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: Majeed M. and Badmaev V. Curcuminoids-Pharmacological Actions Including Pre-Clinical  and  Clinical Evaluations. In: Curcuminoids: Antioxidant phytonutrients, New Jersey, Nutriscience Publishers Inc., 2003;pp. 32
Potentiating Therapeutic Utility of Curcumin C3 Complex® with BioPerine®
  • Conjugates like glucuronides and sulphates were found to be pharmacologically inactive
  • Recent studies on tetrahydrocurcuminoids (THCs)—reduced metabolites provided interesting comparison with Curcuminoids in biological activity (antioxidant, anti–inflammatory, antidiabetic, antihyperlipidemic, antiglycation, neuroprotective and hepatoprotective activities)
  • In 2011, Proceeding of National Academy of Sciences (PNAS) published a report that Curcumin was able to generate THCs by undergoing enzymatic reduction through an enzyme-CurA, present in commensal gut microbes E. coli—a path breaking observation (Reference: PNAS. 2011;108(16):6615–20)
  • Scientists at Sabinsa discovered the natural solution to improve biological activity of Curcumin in the form of BioPerine®
  • BioPerine® is the extract standardized to 95% piperine, obtained from black pepper fruits (Piper nigrum) — well known for its thermogenic activity and is an inhibitor of hepatic and intestinal glucuronidation
  • Sabinsa evaluated the bioavailability of Curcumin C3 Complex® in presence of BioPerine® (a patented product of Sabinsa) both preclinical and clinical

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 studyResults 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.