Azacitidine Nanoemulsion Formulation and Characterization for the Tumor Treatment Suppressor Genes Activity in Myeloid Leukemia Cell Lines

Abstract

The present study aimed to develop and evaluate an Azacitidine (AZA) nanoemulsion to enhance absorption
and therapeutic effectiveness. AZA, a pyrimidine nucleoside analogue, interferes with DNA methylation by inhibiting
DNA methyltransferase and acts as a cytidine antimetabolite incorporated predominantly into RNA. Although
clinically effective as an anticancer drug, its low absorption limits its utility. Materials and Methods: Nanoemulsions
were formulated using distilled water, co-surfactants (Transcutol P, plysorbate 80), AZA, and selected oils such
as oleic acid. Various water-in-oil nanoemulsion systems were prepared by high-speed homogenization. The
formulations were evaluated for stability, Fourier transform infrared (FTIR) compatibility, pH, thermodynamic
stability, viscosity, and in vitro drug release profiles. Results and Discussion: The optimized nanoemulsion displayed
favorable physicochemical characteristics, including acceptable pH, viscosity, and thermodynamic stability. FTIR
analysis confirmed the absence of major drug-excipient interactions. In vitro studies showed improved drug
release compared to conventional formulations. The nanoemulsion demonstrated significant inhibitory activity
(85.37%), approaching that of methotrexate (89.09%), suggesting its potential cytotoxic effect. Conclusion: The
developed AZA nanoemulsion exhibited enhanced release and inhibitory activity, indicating improved therapeutic
potential. These findings support its possible application as a treatment strategy for myeloid leukemia cell lines,
with additional studies warranted to confirm its histone deacetylase inhibitory effects.