Background: Piperine is a key bioactive alkaloid found in plants of piperaceae family. The compound
possesses various medicinal and pharmacological activities (cholesterol lowering, anti cancer, alzheimer’s disease etc).
Owing to its various target receptors (TRPV1, P-gp, CYP3A4 etc.) and several mechanisms, piperine has been studied as
bio-enhancer for other drugs and its role has been evidenced in literature. When administered with other drugs, it increases
absorption of other drugs thereby reducing the dose and dose related toxic potential. There are various mechanisms of
piperine as a bio-enhancer and the common ones are i) prevention of efflux of drug molecules out of the cells; ii)
decreased metabolism of drugs thereby prolonging half-life of drugs resulting in reduced urinary excretion. The detailed
mechanism indicating bio-enhancing role of piperine along with various target receptors have not been comprehensively
summarised till date.
Methods: Literature related to the molecular, enzymatic and receptor targets of piperine were studied and database was
collected using various search engines such as j-gate, google scholar, scihub, pubmed, sciencedirect etc. The literature
related to therapeutic activities of piperine and its bio-enhancer role for other drugs has been thoroughly studied and
compiled in brief.
Results: A detailed summary of piperine targets along with related mechanisms has been stated. A brief therapeutic
profile of piperine alone has been produced with supporting literature. Piperine role as a potential bio-enhancer for other
drugs has been summarized.
Conclusion: Piperine is fascinating molecule of natural origin with several modes of its action, not only possess its own
therapeutic activity but also enhances the therapeutic efficacy of other synthetic and natural drug molecules. Combination
dosage forms of various API incorporating piperine as a bio-enhancer can be potential area of thrust for upcoming drug
design and development.