Synthesis, physicochemical characterization and biological activity of anandamide/ε-polycaprolactone nanoparticles obtained by electrospraying

Abstract

Drug encapsulation in nanocarriers such as polymeric nanoparticles (Nps) may help to overcome the limitations associated with cannabinoids. In this sense, our work aimed to highlight the use of electrospraying technique for the development of carrier Nps of anandamide (AEA), an endocannabinoid with attractive pharmacological effects but underestimated due to its unfavorable physicochemical and pharmacokinetic properties added to its undesirable effects at the level of the central nervous system. We characterized physicochemically and evaluated in vitro biological activity of anandamide/ε-polycaprolactone nanoparticles (Nps-AEA/PCL) obtained by electrospraying in epithelial cells of human proximal tubule (HK2), to prove the utility of this method and to validate the biological effect of Nps-AEA/PCL. We obtained particles from 100 to 900 nm of diameter with a predominance of 200 a 400 nm. Their zeta potential was -20±1.86 mV. We demonstrated the stable encapsulation of AEA in Nps-AEA/PCL, as well as its dose-dependent capacity to induce the expression of iNOS and NO levels and to decrease the Na+/K+ ATPase activity in HK2 cells. Obtaining Nps-AEA/PCL by electrospraying would represent a promising methodology for a novel AEA pharmaceutical formulation development with optimal physicochemical properties, physical stability and biological activity on HK2 cells.