{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,1,19]],"date-time":"2026-01-19T03:05:00Z","timestamp":1768791900528,"version":"3.49.0"},"reference-count":25,"publisher":"MDPI AG","issue":"1","license":[{"start":{"date-parts":[[2022,1,4]],"date-time":"2022-01-04T00:00:00Z","timestamp":1641254400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100003130","name":"Research Foundation - Flanders","doi-asserted-by":"publisher","award":["G078417N"],"award-info":[{"award-number":["G078417N"]}],"id":[{"id":"10.13039\/501100003130","id-type":"DOI","asserted-by":"publisher"}]},{"name":"SMB (Belgium)","award":["-"],"award-info":[{"award-number":["-"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>The bioavailability of lipophilic drugs may or may not be increased when administered with food due to increased solubilisation in fed state gastrointestinal (GI) fluids. The in vivo interplay between drug solubilisation, lipid phase digestion and drug absorption is complex and remains poorly understood. This study aimed to investigate the role of fed state GI lipolysis on the intraluminal behaviour and absorption of fenofibrate, formulated as the lipid-based formulation Fenogal. Therefore, a crossover study was performed in healthy volunteers using orlistat as lipase inhibitor. Fenofibrate concentrations were determined in the proximal jejunum and linked to simultaneously assessed systemic fenofibric acid concentrations. Inhibition of lipolysis by orlistat resulted in a faster onset of absorption in 4 out of 6 volunteers, reflected by a decrease in systemic Tmax between 20 and 140 min. In addition, the increase of undigested lipids present in the small intestine upon orlistat co-administration sustained drug solubilisation for a longer period, resulting in higher fenofibrate concentrations in the jejunum and improved absorption in 5 out of 6 volunteers (median AUC0\u20138h 8377 vs. 5832 \u03bcM.min). Sustaining drug solubilisation in the lipid phase may thus contribute to the absorption of lipophilic drugs. More research into the different mechanisms underlying lipophilic drug absorption from fed state media at different levels of digestion is warranted.<\/jats:p>","DOI":"10.3390\/pharmaceutics14010119","type":"journal-article","created":{"date-parts":[[2022,1,9]],"date-time":"2022-01-09T20:21:56Z","timestamp":1641759716000},"page":"119","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["The Influence of Fed State Lipolysis Inhibition on the Intraluminal Behaviour and Absorption of Fenofibrate from a Lipid-Based Formulation"],"prefix":"10.3390","volume":"14","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-5668-1958","authenticated-orcid":false,"given":"Marlies","family":"Braeckmans","sequence":"first","affiliation":[{"name":"Drug Delivery and Disposition, KU Leuven, Gasthuisberg O&N II, Herestraat 49-Box 921, 3000 Leuven, Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1478-6174","authenticated-orcid":false,"given":"Joachim","family":"Brouwers","sequence":"additional","affiliation":[{"name":"Drug Delivery and Disposition, KU Leuven, Gasthuisberg O&N II, Herestraat 49-Box 921, 3000 Leuven, Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Danny","family":"Riethorst","sequence":"additional","affiliation":[{"name":"Drug Delivery and Disposition, KU Leuven, Gasthuisberg O&N II, Herestraat 49-Box 921, 3000 Leuven, Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"C\u00e9cile","family":"Servais","sequence":"additional","affiliation":[{"name":"Galephar M\/F Research Center, 6900 Marche-en-Famenne, Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jan","family":"Tack","sequence":"additional","affiliation":[{"name":"Translational Research Center for Gastrointestinal Disorders, TARGID, KU Leuven, 3000 Leuven, Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2595-388X","authenticated-orcid":false,"given":"Patrick","family":"Augustijns","sequence":"additional","affiliation":[{"name":"Drug Delivery and Disposition, KU Leuven, Gasthuisberg O&N II, Herestraat 49-Box 921, 3000 Leuven, Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,1,4]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"64","DOI":"10.5414\/CPP44064","article-title":"Absence of a food effect with a 145 mg nanoparticle fenofibrate tablet formulation","volume":"44","author":"Sauron","year":"2006","journal-title":"Int. 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