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A pharmacokinetic study and critical reappraisal of curcumin formulations enhancing bioavailability.

Maurice A G M Kroon1, Hanneke W M van Laarhoven2,3, Eleonora L Swart1

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Curcumin bioavailability is limited, with most formulations showing minimal unconjugated curcumin in plasma. Enhanced absorption formulations did not significantly increase levels, and piperine offered no benefit.

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Area of Science:

  • Pharmacokinetics
  • Nutritional Science
  • Natural Product Chemistry

Background:

  • Curcumin, a compound from turmeric, has shown therapeutic potential but suffers from poor bioavailability.
  • Various formulations aim to enhance curcumin absorption and efficacy.
  • Understanding the fate of curcumin in the body is crucial for its therapeutic application.

Purpose of the Study:

  • To compare the bioavailability and excretion of three curcumin formulations (AOV, Longvida, NovaSOL) in healthy males.
  • To evaluate the effect of piperine on curcumin bioavailability.
  • To determine whether enhanced uptake formulations achieve clinically relevant plasma concentrations of unconjugated curcumin.

Main Methods:

  • Independent crossover study involving nine healthy male participants.
  • Administration of three curcumin formulations (AOV, Longvida, NovaSOL) at ~570 mg, with AOV also tested at 2280 mg, with and without piperine.
  • Measurement of plasma curcumin levels (unconjugated and conjugates) and fecal excretion.

Main Results:

  • Plasma levels of unconjugated curcumin were generally low (<2 nM) across most formulations, including high-dose AOV with piperine.
  • NovaSOL formulation resulted in transiently higher plasma curcumin levels (6.7-38 nM), but these declined rapidly and were significantly lower than in vitro effective concentrations.
  • Curcumin conjugates were present at higher levels than unconjugated curcumin, especially with NovaSOL.
  • Fecal recovery indicated significant excretion of unconjugated curcuminoids, suggesting limited absorption, except for NovaSOL.
  • Piperine addition did not improve curcumin bioavailability.

Conclusions:

  • Bioavailability of curcumin, even with enhanced formulations, remains a challenge, with minimal unconjugated curcumin reaching systemic circulation.
  • Plasma concentrations achieved are substantially lower than those demonstrating biological effects in vitro.
  • Bioavailability assessments should focus on unconjugated curcumin, not its conjugates, due to differences in membrane permeability and biological relevance.