Cancer is the second leading cause of death worldwide. Surgery, chemotherapy, radiotherapy, and photodynamic therapy are widely used treatment modalities for cancer. However, the toxicities of cancer treatments and the tendency to induce drug resistance cause limitations to combat this disease with monotherapeutic approaches. To address this issue, combination therapy, a treatment modality that combines more than one therapeutics, has been introduced to improve the current treatments based on a synergistic outcome. This approach can potentially reduce serious side effects while providing the enhancement to therapeutic efficacy. In this dissertation, I performed different modules of combinatorial cancer therapy methods to verify the enhancement of anti-tumor efficacy both in vitro and in vivo. Chapter 1 provided the introductory research background as well as current challenges in cancer therapeutic methods. In Chapter 2, I present the study that photodynamic therapy efficacy was excited by the Cerenkov Radiation from Cesium-137 irradiator. In Chapter 3, I outlined the findings of multiple anti-cancer agents: camptothecin derivative and curcuminoids assembled into nanoparticles, and these nanoparticles exhibit better tumor targeting and eliminate the severe side effects caused by camptothecin derivatives. In Chapter 4, I applied a combination of the chemotherapy anti-cancer agents with photodynamic therapy to achieve the enhancement of anti-tumor efficacy both in vitro and in vivo. And finally, in Chapter 5, I concluded that the combination therapy compared to the monotherapy will achieve better anti-tumor performance. Altogether, our data showed that combination therapy exhibited better anti-cancer performance. These results provide new opportunities to develop better cancer therapy methods.