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

Autor: Jan Macku, Katerina Kubova, Martina Urbanova, Jan Muselik, Ales Franc, Gabriela Koutna, Miroslava Pavelkova, David Vetchy, Josef Masek, Eliska Maskova, Jiri Brus
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Pharmaceutics, Vol 14, Iss 8, p 1545 (2022)
Druh dokumentu: article
ISSN: 1999-4923
DOI: 10.3390/pharmaceutics14081545
Popis: 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 (
Databáze: Directory of Open Access Journals
Nepřihlášeným uživatelům se plný text nezobrazuje