Oral delivery of poorly bioavailable therapeuticals is challenging. The challenges are more serious
when physiological factors of gut such as cytochrome P450, P-glycoprotein, permeability, pH triggered precipitation
and degradation are responsible for poor bioavailability. P-Glycoprotein mediated multidrug resistance is on high
agenda for anti-cancer drugs. The present article compiled different methodologies used to curb these challenges of
bioavailability. The concepts of poor bioavailability are illustrated along with possible management. Numerous
relevant patents for bioavailability enhancement are also highlighted. Though, there is no universal approach for
bioavailability enhancement, the drug related challenges are managed by altering its physicochemical characteristics or
employing formulation technology, while the effects of physiological factors are minimized by using efflux transport
inhibitor or cytochrome P-450 inhibitor or prodrug or through formulation technologies (enteric coating or microenvironment
of pH etc.).
Keywords: Bioavailability, cytochrome P-450, gastrointestinal tract, P-glycoprotein, multidrug resistance, prodrug.
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