A single-dose, randomized, cross-over, two-way, open-label study for comparing the absorption of boswellic acids and its lecithin formulation

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• 作者：Antonella Riva^a ; Paolo Morazzoni^a ; Christian Artaria^a ; Pietro Allegrini^a ; Jü ; rgen Meins^b ; Daniele Savio^c ; Giovanni Appendino^d ; Manfred Schubert-Zsilavecz^e ; Mona Abdel-Tawab^b ; ^{m.tawab@zentrallabor.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Boswellia serrata ; Frankincense ; Boswellic acids ; Triterpenoids ; Lecithin ; Absorption
• 刊名：Phytomedicine
• 出版年：2016
• 出版时间：15 November 2016
• 年：2016
• 卷：23
• 期：12
• 页码：1375-1382
• 全文大小：800 K

文摘

The oral administration of the gum resin extracts of Indian frankincense (Boswellia serrata Roxb. ex Colebr) results in very low plasma concentrations of boswellic acids (BAs), being far below the pharmacologically active concentrations required in vitro for anti-inflammatory activity. For that reason the use of Indian frankincense in clinical practice and pharmaceutical development has substantially lagged behind. Recently the application of new formulation technologies resulted in a formulation of frankincense extract with lecithin, which revealed improved absorption and tissue penetration of BAs in a rodent study, leading for the first time to plasma concentrations of BAs in the range of their anti-inflammatory activity.

Purpose

In order to verify these encouraging results in humans, the absorption of a standardized Boswellia serrata extract (BE) and its lecithin formulation (CSP) was comparatively investigated in healthy volunteers.

Study design

According to a randomized cross-over design with two treatments, two sequences and two periods, 12 volunteers alternatively received the lecithin-formulated Boswellia extract (CSP) or the non-formulated Boswellia extract (BE) at a dosage of 2 × 250 mg capsules.

Methods

The plasma concentrations of the six major BAs (KBA, AKBA, βBA, αBA, AβBA, AαBA) were determined using LC/MS.

Results

With the exception of KBA, a significantly higher (both in terms of weight-to-weight and molar comparison) and quicker absorption of BAs from the lecithin formulation was observed, leading to C_max in the range required for the interaction with their molecular targets.

Conclusion

These findings pave the way to further studies evaluating the clinical potential of BAs, and verify the beneficial effect of lecithin formulation to improve the absorption of poorly soluble phytochemicals.