Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man
Martens, Mark A.
Van Speybroeck, Michiel
Martens, Johan A.
Van Den Mooter, Guy
De Gieter, Marjan
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Formulating poorly water soluble drugs using ordered mesoporous silica materials is an emerging approach to tackle solubility-related bioavailability problems. The current study was conducted to assess the bioavailability-enhancing potential of ordered mesoporous silica in man. In this open-label, randomized, two-way cross-over study, 12 overnight fasted healthy volunteers received a single dose of fenofibrate formulated with ordered mesoporous silica-or a marketed product based on micronized fenofibrate. Plasma concentrations of fenofibric acid, the pharmacologically active metabolite of fenofibrate, were monitored up to 96 h post-dose. The rate (C-max/dose increased by 77%; t(max) reduced by 0.75 h) and extent of absorption (AUC(0-24h)/dose increased by 54%) of fenofibrate were significantly enhanced following administration of the ordered mesoporous silica based formulation. The results of this study serve as a proof of concept in man for this novel formulation approach.
Кључне речи:Ordered mesoporous silica / Solubility / Absorption / Bioavailability / Fenofibrate
Извор:European Journal of Pharmaceutics and Biopharmaceutics, 2016, 108, 220-225
- Elsevier Science Bv, Amsterdam
Финансирање / пројекти:
- Flemish Institute for the Promotion of Innovation through Science and Technology (IWT-Vlaanderen)
- Flemish Government