Amelioration of bioavailability through formulating and optimizing Azilsartan Entrapped nanostructured lipid carriers and its pharmacokinetic assessment

Abstract

Azilsartan is a typical BCS class II medication having good permeability but poor solubility, making it an excellent option for use as a model drug in our nanostructured lipid carrier study. Our major research goal was to construct and produce Azilsartan Nanostructured Lipid Carriers using a heated high-pressure homogenization approach in order to improve oral bioavailability. 3D Response surface plots show a visual representation of the relationship between the response variables and the set of controlled variables. The attainment of the objective was supported by the evaluation parameters profile, in-vitro drug release profile, and accelerated stability study of the optimised 23 full factorial design formulation. An optimised batch of AZL-NLCs displayed a particle size of 274.2 nm, a Zeta potential of −22.9 Mv, and an entrapment efficiency of 88%. The AZL-NLC's formulation had a biphasic pattern of release, with the burst release at the start, trailed by a steady release for up to 72 h. With a value of n > 0.5, the release curve was found to follow the Higuchi model, indicating a non-Fickian drug release mechanism with in-vivo pharmacokinetic experiments in Azilsartan-loaded NLCs showed a rise in t1/2, AUC0-∞, and Cmax compared to free drugs, indicating that bioavailability has been improved while elimination (Kel) has been reduced, implying that Azilsartan's action has been prolonged by loading in NLCs. These positive results show that designed AZL-NLCs for oral delivery have a lot of promise and could be a useful strategy for increasing bioavailability and hence improving therapeutic outcomes.