Characterization of organic cation transport in rabbit alveolar epithelial cells

摘要

The pulmonary route is an attractive alternative to the oral route for non-invasive drug delivery. The distal airspace, its large surface area, relatively low enzyme activity, extensive vasculature, and very thin epithelium lining are attractive features for the administration of drugs that are vulnerable to destruction following oral administration. Three different models have been employed for pulmonary drug permeability studi3s: the in vivo animal model, isolated perfused whole lung model, and in vitro cell culture model. The convenience associated with cell culture model has lead to its usage in many pulmonary drug absorption studies, for drugs including #beta# adrenergic antagonists, di- and tri-peptides, and macro-molecules such as horseradish peroxidase. However, no study has been conducted with organic cation compounds, which represent a large family of drug molecules. Therefore, the goal of the present study is to present evidence for the active transport of organic cations in a primary culture model of alveolar epithelial cells.