Kuentz, Martin

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Kuentz, Martin

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2019 - 20202
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Autor:in: Koehl, Niklas × Autor:in: Kuentz, Martin × Item-Typ: Publikation × Dateien dazu vorhanden?: Nein × Thema: lipid based formulation ×

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  • Vorschaubild nicht verfügbar
    Publikation
    Chase Dosing of Lipid Formulations to Enhance Oral Bioavailability of Nilotinib in Rats
    (Springer, 10.06.2020) Koehl, Niklas; Kuentz, Martin [in: Pharmaceutical Research]
    Conclusion: Chase dosed LBF enhanced the in vivo bioavailability of nilotinib. Long chain lipids showed superior performance compared to medium chain lipids. Chase dosing appeared to prolong the absorption phase of the drug. Therefore, chase dosing of LBF is favourable compared to lipid suspensions for 'brick dust' molecules such as nilotinib. Graphical Abstract The potential of bio-enabling lipid vehicles, administered via chase dosing and lipid suspensions, has been evaluated as an approach to enhance oral bioavailability of nilotinib.
    01A - Beitrag in wissenschaftlicher Zeitschrift
  • Vorschaubild nicht verfügbar
    Publikation
    New Insights into Using Lipid Based Suspensions for 'Brick Dust' Molecules: Case Study of Nilotinib
    (Springer, 22.02.2019) Koehl, Niklas; Kuentz, Martin [in: Pharmaceutical Research]
    PurposeLipid suspensions have been shown to be a suitablebio-enabling formulation approach for highly lipophilic or‘grease ball’drug molecules, but studies on‘brick dust’drugsare lacking. This study explored the utility of lipid suspensionsfor enhancing oral bioavailability of the rather hydrophobicdrug nilotinibin vivoin rats.MethodsFour lipid suspensions were developed containinglong chain triglycerides, medium chain triglyceride, longchain monoglycerides and medium chain monoglyceridesandin vivobioavailability was compared to an aqueous suspen-sion. Additionally,in vitrolipolysis and wettability tests wereconducted.ResultsNilotinib lipid suspensions did not show a bioavail-ability increase compared to an aqueous suspension. The bio-availability was lower for triglyceride suspensions, relative toboth monoglyceride and an aqueous suspension. The longchain monoglyceride displayed a significantly higher bioavail-ability relative to triglycerides.In vitrolipolysis results suggestedentrapment of nilotinib crystals within poorly dispersible tri-glycerides, leading to slower nilotinib release and absorption.This was further supported by higher wettability of nilotinibby lipids.ConclusionMonoglycerides improved oral bioavailability ofnilotinib in rats, relative to triglycerides. For‘brick dust’drugsformulated as lipid suspensions, poorly dispersible formula-tions may delay the release of drug crystals from the formula-tion leading to reduced absorption.
    01A - Beitrag in wissenschaftlicher Zeitschrift