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Maximizing oral bioavailability is therapeutically important because the extent of bioavailability directly influences plasma concentrations and therapeutic efficacy after oral drug administration. Bioavailability of poor bioavailable drugs can be increased from the many available approaches in the literature and the most recent approach is the use of bioavailability enhancers. The use of bioenhancers seems to be a fruitful method for increasing bioavailability of an orally administered drug and nutraceutical. This approach leads to improved formulation with enhanced oral bioavailability of the active ingredient. Bioenhancers constitute an innovative concept and judicious use of bioenhancers lead to reductions in drug cost, toxicity, and other adverse effects, and have a beneficial influence on the national economy. This patent review article classifies and describes the various bioenhancers and emphasizes their diverse mechanism of action by virtue of which they act as bioenhancers.