Physiological barriers to the oral delivery of curcumin
Berginc, Katja (Author), Trontelj, Jurij (Author), Škalko-Basnet, Nataša (Author), Kristl, Albin (Author)

URLURL - Presentation file, Visit http://pharmazie.govi.de/contents_0612.htm This link opens in a new window

Curcumin, a principal component from Curcuma longa, with antioxidant and anti-inflammatory activities was proposed as a potential candidate for the preventation and/or treatment of cancer and chronic diseases. However, curcumin could not achieve its expected therapeutic outcome in clinical trialsdue to its low solubility and poor bioavailability. The actual intestinal physiological barriers limiting curcumin absorption after oral administration have not been fully investigated. To identify the main barrierscurtailing its absorption, in vitro permeability of curcumin and flux of its glucuronide were monitored in rat jejunum and Transwell grown Caco-2 cells. Curcumin was more permeable under acidic conditions, but the permeability was substantially below the permeability of highly permeable standards. Its efflux could not be inhibited by specific Pgp and MRP inhibitors. BCRP was found to participate in curcumin transport, but the Organic Anion Transporting Polypeptide (OATP) did not. The permeability of curcumin significantly increased when the structure of mucus was compromised. The inhibitor of curcumin metabolism, piperin, failed to act as a permeabilityenhancer. Piperin inhibited Pgp and MRP transporters and decreasedthe amount of glucuronide transported back into the intestine. Inclusion of piperin in curcumin-containing formulations is highly recommendedas to inhibit curcumin glucuronidation and to increase the transport of formed glucuronides into the plasma, therefore increasing the probability of glucuronide distribution into target tissue and inter-convertion to curcumin. It would also be beneficial, if curcumin delivery systems could reversibly compromise the mucous integrity to minimize the non-specific binding of curcumin to its constituents.

Keywords:Curcuma longa, Caco-2 celice, MRP inhibitorji, permeabilnost
Work type:Not categorized (r6)
Tipology:1.01 - Original Scientific Article
Organization:FFA - Faculty of Pharmacy
Number of pages:str. 518-524
Numbering:Vol. 67, no. 6
ISSN on article:0031-7144
DOI:10.1691/ph.2012.1112 Link is opened in a new window
COBISS.SI-ID:3251313 Link is opened in a new window
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Shortened title:Pharmazie
Publisher:Verlag Volk und Gesundheit
COBISS.SI-ID:1720079 This link opens in a new window

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