Black pepper (family Piperaceae), is called king of spices because it is one of the oldest spice andalone accounts for about 35% of the world’s total spice trade. The pepper is used in Ayurvedicmedicine for the treatment of various ailments particularly neurological, broncho-pulmonary andgastrointestinal disorders. Pepper has also been reported to have various pharmacological actions butrecently, it is highlighted as a bioavailability enhancer. This results in higher plasma concentration ofdrugs, nutrients, ions and other xenobiotics, rendering them more bioavailable for physiologicalas well as pharmacological actions in the body. Numerous scientific studies reported thatpiperine; a main bioactive compound of pepper, is responsible for its bioavailability enhancingproperty. It’s a well known fact that pepper enhances bioavailability by inhibition of microsomal enzymesystem but other mechanisms are also responsible to acts as a bioavailability enhancer. The briefoverview of the mechanism of action of pepper as well as its applications as bioavailability enhancer isgiven in the present article.