This data is used in the PhD thesis "Dendrimer nanoparticles in anticancer treatment applications" and contain the findings about in vitro and in vivo efficacy and toxicity of dendrimer-enhanced small molecules and siRNAs. We used dendrimer nanoparticles as anti-LMP1 siRNA carriers for nasopharyngeal carcinoma targeted therapy, and applied bola-lipid dendrimers as vehicles for imatinib mesylate to successfully inhibit ovarian cancer stem cells, both in vitro and in vivo, without serious adverse effects.