Comparing a Single Dose of Two Boswellia Supplements in Healthy Volunteers

Jenn Hoskins
22nd July, 2024

Comparing a Single Dose of Two Boswellia Supplements in Healthy Volunteers

Image Source: Natural Science News, 2024

Key Findings

  • Researchers at Ulm University found that a micellar formulation of Boswellia serrata significantly increased the bioavailability of its active compounds compared to a native formulation
  • The micellar extract improved the absorption of boswellic and lupeolic acids by 1,720-4,291%, with acetyl-11-keto-β-boswellic acid (AKBA) showing the highest increase
  • Despite the higher bioavailability, both the micellar and native formulations showed similar anti-inflammatory effects, reducing the release of the proinflammatory cytokine TNF-α
The anti-inflammatory properties of Boswellia serrata, a traditional Ayurvedic remedy, have garnered significant attention in recent years. Extracts from the oleogum resins of Boswellia trees are known for their potential to treat various inflammatory conditions. However, the challenge of improving the oral bioavailability of these extracts has persisted. A recent study conducted by researchers at Ulm University aimed to address this issue by comparing the pharmacokinetics and pharmacodynamics of two Boswellia serrata nutraceuticals: the native Biotikon® BS-85 and the micellar Boswellia-Loges®[1]. The study involved a single-dose crossover clinical trial with 20 healthy volunteers. Each participant received an 800 mg dose of either the native or micellar formulation. Plasma concentrations of eight boswellic and lupeolic acids were measured over 48 hours using high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS/MS). Additionally, blood samples collected at 2 and 5 hours post-administration were analyzed for proinflammatory cytokine release following stimulation with lipopolysaccharide. The findings revealed that the micellar extract significantly increased the maximum plasma concentration (Cmax) and the area under the curve (AUC0-48) while shortening the time to reach maximum concentration (Tmax) for all boswellic and lupeolic acids compared to the native extract. Specifically, the relative bioavailability of these acids increased by 1,720-4,291%, with acetyl-11-keto-β-boswellic acid (AKBA) showing the highest difference. This increase in bioavailability is particularly noteworthy given previous studies that highlighted the poor absorption of AKBA following oral administration[2]. The enhanced bioavailability of the micellar formulation suggests that it could potentially overcome the limitations observed in earlier research. Despite the improved bioavailability, the study found no significant differences in the anti-inflammatory efficacy between the micellar and native formulations. Both preparations reduced the release of the proinflammatory cytokine TNF-α. The native Biotikon® BS-85 formulation also diminished the release of IL-1β and IL-6, although the micellar formulation did not show a significant difference in this regard. In a lymphocytic gene reporter cell line, both nutraceuticals inhibited the activity of the NF-κB transcription factor and the release of TNF-α, with the native formulation being more efficient in inhibiting TNF-α. These results align with earlier findings that suggest the anti-inflammatory properties of Boswellia serrata may not solely depend on its bioavailability. For instance, previous research indicated that β-boswellic acid, rather than AKBA, might be responsible for the anti-inflammatory effects due to its ability to inhibit microsomal prostaglandin E synthase-1 and cathepsin G[2]. This study further supports the notion that the pharmacodynamic effects of Boswellia extracts are complex and not solely determined by plasma concentrations of specific acids. Moreover, the study's methodology highlights the importance of considering drug formulation design in enhancing oral absorption. Previous reviews have discussed how surfactants can modulate the activity of transporters and carriers, potentially influencing drug absorption[3]. The micellar formulation's success in increasing bioavailability may be attributed to such interactions, although further research is needed to elucidate the exact mechanisms. In conclusion, the study by Ulm University demonstrates that while micellar formulations of Boswellia serrata significantly enhance the bioavailability of its active compounds, this does not necessarily translate to increased anti-inflammatory efficacy. These findings underscore the complexity of Boswellia's pharmacodynamics and suggest that factors beyond bioavailability, such as specific molecular targets and interactions, play crucial roles in its therapeutic effects. Further research is warranted to fully understand these mechanisms and optimize the clinical use of Boswellia serrata extracts.

MedicineHealthBiochem

References

Main Study

1) Single-dose comparative pharmacokinetic/pharmacodynamic study of a micellar formulation versus a native Boswellia serrata dry extract in healthy volunteers.

Published 20th July, 2024

https://doi.org/10.1016/j.phymed.2024.155863

Related Studies

2) Boswellia serrata: an overall assessment of in vitro, preclinical, pharmacokinetic and clinical data.

https://doi.org/10.2165/11586800-000000000-00000

3) Nonionic surfactants modulate the transport activity of ATP-binding cassette (ABC) transporters and solute carriers (SLC): Relevance to oral drug absorption.

https://doi.org/10.1016/j.ijpharm.2019.05.033


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