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Piperine is the major bio-active component of pepper, which imparts pungency and biting taste to it. This naturally occurring alkaloid has numerous demonstrated health effects and beneficial therapeutic properties; nevertheless, its biological applications are limited due to its poor solubility in aqueous environments. This emphasizes an implementation of advanced extraction approaches which could enhance the extraction yield of piperine from pepper and also the development of new formulations containing piperine to improve its in vivo bioavailability. This paper presents a review on the therapeutic and medicinal effects of piperine, its isolation from pepper fruit and the development of new formulations for its medicinal (pharmaceutical) applications. A thorough review on conventional and advanced separation techniques for the extraction of piperine from pepper is presented and an outline of the most significant conditions to improve the extraction yield is provided and discussed. Different methods used to measure and quantify the isolated piperine are also reviewed. An overview of biotechnological advancements for nanoparticle formulations of piperine or its incorporation in lipid formulations, which could enhance its bioavailability, is also presented.

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