申请人:Kosak M. Kenneth
公开号:US20070060499A1
公开(公告)日:2007-03-15
This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.
这项发明揭示了氯喹偶联活性药剂的组合物,包括其制备方法。先前的技术已经表明,以足够高浓度给予氯喹作为游离药物,可以增强细胞内体内各种药剂从细胞内体释放到细胞质中。这些组合物的目的是在传递活性药剂的相同部位提供受控量的氯喹,从而减少所需的总剂量。这些组合物包括将氯喹物质直接或通过各种药用载体物质偶联到活性药剂。载体物质包括多糖、合成聚合物、蛋白质、胶束和其他用于在体内携带和释放氯喹组合物以产生治疗效果的物质。这些组合物还可以包括用于携带和释放活性药剂以用于治疗或其他医疗用途的生物可降解连接。该发明还揭示了与靶向分子偶联的载体组合物,用于将氯喹物质和活性药剂定位传递到它们的作用部位。