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.
TY - JOUR
AU - Bukara, Katarina
AU - Schueller, Laurent
AU - Rosier, Jan
AU - Martens, Mark A.
AU - Daems, Tinne
AU - Verheyden, Loes
AU - Eelen, Siemon
AU - Van Speybroeck, Michiel
AU - Libanati, Cristian
AU - Martens, Johan A.
AU - Van Den Mooter, Guy
AU - Frerart, Francoise
AU - Jolling, Koen
AU - De Gieter, Marjan
AU - Bugarski, Branko
AU - Kiekens, Filip
PY - 2016
UR - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/3326
AB - 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.
PB - Elsevier Science Bv, Amsterdam
T2 - European Journal of Pharmaceutics and Biopharmaceutics
T1 - Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man
EP - 225
SP - 220
VL - 108
DO - 10.1016/j.ejpb.2016.08.020
ER -
@article{
author = "Bukara, Katarina and Schueller, Laurent and Rosier, Jan and Martens, Mark A. and Daems, Tinne and Verheyden, Loes and Eelen, Siemon and Van Speybroeck, Michiel and Libanati, Cristian and Martens, Johan A. and Van Den Mooter, Guy and Frerart, Francoise and Jolling, Koen and De Gieter, Marjan and Bugarski, Branko and Kiekens, Filip",
year = "2016",
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 (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.",
publisher = "Elsevier Science Bv, Amsterdam",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
title = "Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man",
pages = "225-220",
volume = "108",
doi = "10.1016/j.ejpb.2016.08.020"
}
Bukara, K., Schueller, L., Rosier, J., Martens, M. A., Daems, T., Verheyden, L., Eelen, S., Van Speybroeck, M., Libanati, C., Martens, J. A., Van Den Mooter, G., Frerart, F., Jolling, K., De Gieter, M., Bugarski, B.,& Kiekens, F.. (2016). Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man. in European Journal of Pharmaceutics and Biopharmaceutics
Elsevier Science Bv, Amsterdam., 108, 220-225.
https://doi.org/10.1016/j.ejpb.2016.08.020
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, Frerart 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. in European Journal of Pharmaceutics and Biopharmaceutics. 2016;108:220-225.
doi:10.1016/j.ejpb.2016.08.020 .
Bukara, Katarina, Schueller, Laurent, Rosier, Jan, Martens, Mark A., Daems, Tinne, Verheyden, Loes, Eelen, Siemon, Van Speybroeck, Michiel, Libanati, Cristian, Martens, Johan A., Van Den Mooter, Guy, Frerart, Francoise, Jolling, Koen, De Gieter, Marjan, Bugarski, Branko, Kiekens, Filip, "Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man" in European Journal of Pharmaceutics and Biopharmaceutics, 108 (2016):220-225,
https://doi.org/10.1016/j.ejpb.2016.08.020 . .
