Azacitidine is a potent inhibitors of DNA methylation used for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) and may also be effective in solid tumours. After administration, azacitidine undergoes spontaneous hydrolysis and deamination by cytidine deaminase leading to its degradation, this drug has short half-life and is unable to remain long enough to affect cancer cells. One reported strategy to protect azacitidine from enzymatic deamination is the incorporation in solid lipid nanoparticles. Folate-receptor targeted nanoparticles have been found to increase cellular uptake and cell cytotoxicity of several anticancer drugs and this approach will be studied for the first time for azacitidine in the present work. The aim of the present study is to develop and characterize azacitidine-loaded folate-receptor nanoparticle formulations in order to overcome azacitidine instability and enhance the therapeutic index of this drug.