公开(公告)号：US5679377A

公开(公告)日：1997-10-21

申请号：US261690

申请日：1994-06-17

申请人： Howard Bernstein ,  Eric Morrel ,  Edith Mathiowitz ,  Kirsten Schwaller ,  Thomas R. Beck

发明人： Howard Bernstein ,  Eric Morrel ,  Edith Mathiowitz ,  Kirsten Schwaller ,  Thomas R. Beck

IPC分类号： A01N25/28 ,  A61K9/16 ,  A61K9/50 ,  A61K9/52 ,  A61K47/42 ,  B01J13/02 ,  B01J13/12 ,  C05G5/00

CPC分类号： B01J13/12 ,  A01N25/28 ,  A61K9/1658 ,  B01J13/125 ,  Y10S514/866 ,  Y10S514/963 ,  Y10S514/965 ,  Y10T428/2984 ,  Y10T428/2985 ,  Y10T428/2989

摘要： Biodegradable, protein microspheres for in vivo release of a biologically active agent, as well as agricultural and environmental applications. The microspheres can be administered orally, intravenously, or subcutaneously for subsequent release. By selecting particular size ranges and the specific protein used to form the microsphere, it is possible to target the microspheres to a cell types such as macrophages, or to effect localized absorption of the microspheres to regions such as the mucosal membranes of the mouth, gastrointestinal tract, or urogenital areas. Larger forms of the microspheres can also be made using standard techniques of the desirable degradation properties.

摘要翻译： 可生物降解的蛋白质微球，用于体内释放生物活性剂，以及农业和环境应用。 微球可以口服，静脉内或皮下给药以便随后释放。 通过选择特定尺寸范围和用于形成微球的特定蛋白质，可以将微球靶向诸如巨噬细胞的细胞类型，或者将微球局部吸收到诸如口腔粘膜的区域，胃肠道 道或泌尿生殖系。 也可以使用所需降解性能的标准技术制备较大形式的微球。

公开(公告)号：US5271961A

公开(公告)日：1993-12-21

申请号：US902505

申请日：1992-06-23

申请人： Edith Mathiowitz ,  Howard Bernstein ,  Eric Morrel ,  Kirsten Schwaller

发明人： Edith Mathiowitz ,  Howard Bernstein ,  Eric Morrel ,  Kirsten Schwaller

IPC分类号： A61K9/16 ,  A61K9/50 ,  B01J13/12 ,  A61K9/52 ,  A61K9/54

CPC分类号： A61K9/1658 ,  A61K9/1647 ,  A61K9/5052

摘要： Protein microspheres are formed by phase separation in a non-solvent followed by solvent removal. The preferred proteins are prolamines, such as zein, that are hydrophobic, biodegradable, and can be modified proteolytically or chemically to endow them with desirable properties, such as a selected degradation rate. Composite microspheres can be prepared from a mixture of proteins or a mixture of proteins with one or more bioerodible polymeric materials, such as polylactides. Protein coatings can also be made. Compounds are readily incorporated into the microspheres for subsequent release. The process does not involve agents which degrade most labile proteins. The microspheres have a range of sizes and multiple applications, including drug delivery and delayed release of pesticides, fertilizers, and agents for environmental cleanup. Selection of microsphere size in the range of less than five microns and mode of administration can be used to target the microparticles to the cells of the reticuloendothelial system, or to the mucosal membranes of the mouth or gastrointestinal tract. Larger implants formed from the microspheres can also be utilized, especially for agricultural applications.

摘要翻译： 通过在非溶剂中相分离形成蛋白质微球，随后除去溶剂。 优选的蛋白质是疏水性的，可生物降解的，可以被蛋白水解或化学修饰以赋予它们所需性质（例如选择的降解速率）的醇溶蛋白，例如玉米醇溶蛋白。 复合微球可以由蛋白质或蛋白质与一种或多种生物可腐蚀的聚合物材料如聚交酯的混合物的混合物制备。 蛋白质涂层也可以制成。 化合物容易地并入微球体中用于随后的释放。 该过程不涉及降解大多数不稳定蛋白质的试剂。 微球具有一定范围的尺寸和多种应用，包括药物输送和农药，肥料和环境清洁剂的延迟释放。 可以使用在小于5微米范围内的微球大小的选择和给药方式将微粒靶向网状内皮系统的细胞，或将其靶向口腔或胃肠道的粘膜。 也可以利用由微球形成的更大的植入物，特别是在农业应用中。