Background: 3-Acetyl-11-keto-β-boswellic acid (AKBA) has attracted considerable interest due to its therapeutic potential against inflammatory and cancer-related disorders. However, its poor oral bioavailability remains a critical limitation for clinical application. This study aimed to enhance the bioavailability of AKBA by developing a nanoemulsion (NE)-based delivery system.
Results: Several NE formulations were optimized and characterized based on drug loading, stability, and droplet size. The optimized NE-AKBA showed a particle size of 12–15 nm and was further tested for permeability across Caco-2 cell monolayers, followed by in vivo pharmacokinetic evaluation. Permeability studies revealed significantly improved transport of NE-AKBA within the first hour. Pharmacokinetic analysis indicated a notable increase in systemic exposure: the Cmax of AKBA rose from 3.36 to 12.23 μg/mL, while the AUC₀₋t increased from 4257 to 6222 μg·h/mL, with Tmax remaining steady at 6 hours.
Conclusion: These findings demonstrate that nanoemulsion-based delivery significantly improves the oral bioavailability of AKBA and provides a promising platform for its future therapeutic development.