The artificial membrane insert system as predictive tool for formulation performance evaluation

Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Philippe Berben, Joachim Brouwers, Patrick Augustijns In view of the increasing interest of pharmaceutical companies for cell- and tissue-free models to implement permeation into formulation testing, this study explored the capability of an artificial membrane insert system (AMI-system) as predictive tool to evaluate the performance of absorption-enabling formulations. Firstly, to explore the usefulness of the AMI-system in supersaturation assessment, permeation was monitored after induction of different degrees of loviride supersaturation. Secondly, to explore the usefulness of the AMI-system in formulation evaluation, a two-stage dissolution test was performed prior to permeation assessment. Different case examples were selected based on the availability of in vivo (intraluminal and systemic) data: (i) a suspension of posaconazole (Noxafil®), (ii) a cyclodextrin-based formulation of itraconazole (Sporanox®), and (iii) a micronized (Lipanthyl®) and nanosized (Lipanthylnano®) formulation of fenofibrate. The obtained results demonstrate that the AMI-system is able to capture the impact of loviride supersaturation on permeation. Furthermore, the AMI-system correctly predicted the effects of (i) formulation pH on posaconazole absorption, (ii) dilution on cyclodextrin-based itraconazole absorption, and (iii) food intake on fenofibrate absorption. Based on...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research