Piperine-mediated drug interactions and formulation strategy for piperine: recent advances and future perspectives

Abstract

Piperine has various pharmacological effects and can modulate the functional activity of metabolic enzymes and drug transporters. Consequently, there is a great interest in the application of piperine as an alternative medicine or bioavailability enhancer. Areas covered: This review deals with the effects of piperine on metabolizing enzymes and drug transporters. It provides the readers with an update on transporter-mediated and also metabolic enzyme-mediated piperine-drug interactions, with emphasis on its in vivo implications. This article also encompasses recent advances in the formulation approaches and technologies for optimizing the delivery of piperine. Expert opinion: Piperine can influence the pharmacokinetics of coadministered drugs, which may result in a therapeutically beneficial or adverse effect. Given that piperine inhibits or stimulates the activity of metabolic enzymes and transporters depending on the treatment conditions, the clinical significance of piperine-drug interactions should be assessed by varying the dose, dosing frequency, and the duration of treatment. In particular, better understanding the clinical relevance of piperine-drug interactions based on long-term assessments will provide a strong basis for the feasibility and applicability of piperine as a bioenhancer or a health-promoting agent. The development of effective formulations is also critical to facilitate the therapeutic applications of piperine.

Modulation of Exercise-Induced Muscle Damage, Inflammation, and Oxidative Markers by Curcumin Supplementation in a Physically Active Population: A Systematic Review

“…One consideration that should be taken into account in supplementation with curcumin in athletes, who are themselves susceptible to iron deficiencies with or without anemia, is the interaction between high doses of curcumin and the alteration of iron metabolism by the chelation of iron and elevation of hepcidin, which could be another potential cause of decreased iron levels [38]. For this reason, piperine increases in importance because it allows a high bioavailability of curcumin with lower doses [39]. In this sense, Delecroix et al [31] used curcumin (6 g) plus piperine (20 mg) per day.…”

Herbal Bioenhancers in Veterinary Phytomedicine

“…First purified bioenhancer molecule piperine were found to inhibit different forms of cytochrome p450 (CYP) (especially CYP3A4) ( 11 ) and hepatic/intestinal UDP-glucuronosyltransferases (UDP); while this inhibition is dependent on the administration route, dose and duration of exposure ( 12 ). Various studies reveal the potentiating effect of piperine in drug bioavailability and bioefficacy for laboratory animals such as rats, mice and rabbit along with human volunteers ( 11 ); while few are available for veterinary medicine.…”

Iron and Physical Activity: Bioavailability Enhancers, Properties of Black Pepper (Bioperine®) and Potential Applications

“…Black pepper is used to treat epilepsy, headaches, and diabetes. In addition, Piper nigrum L. is used in the cooking of some foods with a unique flavor and as a preservative in food additives or perfumes [ 40 ].…”