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公开(公告)号：US07943179B2
公开(公告)日：2011-05-17
申请号：US11002542
申请日：2004-12-02
IPC分类号： A61K9/16
CPC分类号： A61K9/1617 , A61K9/1623 , A61K9/1647 , A61K9/1658
摘要： A drug delivery system comprising pH triggerable particles is described. The pH triggerable particles comprise and agent(s) to be delivered, which is encapsulated in a matrix comprising a pH trigger agent and a polymer. Agents including nucleic acids may be delivered intracellularly using the inventive pH triggerable particles. Upon exposure to an acidic environment such as the endosome or phagosome of a cell, the particles dissolve or disrupt due to protonation or an increase in solubility of the pH triggering agent. Pharmaceutical compositions and methods of preparing and administering these particles are also described. These particles may be particularly useful in genetic vaccination.
摘要翻译： 描述了包含pH可触发颗粒的药物递送系统。 pH可触发颗粒包含待运送的试剂，其被包封在包含pH触发剂和聚合物的基质中。 包含核酸的试剂可以使用本发明的pH可触发颗粒在细胞内递送。 当暴露于诸如细胞的内体或吞噬体的酸性环境中时，由于质子化或pH引发剂的溶解度的增加，颗粒溶解或破坏。 还描述了制备和施用这些颗粒的药物组合物和方法。 这些颗粒在基因疫苗接种中可能特别有用。
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公开(公告)号：US20120065358A1
公开(公告)日：2012-03-15
申请号：US13301315
申请日：2011-11-21
IPC分类号： C08G63/685
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（＆（bgr。 - 氨基酯））。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。
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公开(公告)号：US07427394B2
公开(公告)日：2008-09-23
申请号：US10446444
申请日：2003-05-28
IPC分类号： A61K31/765 , C08G69/44 , C08G63/44 , C07C327/00
CPC分类号： C08G69/44 , A61K9/5138 , A61K47/59 , A61K47/593 , A61K47/645 , A61K47/6925 , B82Y5/00 , C08G63/40 , C08G63/6856 , C08G73/02 , C08G73/0273 , C08G73/028 , C08G73/06 , C08G73/0611 , C08G73/0616 , C08L67/02 , C08L67/04 , C08L77/04 , C08L79/02 , C08L89/00 , C08L99/00 , C12N15/88 , C08L2666/02
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings. A system for preparing and screening polymers in parallel using semi-automated robotic fluid delivery systems is also provided.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（β-氨基酯）。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。 还提供了使用半自动机器人流体输送系统并行制备和筛选聚合物的系统。
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公开(公告)号：US08557231B2
公开(公告)日：2013-10-15
申请号：US11099886
申请日：2005-04-06
IPC分类号： A61K31/785 , A61K31/765 , C08G69/08
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
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公开(公告)号：US08287849B2
公开(公告)日：2012-10-16
申请号：US12507999
申请日：2009-07-23
IPC分类号： A61K31/765 , A61K9/00 , C08F26/00
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（＆（bgr。 - 氨基酯））。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。
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公开(公告)号：US20100036084A1
公开(公告)日：2010-02-11
申请号：US12507999
申请日：2009-07-23
IPC分类号： C08G63/685
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（β-氨基酯）。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。
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公开(公告)号：US06998115B2
公开(公告)日：2006-02-14
申请号：US09969431
申请日：2001-10-02
IPC分类号： A61K31/765 , C08G69/44 , C08G63/44 , C07C327/00
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
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公开(公告)号：USRE43612E1
公开(公告)日：2012-08-28
申请号：US12568481
申请日：2009-09-28
IPC分类号： A61K31/765 , C08G69/44 , C08G63/44 , C07C327/00
CPC分类号： C12N15/88 , A61K9/1641 , A61K9/5146 , A61K47/59 , A61K47/593 , A61K47/6935 , B82Y5/00 , C08G73/02 , C08G73/06 , C08G73/0611 , C08G73/0616 , C08G73/0627
摘要： Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings. A system for preparing and screening polymers in parallel using semi-automated robotic fluid delivery systems is also provided.
摘要翻译： 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（＆（bgr。 - 氨基酯））。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。 还提供了使用半自动机器人流体输送系统并行制备和筛选聚合物的系统。
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公开(公告)号：US08574420B2
公开(公告)日：2013-11-05
申请号：US13301466
申请日：2011-11-21
申请人： David M. Lynn , Jingtao Zhang , Xianghui Liu
发明人： David M. Lynn , Jingtao Zhang , Xianghui Liu
IPC分类号： C25D5/48 , C08F26/06 , C08F126/06 , C08F226/06 , C08F12/28 , C08F20/52 , C08F20/70 , C08F22/40 , C08F120/52 , C08F120/70 , C08F122/40 , C08F220/52 , C08F220/70 , C08F118/02 , C08F22/10 , C08F122/10 , C08F222/10 , A61K31/715
CPC分类号： A61K9/7007 , C08L33/24 , C08L39/02 , C08L2666/02
摘要： Multilayered films, particularly ultrathin multilayered films comprising cationic polymers which are useful for controlled release of anionic species, particularly for controlled release of nucleic acids. The multilayer films herein are useful for temporal controlled released of anionic species, particularly one or more anionic peptides, proteins, nucleic acids or other anionic biological agents. In one aspect, the invention relates to multilayer films which release anionic species (anions) with separate and/or distinct release profiles, particularly wherein the anions are one or more anionic peptides, proteins or nucleic acids or other anionic biological agents.
摘要翻译： 多层膜，特别是包含阳离子聚合物的超薄膜，其可用于阴离子物质的控制释放，特别是用于控制释放核酸。 本文中的多层膜可用于阴离子物质，特别是一种或多种阴离子肽，蛋白质，核酸或其它阴离子生物试剂的时间控制释放。 一方面，本发明涉及用分离和/或不同释放曲线释放阴离子物质（阴离子）的多层膜，特别是其中阴离子是一种或多种阴离子肽，蛋白质或核酸或其它阴离子生物试剂。
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公开(公告)号：US08324333B2
公开(公告)日：2012-12-04
申请号：US12479582
申请日：2009-06-05
申请人： Xianghui Liu , Jingtao Zhang , David M. Lynn
发明人： Xianghui Liu , Jingtao Zhang , David M. Lynn
CPC分类号： A61K47/48176 , A61K47/58 , C08F20/58 , C08F26/02
摘要： Materials and methods for the generation of polyelectrolyte multilayers that can erode to release cationic components. The multilayers comprise layers that contain one or more cations and one or more charge-dynamic anionic polymers. Charge-dynamic anionic polymers contain side chains having removable functional groups. Removal of the functional groups results in a change in the net change in the charge of the polymer which can disrupt interactions between cations and the anionic polymers and facilitate release of cations.
摘要翻译： 用于产生可能侵蚀阳离子组分的聚电解质多层的材料和方法。 多层包含含有一种或多种阳离子和一种或多种电荷 - 动态阴离子聚合物的层。 充电 - 动态阴离子聚合物含有具有可除去的官能团的侧链。 官能团的去除导致聚合物电荷的净变化的变化，这可以破坏阳离子和阴离子聚合物之间的相互作用并促进阳离子的释放。
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