Curcumin possesses tremendous potential to benefit human health; however, its rapid biotransformation has often been cited as a reason for its limited bioavailability. Initial studies carried out to understand its pharmacokinetic properties indicated that following oral administration, Curcumin showed poor absorption resulting in lower blood concentration (traces) and most of it getting excreted in the faeces.
Since Curcumin undergoes rapid biotransformation in the gut and liver, it leads to speculations regarding the bioavailability and metabolic fate of Curcumin. As the research on Curcumin progressed with time, today we have a better insight of Curcumin’s metabolism in the body. Curcumin is metabolized by both conjugation and reduction pathways in the body resulting in formation of several metabolites.
Reference: Aggarwal BB, Nagabhushanam K, Pande A, Vaidyanathan P, Nayak M, Bani S, et al. Modulation of Immune System by Curcumin. In: Majeed M and Majeed A (Eds.), Curry Powder to Clinical Significance, 1st edition, New Jersey, NutriScience Publishers, LLC. 2015; pp.159.
Influence of Piperine on the Pharmacokinetics of Curcumin
Preclinical Study Findings:
- For the study, albino wistar rats (n=96) of both sexes were selected
- Animals were divided into two groups: one group received Curcumin (2 g/kg) alone, whereas second group was given Curcumin (2 g/kg) followed by BioPerine® (20 mg/kg)
- Pharmacokinetic profile was determined for both groups at different intervals: 0, 0.25, 0.50, 0.75, 1, 2, 3, 4, 5 & 6 h
- Results clearly showed the presence of Curcuminoids in higher concentration in the serum at 1 h and 2 h of administration of the combination of Curcumin and BioPerine®
- These encouraging results led to carry out the clinical trial for this combination
Clinical Study Findings:
- Shobha et al. carried out a randomized, cross-over clinical study at St. John’s Medical College, Bangalore, India to assess the potential of BioPerine® for increasing the bioavailability of Curcuminoids
- Ten healthy volunteers aged between 20–26 years were enrolled in this study
- The subjects were administered 2 g Curcumin followed by two weeks of washout period and crossed-over to receive 2 g of Curcumin and BioPerine® (20 mg) combination
- Blood samples were taken at 0.25, 0.5, 0.75, 1, 2, 3, 4, 5 and 6 h post administration on each occasion
- The outcome results were in accordance with earlier performed preclinical study
- Results demonstrated that BioPerine® enhanced the oral bioavailability of Curcumin with Curcumin serum concentration peaking at 1 h and relative bioavailability of Curcumin was found to be increased by 2000% or 20 folds by BioPerine®
- Both Curcumin and Curcumin-BioPerine® combination were well tolerated by the subjects with no adverse events
This study was path-breaking and first of its kind to demonstrate bio-enhancing potential of piperine in BioPerine®. The evidence showed that piperine is a potent inhibitor for metabolism of certain nutrients/dietary ingredients, which can alter the rate of glucuronidation in gut and liver, thus slowing down the transformation and increasing bioavailability of the nutrients.
Reference: Shoba et al. Influence of Piperine on the Pharmacokinetics of Curcumin in Animals and Human Volunteers. Planta Med.1998;64(4):353–56.