▎ 摘　　要

Due to the high surface area and convenient functionalization, graphene oxide has a significant potential application in biomedicine. It can serve as multi-purpose platform for bioimaging, gene and drug delivery, photothermal and photodynamic therapy. To implement graphene oxide in diagnostics and therapeutics suc-cessfully, it is essential to investigate its mechanisms of uptake into mammalian cells thoroughly. Herein, up to date knowledge about graphene oxide internalization pathways is presented. Nanomaterial lateral dimensions, surface modifications and biotransformation phenomenon as well as a type of the cell may play a pivotal role in a graphene oxide cellular uptake. Hence, the impact of these factors is comprehensively discussed based on so far published studies. Although great progress has been made in elucidating graphene oxide internalization pathway, there are still challenges to overcome. These are discussed along with the prospects concerning further studies in this field of science.