Enhanced absorption of boswellic acids by a lecithin delivery form (Phytosome®) of Boswellia extract

Abstract

The anti-inflammatory potential of Boswellia serrata gum resin extracts has been demonstrated in vitro and in animal studies as well as in pilot clinical trials. However, pharmacokinetic studies have evidenced low systemic absorption of boswellic acids (BAs), especially of KBA and AKBA, in rodents and humans. This observation has provided a rationale to improve the formulation of Boswellia extract. We present here the results of a murine comparative bioavailability study of Casperome™, a soy lecithin formulation of standardized B. serrata gum resin extract (BE), and its corresponding non-formulated extract. The concentration of the six major BAs [11-keto-β-boswellic acid (KBA), acetyl-11-keto-β-boswellic acid (AKBA), β-boswellic acid (βBA), acetyl-β-boswellic acid (AβBA), α-boswellic acid (αBA), and acetyl-α-boswellic acid (AαBA)] was evaluated in the plasma and in a series of tissues (brain, muscle, eye, liver and kidney), providing the first data on tissue distribution of BAs. Weight equivalent and equimolar oral administration of Casperome™ provided significantly higher plasma levels (up to 7-fold for KBA, and 3-fold for βBA quantified as area under the plasma concentration time curve, AUC(last)) compared to the non-formulated extract. This was accompanied by remarkably higher tissue levels. Of particular relevance was the marked increase in brain concentration of KBA and AKBA (35-fold) as well as βBA (3-fold) following Casperome™ administration. Notably, up to 17 times higher BA levels were observed in poorly vascularized organs such as the eye. The increased systemic availability of BAs and the improved tissue distribution, qualify Casperome™ for further clinical development to fully exploit the clinical potential of BE.

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

“…Incorporating bioactive phytoconstituents into phospholipid molecules is reported to improve the aqueous solubility, the membrane permeability, and hence the systemic absorption and bioavailability of the active phytoconstituents. Such complexes are appropriately called phytosomes, herbosomes, or naturosomes (3,4). Studies have reported success in improving the pharmacological profiles of several bioactive phytoconstituents using drugphospholipid complexation technique (5-9).…”

Comparative studies of pharmacokinetics and anticoagulatory effect in rats after oral administration of Frankincense and its processed products

“…Therefore, poor absorption and tissue penetration of BAs have been speculated. It was reported that a lecithin delivery form significantly improved absorption of BAs (Hüsch et al, 2013). To our knowledge, efficacy of FRA was significantly enhanced after processed.…”

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“…The study showed significantly higher plasma levels (up to 7-fold for KBA, and 3-fold for βBA quantified as area under the plasma concentration time curve, AUC last ) for weight equivalent and equimolar oral administration of Casperome™ compared to the non-formulated extract 69 .…”