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Synthesis,physicochemical characterisation and biological activity of anandamide/ɛ‐polycaprolactone nanoparticles obtained by electrospraying
Authors:Virna M Martín Gimnez  Marcos G Russo  Griselda E Narda  Lucía B Fuentes  Luciana Mazzei  Carlos Gamarra&#x;Luques  Diego E Kassuha  Walter Manucha
Abstract:Drug encapsulation in nanocarriers such as polymeric nanoparticles (Nps) may help to overcome the limitations associated with cannabinoids. In this study, the authors’ work aimed to highlight the use of electrospraying techniques for the development of carrier Nps of anandamide (AEA), an endocannabinoid with attractive pharmacological effects but underestimated due to its unfavourable physicochemical and pharmacokinetic properties added to its undesirable effects at the level of the central nervous system. The authors characterised physicochemically and evaluated in vitro biological activity of anandamide/ɛ‐polycaprolactone nanoparticles (Nps‐AEA/PCL) obtained by electrospraying in epithelial cells of the human proximal tubule (HK2), to prove the utility of this method and to validate the biological effect of Nps‐AEA/PCL. They obtained particles from 100 to 900 nm of diameter with a predominance of 200–400 nm. Their zeta potential was −20 ± 1.86 mV. They 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.Inspec keywords: cellular biophysics, molecular biophysics, nanoparticles, nanofabrication, biochemistry, encapsulation, drugs, neurophysiology, electrokinetic effects, enzymes, biomedical materials, nanomedicine, polymers, sprayingOther keywords: electrospraying techniques, pharmacological effects, pharmacokinetic properties, in vitro biological activity, biological effect, HK2 cells, optimal physicochemical properties, polymeric nanoparticles, AEA pharmaceutical formulation development, anandamide‐ε‐polycaprolactone nanoparticles, drug encapsulation, nanocarriers, endocannabinoid, central nervous system, epithelial cells, human proximal tubule, zeta potential, stable encapsulation, dose‐dependent capacity, Na+ ‐K+ ATPase activity, physical stability, size 100.0 nm to 900.0 nm, NO, Na+ ‐K+
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