Characterization and in vitro cytotoxicity of piperine-loaded nanoemulsion in breast cancer cells

Abstract Piperine, an alkaloid of natural origin with potent anti-cancer activity. However, due to its physical-chemical characteristics, piperine's biological performance is limited, with low bioavailability resulting from high lipophilicity and low water solubility. To improve its cytotoxic activity 4T1 and MCF7 breast cancer cell lines, we developed and characterized piperine-loaded nanoemulsions (Pip-NE). The nanoemulsions were obtained by spontaneous emulsification followed by sonication and were characterized regarding their size by dynamic light scattering techniques and their zeta potential by electrophoretic mobility. NE-Pip showed an average hydrodynamic diameter of 102 nm, polydispersity index of 0.2, and zeta potential of -31.8 mV. Compared to piperine in solution, NE-Pip showed sustained in vitro release, preserving the cytotoxic activity of piperine. The formulations presented no irritancy potential in the Hen’s Egg Test on Chorioallantoic Membrane assay. Additionally, the nanoemulsification increased the piperine cytotoxicity against both breast cancer cell lines, as evidenced by the IC50 values. Overall, this study contributes to understanding the potential of drug delivery nanosystems as a novel strategy to optimize the delivery and enhance the cytotoxic properties of lipophilic drugs such as piperine in breast cancer cell lines.