In vitro and in vivo comparison of microcontainers and microspheres for oral drug delivery

Microcontainers, which are microfabricated cylindrical devices with a reservoir function, have shown promise as an oral drug delivery system for small molecular compounds. However, they never been evaluated against relevant control formulation. In the current study, we prepared microcrystalline cellulose (MCC) microspheres in vitro and vivo testing of SU-8 microcontainers system. Both dosage forms were loaded paracetamol coated chitosan or polyethylene glycol (PEG) (12 kDa). These coatings followed by additional enteric coating Eudragit® S100. addition, form was alone. The vitro, physiologically two-step model simulating rat gastrointestinal fluids, administration to rats. PEG/Eudragit® resulted prolonged release compared respective microspheres, consistent observations later time (Tmax) maximum plasma concentration (Cmax) microcontainers. For chitosan/Eudragit®, complete very similar, due earlier from This trend supported similar Tmax values vivo. relation confirmed linear regression R2 = 0.9, when each plotted function 90% vitro. From average 120 min after dosing significantly higher than (0.3 ± 0.1 µg/mL <0.1 µg/mL, respectively) – regardless applied.