In vivo evaluation and in vitro prediction of the performance of supersaturating drug delivery systems in the gastrointestinal environment.

The increasing number of poorly water-soluble drug candidates necessitates novel formulation strategies to obtain adequate oral bioavailability. In order to overcome solubility-limited intestinal absorption, supersaturating drug delivery systems (SDDS) aim to generate and stabilize gastrointestinal drug concentrations that exceed the drugs solubility. However, as supersaturation has never been investigated in the gastrointestinal environment, current in vitro procedures to evaluate SDDS cannot forecast their in vivo performance. Using a unique in vivo methodology, this research project will characterize the intraluminal behavior of SDDS and the impact on intestinal absorption in man. In combination with in vitro studies, the in vivo evaluation will provide insight into the influence of the intraluminal environment on supersaturation. This will enable the definition of novel and biorelevant in vitro procedures to predict the in vivo performance of SDDS during early development and reduce failure of these formulations in expensive clinical trials. As such, the research project will contribute to the successful exploitation of supersaturation as absorption-enhancing strategy.

Keywords:Biopharmacy, Gastrointestinal environment

Disciplines:Biomarker discovery and evaluation, Drug discovery and development, Medicinal products, Pharmaceutics, Pharmacognosy and phytochemistry, Pharmacology, Pharmacotherapy, Toxicology and toxinology, Other pharmaceutical sciences