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dc.contributor.authorJong Bong Lee, Tae Hwan Kim-
dc.contributor.authorWanshan Feng, Hyeon Gwan Choi-
dc.contributor.authorAtheer Zgair, Soyoung Shin-
dc.contributor.authorSun Dong Yoo, Pavel Gershkovich-
dc.contributor.authorBeom Soo Shin-
dc.date.accessioned2022-10-15T08:33:17Z-
dc.date.available2022-10-15T08:33:17Z-
dc.date.issued2018-
dc.identifier.issn0022-3549-
dc.identifier.urihttp://localhost:8080/xmlui/handle/123456789/1058-
dc.description.abstractFor performance assessment of the lipid-based drug delivery systems (LBDDSs), in vitro lipolysis is commonly applied because traditional dissolution tests do not reflect the complicated in vivo micellar formation and solubilization processes. Much of previous research on in vitro lipolysis has mostly focused on rank-ordering formulations for their predicted performances. In this study, we have incorporated in vitro lipolysis with microsomal stability to quantitatively predict the oral bioavailability of a lipophilic antineoplastic drug bexarotene (BEX) administered in LBDDS. Two types of LBDDS were applied: lipid solution and lipid suspension. The predicted oral bioavailability values of BEX from linking in vitro lipolysis with microsomal stability for lipid solution and lipid suspension were 34.2 ± 1.6% and 36.2 ± 2.6%, respectively, whereas the in vivo oral bioavailability of BEX was tested as 31.5 ± 13.4% and 31.4 ± 5.2%, respectively. The predicted oral bioavailability corresponded well with the oral bioavailability for both formulations, demonstrating that the combination of in vitro lipolysis and microsomal stability can quantitatively predict oral bioavailability of BEX. In vivo intestinal lymphatic uptake was also assessed for the formulations and resulted in <1% of the dose, which confirmed that liver microsomal stability was necessary for correct prediction of the bioavailabilityen_US
dc.language.isoen_USen_US
dc.publisherJournal of Pharmaceutical Sciencesen_US
dc.subjectlipid-based formulationen_US
dc.subjectabsorptionen_US
dc.subjectsolubilityen_US
dc.subjectbioavailabilityen_US
dc.subjectymphatic transporten_US
dc.titleQuantitative Prediction of Oral Bioavailability of a Lipophilic Antineoplastic Drug Bexarotene Administered in Lipidic Formulation Using a Combined In Vitro Lipolysis/Microsomal Metabolism Approachen_US
dc.typeArticleen_US
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