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

• Published in: NFS journal 2018-06, Vol.11, p.12-16
• Main Authors: Meins, Jürgen, Behnam, Dariush, Abdel-Tawab, Mona
• Format: Article
• Language: English
• Subjects: Absorption; Bioavailability; Boswellia serrata extract; Boswellic acids; Micellar solubilisation; Pharmacokinetics
• ISSN: 2352-3646; 2352-3646
• DOI: 10.1016/j.nfs.2018.04.001

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. 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. 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. Micellar solubilisation represents a promising approach for enhancing the bioavailability of poorly soluble substances. [Display omitted]