Nowadays, nanoparticle-based cancer therapy plays a prominent role in the medicine. In present work, two nanoliposomes LIP-PEG-FA-FITC-Fe3O4-Cis (N-Cis) and LIP-PEG-FA-FITC-Fe3O4-Gem (N-Gem) were synthesized and characterized by analytical devices such as FT-IR, DLS, TEM, and SEM. The size, drug entrapment efficiency and drug release behavior of liposomal derivatives were investigated. The cytotoxicity, apoptosis, cellular uptake, and gene expression analysis were carried out on A549, MCF-7, and MRC5 cell lines. The IC50 values of the nanocomplexes exhibit cytotoxic effects more than pure drugs (P-Cis and P-Gem) and also, N-Cis reveals more cytotoxicity as compared to N-Gem on studied cell lines, significantly. While N-Gem showed somewhat better apoptosis-inducing performance than N-Cis sample by Flow cytometry analysis. The results of cellular uptake display that folate receptor-targeted liposomal nano-complexes are able to improve cellular uptake in MCF-7 than A549 cancer cells. N-Cis and N-Gem liposomal nano-complexes increased the expression of P21 and P53 genes in cancer cells more than that of P-Cis and P-Gem. Also, up regulation of mentioned genes expression using N-Cis is more than N-Gem. Ultimately, these data are depicting that our targeted nano-complexes can be considered as a promising useful and effective delivery system in active cancer therapy.