As an efficient strategy for imparting the hydrophilic, nontoxic, non-immunogenic and nonantigenic properties of polyethylene glycol (PEG) to biological molecules, PEGylation has been studied intensively in recent years. By using PEGylation in the construction of antitumor drug delivery systems, many different kinds of PEGylated nanocarriers have been developed for effective and targeted cancer therapy, including liposomes, micelles, dendrimers, microspheres, nanoparticles and quantum dots. These PEGylated nanocarriers have the advantages of reduced drug leakage, cytotoxicity and immunogenicity, as well as increased plasma circulation time and tumor cell targeting potential. This short review focuses on recent progress in the application of PEGylated nanocarriers for delivery of antitumor drugs.