Enhanced Bioavailability of Boswellic Acid by Piper longum: A Computational and Pharmacokinetic Study

Abstract

Chronic inflammation is a key culprit factor in the onset and progression of several diseases. Novel and pharmacologically effective therapeutic approaches are needed for new treatment remedy or improved pharmacokinetics and pharmacodynamics for existing synthetic drugs, in particular natural products. Boswellic acids are well-known natural products, with capacity to effectively retard inflammation without severe adverse effects. However, the therapeutic use of Boswellic acids are greatly hindered by its poor pharmacokinetic properties. Co-administration strategies that facilitate the oral absorption and distribution of Boswellic acids should lead to a safe and more effective use of this product prophylactically and therapeutically in inflammatory disorders. In this study, we examined the effect of Piper longum extract on the absorption and bioavailability of Boswellic acid in rabbits. In addition, we further explored computational pharmacodynamic interactions between Piper longum and Boswellic acid. Piper longum extract at 2.5 and 10 mg/kg, increased the bioavailability of Boswellic acid (p < 0.05). Based on our drug-based computational modeling, cytochrome P450 (CYP450)-mediated mechanism was involved in increased bioavailability. These findings confirmed that Piper longum with Boswellic acid may be administered orally together for effective therapeutic efficacy. Thus, our studies support the application of Piper longum with Boswellic acid as a novel therapeutic avenue in diseases associated with inflammation.

Piper longum L.: A comprehensive review on traditional uses, phytochemistry, pharmacology, and health‐promoting activities

“…Piper longum extract was found to increase the bioavailability of boswellic acid ( p < .05). The results confirmed that P. longum may be administered orally with boswellic acid together for effective therapeutic efficacy (Vijayarani et al, 2020). Oxytetracycline (OTC) is used for the treatment of various bacterial, rickettsial, and mycoplasmal infections of poultry and other avian species.…”

Boswellic acids/Boswellia serrata extract as a potential COVID-19 therapeutic agent in the elderly

“…In addition, the bioavailability of the active ingredients after conventional use of chewable B. serrata has not yet been published. To overcome the poor bioavailability of the concentrated or isolated boswellic acids, attempts have been made to enhance the bioavailability by the combination of Piper longum (long pepper) and by producing specific compounds such as boswellic acids attached to phospholipids or incorporated into micelles (Hüsch et al 2013 ; Meins et al 2018 ; Vijayarani et al 2020 ). On the basis of the aforementioned studies, it is clear that B. serrata extract and boswellic acids may have a therapeutic effect against virus-induced secondary microbial infection and may be effective in preventing COVID-19 causing secondary infection and COVID-19 causing complications.…”

Cardiovascular toxin-induced hyperglycemic and hypoarousal pathology-associated cognitive impairment: an in silico and in vivo validation

“…To investigate the absorption, distribution, metabolism, and elimination (ADME) properties of alloxan and phenytoin, we used Schrödinger release 2021–1: (QikProp, Schrödinger, LLC, New York, NY, USA). QikProp was used to estimate various pharmacokinetic and pharmacodynamic properties (solvent accessible surface area [SASA], a hydrophobic component of SASA [FOSA], a hydrophilic component of SASA [FISA], carbon and attached hydrogen) component of the SASA [PISA–π], number of metabolites [#], CNS distribution, predicted brain/blood partition coefficient [QPlog BB], estimated number of donor hydrogen bonds [Donor HB], estimated number of accepted hydrogen bonds [Accept HB], logP, and % human oral absorption [percentage]) [5] .…”