Objective:
Olmesartan medoxomil (OLM) is a low bioavailability antihypertensive drug. This study was aimed to prepare and optimize an OLM niosomal gel and investigate the drug permeation via a chicken buccal pouch.
Methods:
OLM loaded niosomes were prepared using a film hydration technique. The vesicle size, zeta potential, entrapment efficiency, and percentage cumulative drug release of niosomes were evaluated. The niosomes were incorporated into a Carbopol 974P (1.5 % w/v) gel and drug permeability of niosomal gel was evaluated. The formulations of the niosomal gel were optimized using the Box-Behnken design. The optimized formulation was further characterized using transmission electron microscopy (TEM) and FTIR analysis.
Results:
The particle size and zeta potentials of optimized niosomal formulations were found to be 296.4 nm and -38.4 mV, respectively. Based on TEM analysis, the niosomes were found spherical in shape. The permeability, flux, and permeability coefficient of optimized niosomal gel was found to be 0.507 mg/cm2, 0.083 mg/cm2 × h, 041 cm/h, respectively. The histopathology evaluation revealed that the niosomal gel had better permeability compared to OLM gel.
Conclusion:
Based on the results of the OLM niosomal gel, it can be concluded that the formulation can be beneficial in increasing the bioavailability, resulting in better therapeutic efficacy.
Keywords: Box-Behnken design, Buccal delivery, Histopathology, Niosomal gel, Olmesartan medoxomil, Permeability