The in vitro experiments carried out on A549 cells clearly demonstrated as the optimized formula (PIC-BZ) significantly improved all the parameters related to the cytotoxic potential towards cancer cells, including the decrease of IC50, the enhancement of anti-proliferative activity, the increase of apoptosis and necrosis cell populations paralleled by an increment of intracellular caspase-3 concentration, and inhibition of wound closure. Here, CASP3 is linked to cancer.