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.).
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Redox mechanisms in pathological angiogenesis in the retina: roles for NADPH oxidase
Current Pharmaceutical Design Production and Purification of Functional Lipids Through Enzymatic and Microorganism-Mediated Processes
Current Organic Chemistry Development and Validation of Predictive Molecular Signatures
Current Molecular Medicine Recent Advances on the Roles of NO in Cancer and Chronic Inflammatory Disorders
Current Medicinal Chemistry Recent Advances in the Development of Selective Small Molecule Inhibitors for Cyclin-Dependent Kinases
Current Topics in Medicinal Chemistry Design, Synthesis and Biological Evaluation of 5-Amino-1H-pyrazole-4- carboxamide Derivatives as Potential Antitumor Agents
Letters in Drug Design & Discovery Stromal Derived Growth Factor-1alpha as a Beacon for Stem Cell Homing in Development and Injury
Current Neurovascular Research Targeting Signaling Pathways in Multiple Myeloma
Current Pharmaceutical Biotechnology Editorial [Hot topic: Special Edition Myeloproliferative Neoplasia – Disease Pathogenesis and Treatment Options (Guest Editors: D. Wolf and H. Rumpold)]
Current Cancer Drug Targets Oral Mucosal Immunization: Recent Advancement and Future Prospects
Current Immunology Reviews (Discontinued) Is the Cytoskeleton an Intracellular Receptor for Adrenomedullin and PAMP?
Current Protein & Peptide Science Blocking IL-6/GP130 Signaling Inhibits Cell Viability/Proliferation, Glycolysis, and Colony Forming Activity in Human Pancreatic Cancer Cells
Current Cancer Drug Targets Preparation of Therapeutic Dose of <sup>177</sup>Lu-DOTA-TATE Using a Novel Single Vial Freeze-dried Kit: A Comparison with ‘In-situ’ Preparation at Hospital Radiopharmacy
Current Radiopharmaceuticals Cancer Molecular Imaging: Radionuclide-Based Biomarkers of the Epidermal Growth Factor Receptor (EGFR)
Current Topics in Medicinal Chemistry Investigating Drug Repositioning Approach to Design Novel Prodrugs for Colon-specific Release of Fexofenadine for Ulcerative Colitis
Current Drug Delivery Patent Selections
Recent Patents on Drug Delivery & Formulation Biological Evaluation of <sup>99m</sup>Tc-HYNIC-EDDA/tricine-(Ser)<sub>3</sub>-D4 Peptide for Tumor Targeting
Current Radiopharmaceuticals Eco-Friendly and Highly Efficient Multigram Synthesis of N-(2- Hydroxyethyl)-2-Oxo-2H-Chromene-3-Carboxamide as a Useful Intermediate Using Sonochemistry
Current Green Chemistry Glucocorticoids Selectively Inhibit Paclitaxel-Induced Apoptosis: Mechanisms and Its Clinical Impact
Current Medicinal Chemistry Translational Gap in Glioma Research
Anti-Cancer Agents in Medicinal Chemistry