The present study was aimed at developing and exploring the use of PEGylated poly (propylene imine) dendritic architecture for the delivery of an anti-tuberculosis drug, rifampicin. For this study, PEGylated poly(propylene imine) dendritic architecture was synthesized and loaded with rifampicin. Various physicochemical and physiological parameters UV, IR, NMR, TEM, DSC, drug entrapment, drug release and hemolytic toxicity of both PEGylated and non- PEGylated systems were determined and compared. The PEGylation of the systems was found to have increased their drug-loading capacity, reduced their drug release rate and hemolytic toxicity. The systems were found suitable for prolonged delivery of rifampicin.