title: Intracellular macrophage uptake of rifampicin loaded mannosylated dendrimers.
abstract: 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.
authors.affiliation: Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar 470 003, India. vijayarajkumar_p@yahoo.com
authors.forename: Palanirajan Vijayaraj
authors.initials: PV
authors.lastname: Kumar
authors.forename: Abhay
authors.initials: A
authors.lastname: Asthana
authors.forename: Tathagata
authors.initials: T
authors.lastname: Dutta
authors.forename: Narendra K
authors.initials: NK
authors.lastname: Jain
mesh_terms: D000818:Animals; D000904:Antibiotics, Antitubercular / Q000493:pharmacokinetics* / Q000633:toxicity; D002152:Calorimetry, Differential Scanning; D002522:Chlorocebus aethiops; D050091:Dendrimers / Q000737:chemistry*; D016503:Drug Delivery Systems; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D006863:Hydrogen-Ion Concentration; D016676:Macrophages, Alveolar / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008358:Mannose / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D010587:Phagocytosis; D051381:Rats; D012293:Rifampin / Q000493:pharmacokinetics* / Q000633:toxicity; D012995:Solubility; D013055:Spectrophotometry, Infrared
chemical_list: D000904:Antibiotics, Antitubercular; D050091:Dendrimers; D008358:Mannose; D012293:Rifampin