Permeation of Boswellia extract in the Caco-2 model and possible interactions of its constituents KBA and AKBA with OATP1B3 and MRP2
Language: 
English
Abstract: 

Traditionally Boswellia serrata extract is used in the Indian Ayurvedic medicine for the treatment of inflammatory diseases. In 2002 the EMEA designated Boswellia an orphan drug status for the treatment of peritumoral oedema. Pharmacokinetic studies yielded low plasma concentrations of the active ingredients 11-keto-beta-boswellic acid (KBA) and 3-acetyl-11-keto-beta-boswellic acid (AKBA). In continuation of the tests investigating the factors limiting bioavailability of boswellic acids, the present study examined the permeability of KBA and AKBA in human Caco-2 cell lines. In addition, the interaction of KBA and AKBA with the organic anion transporter OATP1B3 and the multi drug resistant proteins P-glycoprotein and MRP2 was evaluated using partly fluorescent-based assays. The permeability studies revealed poor permeability of AKBA and moderate absorption of KBA with a P(app) value of 1.69 x 10(-6) cm/s. Most of KBA and AKBA were found to be retained by the Caco-2 monolayer. Neither KBA nor AKBA could be identified as substrates of P-glycoprotein. However, both KBA and AKBA modulated the activity of OATP1B3 and MRP2, indicating that therapeutic relevant interactions with other anionic drugs may be expected. The results of the present study provide the first explanation for the pharmacokinetic properties of KBA and AKBA.

Author(s): 
Krüger, Phillip
Kanzer, Johanna
Hummel, Jessica
Fricker, Gert
Schubert-Zsilavecz, Manfred
Abdel-Tawab, Mona
Item Type: 
Journal Article
Publication Title: 
European Journal of Pharmaceutical Sciences: Official Journal of the European Federation for Pharmaceutical Sciences
Journal Abbreviation: 
Eur J Pharm Sci
Publication Date: 
Feb 15, 2009
Publication Year: 
2009
Pages: 
275-284
Volume: 
36
Issue: 
2-3
ISSN: 
1879-0720
DOI: 
10.1016/j.ejps.2008.10.005
Library Catalog: 
NCBI Published Medical (?)
Extra: 
PMID: 19010411

Turabian/Chicago Citation

Phillip Krüger, Johanna Kanzer, Jessica Hummel, Gert Fricker, Manfred Schubert-Zsilavecz and Mona Abdel-Tawab. Feb 15, 2009. "Permeation of Boswellia extract in the Caco-2 model and possible interactions of its constituents KBA and AKBA with OATP1B3 and MRP2." European Journal of Pharmaceutical Sciences: Official Journal of the European Federation for Pharmaceutical Sciences 36: 2-3: 275-284. 10.1016/j.ejps.2008.10.005.

Wikipedia Citation

<ref> {{Cite journal | doi = 10.1016/j.ejps.2008.10.005 | issn = 1879-0720 | volume = 36 | pages = 275-284 | last = Krüger | first = Phillip | coauthors = Kanzer, Johanna, Hummel, Jessica, Fricker, Gert, Schubert-Zsilavecz, Manfred, Abdel-Tawab, Mona | title = Permeation of Boswellia extract in the Caco-2 model and possible interactions of its constituents KBA and AKBA with OATP1B3 and MRP2 | journal = European Journal of Pharmaceutical Sciences: Official Journal of the European Federation for Pharmaceutical Sciences | date = Feb 15, 2009 | pmid = | pmc = }} </ref>