Rational design of self-emulsifying pellet formulation of thymol: technology development guided by molecular-level structure characterization and ex vivo testing
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389013%3A_____%2F22%3A00559618" target="_blank" >RIV/61389013:_____/22:00559618 - isvavai.cz</a>
Alternative codes found
RIV/00027162:_____/22:N0000071 RIV/00216224:14160/22:00126642
Result on the web
<a href="https://www.mdpi.com/1999-4923/14/8/1545" target="_blank" >https://www.mdpi.com/1999-4923/14/8/1545</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/pharmaceutics14081545" target="_blank" >10.3390/pharmaceutics14081545</a>
Alternative languages
Result language
angličtina
Original language name
Rational design of self-emulsifying pellet formulation of thymol: technology development guided by molecular-level structure characterization and ex vivo testing
Original language description
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.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10404 - Polymer science
Result continuities
Project
<a href="/en/project/GA22-03187S" target="_blank" >GA22-03187S: Rational Design of Polysaccharide‐based Particulate Systems for the Delivery of Mucosal Therapeutics with Broad Spectrum of Biological Activities</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2022
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Pharmaceutics
ISSN
1999-4923
e-ISSN
1999-4923
Volume of the periodical
14
Issue of the periodical within the volume
8
Country of publishing house
CH - SWITZERLAND
Number of pages
22
Pages from-to
1545
UT code for WoS article
000847103700001
EID of the result in the Scopus database
2-s2.0-85137410757