From concept to in vivo testing: Microcontainers for oral drug delivery

• DOI: 10.1016/j.jconrel.2017.10.013
• Publication Date: 2017-10-18T14:51:14Z
• Authors: Chiara Mazzoni; Fabio Tentor; Sophie Andersen S...; Line Hagner Nielsen; Stephan Sylvest K...; Tommy Sonne Alstrøm; Carsten Gundlach; Anette Müllertz; Paolo Marizza; Anja Boisen
• Keywords: Male; Enteric coating; Administration, Oral; Povidone; Capsules; 02 engineering and technology; 3. Good health; Rats, Sprague-Dawley; Drug Liberation; Drug Delivery Systems; Jejunum; Polymethacrylic Acids; Supercritical impregnation; Gastric Mucosa; Ketoprofen; Microtechnology; Animals; Oral drug delivery; Dicarboxylic Acids; 0210 nano-technology

This work explores the potential of polymeric micrometer sized devices (microcontainers) as oral drug delivery systems (DDS). Arrays of detachable microcontainers (D-MCs) were fabricated on a sacrificial layer to improve the handling and facilitate the collection of individual D-MCs. A model drug, ketoprofen, was loaded into the microcontainers using supercritical CO2 impregnation, followed by deposition of an enteric coating to protect the drug from the harsh gastric environment and to provide a fast release in the intestine. In vitro, in vivo and ex vivo studies were performed to assess the viability of the D-MCs as oral DDS. D-MCs improved the relative oral bioavailability by 180% within 4h, and increased the absorption rate by 2.4 times compared to the control. This work represents a significant step forward in the translation of these devices from laboratory to clinic.