Abstract
The pulmonary administration of drugs plays a crucial role in the management of various respiratory and systemic diseases. While the cellular properties of airway epithelial cells offer a great potential to deliver drugs into the lungs or the circulation, only little is known about the exact transport pathways. Recently, the high-affinity proton-coupled drug and peptide transporter PEPT2 was identified in the human respiratory tract. The expression of transporter mRNA and protein was localized to the airway epithelium and alveolar type II pneumocytes. In addition, transport studies revealed transporter-mediated uptake of substrates into epithelial cells indicating that the transporter is the molecular basis for the transport of peptides and peptidomimetic drugs in pulmonary epithelial cells. Since genotype analysis revealed no significant differences amongst different transporter genotypes concerning expression and function, the transporter displays an interesting novel target for pulmonary delivery of drugs.
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