Vitamin E succinate(VES), asuccinic acidester ofvitamin E, is one of the most effective anticancer compounds of thevitamin Efamily. VES can inhibit tumor growth by multiple pathways mainly involve tumor proliferation inhibition, apoptosis induction, and metastasis prevention. More importantly, the mitochondrial targeting and damaging property of VES endows it with great potential in exhibiting synergetic effect with conventional chemotherapeutic drugs and overcomingmultidrug resistance(MDR). Given thelipophilicityof VES that hinders its bioavailability and therapeutic activity, nanotechnology with multiple advantages has been widely explored to deliver VES and opened up new avenues for itsin vivoapplication. This review aims to introduce the anticancer mechanisms of VES and summarize its delivery strategies using nano-drug delivery systems. Specifically, VES-based combination therapy for synergetic anticancer effect, MDR-reversal, and oral chemotherapy improvement are highlighted. Finally, the challenges and perspectives are discussed.Vitamin E succinate(VES), asuccinic acidester ofvitamin E, is one of the most effective anticancer compounds of thevitamin Efamily. VES can inhibit tumor growth by multiple pathways mainly involve tumor proliferation inhibition, apoptosis induction, and metastasis prevention. More importantly, the mitochondrial targeting and damaging property of VES endows it with great potential in exhibiting synergetic effect with conventional chemotherapeutic drugs and overcomingmultidrug resistance(MDR). Given thelipophilicityof VES that hinders its bioavailability and therapeutic activity, nanotechnology with multiple advantages has been widely explored to deliver VES and opened up new avenues for itsin vivoapplication. This review aims to introduce the anticancer mechanisms of VES and summarize its delivery strategies using nano-drug delivery systems. Specifically, VES-based combination therapy for synergetic anticancer effect, MDR-reversal, and oral chemotherapy improvement are highlighted. Finally, the challenges and perspectives are discussed.