Enhanced absorption of boswellic acids by a micellar solubilized delivery form of Boswellia extract

Background: Boswellic acids (BAs) the pharmacologically active ingredients of the gum resin extract of Boswellia serrata are known for their anti-inflammatory effects. However they suffer from poor bioavailability because of their hydrophobicity and poor water solubility. Purpose: The present study aimed at investigating the effect of AQUANOVA micellation technology on the bioavailability of Boswellia extract in rats compared to its native form.Study design.Female albino wistar rats (n = 6) weighing around 250 g were orally administered solubilized (Sol-BE) and native (Nat-BE) Boswellia extract at an equimolar dosage of 128 mg/kg. Plasma samples collected at defined time points (0, 0.5, 1, 2, 3, 4, 6 and 8 h) were analyzed for the content of the six major boswellic acids (KBA, AKBA, αBA, βBA, AαBA and AβBA - 11-keto-β-boswellic acid (KBA), acetyl-11-keto-β-boswellic acid (AKBA), α-boswellic acid (αBA), β-boswellic acid (βBA), acetyl-α-boswellic acid (AαBA) and acetyl-β-boswellic acid (AβBA)) using a sensitive LC-MS/MS method. Results: The oral administration of Sol-BE led to a remarkable increase in the AUC and Cmax of all BAs in plasma compared to Nat-BE. Whereas no KBA could be detected after the administration of Nat-BE, KBA could be detected at a maximal plasma concentration of 439.21 ng/mL and an AUClast of 1185.37 ng/mL*h following the administration of Sol-BE. The highest increase was observed in the case of AKBA where a 56-fold increase in the AUClast and a 25-fold increase in the Cmax was determined compared to Nat-BE. Conclusions: Micellar solubilisation represents a promising approach for enhancing the bioavailability of poorly soluble substances. Keywords: Boswellia serrata extract, Boswellic acids, Micellar solubilisation, Bioavailability, Absorption, Pharmacokinetic