Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man
Abstract: 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 (Cmax/dose increased by 77%; tmax reduced by 0.75 h) and extent of absorption (AUC0–24h/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.
Full Reference: Bukara K, Schueller L, Rosier J, Martens MA, Daems T, Verheyden L, Eelen S, Van Speybroeck M, Libanati C, Martens JA, Van Den Mooter G, Frérart F, Jolling K, De Gieter M, Bugarski B, Kiekens F. Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man. Eur J Pharm Biopharm. 2016 Nov;108:220-225. doi: 10.1016/j.ejpb.2016.08.020. Epub 2016 Sep 17.