Rational Design of Self-Emulsifying Pellet Formulation of Thymol: Technology Development Guided by Molecular-Level Structure Characterization and Ex Vivo Testing

The growing need for processing natural lipophilic and often volatile substances such as thymol, a promising candidate for topical treatment of intestinal mucosa, led us to the utilization of solid-state nuclear magnetic resonance (ss-NMR) spectroscopy for the rational design of enteric pellets with...

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Veröffentlicht in:Pharmaceutics Jg. 14; H. 8; S. 1545
Hauptverfasser: Macku, Jan, Kubova, Katerina, Urbanova, Martina, Muselik, Jan, Franc, Ales, Koutna, Gabriela, Pavelkova, Miroslava, Vetchy, David, Masek, Josef, Maskova, Eliska, Brus, Jiri
Format: Journal Article
Sprache:Englisch
Veröffentlicht: Switzerland MDPI AG 25.07.2022
MDPI
Schlagworte:
Bioavailability
Bowel disease
Care and treatment
Cellulose
Chemical properties
Colorectal diseases
COVID-19
Dosage and administration
Drug delivery systems
Drug dosages
Drug therapy
Drugs
ex vivo testing
Gastrointestinal agents
Gastrointestinal diseases
Health aspects
Pharmaceutical industry
Pharmaceutical research
Pharmacokinetics
Phenols
rational design
self-emulsifying pellet
solid-state NMR
structure
Surfactants
thymol
Vehicles
Czech Republic
United States > US
Germany
rational design
thymol
ex vivo testing
solid-state NMR
self-emulsifying pellet
structure
ISSN:1999-4923, 1999-4923
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Zusammenfassung:The growing need for processing natural lipophilic and often volatile substances such as thymol, a promising candidate for topical treatment of intestinal mucosa, led us to the utilization of solid-state nuclear magnetic resonance (ss-NMR) spectroscopy for the rational design of enteric pellets with a thymol self-emulsifying system (SES). The SES (triacylglycerol, Labrasol®, and propylene glycol) provided a stable o/w emulsion with particle size between 1 and 7 µm. The ex vivo experiment confirmed the SES mucosal permeation and thymol delivery to enterocytes. Pellets W90 (MCC, Neusilin®US2, chitosan) were prepared using distilled water (90 g) by the M1–M3 extrusion/spheronisation methods varying in steps number and/or cumulative time. The pellets (705–740 µm) showed mostly comparable properties—zero friability, low intraparticular porosity (0–0.71%), and relatively high density (1.43–1.45%). They exhibited similar thymol release for 6 h (burst effect in 15th min ca. 60%), but its content increased (30–39.6 mg/g) with a shorter process time. The M3-W90 fluid-bed coated pellets (Eudragit®L) prevented undesirable thymol release in stomach conditions (<10% for 3 h). A detailed, ss-NMR investigation revealed structural differences across samples prepared by M1–M3 methods concerning system stability and internal interactions. The suggested formulation and methodology are promising for other lipophilic volatiles in treating intestinal diseases.
Bibliographie:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics14081545