Intracellular macrophage uptake of rifampicin loaded mannosylated dendrimers

被引：167

作者：

Kumar, Palanirajan Vijayaraj ^{[1
]}

Asthana, Abhay ^{[1
]}

Dutta, Tathagata ^{[1
]}

Jain, Narendra K. ^{[1
]}

机构：

[1] Dr Hari Singh Gour Vishwavidyalaya, Dept Pharmaceut Sci, Pharmaceut Res Lab, Sagar 470003, India

来源：

JOURNAL OF DRUG TARGETING | 2006年 / 14卷 / 08期

关键词：

dendrimers; mannosylation; rifampicin; macrophage uptake; pH dependent drug release;

D O I：

10.1080/10611860600825159

中图分类号：

R9 [药学];

学科分类号：

1007 ;

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.

引用

页码：546 / 556

页数：11

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