Transecullar diffusion across the absorptive epithelial cells (enterocytes) of the small intestine is the main route of absorption for most orally administered drugs. The process by which lipophilic compounds transverse the aqueous environment of the cytoplasm, however, remains porrly defined. In the present study, we have identified a structurally diverse group of lipophilic drugs that display low microloar binding affinitites for a ctyosolic lipid-binding protein-intestinal fatty acid-binding protein (I-FABP). Binding to I-FABP significantly enhanced the trasnport of lipophilic drug molecules across a model membrane, and the degree of transport enhancement was related to both drug lipophilicity and I-FABP may enhance the membrane transport of lipophilic xenobiotics and facilitate drug access to the enterocyte cytoplasm and cytoplasmic organelles.
|Pages (from-to)||453 - 465|
|Number of pages||13|
|Journal||Chemistry and Biology|
|Publication status||Published - 2007|