Obtaining, characterization and evaluation of in vitro activity of anandamide/polycaprolactone nanoparticles.

MARTíN GIMENEZ V; ALVAREZ LORENZO C; MAZZEI L; GAMARRA LUQUES C; KASSUHA D; MANUCHA W

Mendoza

Congreso; XXXVI Reunion Anual de la Sociedad de Biologia de Cuyo.; 2018

Sociedad de Biologia de Cuyo

Endogenous cannabinoids, such as anandamide, represent an attractive therapeutic potential in a significate number of pathologies. The present study had as objective to synthesize, to characterize and to assess the biological activity of anandamide/å-polycaprolactone nanoparticles (Nps-AEA/PCL) in cell culture of epithelial cells of human proximal tubule (HK2). Nps-AEA/PCL were produced by electrospraying method and characterized by Differential Calorimetry Scanning (DSC), Thermogravimetry (TGA), Scanning Electron Microscopy (SEM), Infrared Spectroscopy by Fourier Transform (FTIR), UV-Visible spectroscopy (UV-Vis), and Dynamic Light Scattering (DLS). Physical stability studies were carried out on these nanoparticles. Also, we measured inducible nitric oxide synthase (iNOS) expression by Western blot, nitric oxide (NO) levels (nitrites) by Griess reaction, and Na+/K+ ATPase activity by a colorimetric method in HK2 cells. The obtained particles had a size between 100 to 900 nm of diameter with a predominance of 200 to 400 nm, with a Z potential value of -20±1.86 mV, indicating their good stability in solution. We observed the stable encapsulation of AEA in Nps-AEA/PCL, as well as its ability to induce the expression of iNOS and NO levels and to decrease the Na+/K+ ATPase activity in HK2 cells, in a dose-dependent manner. We concluded that obtaining Nps-AEA/PCL by electrospraying would be a useful methodology for a new pharmaceutical formulation development with optimal physicochemical properties, physical stability and biological activity on HK2 cells. Future works should increase the know-how about this novel alternative and its feasibility as treatment of cardiovascular diseases, particularly of arterial hypertension.