Abstract
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 droplet size of 12-15 nm, a low polydispersity index, and a zeta potential of - 14.5 mV. Permeability studies revealed significantly improved transport of NE-AKBA across Caco-2 monolayers within the first hour. Pharmacokinetic analysis revealed a notable increase in systemic exposure: C(max) increased from 3.36 to 12.23 µg/mL and AUC(0 - t) increased from 40.9 to 72.1 µg·h/mL, while T(max) remained unchanged at 6 h, indicating an enhanced extent of absorption without alteration of absorption kinetics. 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.