Oral administration remains the most preferred route for the treatment of many diseases due to its convenience and adaptability.
However, the presystemic metabolism may be an important barrier that prevents lipophilic drugs from achieving their pharmacological
effects following oral delivery. Nano-based drug delivery system provides an effective strategy to reduce the presystemic metabolism
and increase the systemic exposure of lipophilic drugs. In this review, we described the physiological factors affecting the presystemic
metabolism of lipophilic drugs, intestinal transport of nanosystems, strategy of nanosystems to avoid the presystemic metabolism, and the
current application of various oral nanosystems including lipid and polymeric nanocarriers. The nano-based drug delivery system has a
lot of potential for reducing the presystemic metabolism and enhancing the bioavailability of orally administrated lipophilic drugs.
Nanosystems, lipophilic drugs, presystemic metabolism, oral delivery, bioavailability, Nano-based Drug Delivery System, Oral Absorption, Lipophilic Drugs, Presystemic, Metabolism, anti-cancer drugs, inhibitors, ketoconazole, lumen.