Preparation and Evaluation of Eprosartan Mesylate loaded PLGA Nanostructures

Abstract

In modern medication, drug-loaded novel polymeric nanoparticles have potential advantages over conventional dosage forms. The present study focused on the formulation development and evaluation of newly introduced angiotensin receptor blocker (ARB) eprosartan mesylate loaded biodegradable acid terminated poly(lactide-co-glycolide) (50:50) nanoparticle using double emulsion solvent evaporation technique. This methodology was found to improve the therapeutic efficacy as Eprosartan Mesylate belongs to BCS class-II and water-insoluble antihypertensive drug with 13% bioavailability. In the earlier stage, screening was performed to find out the suitable combination of excipients (Polyvinyl alcohol, Dichloromethane and Ethanol) to formulate the nanoparticles. In this present study, the physical and chemical properties of polymer and drug were determined before and after the formulation of nanoparticles using experimental techniques, such as Differential Light Scattering (DLS), zeta potential, X-ray Deffractometry (XRD), Fourier-Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Liquid Chromatography-Mass Spectrometry (LC-MS/MS) analysis. The eprosartan mesylate loaded PLGA nanoparticles showed fairly monodispersive, as determined from DLS (average particle diameter 136 nm, Poly Dispesity Index = 0.3). The zeta potential was found to be -10.8mV. This formulation showed a prolonged improved drug release (82.03%) for 360 hours in phosphate buffer (pH7.4) as compared to the conventional marketed dosage form. In-vitro release kinetics data of NPs (R2=0.8979) and diffusion exponent values (n=0.3328) suggested that optimized followed the Korsmeyer-Peppas model with Fickian mechanism.