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

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.