Application of a novel gastrointestinal tract simulator system based on a membrane bioreactor (SimuGIT) to study the stomach tolerance and effective delivery enhancement of nanoencapsulated macelignan

• Encapsulation of macelignan performed in the form of lipid nanoparticles (LNPs).
• Novel, simple and reliable gastrointestinal tract simulator (GITS) is presented.
• Conditions in the stomach and duodenum simulated by continuous stirred tank reactor.
• Continuous plug-flow tubular reactor connected in series simulating the intestine.
• Absorption of macelignan LNPs in GITS over 10 times higher than free macelignan.

In this research work, encapsulation of macelignan was performed in the lab by means of solid lipid nanoparticles (LNPs). The efficiency of the used nanoencapsulation technology was addressed with a focus on the enhancement towards the toleration of macelignan to the conditions of the stomach’s environment and in the intestine, for its effective delivery. Results were evaluated and contrasted with the absorption of free macelignan. For this purpose, a novel in-vitro gastrointestinal tract simulator system (GITS) named SimuGIT is presented, comprising a continuous stirred tank reactor (CSTR), simulating the conditions in the stomach and duodenum, connected in series to a continuous plug-flow tubular reactor (PFR) equipped with a tubular ceramic microfiltration (MF) membrane simulating the conditions and microvilli in the intestine. The net amount of macelignan LNPs within the absorbed product in the GITS was found to be over 10 times higher in terms of relative abundance than free macelignan. These promising results indicate that the produced LNPs permit macelignan resist the digestion process and enable the subsequent absorption of macelignan in the intestine. Furthermore, the LNPs were prepared from natural sources by using biocompatible components. Finally, the novel in-vitro GITS proposed stands out for its simplicity if compared to multi-vessel systems used in previous studies, and could be an easy platform to perform quick tests in order to assess the effective delivery of other compounds of interest.