Contribution of Efflux Pump Activity to the Delivery of Pulmonary Therapeutics

Authors: Hamilton K.O.; Yazdanian M.A.; Audus K.L.

Source: Current Drug Metabolism, Volume 3, Number 1, February 2002 , pp. 1-12(12)

Publisher: Bentham Science Publishers

Abstract:

To date, there are few in vitro models of the human lung that have been used to characterize multidrug resistant (MDR) efflux pump activity. It is expected that the presence of these protein transporter molecules, such as P-glycoprotein (Pgp) and the multidrug resistance protein associated protein- 1 (MRP1), might play a role in limiting drug absorption through the pulmonary epithelium, as has been reported for other epithelial drug delivery barriers such as the intestine and brain. To date, the exact role of the lung resistance related protein (LRP) in MDR is unclear. In this article, we have summarized the biochemistry, function and in vitro / in vivo modulation of Pgp and MRP1. These topics are discussed in light of pulmonary delivery of therapeutic agents, with particular emphasis being placed on the bronchial region of human airways.

Keywords: Efflux Pump; Pulmonary Therapeutics; P-glycoprotein (Pgp); lung resistance related protein (LRP); Rhodamine; Transmembrane domain; Hexakis

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389200023338170

Publication date: 2002-02-01

• Current Drug Metabolism aims to cover all the latest and outstanding developments in drug metabolism and disposition. The journal serves as an international forum for the publication of timely reviews in drug metabolism. Current Drug Metabolism is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments. The journal covers the following areas:
  
  In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites and adducts.

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• In this Subject: Anatomy & Physiology ,  Pharmacology
• By this author: Hamilton K.O. ;  Yazdanian M.A. ;  Audus K.L.

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