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Comparison of systemic availability of curcumin with that of curcumin formulated with phosphatidylcholine

By Timothy H. Marczylo, Richard D. Verschoyle, Darren N. Cooke, Paolo Morazzoni, William P. Steward and Andreas J. Gescher

Abstract

This is the author's final draft. 'The original publication is available at www.springer-link.com'Purpose: Curcumin, a major constituent of the spice turmeric, suppresses expression of the enzyme cyclooxygenase 2 (Cox-2) and has cancer chemopreventive properties in rodents. It possesses poor systemic availability. We explored whether formulation with phosphatidylcholine increases the oral bioavailability or affects the metabolite profile of curcumin. Methods: Male Wistar rats received 340 mg/Kg of either unformulated curcumin or curcumin formulated with phosphatidylcholine by oral gavage. Rats were killed at 15, 30, 60 and 120 min post intubation. Plasma, intestinal mucosa and liver were analysed for the presence of curcumin and metabolites using HPLC with UV detection. Identity of curcumin and metabolites was verified by negative ion electrospray liquid chromatography/tandem mass spectrometry. Results: Curcumin, the accompanying curcuminoids desmethoxycurcumin and bisdesmethoxycurcumin, and the metabolites tetrahydrocurcumin, hexahydrocurcumin, curcumin glucuronide and curcumin sulfate were identified in plasma, intestinal mucosa and liver of rats which had received formulated curcumin. Peak plasma levels and area under the plasma concentration time curve (AUC) values for parent curcumin after administration of formulated curcumin were five-fold higher than the equivalent values seen after unformulated curcumin. Similarly, liver levels of curcumin were higher after administration of formulated curcumin as compared to unformulated curcumin. In contrast, curcumin concentrations in the gastrointestinal mucosa after ingestion of formulated curcumin were somewhat lower than those observed after administration of unformulated curcumin. Similar observations were made for curcumin metabolites as for parent compound. Conclusion: The results suggest that curcumin formulated with phosphatidylcholine furnishes higher systemic levels of parent agent than unformulated curcumin

Publisher: Springer
Year: 2007
OAI identifier: oai:lra.le.ac.uk:2381/511

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  1. 3). Star indicates that values at that time point were significantly different from each other (p <0.01). For details of administration and hplc analysis see Materials and methods.
  2. (2003). Cancer chemoprevention with dietary phytochemicals. doi
  3. (1995). Chemoprevention of colon carcinogenesis by dietary curcumin, a naturally occurring plant phenolics compound.
  4. (2002). Curcumin exerts multiple suppressive effects on human breast carcinoma cells. doi
  5. (1987). Diarylheptanoids from the rhizomes of curcuma xanthorrhiza and alponia officinarum. doi
  6. (2005). Improvement of antischistosomal activity of praziquantel by incorporation into phosphatidylcholine-containing liposomes. doi
  7. (1999). Inhibition of cyclo-oxygenase 2 expression in colon cells by the chemopreventive agent curcumin involves inhibition of NF- kappa B activation via the NIK/IKK signalling complex. doi
  8. (2005). Liposome-encapsulated curcumin - In vitro and in vivo effects on proliferation, apoptosis, signaling, and angiogenesis. doi
  9. (2004). Phase I clinical trial of oral curcumin: Biomarkers of systemic activity and compliance.

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