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    • 1. 发明申请
    • NANOPARTICLES FOR DRUG-DELIVERY
    • 用于药物递送的纳米颗粒
    • WO2005020933A3
    • 2005-06-09
    • PCT/US2004028995
    • 2004-09-02
    • UNIV SOUTH FLORIDATUROS EDWARDSHIM JEUNG-YEOP
    • TUROS EDWARDSHIM JEUNG-YEOP
    • A61K20060101A61K9/14A61K9/51
    • A61K9/5138A61K9/5192
    • This invention relates to a unique process for the preparation of polymeric nanoparticles with target molecules bonded to the surface of the particles and having sizes of up to 1000nm, preferably Inm to 400nm, more preferably Inm to 200nm, that are dispersed homogeneously in aqueous solution. To accomplish the above objective, the polymeric nanoparticles of the subject invention are prepared using a novel technique of microemulsion polymerization. The resulting aqueous solution of polymeric nanoparticles is comprised of about 1 to 100 parts per weight of water or buffer, about 1 to 80 parts per weight of polymeric nanoparticles, which the bio-active molecules are conjugated, about 0.001 to 10 parts per weight of emulsifier, and about 0.00001 to 5 parts per weight of radical initiator based on the weight of the solution. In the method of this invention, the target drug/target substance is covalently bonded to the polymeric nanoparticles to secure them from outer intervention in vivo or cell culture in vitro until they are exposed at the target site within the cell.
    • 本发明涉及一种制备聚合物纳米颗粒的独特方法,其中目标分子与颗粒表面结合并具有最高达1000nm,优选Inm至400nm,更优选Inm至200nm的尺寸,其均匀分散于水溶液中。 为了实现上述目的,本发明的聚合物纳米颗粒使用微乳液聚合的新技术制备。 所得到的聚合物纳米粒子的水溶液由约1至100重量份的水或缓冲剂,约1至80重量份的生物活性分子缀合的聚合物纳米粒子,约0.001至10重量份的 乳化剂和约0.00001-5重量份的基于溶液重量的自由基引发剂。 在本发明的方法中,目标药物/目标物质共价结合到聚合物纳米粒子上,以确保它们免于体外外部干预或体外细胞培养,直到它们暴露于细胞内的靶位点。