<p>Baicalein, a naturally occurring flavonoid predominantly obtained from the roots of <i>Scutellaria baicalensis</i> and leaves of <i>Scutellaria lateriflora,</i> belonging to the family&#xa0;Lamiaceae has gained significant interest for its therapeutic potential in the treatment and management of various chronic conditions, including cancer, cardiovascular diseases, metabolic disorders and neurological, respiratory and reproductive diseases. Its beneficial effects are attributed to its diverse pharmacological properties, such as anti-inflammatory, antioxidant, antibacterial, antiviral, anti-apoptotic, and immunomodulatory properties. A comprehensive understanding of its pharmacokinetic profile is essential to substantiate these potential health benefits and to elucidate the molecular mechanisms underlying its biological activities. Despite these numerous benefits, its clinical translation is restricted due to poor aqueous solubility, extensive presystemic metabolism, and consequently low oral bioavailability. To overcome these limitations, several strategies, including solubility enhancement approaches and nanoformulation based delivery systems, have been explored to improve its oral bioavailability. This article gives an overview of flavonoids, with emphasis on baicalein, and highlights its pharmacokinetics, pharmacodynamics, and formulation strategies aimed at enhancing its oral bioavailability.</p> Graphical Abstract <p></p>