首页> 外文期刊>Journal of drug targeting >Intracellular macrophage uptake of rifampicin loaded mannosylated dendrimers.
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Intracellular macrophage uptake of rifampicin loaded mannosylated dendrimers.

机译:利福平负载甘露糖基化树枝状大分子的细胞内巨噬细胞摄取。

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摘要

The present study was aimed at developing and exploring the use of mannosylated dendritic architecture for the selective delivery of an anti-tuberculosis drug, rifampicin (RIF) to alveolar macrophages (AM). The mannosylated dendritic architecture was synthesized and characterized by using IR and NMR spectroscopy. RIF was efficiently loaded into mannosylated dendrimer using dissolution method. Various physicochemical and physiological parameters such as UV, SEM, DSC, drug loading, solubilization, pH dependent in-vitro release, hemolytic toxicity, phagocytic AM uptake and cytotoxicity concerning the mannosylated dendrimer were evaluated. RIF loaded mannosylated dendrimer reduced release rate of drug in pH 7.4, hemolytic toxicity and cytotoxicity; whereas enhanced drug release in pH 5.0 and AM uptake was observed. The present novel dendritic system displayed suitability in terms of biocompatibility and site-specific delivery of antitubercular drug RIF.
机译:本研究旨在开发和探索甘露糖基化的树突状结构用于将抗结核药物利福平(RIF)选择性递送至肺泡巨噬细胞(AM)的用途。甘露糖基化的树枝状结构被合成并通过IR和NMR光谱表征。使用溶解方法将RIF有效地加载到甘露糖基化的树枝状聚合物中。评估了与甘露糖基化树枝状大分子有关的各种物理化学和生理参数,例如UV,SEM,DSC,载药量,溶解度,pH依赖的体外释放,溶血毒性,吞噬性AM摄取和细胞毒性。负载RIF的甘露糖基化树枝状聚合物可降低pH 7.4下的药物释放速率,溶血毒性和细胞毒性;而在pH 5.0和AM吸收下观察到药物释放增强。本发明的新的树突系统在抗结核药物RIF的生物相容性和部位特异性递送方面显示出适用性。

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