Intracellular macrophage uptake of rifampicin loaded mannosylated dendrimers.
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.
Kumar
Palanirajan Vijayaraj
PV
Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar 470 003, India. vijayarajkumar_p@yahoo.com
Asthana
Abhay
A
Dutta
Tathagata
T
Jain
Narendra K
NK
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
D000904:Antibiotics, Antitubercular; D050091:Dendrimers; D008358:Mannose; D012293:Rifampin