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1. 发明申请

US20130149535A1 BIODEGRADABLE NANO-, MESO-, AND MICRO-POLYMER PARTICLES FOR MAINTAINING A LOW SURFACE TENSION IN THE LUNG AND FOR PROTECTING THE PULMONARY SURFACTANT 审中-公开
标题翻译：用于维持肺中低表面张力和保护肺部表面活性剂的生物可降解的纳米，MESO和微聚合物颗粒
公开(公告)号：US20130149535A1
公开(公告)日：2013-06-13
申请号：US13809626
申请日：2011-07-18
申请人： Moritz Beck-Broichsitter , Thomas Schmehl , Tobias Gessler
发明人： Moritz Beck-Broichsitter , Thomas Schmehl , Tobias Gessler
IPC分类号： C08F220/34
CPC分类号： C08F220/34 , A61K9/007 , A61K9/0073 , A61K9/1635 , A61K9/5138 , A61K31/78 , A61K31/785 , C08L33/14 , Y10T428/2982
摘要： The present invention provides nano-, meso- and micro-polymer particles which are able to bind pathogenic proteins penetrating into the lining layer of the lung. Known pathogenic proteins in the pulmonary lining layer are negatively charged. These proteins damage the pulmonary surfactant system which is essential to maintain a low surface tension in the lung and thus a functional respiration. Polymer particles of this invention have a diameter between 20 nm and 10 μm, are water-insoluble, have a positive surface charge and a low surface hydrophobicity. The isoelectric point of said particles is greater than 5 to that said particles are present in the lining layer of the lung as positively charged particles, and at the same time higher than the isoelectric point of the pathogenic protein to be bound. Polymer particles of this invention can for example be prepared using the precipitation or emulsion method. Polymer particles of this invention can be utilized for maintaining a low surface tension in the lung and for protecting the pulmonary surfactant.
摘要翻译：本发明提供能够结合穿透到肺内衬层的病原性蛋白质的纳米，中等和微聚合物颗粒。肺内衬层中已知的病原性蛋白质带负电荷。这些蛋白质损害肺表面活性剂体系，这对于保持肺中的低表面张力以及功能性呼吸是至关重要的。本发明的聚合物颗粒的直径在20nm和10μm之间，是不溶于水的，具有正的表面电荷和低的表面疏水性。所述颗粒的等电点大于5，所述颗粒作为带正电荷的颗粒存在于肺内衬层中，并且同时高于待结合的致病性蛋白质的等电点。本发明的聚合物颗粒可以例如使用沉淀或乳液法制备。本发明的聚合物颗粒可用于在肺中保持低表面张力并保护肺表面活性剂。

2. 发明申请

US20140099379A1 BIO-COMPATIBLE NANO AND MICROPARTICLES COATED WITH STABILIZERS FOR PULMONARY APPLICATION 审中-公开
标题翻译：生物兼容的纳米和微生物包裹稳定剂用于脉冲应用
公开(公告)号：US20140099379A1
公开(公告)日：2014-04-10
申请号：US14122180
申请日：2012-05-23
申请人： Moritz Beck-Broichsitter , Tobias Gessler , Thomas Schmehl
发明人： Moritz Beck-Broichsitter , Tobias Gessler , Thomas Schmehl
IPC分类号： A61K9/50 , A61K31/519
CPC分类号： A61K9/5089 , A61K9/0078 , A61K9/5026 , A61K9/5138 , A61K9/5153 , A61K31/519
摘要： The present invention provides stabilizers for the coating of biocompatible nano- and microparticles which prevent aggregation of the particles during preparation, storage as well as before and after nebulization and which are suitable to be utilized for the manufacture of a pharmaceutical preparation for pulmonary application.Biocompatible nano- and microparticles of this invention have a stabilizer layer thickness ranging from 1 to 200 nm and contain an active substance. Said biocompatible nano- and microparticles of this invention can be synthesized for example using the emulsion method known to the expert with subsequent coating by mixing of uncoated particles with the stabilizer, by chemical vapor deposition, by spraying or by covalent attachment.
摘要翻译：本发明提供了用于在制备，储存期间以及雾化之前和之后防止颗粒聚集的生物相容性纳米和微粒的涂层的稳定剂，并且适合用于制备用于肺部应用的药物制剂。本发明的生物相容的纳米和微粒的稳定剂层厚度范围为1〜200nm，含有活性物质。所述本发明的生物相容的纳米和微粒可以例如使用专家已知的乳液法合成，随后通过化学气相沉积，通过共价连接混合未涂覆的颗粒与稳定剂进行涂覆。

3. 发明申请

US20120148493A1 Composite Materials Loaded with Therapeutic and Diagnostic Agents Comprising Polymer Nanoparticles and Polymer Fibers 审中-公开
标题翻译：由聚合物纳米颗粒和聚合物纤维组成的包含治疗和诊断剂的复合材料
公开(公告)号：US20120148493A1
公开(公告)日：2012-06-14
申请号：US13256872
申请日：2010-03-16
申请人： Thomas Schmehl , Juliane Nguyen , Moritz Beck-Broichsitter , Tobias Gessler , Thomas Kissel , Marcel Thieme
发明人： Thomas Schmehl , Juliane Nguyen , Moritz Beck-Broichsitter , Tobias Gessler , Thomas Kissel , Marcel Thieme
IPC分类号： A61K9/70 , A61P9/00 , A61P11/00 , A61P11/06 , A61P35/00 , A61P17/00 , A61P17/02 , D01D5/00 , A61K49/00 , A61P3/00 , B82Y5/00
CPC分类号： A61K9/5153 , A61K9/70
摘要： The invention relates to composite materials comprising polymer nanofibers and polymer nanoparticles, wherein at least one of the two polymer materials is loaded with a substance selected from therapeutic and diagnostic agents. Fibers and nanoparticles can comprise identical or different polymers; the polymer materials are, however, biocompatible in every case. Therapeutic and diagnostic agents can be hydrophilic or lipophilic and the two polymer materials likewise. The at least one polymer material and the substance with which said material is loaded are either both hydrophilic or both lipophilic. The polymer nanoparticles of the composite materials have a diameter of 10 nm to 600 nm. The polymer fibers have diameters of 10 nm to 50 μm and lengths of 1 μm to several meters. The invention further relates to a method for producing said composite materials. Polymer nanoparticles can be produced in different ways, such as through controlled precipitation of a polymer solution that optionally comprises a loading substance. The nanoparticles are then mixed with another polymer and a loading substance as applicable, depending on whether particles, fibers or both are to be loaded with substance. The processing of this solution into composites comprising polymer fibers polymer nanoparticles can occur by means of electrospinning, melt spinning, extruding or template process. Composite materials according to the invention are suitable for the production of pharmaceuticals that release therapeutically or diagnostically effective substances slowly and in a controlled manner.
摘要翻译：本发明涉及包含聚合物纳米纤维和聚合物纳米颗粒的复合材料，其中两种聚合物材料中的至少一种负载有选自治疗剂和诊断剂的物质。纤维和纳米颗粒可以包含相同或不同的聚合物; 然而，聚合物材料在每种情况下都是生物相容的。治疗和诊断剂可以是亲水的或亲脂的，并且两种聚合物材料同样。所述至少一种聚合物材料和所述材料被加载的物质既是亲水的，也是亲油的。复合材料的聚合物纳米颗粒具有10nm至600nm的直径。聚合物纤维的直径为10nm〜50μm，长度为1〜数米。本发明还涉及一种生产所述复合材料的方法。聚合物纳米颗粒可以以不同的方式制备，例如通过可选地包含负载物质的聚合物溶液的可控沉淀。然后将纳米颗粒与另一种聚合物和负载物质混合，这取决于颗粒，纤维或两者是否被装载物质。将该溶液加工成包含聚合物纤维聚合物纳米颗粒的复合材料可以通过静电纺丝，熔融纺丝，挤出或模板方法进行。根据本发明的复合材料适用于缓慢地并以受控方式释放治疗或诊断有效物质的药物。

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