Bioenhancers In Pharmaceuticals and Nutraceuticals: A Gateway to Improved Pharmacokinetics and Pharmacodynamics

Abstract

Bioenhancers are compounds that improve the bioavailability and therapeutic efficacy of co-administered drugs and nutrients without producing significant pharmacological effects at their own administered dose. They act by modulating drug absorption, metabolism, distribution, and excretion, thereby enhancing both pharmacokinetic and pharmacodynamic outcomes. Naturally derived phytochemicals, such as alkaloids (piperine, capsaicin), terpenoids (menthol, limonene), flavonoids (quercetin, naringin), glycosides (glycyrrhizin, ginsenosides), phenolics (curcumin, eugenol), and essential oils, are widely studied for their bioenhancing potential, while synthetic agents like surfactants and bile salts contribute to pharmaceutical formulations. Piperine remains the most extensively reported bioenhancer, shown to increase the systemic availability of several drugs and nutraceuticals, including rifampicin, phenytoin, curcumin, resveratrol, and CoQ10. Other bioenhancers, such as quercetin and glycyrrhizin, potentiate therapeutic effects by overcoming multidrug resistance, extending plasma half-life, and improving membrane permeability. By enabling dose reduction, minimizing side effects, and reviving poorly bioavailable drug candidates, bioenhancers hold significant promise in pharmaceuticals, nutraceuticals, and modern drug delivery systems.