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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

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • 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