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公开(公告)号：US20050118718A1
公开(公告)日：2005-06-02
申请号：US10948077
申请日：2004-09-22
申请人： You Bae , Jong Kim , Ajay Taluja
发明人： You Bae , Jong Kim , Ajay Taluja
CPC分类号： A61K48/0041 , A61K47/541 , A61K47/60 , C07H21/04
摘要： Compositions and methods for stabilization and controlled release of ionic biopharmaceuticals are disclosed. Illustrative compositions according to the present invention include polyelectrolyte-PEG diblock copolymers complexed by ionic bonds with the ionic biopharmaceuticals. Additional illustrative compositions include microspheres encapsulating polyelectrolyte-PEG diblock copolymers complexed by ionic bonds with the ionic biopharmaceuticals. A method of delivering a biopharmaceutical to a person in need thereof involves administering microspheres that encapsulate biopharmaceutical/polyelectrolyte-PEG diblock copolymer complexes.
摘要翻译： 公开了用于稳定和控释离子生物药物的组合物和方法。 根据本发明的说明性组合物包括通过与离子生物药物的离子键络合的聚电解质-PEG二嵌段共聚物。 附加的说明性组合物包括通过与离子生物药物的离子键络合的聚电解质-PEG二嵌段共聚物的微球体。 向有需要的人递送生物药物的方法包括给予包封生物药物/聚电解质-PEG二嵌段共聚物复合物的微球体。
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公开(公告)号：US20050186263A1
公开(公告)日：2005-08-25
申请号：US10846487
申请日：2004-05-14
IPC分类号： A01N43/64 , A61K9/00 , A61K9/107 , A61K9/127 , A61K31/41 , C07D233/54 , C07D233/61 , C07D413/06 , C08F8/30
CPC分类号： A61K9/1075 , A61K9/0019 , A61K31/704 , C07D233/64 , C07D413/06 , C08F8/30
摘要： Mixed micelles containing poly(L-histidine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer are a pH-sensitive drug carrier that release the drug in an acidic microenvironment, but not in the blood. Since the microenvironment of solid tumors is acidic, these mixed micelles are useful for treating cancer, including those cancers exhibiting multidrug resistance. Targeting ligands, such as folate, can also be attached to the mixed micelles for enhancing drug delivery into cells. Methods of treating a warm-blooded animal with such a drug are disclosed.
摘要翻译： 含有聚（L-组氨酸） - 聚（乙二醇）嵌段共聚物和聚（L-乳酸） - 聚（乙二醇）嵌段共聚物的混合胶束是在酸性微环境中释放药物的pH敏感药物载体，但是 不在血中 由于实体瘤的微环境是酸性的，所以这些混合胶束可用于治疗癌症，包括那些显示出多药耐药性的癌症。 靶向配体如叶酸也可以连接到混合的胶束上，以增强药物递送到细胞中。 公开了用这种药物治疗温血动物的方法。
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公开(公告)号：US20050118252A1
公开(公告)日：2005-06-02
申请号：US10948078
申请日：2004-09-22
CPC分类号： A61K9/1075
摘要： Drug delivery compositions for specific delivery of a drug to a tumor are described. These compositions include a core for sequestering the drug and a shell to which a ligand is attached for delivery of a drug to target cells. Since normal cells may also be targeted by the ligand, the compositions embed the ligand in the shell until the localized conditions surrounding the tumor cause the ligand to be displayed on the surface of the shell. One composition exhibits shrinkage of the shell at tumor pH, whereas another composition exhibits extension of the ligand at tumor pH. Still another composition causes the ligand to be exhibited at an elevated temperature.
摘要翻译： 描述了将药物特异性递送至肿瘤的药物递送组合物。 这些组合物包括用于螯合药物的核心和附着有配体的壳，以将药物递送至靶细胞。 由于正常细胞也可能被配体靶向，因此组合物将配体嵌入壳中，直到围绕肿瘤的局部条件导致配体显示在壳的表面上。 一种组合物在肿瘤pH下表现出壳的收缩，而另一种组合物在肿瘤pH下表现出配体的延伸。 另一种组合物使配体在升高的温度下显示出来。
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公开(公告)号：US20070244259A1
公开(公告)日：2007-10-18
申请号：US10590959
申请日：2005-01-26
IPC分类号： C08G81/00 , A61K9/00 , C08F265/10 , C08G63/66
CPC分类号： A61L27/50 , A61L27/26 , A61L27/52 , C08F265/10 , C08F290/06 , C08F293/005 , C08G63/664 , C08G63/6852 , C08G63/6882 , C08G63/912 , C08G75/30 , C08G81/00 , C08G2261/126 , C08J3/075 , C08J2300/16 , C08J2367/04 , C08L53/00 , C08L67/00 , Y10S524/916 , C08L71/02 , C08L81/10 , C08L2666/02
摘要： The present invention relates to a block copolymer formed by coupling the following components with each other, as well as a hydrogel composition comprising the block copolymer and a hydrogel formed from the composition: (a) a copolymer of a polyethylene glycol (PEG)-based compound with a biodegradable polymer; and (b) a sulfonamide-based oligomer. The inventive block copolymer shows the sol-gel transition behavior sensitive to changes in not only temperature but also pH. Thus, the inventive block copolymer overcomes the shortcomings of temperature-sensitive copolymers, form a more strong and stable hydrogel, and is stable in vivo. Accordingly, the inventive block copolymer can be used in various applications in the medical and drug delivery fields.
摘要翻译： 本发明涉及通过将以下组分彼此偶联而形成的嵌段共聚物，以及包含嵌段共聚物和由以下组合物形成的水凝胶的水凝胶组合物：（a）基于聚乙二醇（PEG） 与生物降解聚合物的化合物; 和（b）磺酰胺类低聚物。 本发明的嵌段共聚物显示溶胶 - 凝胶转变行为不仅对温度而且pH的变化敏感。 因此，本发明的嵌段共聚物克服了温度敏感性共聚物的缺点，形成了更强和稳定的水凝胶，并且在体内是稳定的。 因此，本发明的嵌段共聚物可用于医药和药物输送领域的各种应用。
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公开(公告)号：US20050070721A1
公开(公告)日：2005-03-31
申请号：US10640739
申请日：2003-05-19
IPC分类号： A01N43/64 , A61K9/00 , A61K9/107 , A61K9/127 , A61K31/41 , C07D233/54 , C07D233/61 , C07D413/06 , C08F8/30
CPC分类号： C07D233/64 , A61K9/0019 , A61K9/1075 , C07D413/06 , C08F8/30
摘要： Mixed micelles containing poly(L-histidine)-poly(ethylene glycol) block copolymer and poly(L-lactic acid)-poly(ethylene glycol) block copolymer are a pH-sensitive drug carrier that release the drug in an acidic microenvironment, but not in the blood. Since the microenvironment of solid tumors is acidic, these mixed micelles are useful for treating cancer, including those cancers exhibiting multidrug resistance. Targeting ligands, such as folate, can also be attached to the mixed micelles for enhancing drug delivery into cells. Methods of making poly(L-histidine), synthetic intermediates, and block copolymers are also described.
摘要翻译： 含有聚（L-组氨酸） - 聚（乙二醇）嵌段共聚物和聚（L-乳酸） - 聚（乙二醇）嵌段共聚物的混合胶束是在酸性微环境中释放药物的pH敏感药物载体，但是 不在血中 由于实体瘤的微环境是酸性的，所以这些混合胶束可用于治疗癌症，包括那些显示出多药耐药性的癌症。 靶向配体如叶酸也可以连接到混合的胶束上，以增强药物递送到细胞中。 还描述了制备聚（L-组氨酸），合成中间体和嵌段共聚物的方法。
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