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A liquid phospholipid formulation of a Curcumin extract with high concentration of phosphatidylcholine (PHOSAL® Curcumin) improves the transport of Curcuminoids across Caco-2 intestinal epithelial cells

corresponding

PHILIPP GEBHARDT*1, PETER VAN HOOGEVEST1, KARIN ENGELHART-JENTZSCH2
*Corresponding author
1. Lipoid GmbH, Ludwigwshafen am Rhein, Germany,
2. BioTeSys GmbH, Esslingen, Germany

Abstract

The use of curcumin as dietary supplement to ameliorate inflammation, arthritis, stomach, skin, liver, and gallbladder problems, is hampered by the lack of oral absorption. In this study, an in vitro digestion method and Caco-2 cell-lines were used to assess the influence of the solubilisation of curcuminoids in a liquid formulation comprising a high content of phosphatidylcholine on the transport of the curcuminoids across a Caco-2 cell monolayer, compared to powdered curcuminoids. A LC-MS method was used to assess the content of the curcuminoids after digestion and in the basolateral compartment of the Caco-2 model. It was found that the solubilization in the phospholipid concentrate significantly increases curcuminoids transport across the Caco-2 cells.


INTRODUCTION

Curcuminoids are the main yellow pigments found in turmeric (Curcuma longa), a traditional Indian spice. Positive health effects of curcuminoid supplementation have been observed in human clinical studies. Curcuminoids are reported to possess various biological activities, including antioxidant and anti-inflammatory effects (1). The curcuminoids extracted from turmeric are a mixture of three principal compounds curcumin (diferuloylmethane) (CC), desmethoxycurcumin (DMCC) and bisdesmethoxycurcumin (BDMCC), to which the positive health effects are attributed (2). Curcumin has very low water solubility and is therefore poorly absorbed after oral dosing. In addition, curcumin undergoes metabolic O-conjugation in the gastro intestinal (GI) tract epithelium (3) and liver to curcumin glucuronide and curcumin sulfate and bioreduction to tetrahydrocurcumin (THCC), hexahydrocurcumin, octahydrocurcumin, and hexahydrocurcuminol, followed by glucuronidation, with concomitant modification of activity (4). As a result of the poor absorption and metabolism, a dose-escalation study detected free curcumin concentrations of 0.03 to 0.06 ng/mL 1 to 4 h after a 10 ...




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