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 research has explored the properties of tetrahydrocurcuminoids (THCs), which are reduced metabolites, highlighting their potential in supporting overall health. Studies have compared THCs to curcuminoids, noting their biological activities that contribute to antioxidant and anti-inflammatory support. Additionally, these studies suggest that THCs may play a role in supporting healthy blood sugar and lipid levels, contributing to overall metabolic wellness. Their potential neuroprotective and liver-supportive properties have also been observed, indicating a broad spectrum of support for maintaining health and well-being.
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 a black pepper extract (Piper nigrum) standardized to 95% piperine. It is known for its thermogenic properties and is widely used to help enhance nutrient absorption and support bioavailability through its influence on digestive and metabolic processes
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 pioneering and among the first to demonstrate the bio-enhancing potential of piperine in BioPerine®. The findings showed that piperine can influence the way certain nutrients are processed in the body, helping to slow their breakdown and support greater absorption and bioavailability.
Reference: Shoba et al. Influence of Piperine on the Pharmacokinetics of Curcumin in Animals and Human Volunteers. Planta Med.1998;64(4):353–56.
