Conventionally, most of the anticancer agents are administered via the intravenous route. However, the need for hospitalization, nursing care, and severe side effects have directed the researchers to find an alternative means for administration of anticancer agents. Advantages offered by oral route has attracted tremendous interest among the scientific fraternity for anticancer drug delivery. Although seemingly easy, the issues like reduced drug bioavailability due to pre-systemic metabolism and transmembrane efflux of the drug, and high inter-subject variability constraints the delivery of anticancer agents through oral route. The present review elaborates the challenges as well as nanoformulation strategies employed therein to assist anticancer drug delivery via the oral route.A comprehensive literature search was performed to have useful insights on various aspects pertaining to recent advances in oral delivery of anticancer agents using nanoparticles. Information from various literary sources was studied and summarized in order to familiarize the readers about the current status and the recent relevant advancements.Oral delivery of anti-cancer agents by employing nano-drug delivery systems not only improve the quality of life of patients but also provide a pharmacoeconomic advantage, leading to a reduced overall cost of cancer treatment.The review highlights recent approaches employed by nano-drug delivery systems to facilitate oral delivery of anticancer agents.