Lipoate-AmB-oleate-chol nanoparticles: An approach to decrease cytotoxic effects

In this study, we conducted a comprehensive analysis of nanoparticles formed through the interaction of lipoic acid with amphotericin B (AmB), a highly hydrophobic antifungal drug. Sodium lipoate nanostructures spontaneously self-assemble in aqueous environments under specific pH conditions. The incorporation of AmB into lipoate nanostructures occurs in the same way, leading to the formation of nanoscale structures between 25 and 60 nm. These structures exhibit a strong negative surface charge, which contributes to their remarkable stability in aqueous solutions. Under these experimental conditions, Lipoate-AmB complex displayed a biological activity comparable to some commercial micellar and liposomal formulations. Furthermore, to reduce the drug's toxic effects, we supplemented it with nanoparticles of cholesterol (Chol) in sodium oleate. This interaction led to the formation of new quaternary complex of Lipoate-AmB-Oleate-Chol of about 100 nm that retain the biological activity without side effects.