Sustained release olmesartan medoxomil loaded PLGA nanoparticles with improved oral bioavailability to treat hypertension

摘要

In the present study we have developed olmesartan medoxomil (OLM) loaded poly (lactic-co-glycolic) acid (PLGA) nanoparticles to improve the oral bioavailability of OLM. The nanoparticles of OLM-PLGA were prepared using simple one step electrospray method. The process was optimized for the flow rate, voltage applied and the distance between needle and collector. The developed OLM-PLGA was 527?±?50.21?nm in size with low size distribution (0.261?±?0.021). The entrapment efficiency of the particles was found to be 78.65?±?4.31%. The scanning electron microscopy (SEM) studies also revealed the homogenous distribution of particle size with smooth surface. The particles were found to be stable with extended in-vitro release profile and the complete release was obtained in 72?h. The in-vivo pharmacokinetic studies after the oral administration of OLM-PLGA in rats revealed the significantly high Cmax (17.66?±?3.64?μg/mL) and AUC (82.45?±?7.15?μg/mL*h) in comparison with OLM-suspension Cmax (5.21?±?1.12?μg/mL) and AUC (21.62?±?4.41?μg/mL*h). The current study revealed that the OLM could be well encapsulated in OLM-PLGA which could address the bioavailability issue of OLM and enhance its potency in the treatment of hypertension.