Journal
ACS APPLIED MATERIALS & INTERFACES
Volume 10, Issue 21, Pages 17571-17581Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsami.8b02637
Keywords
lipid digestion; gastric digestion; intestine digestion; interfacial design; human studies; in vitro-in vivo correlation
Funding
- Swiss National Foundation (SNF) [406940-145141, 200021-137941, 200020-159898]
- Swiss National Science Foundation (SNF) [200021_137941, 200020_159898, 406940_145141] Funding Source: Swiss National Science Foundation (SNF)
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The use of oil-in-water emulsions for controlled lipid release is of interest to the pharmaceutical industry in the development of poorly water soluble drugs and also has gained major interest in the treatment of obesity. In this study, we focus on the relevant in vitro parameters reflecting gastric and Stomach intestinal digestion steps to reach a reliable in vitro-in vivo correlation for lipid delivery systems. We found that (i) gastric lipolysis determines early lipid release and sensing. This was mainly influenced by the emulsion stabilization mechanism. (ii) Gastric mucin influences the structure of charge-stabilized emulsion systems in the stomach, leading to destabilization or gel formation, which is supported by in vivo magnetic resonance imaging in healthy volunteers. (iii) The precursor structures of these emulsions modulate intestinal lipolysis kinetics in vitro, which is reflected in plasma triglyceride and cholecystokinin concentrations in vivo.
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