In vitro uptake assessment of Amphotericin B-loaded PLGA microspheres

Abstract

Amphotericin B (AmB) is the 'gold standard for systemic antifungal therapy. AmB is an FDA approved polyene antifungal drug with a vast spectrum of activity. AmB is administered intravenously due to its poor stability in acidic pH and poor permeability, which can lead to infusion-related side effects. In addition, AmBs safety profile is affected by its capacity to self-aggregate in aqueous solutions. The AmB-loaded PLGA microspheres were made in an attempt to guarantee the highest therapeutic efficacy of AmB by increasing its solubility, lowering its toxic adverse effects, and facilitating delivery in monomeric form. The aim of this project is to evaluate the in vitro uptake of AmB-loaded PLGA microspheres on a monolayer cell line of Caco-2 cells. AmB-loaded PLGA microspheres were found to have medium permeability. The used concentration of AmB-loaded PLGA microspheres did not lead to apoptosis in Caco-2 cells, when cell viability assay was performed. Our promising results suggest that the AmB-loaded PLGA microspheres delivery system might be the key that enables us to shift from the intravenous administration to the oral administration of AmB.