CHARACTERIZATION AND ANTI-TUMOR ACTIVITY OF PEGYLATED NANOLIPOSOMES CONTAINING SAFRANAL IN MICE BEARING C26 COLON CARCINOMA

The cytotoxic effect of safranal, a pharmacologically active component of saffron, has been established in vitro. The aim of this study was to develop safranal nanoliposomes with a higher therapeutic index for the treatment of cancer. Thus, various PEGylated safranal nanoliposomes were prepared using HSPC and cholesterol by solvent evaporation. The liposomes were characterized by their size, in vitro cytotoxicity and in vivo therapeutic efficacy against C26 tumor bearing mice. Liposome characterization illustrated the size range of 140-230 nm and PDI of 0.2-0.3. The entrapment efficiency was considerably low due to the high instability of safranal in liposomes, causing a substantial in vitro release. In vitro cytotoxicity indicated higher toxic effects of safranal liposomes compared to free form. Treatment of tumor-bearing mice with selected safranal liposomes (50 mg/kg) did not improve the tumor size and survival of animals compared to controls. These results were presumably due to the physicochemical properties and dose dependent effects of safranal molecules. In addition, the intensive hydrophobic molecular interaction between safranal and cholesterol within the bilayers of liposomes cause the low percentage of encapsulation, high instability while in the circulation and untoward site directed drug delivery. Results indicated that the current safranal liposomes could increase the in vitro cytotoxicity, however did not enhance the antitumor activity at a dose of 50 mg/kg; thus, to obtain an optimal formulation, it merit further investigation.