johnson , Patrick S. Stayton , Allan S. Hoffman , Robert Overell , Anna Gall , Mary Prieve , Amber Paschal , Charbel Diab , Priyadarsi De
发明人： Paul Johnson , Patrick S. Stayton , Allan S. Hoffman , Robert Overell , Anna Gall , Mary Prieve , Amber Paschal , Charbel Diab , Priyadarsi De
CPC分类号： A61K9/0019 , A61K9/1075 , A61K47/58 , C08L53/00 , C12N15/88 , C08L2666/24
摘要： Compositions comprising a heterogeneous polymeric micelle and an agent (e.g., a polynucleotide) associated with the micelle are disclosed, together with methods for intracellular delivery of such agent.
摘要翻译： 公开了包含非均相聚合物胶束和与胶束相关的试剂（例如，多核苷酸）的组合物，以及用于细胞内递送该试剂的方法。
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公开(公告)号：US20120021514A1
公开(公告)日：2012-01-26
申请号：US13059946
申请日：2009-05-13
申请人： Paul Johnson , Patrick S. Stayton , Allan S. Hoffman , Robert Overell , Anna Gall , Mary Prieve , Amber Paschal , Charbel Diab , Priyadarsi De
发明人： Paul Johnson , Patrick S. Stayton , Allan S. Hoffman , Robert Overell , Anna Gall , Mary Prieve , Amber Paschal , Charbel Diab , Priyadarsi De
CPC分类号： A61K9/0019 , A61K9/1075 , A61K47/58 , C08L53/00 , C12N15/88 , C08L2666/24
摘要： Compositions comprising a heterogeneous polymeric micelle and an agent (e.g., a polynucleotide) associated with the micelle are disclosed, together with methods for intracellular delivery of such agent.
摘要翻译： 公开了包含非均相聚合物胶束和与胶束相关的试剂（例如，多核苷酸）的组合物，以及用于细胞内递送该试剂的方法。
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公开(公告)号：US20110281934A1
公开(公告)日：2011-11-17
申请号：US13127962
申请日：2009-05-13
申请人： Paul Johnson , Patrick S. Stayton , Allan S. Hoffman , Robert Overell , Anna Gall , Mary Prieve , Amber Paschal , Charbel Diab , Priyadarsi De
发明人： Paul Johnson , Patrick S. Stayton , Allan S. Hoffman , Robert Overell , Anna Gall , Mary Prieve , Amber Paschal , Charbel Diab , Priyadarsi De
IPC分类号： A61K31/713 , C08F271/02 , C08F265/04
CPC分类号： A61K9/1075 , A61K47/549 , A61K47/58 , A61K47/60 , A61K47/6907
摘要： Provided herein are micelles comprising a plurality of copolymers. In certain instances, micelles provided herein are pH sensitive particles.
摘要翻译： 本文提供了包含多种共聚物的胶束。 在某些情况下，本文提供的胶束是pH敏感颗粒。
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公开(公告)号：US20110266492A1
公开(公告)日：2011-11-03
申请号：US13161233
申请日：2011-06-15
CPC分类号： G01N33/54326 , B82Y25/00 , C01G49/02 , H01F1/0054
摘要： Stimuli-responsive magnetic nanoparticles, methods of making the nanoparticles, and methods of using the nanoparticles.
摘要翻译： 刺激响应磁性纳米颗粒，制备纳米颗粒的方法和使用纳米颗粒的方法。
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公开(公告)号：US07625764B2
公开(公告)日：2009-12-01
申请号：US11197771
申请日：2005-08-03
IPC分类号： C12M1/34 , C12M3/00 , G01N33/543
CPC分类号： G01N33/54353 , C12N15/1006 , C12N15/1034 , G01N33/54346 , G01N33/545
摘要： Conjugates that include polymers that are reversibly self-associative in response to a stimulus and methods for using the conjugates.
摘要翻译： 包括响应于刺激的可逆地自缔合的聚合物和使用共轭物的共轭物。
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公开(公告)号：US08318816B2
公开(公告)日：2012-11-27
申请号：US12771850
申请日：2010-04-30
IPC分类号： A61K38/00 , A61K47/00 , A61K31/105 , A61K31/075
CPC分类号： A61K47/6883 , A61K47/56 , A61K47/62
摘要： Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes (at physiologic pH, but can become active toward cell membranes if the environment is acidified below ca. pH 6.8), coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof. The compounds can be coupled by ionic, covalent or H bonds to an agent to be delivered or to a ligand which forms a complex with the agent to be delivered. Agents to be delivered can be therapeutic and/or diagnostic agents. Treatments which enhance delivery such as ultrasound, iontopheresis, and/or electrophereis can also be used with the disrupting agents.
摘要翻译： 描述了用于从细胞，细胞内的细胞室或通过细胞层或屏障转运或释放治疗和诊断试剂或代谢物或其它分析物的组合物和方法。 组合物包括膜屏障转运增强剂，并且通常与增强剂和/或暴露于刺激物一起施用以实现破坏或改变渗透性，运输或释放。 在优选的实施方案中，组合物包括响应于内体中的低pH而破坏内体膜的化合物，但是对于细胞膜（在生理pH下）相对无活性的化合物，但是如果环境被酸化至低于约5℃，则可以变得对细胞膜有活性。 pH 6.8），直接或间接地与治疗剂或诊断剂偶联。 还可以使用其它破坏剂，对除了pH之外的刺激和/或增强剂如光，电刺激，电磁刺激，超声，温度或其组合都有反应。 这些化合物可以通过离子，共价键或H键连接到待递送的试剂上，或者与配制剂形成配合物。 待递送的药剂可以是治疗和/或诊断剂。 还可以与破坏剂一起使用增强交付如超声，离子层析和/或电穿孔的处理。
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公开(公告)号：US07981688B2
公开(公告)日：2011-07-19
申请号：US11683889
申请日：2007-03-08
IPC分类号： G01N25/18
CPC分类号： G01N33/54326 , B82Y25/00 , C01G49/02 , H01F1/0054
摘要： Stimuli-responsive magnetic nanoparticles, methods of making the nanoparticles, and methods of using the nanoparticles.
摘要翻译： 刺激响应磁性纳米颗粒，制备纳米颗粒的方法和使用纳米颗粒的方法。
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公开(公告)号：US20100210504A1
公开(公告)日：2010-08-19
申请号：US12771850
申请日：2010-04-30
IPC分类号： A61K38/02 , A61K31/70 , A61K31/715 , A61K31/7052 , A61K31/7088 , C12N5/00
CPC分类号： A61K47/6883 , A61K47/56 , A61K47/62
摘要： Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes (at physiologic pH, but can become active toward cell membranes if the environment is acidified below ca. pH 6.8), coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof. The compounds can be coupled by ionic, covalent or H bonds to an agent to be delivered or to a ligand which forms a complex with the agent to be delivered. Agents to be delivered can be therapeutic and/or diagnostic agents. Treatments which enhance delivery such as ultrasound, iontopheresis, and/or electrophereis can also be used with the disrupting agents.
摘要翻译： 描述了用于从细胞，细胞内的细胞室或通过细胞层或屏障转运或释放治疗和诊断试剂或代谢物或其它分析物的组合物和方法。 组合物包括膜屏障转运增强剂，并且通常与增强剂和/或暴露于刺激物一起施用以实现破坏或改变渗透性，运输或释放。 在优选的实施方案中，组合物包括响应于内体中的低pH而破坏内体膜的化合物，但是对于细胞膜（在生理pH下）相对无活性的化合物，但是如果环境被酸化至低于约100℃，则可以变得对细胞膜有活性。 pH 6.8），直接或间接地与治疗剂或诊断剂偶联。 还可以使用其它破坏剂，对除了pH之外的刺激和/或增强剂如光，电刺激，电磁刺激，超声，温度或其组合都有反应。 这些化合物可以通过离子，共价键或H键连接到待递送的试剂上，或者与配制剂形成配合物。 待递送的药剂可以是治疗和/或诊断剂。 还可以与破坏剂一起使用增强交付如超声，离子层析和/或电穿孔的处理。
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