Gastro-resistant self-emulsifying pellets as a stable delivery
system for volatile monoterpene plant drug

k 2022

Gastro-resistant self-emulsifying pellets as a stable delivery system for volatile monoterpene plant drug

MACKŮ, Jan, Kateřina KUBOVÁ, Gabriela KOUTNÁ, Martina ČUBOVÁ URBANOVÁ, Eliška MAŠKOVÁ et. al.

Basic information

Original name

Gastro-resistant self-emulsifying pellets as a stable delivery system for volatile monoterpene plant drug

Authors

MACKŮ, Jan (203 Czech Republic, belonging to the institution), Kateřina KUBOVÁ (203 Czech Republic, guarantor, belonging to the institution), Gabriela KOUTNÁ (203 Czech Republic, belonging to the institution), Martina ČUBOVÁ URBANOVÁ (203 Czech Republic), Eliška MAŠKOVÁ (203 Czech Republic), Josef MAŠEK (203 Czech Republic), Miroslava PAVELKOVÁ (203 Czech Republic, belonging to the institution), Jan MUSELÍK (203 Czech Republic, belonging to the institution), Jakub VYSLOUŽIL (203 Czech Republic, belonging to the institution), Aleš FRANC (203 Czech Republic, belonging to the institution), David VETCHÝ (203 Czech Republic, belonging to the institution) and Jiří BRUS (203 Czech Republic)

Edition

NanoMed 2022, 2022

Other information

Language

English

Type of outcome

Prezentace na konferencích

Field of Study

30104 Pharmacology and pharmacy

Country of publisher

Czech Republic

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

URL

RIV identification code

RIV/00216224:14160/22:00127132

Organization unit

Faculty of Pharmacy

Keywords (in Czech)

thymol; pevné samoemulgující systémy; ssNMR; přívod léřiva

Keywords in English

thymol; solid self-emulsifying systems; ssNMR; drug delivery

Abstract

V originále

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.

Links

GA22-03187S, research and development project

Name: Racionální design částicových polysacharidových systémů pro přívod léčiv s širokým spekterem biologické aktivity k terapii sliznic (Acronym: 22-03187S)

Investor: Czech Science Foundation

Citovat

MACKŮ, Jan, Kateřina KUBOVÁ, Gabriela KOUTNÁ, Martina ČUBOVÁ URBANOVÁ, Eliška MAŠKOVÁ, Josef MAŠEK, Miroslava PAVELKOVÁ, Jan MUSELÍK, Jakub VYSLOUŽIL, Aleš FRANC, David VETCHÝ and Jiří BRUS. Gastro-resistant self-emulsifying pellets as a stable delivery system for volatile monoterpene plant drug. In NanoMed 2022. 2022.

@proceedings{2230924,
   author = {Macků, Jan and Kubová, Kateřina and Koutná, Gabriela and Čubová Urbanová, Martina and Mašková, Eliška and Mašek, Josef and Pavelková, Miroslava and Muselík, Jan and Vysloužil, Jakub and Franc, Aleš and Vetchý, David and Brus, Jiří},
   booktitle = {NanoMed 2022},
   keywords = {thymol; solid self-emulsifying systems; ssNMR; drug delivery},
   language = {eng},
   title = {Gastro-resistant self-emulsifying pellets as a stable delivery system for volatile monoterpene plant drug},
   url = {https://www.setcor.org/conferences/nanomed-2022},
   year = {2022}
}

TY  - CONF
ID  - 2230924
AU  - Macků, Jan - Kubová, Kateřina - Koutná, Gabriela - Čubová Urbanová, Martina - Mašková, Eliška - Mašek, Josef - Pavelková, Miroslava - Muselík, Jan - Vysloužil, Jakub - Franc, Aleš - Vetchý, David - Brus, Jiří
PY  - 2022
TI  - Gastro-resistant self-emulsifying pellets as a stable delivery system for volatile monoterpene plant drug
KW  - thymol
KW  - solid self-emulsifying systems
KW  - ssNMR
KW  - drug delivery
UR  - https://www.setcor.org/conferences/nanomed-2022
N2  - 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.
ER  -

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