Analysis of different innovative formulations of curcumin for improved relative oral bioavailability in human subjects

Martin Purpura,Jacob M Wilson,Gerald Münch,Valentina Razmovski-Naumovski,Ryan P Lowery,Haider Mannan

doi:10.1007/s00394-016-1376-9

Abstract

PurposeThe optimal health benefits of curcumin are limited by its low solubility in water and corresponding poor intestinal absorption. Cyclodextrins (CD) can form inclusion complexes on a molecular basis with lipophilic compounds, thereby improving aqueous solubility, dispersibility, and absorption. In this study, we investigated the bioavailability of a new γ-cyclodextrin curcumin formulation (CW8). This formulation was compared to a standardized unformulated curcumin extract (StdC) and two commercially available formulations with purported increased bioavailability: a curcumin phytosome formulation (CSL) and a formulation of curcumin with essential oils of turmeric extracted from the rhizome (CEO).MethodsTwelve healthy human volunteers participated in a double-blinded, cross-over study. The plasma concentrations of the individual curcuminoids that are present in turmeric (namely curcumin, demethoxycurcumin, and bisdemethoxycurcumin) were determined at baseline and at various intervals after oral administration over a 12-h period.ResultsCW8 showed the highest plasma concentrations of curcumin, demethoxycurcumin, and total curcuminoids, whereas CSL administration resulted in the highest levels of bisdemethoxycurcumin. CW8 (39-fold) showed significantly increased relative bioavailability of total curcuminoids (AUC0−12) in comparison with the unformulated StdC.ConclusionThe data presented suggest that γ-cyclodextrin curcumin formulation (CW8) significantly improves the absorption of curcuminoids in healthy humans.

Highlights

Curcuma longa L. (Zingiberaceae), known as turmeric, has been used in the traditional medicine in China and India for centuries
In microglia and macrophage cell lines, curcumin has shown to have an inhibitory effect on cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase expression, leading to decreased levels of prostaglandin E 2 (PGE2) and nitric oxide (NO) [7,8,9]
After a single dose of a capsule containing the inclusion complex of coenzyme Q10 with γ-cyclodextrin, the coenzyme Q10 plasma levels were significantly elevated [28]. These findings suggest that the complexation of lipophilic curcumin with γ-cyclodextrin may improve its bioavailability

Summary

Introduction

Curcuma longa L. (Zingiberaceae), known as turmeric, has been used in the traditional medicine in China and India for centuries. Curcumin has been shown to inhibit IL-6-induced STAT3 phosphorylation and consequent STAT3 nuclear translocation in multiple types of myeloma cell lines [4]. Cell culture studies have shown that curcumin. In microglia and macrophage cell lines, curcumin has shown to have an inhibitory effect on cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression, leading to decreased levels of prostaglandin E 2 (PGE2) and nitric oxide (NO) [7,8,9]. Curcumin decreases TNFα, IL-1, -2, -8, and -12 production in phorbol myristate acetate (PMA) or lipopolysaccharide (LPS) stimulated monocytes and alveolar macrophages in a concentrationand time-dependent manner, depicting its broad cytokinesuppressive anti-inflammatory action [10]

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