The delivery of cancer chemotherapeutics has shifted dramatically in the last two decades from parenteral to oral administration. Improved patient compliance, drug tolerability, ease of administration, and potential effectiveness for oral therapy relative to intravenous administration have appeared as the main reasons to use cancer chemotherapeutics through the oral route of administration. However, most of the cancer chemotherapeutics show very poor oral absorption due to the drug’s physicochemical characteristics, stability, and biological barrier (multidrug efflux proteins: P-glycoproteins) present in the GI tract. With advanced research in homolipids and heterolipids as excipients, lipid-based formulations were exploited to enhance the oral efficacy of poorly absorbable cancer chemotherapeutics in recent years. Self-nanoemulsifying drug delivery system (SNEDDS) is the highly developed strategy of emulsion dependent drug delivery systems and relies on the GI fluids for the formation of nanoemulsion inside the in vivo system. The advancement in the field of biocompatible lipid and their derivatives in addition to finding on pharmaceutical excipients such as oil, surfactants, co-surfactants having P-gp modulating potential further extend the interest in SNEDDS for delivery of cancer chemotherapeutics through oral administration. This chapter provides a comprehensive discussion about contemporary advancement in the application of SNEDDS for oral delivery of cancer chemotherapeutics.