Lipid based drug delivery system to enhance the oral bioavailability of olmesartan and azilsartan

Abstract

Dissolution rate is the limiting step in the absorption of water insoluble drugs (Both BCS newlineClass II and Class IV drugs) which in turn limits the therapeutic efficacy. The challenge for newlinethese drugs is to enhance the rate of dissolution without impacting their permeability. newlineHence, the present investigation was aimed to improve the bioavailability of insoluble newlinedrugs Olmesartan Medoxomil (BCS Class II) and Azilsartan Medoxomil (BCS Class IV) newlineby two novel lipid based approaches such as Lipid Base Liquisolid Compaction and Lipid newlineBased Solid Dispersions. Formulations of both the drugs prepared by liquisolid compaction newlineand solid dispersion have shown enhanced drug release compared to pure drug. More newlineimprovement in dissolution rate was observed with lipid based liquisolid compaction than newlinelipid based solid dispersion. This might be due to the presence of liquid inside the newlineformulation which might be acted as co-solvent. In support of in vitro dissolution studies, newlineEx Vivo goat intestinal permeability studies performed were also revealed that the liquisolid newlineformulations have shown greater drug diffusion than remaining formulations. In Vivo newlinestudies revealed that bioavailability of final optimized formulations of both the drugs was newlinehigher than the marketed formulation as well as pure drug. Hence, it can be concluded that, newlineliquisolid technique would be a promising approach in improving dissolution rate and newlinehence the bioavailability of water insoluble drugs such as Olmesartan and Azilsartan. newline