Nanoparticle formulation of 11-keto-β-boswellic acid (KBA): anti-inflammatory activity and in vivo pharmacokinetics

Pharm Biol. 2016 Dec;54(12):2909-2916. doi: 10.1080/13880209.2016.1194437. Epub 2016 Jun 16.


Context: The oleo-gum-resin of Boswellia serrata Roxb. (Burseraceae) is widely used for the treatment of inflammatory diseases such as osteoarthritis, rheumatoid arthritis and cancer. Anti-inflammatory activity of 11-keto-β-boswellic acid (KBA) is impeded by poor oral bioavailability due to its high lipid solubility, rapid phase-1 metabolism and poor intestinal permeability.

Objective: This study developed a poly-dl-lactide-co-glycolide-based nanoparticle formulation of KBA to improve its oral bioavailability and in vivo anti-inflammatory activity.

Materials and methods: KBA was isolated from the oleo-gum resin of B. serrata, and its nanoparticle formulation (KBA-NPs) was prepared by the emulsion-diffusion-evaporation method. Oral bioavailability of KBA and KBA-NPs was studied at 50 mg/kg p.o. dose in Sprague-Dawley rats, and further evaluated for in vivo anti-inflammatory activity in carrageenan-induced rat paw oedema assay at the same dose level.

Results: The prepared KBA-NPs had a particle size of 152.6 nm with polydispersity index of 0.194, 79.7% entrapment efficiency and a cumulative 61.5% release of KBA from KBA-NPs, at 72 h. KBA-NPs showed 60.8% inhibition of rat paw oedema at 5 h as compared to 34.9% as that of KBA. The results of oral bioavailability study and in vivo anti-inflammatory activity showed 7- and 1.7-fold increase in bioavailability and anti-inflammatory activity, respectively, of KBA in KBA-NPs as compared to KBA alone.

Conclusion: The results of improved oral bioavailability and in vivo anti-inflammatory activity of KBA-NPs suggested successful development of KBA nanoparticle formulation.

Keywords: Boswellia serrata; PLGA-based nanoparticles; in vitro drug release; oral bioavailability.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry*
  • Anti-Inflammatory Agents / pharmacokinetics*
  • Boswellia*
  • Chemistry, Pharmaceutical
  • Drug Liberation / physiology
  • Nanoparticles / chemistry*
  • Rats
  • Rats, Sprague-Dawley
  • Triterpenes / chemistry*
  • Triterpenes / pharmacokinetics*
  • X-Ray Diffraction


  • 11-keto-boswellic acid
  • Anti-Inflammatory Agents
  • Triterpenes