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pubmed-article:21413912pubmed:dateCreated2011-3-18lld:pubmed
pubmed-article:21413912pubmed:abstractTextINTRODUCTION: The ATP-binding cassette superfamily contains membrane transporter proteins that transport a wide range of diverse compounds across cellular membranes. The P-glycoprotein (P-gp) is an important member of this family and a multi-specific drug efflux transporter that plays a significant role in governing the bioavailability of many clinically active drugs. The inhibition of this efflux transporter by various P-gp inhibitors forms a distinctive approach in improving bioavailability and conquering drug resistance. Most P-gp inhibitors exhibit limitations associated with their safety and unwanted pharmacokinetic interactions, thereby restraining their clinical applicability. AREAS COVERED: This review explores the investigations on the feasibility and applicability of various classes of P-gp inhibitors as described in recent patents for enhanced drug delivery. EXPERT OPINION: Several candidates presently under development look promising as P-gp inhibitors, e.g., tariquidar and elacridar. Pharmaceutical excipients currently constitute the most promising class of P-gp inhibitors and are considered safe and pharmaceutically acceptable for use in formulations. In addition, lipid-based excipients and thiolated polymers play an active role in affecting P-gp-mediated transport not only by altering the membrane fluidity or ATPase activity but by down regulating P-gp expression. An additional overture such as the prodrug derivatization of P-gp substrates is a feasible approach to bypass P-gp-mediated efflux.lld:pubmed
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pubmed-article:21413912pubmed:volume21lld:pubmed
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pubmed-article:21413912pubmed:pagination561-76lld:pubmed
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pubmed-article:21413912pubmed:year2011lld:pubmed
pubmed-article:21413912pubmed:articleTitleThe emerging role of P-glycoprotein inhibitors in drug delivery: a patent review.lld:pubmed
pubmed-article:21413912pubmed:affiliationDepartment of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard Hamdard University, New Delhi 110062, India.lld:pubmed
pubmed-article:21413912pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:21413912pubmed:publicationTypeReviewlld:pubmed
pubmed-article:21413912pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed