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
Current Drug Metabolism
Title: Contribution of Efflux Pump Activity to the Delivery of Pulmonary Therapeutics
Volume: 3 Issue: 1
Author(s): K. O. Hamilton, M. A. Yazdanian and K. L. Audus
Affiliation:
Keywords: Efflux Pump, Pulmonary Therapeutics, P-glycoprotein (Pgp), lung resistance related protein (LRP), Rhodamine, Transmembrane domain, Hexakis
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.
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Cite this article as:
Hamilton O. K., Yazdanian A. M. and Audus L. K., Contribution of Efflux Pump Activity to the Delivery of Pulmonary Therapeutics, Current Drug Metabolism 2002; 3 (1) . https://dx.doi.org/10.2174/1389200023338170
DOI https://dx.doi.org/10.2174/1389200023338170 |
Print ISSN 1389-2002 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5453 |
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