The application of lipid-based drug delivery systems on the industrial scale has successfully demonstrated
their therapeutic and manufacturing advantages. Recently, various lipid-based formulations were successfully
prepared for oral delivery of compounds that are difficult to administer. Nevertheless, an improved understanding
of how these formulations affect drug absorption and metabolism is required to support the rapid and successful
completion of drug development programs. In this review, we report the detailed mechanisms whereby lipids
and lipid-based excipients affect drug absorption and metabolism, and summarize the capacity of lipids and
lipid-based formulations to improve drug absorption by improving drug solubility, mucosa penetration, lymphatic
transport, and hepatic metabolism. Finally, we discuss the progress made toward the use of novel lipid formulations
to enhance oral absorption by surmounting specific absorption barriers.
Keywords: Absorption, lipid formulations, metabolism, poorly soluble drug, systemic exposure.
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