Abstract
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.
Recent Patents on Anti-Cancer Drug Discovery
Title:Understanding and Managing Oral Bioavailability: Physiological Concepts and Patents
Volume: 10 Issue: 1
Author(s): Mohd A. Alam, Fahad I. Al-Jenoobi, Abdullah M. Al-Mohizea and Raisuddin Ali
Affiliation:
Keywords: Bioavailability, cytochrome P-450, gastrointestinal tract, P-glycoprotein, multidrug resistance, prodrug.
Abstract: 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.).
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Cite this article as:
Alam A. Mohd, Al-Jenoobi I. Fahad, Al-Mohizea M. Abdullah and Ali Raisuddin, Understanding and Managing Oral Bioavailability: Physiological Concepts and Patents, Recent Patents on Anti-Cancer Drug Discovery 2015; 10 (1) . https://dx.doi.org/10.2174/1574892809666140917103834
DOI https://dx.doi.org/10.2174/1574892809666140917103834 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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