In the recent years, conjugation of polyethylene glycol (PEG) on dendrimer has become an established and highly refined technology for delivery of bioactives. Dendrimers provide an ideal platform for delivery of bioactive as they represent well-defined, highly branched, nanoscale architecture with several modifiable surface groups. However, the actual potential of dendrimers is not realized due to toxicity limitations. PEG molecules are nontoxic, non-immunogenic, and non-antigenic; highly water soluble, FDA approved and is endowed with tremendous potential to impart these properties to other biomolecules through the process of PEGylation. PEGylated dendrimer-mediated drug delivery overcomes the shortcomings of dendrimer reticuloendothelial system (RES) uptake, drug leakage, immunogenicity, hemolytic toxicity, cytotoxicity, hydrophobicity, facilitates the solubilization as well as raises the overall aptitude for DNA transfection, siRNA delivery, transepithelial transport and tumor targeting. This review focuses on various types of PEGylated dendrimer with a detailed note on various modes of PEG usage as well as their influence on various biopharmaceutical properties of dendrimer. (C) 2014 Elsevier Ltd. All rights reserved.