Gastro-resistant self-emulsifying pellets as a stable delivery system for volatile monoterpene plant drug
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|To avoid standard therapies for gastrointestinal inflammatory diseases, an interest in finding new alternatives is rising. Plant monoterpene substances, such as thymol, carvacrol, eugenol, etc., exhibit many valuable biological activities in treating intestinal inflammation. The basic problem is that monoterpenes are volatile hydrophobic substances with poor oral bioavailability. Thymol is only partially absorbed mainly from the stomach, resulting in a 16% bioavailability. It is cumulated in a higher amount of intestinal mucosa. Thymol could be incorporated into solid self-emulsifying (SE) pellets with gastro-resistant properties to overcome drawbacks and support intestinal wall cumulation. During pellets formulation by extrusion/spheronisation, liquid and solid phases are in temporary or permanent contact. It opens the scope for interactions, instabilities, and components transfer within the dosage form. Therefore, a deep investigation of such a system by solid-state nuclear magnetic resonance spectroscopy (ss-NMR) is also necessary. ss-NMR spectroscopy confirms that thymol and SES molecules forms homogenous liquid films/phases on the surface. A more detailed investigation revealed that the thymol molecules in the uncoated sample with long-time prepareation exhibited lower molecular dynamics compared to shorter methods, indicating a higher impact of interactions between the Neusilin surface and drug.