Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Randomized Controlled Trial
. 2016 Nov:108:220-225.
doi: 10.1016/j.ejpb.2016.08.020. Epub 2016 Sep 17.

Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man

Katarina Bukara  1 , Laurent Schueller  2 , Jan Rosier  2 , Mark A Martens  2 , Tinne Daems  2 , Loes Verheyden  2 , Siemon Eelen  2 , Michiel Van Speybroeck  2 , Cristian Libanati  3 , Johan A Martens  4 , Guy Van Den Mooter  5 , Françoise Frérart  6 , Koen Jolling  7 , Marjan De Gieter  7 , Branko Bugarski  8 , Filip Kiekens  9
Affiliations
Randomized Controlled Trial

Ordered mesoporous silica to enhance the bioavailability of poorly water-soluble drugs: Proof of concept in man

Katarina Bukara et al. Eur J Pharm Biopharm. 2016 Nov.

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 96h post-dose. The rate (Cmax/dose increased by 77%; tmax reduced by 0.75h) 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.

Keywords: Absorption; Bioavailability; Fenofibrate; Ordered mesoporous silica; Solubility.

PubMed Disclaimer

Publication types