Lung cancer is the type that has the highest incidence and mortality rate. Several methods or agents, for the diagnosis and treatment of lung cancer, fall short of when it comes to early and accurate diagnosis and eradication of tumor tissue. In this study, nanosized, folate-targeted, co-drug encapsulated (paclitaxel and vinorelbine), radiolabeled liposomal formulations were designed for effective diagnosis and therapy of Non-Small Cell Lung Cancer. Theranostic liposomes were appropriately observed according to their particle size (about 150-180 nm) and encapsulation efficiency of 15% for PCX and 20% for VNB as well as their zeta potential of about -10 mV. The uptake of actively targeted liposomes was higher than passively targeted ones in H1299 cells, as well as actively targeted formulations were uptaken with a higher rate in H1299 cells than A549 cells. Empty liposomal formulations exhibited biocompatible profile on cells, as well as the anti-cancer efficacy of co-drug encapsulated liposomes was found to be significantly higher than only-one drug encapsulated liposomal formulations. Therefore, theranostic nanosized, radiolabeled, co-drug encapsulated liposomes were found to be potential for the diagnosis and therapy of Non-Small Cell Lung Cancer. Further in vivo studies are surely needed, and our studies are continuing.