The aim of this study was to investigate cytotoxic activities, acute oral toxicity and gene mutagenicity in form of Salmonella/microsome mutagenicity assay (Ames) of imatinib microemulsion systems (IM MEs). The MEs were prepared by the titration method using pseudo ternary phase diagram. For the cytotoxicity tests, the hepatocellular cell lines Hep 3B (CRL-10741) and Hep G2 (HB-8064) were used. The acute oral toxicity was assessed using the limit test in mice with a dose of 2000 mg/kg body weight. The MEs consisted mainly of Labrasol/Capyrol 90/ Cremophor EL/ Cremophor EL-Span 80/Transcutol /water. In conclusion, no cytotoxic effects, no lethality during the acute oral toxicity test and no mutagenic potential in the TA98 nor in the TA100 strains could be observed on the here investigated cells. According to the obtained results, the developed MEs could be a promising alternative to the available marketed oral drug delivery.