Itraconazole is a potent antifungal agent, which has poor solubility and high first-pass metabolism, thus limiting its oral bioavailability. The present research work focuses on the enhancement of itraconazole's bioavailability through the formulation and evaluation of a nanoemulsion. A nanoemulsion was prepared with the help of Tween 80, medium-chain triglycerides, and propylene glycol. It was ensured the stability of the drug was ensured through mean particle size, 180 nm, polydispersity index of 0.15, and zeta potential of -22.4 mV. In vitro drug release experiments showed that the amount released was 88% within 4 hours, which is significantly higher compared to the output from the basic suspension with around 50% release. The ex vivo permeation experiments showed improvement in the drug permeability, sixfold. Pharmacokinetic studies in rats demonstrated high values of the obtained peak concentrations C_max of 25.4 μg/ml, and AUC_0-∞ of 110.2 μg·hr/ml. Stability studies from three months' duration showed a broader durability of the formulation. Noticeably, the outcome is a novel agent in this clinical environment that can increase oral bioavailability and simultaneously enhance drug activity.