The gastrointestinal lymphatic system is a specific transport pathway through which dietary lipids, fat-soluble vitamins, and water-insoluble peptide-type molecules (e.g., cyclosporine A) can gain access to the systemic circulation. Drugs transported by way of the gastrointestinal lymphatic system bypass the liver and avoid potential hepatic first-pass metabolism. Lymphatic delivery of immunomodulatory and low therapeutic index protein and peptide drugs used in the treatment of cancer cell metastases and HIV presents an opportunity to maximize therapeutic benefit while minimizing general systemic drug exposure. Furthermore, lymphatic drug transport may promote drug incorporation into the body's lipid-handling system, thus offering the potential to manipulate drug distribution and residence time within the body. This review article will discuss the potential utilization of lymphatic transport in enhancing the oral absorption of protein- and peptide-like drugs.
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Comparison of monomeric and oligomeric transferrin as potential carrier in oral delivery of protein drugs
An evolutionary perspective on intestinal lymphatic fat absorption, the industrialization of food, and allergy
Biomimetic reassembled chylomicrons as novel association model for the prediction of lymphatic transportation of highly lipophilic drugs via the oral route
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis
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