title: Development and optimisation of 3-Acetyl-11-keto-β-boswellic acid loaded poly-lactic-co-glycolic acid-nanoparticles with enhanced oral bioavailability and in-vivo anti-inflammatory activity in rats.
abstract: OBJECTIVE
  3-Acetyl-11-keto-β-boswellic acid (AKBA) is a potent anti-inflammatory compound of Boswellia serrata. However, anti-inflammatory activity of AKBA is impeded by poor oral bioavailability due to its poor aqueous solubility. In this context, we aimed to develop poly lactic-co-glycolic acid (PLGA)-based nanoparticle formulation of AKBA (AKBA-NPs) in order to improve its oral bioavailability and in-vivo anti-inflammatory activity in rats.
  
  
  METHODS
  AKBA-NPs were prepared and characterised by analysing particle size and zeta potential using zeta sizer, surface morphology by scanning electron microscopy and transmission electron microscopy, and physical property using differential scanning calorimetry and X-ray diffraction techniques. The optimised nanoparticles were evaluated for in-vitro drug release and oral bioavailability studies, and in-vivo anti-inflammatory activity by carrageenan-induced rat paw oedema method.
  
  
  RESULTS
  The optimised AKBA-NPs showed the particle size of 179.6 nm with 0.276 polydispersity index and entrapment efficiency of 82.5%. AKBA-NPs showed increased in-vivo anti-inflammatory activity as compared with AKBA. Bioavailability study revealed about six times higher peak plasma concentration of AKBA in AKBA-NPs. Moreover, t1/2 and total area under the curve of AKBA were also enhanced by two and ninefold, respectively, in AKBA-NPs as compared with corresponding AKBA.
  
  
  CONCLUSIONS
  The promising results of improved oral bioavailability and in-vivo anti-inflammatory activity of AKBA suggested the successful nanoparticle formulation of AKBA.
authors: Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), SAS Nagar, Punjab, India.
authors: Khemraj
authors: K
authors: Bairwa
authors: Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), SAS Nagar, Punjab, India.
authors: Sanjay Madhukar
authors: SM
authors: Jachak
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D029743:Boswellia / Q000187:drug effects; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005260:Female; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D014315:Triterpenes / Q000737:chemistry*
chemical_list: D000893:Anti-Inflammatory Agents; D014315:Triterpenes; C094432:acetyl-11-ketoboswellic acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid
keywords: AKBA; Boswellia serrata; anti-inflammatory activity; nanoparticles; oral bioavailability