Background <p>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.</p> Results <p>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&#xa0;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<sub>max</sub> increased from 3.36 to 12.23&#xa0;µg/mL and AUC<sub>0 − t</sub> increased from 40.9 to 72.1&#xa0;µg·h/mL, while T<sub>max</sub> remained unchanged at 6&#xa0;h, indicating an enhanced extent of absorption without alteration of absorption kinetics.</p> Conclusion <p>These findings demonstrate that nanoemulsion-based delivery significantly improves the oral bioavailability of AKBA and provides a promising platform for its future therapeutic development.</p> Graphical Abstract <p></p>

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Development of a nanoemulsion incorporating 3-acetyl-11-keto-β-boswellic acid (AKBA): solubility and oral bioavailability through in vitro and in vivo studies

  • Najmeh Ketabchi,
  • Seyed Nasser Ostad,
  • Mahmoud Ghazi-Khansari,
  • Hossein Ghanbari,
  • Fariba Esmaeili,
  • Amir Amani

摘要

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: Cmax increased from 3.36 to 12.23 µg/mL and AUC0 − t increased from 40.9 to 72.1 µg·h/mL, while Tmax 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.

Graphical Abstract