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Development of lipid-based gastroretentive delivery system for gentian extract by double emulsion–melt dispersion technique

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2021
Development_of_Lipid-Based_pub_2021.pdf (4.634Mb)
Authors
Mudrić, Jelena
Šavikin, Katarina
Ðekić, Ljiljana
Pavlović, Stefan
Kurćubić, Ivana
Ibrić, Svetlana
Ðuriš, Jelena
Article (Published version)
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Abstract
Gentian (Gentiana lutea L., Gentianaceae) root extract (GRE) is used for the treatment of gastrointestinal disorders. However, its bioactive potential is limited in conventional forms due to the low bioavailability and short elimination half-life of the dominant bioactive compound, gentiopicroside. The aim of study was to encapsulate GRE in the lipid-based gastroretentive delivery system that could provide high yield and encapsulation efficiency, as well as the biphasic release of gentiopicroside from the tablets obtained by direct compression. Solid lipid microparticles (SLM) loaded with GRE were prepared by freeze-drying double (W/O/W) emulsions, which were obtained by a multiple emulsion–melt dispersion technique, with GRE as the inner water phase, Gelucire® 39/01 or 43/01, as lipid components, with or without the addition of porous silica (Sylysia® 350) in the outer water phase. Formulated SLM powders were examined by SEM and mercury intrusion porosimetry, as well as by determinati...on of yield, encapsulation efficiency, and flow properties. Furthermore, in vitro dissolution of gentiopicroside, the size of the dispersed systems, mechanical properties, and mucoadhesion of tablets obtained by direct compression were investigated. The results have revealed that SLM with the macroporous structure were formulated, and, consequently, the powders floated immediately in the acidic medium. Formulation with porous silica (Sylysia® 350) and Gelucire® 43/01 as a solid lipid was characterized with the high yield end encapsulation efficiency. Furthermore, the mucoadhesive properties of tablets obtained by direct compression of that formulation, as well as the biphasic release of gentiopicroside, presence of nanoassociates in dissolution medium, and optimal mechanical properties indicated that a promising lipid-based gastroretentive system for GRE was developed.

Keywords:
Solid lipid microparticles / Biphasic release / Direct compression / Double (W/O/W) emulsion / Gastroretentive system / Gelucire 39/01 / Gelucire 43/01 / Gentiopicroside / Mucoadhesion / SLM / Sylysia 350
Source:
Pharmaceutics, 2021, 13, 12
Publisher:
  • MDPI
Funding / projects:
  • Ministry of Education, Science and Technological Development, Republic of Serbia, Grant no. 200003 (Institute for Medicinal Plant Research 'Dr. Josif Pančić ', Belgrade) (RS-200003)
  • Ministry of Education, Science and Technological Development, Republic of Serbia, Grant no. 200161 (University of Belgrade, Faculty of Pharmacy) (RS-200161)

DOI: 10.3390/pharmaceutics13122095

ISSN: 1999-4923

WoS: 000736842000001

Scopus: 2-s2.0-85121443815
[ Google Scholar ]
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/4014
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Mudrić, Jelena
AU  - Šavikin, Katarina
AU  - Ðekić, Ljiljana
AU  - Pavlović, Stefan
AU  - Kurćubić, Ivana
AU  - Ibrić, Svetlana
AU  - Ðuriš, Jelena
PY  - 2021
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4014
AB  - Gentian (Gentiana lutea L., Gentianaceae) root extract (GRE) is used for the treatment of gastrointestinal disorders. However, its bioactive potential is limited in conventional forms due to the low bioavailability and short elimination half-life of the dominant bioactive compound, gentiopicroside. The aim of study was to encapsulate GRE in the lipid-based gastroretentive delivery system that could provide high yield and encapsulation efficiency, as well as the biphasic release of gentiopicroside from the tablets obtained by direct compression. Solid lipid microparticles (SLM) loaded with GRE were prepared by freeze-drying double (W/O/W) emulsions, which were obtained by a multiple emulsion–melt dispersion technique, with GRE as the inner water phase, Gelucire® 39/01 or 43/01, as lipid components, with or without the addition of porous silica (Sylysia® 350) in the outer water phase. Formulated SLM powders were examined by SEM and mercury intrusion porosimetry, as well as by determination of yield, encapsulation efficiency, and flow properties. Furthermore, in vitro dissolution of gentiopicroside, the size of the dispersed systems, mechanical properties, and mucoadhesion of tablets obtained by direct compression were investigated. The results have revealed that SLM with the macroporous structure were formulated, and, consequently, the powders floated immediately in the acidic medium. Formulation with porous silica (Sylysia® 350) and Gelucire® 43/01 as a solid lipid was characterized with the high yield end encapsulation efficiency. Furthermore, the mucoadhesive properties of tablets obtained by direct compression of that formulation, as well as the biphasic release of gentiopicroside, presence of nanoassociates in dissolution medium, and optimal mechanical properties indicated that a promising lipid-based gastroretentive system for GRE was developed.
PB  - MDPI
T2  - Pharmaceutics
T1  - Development of lipid-based gastroretentive delivery system for gentian extract by double emulsion–melt dispersion technique
VL  - 13
IS  - 12
DO  - 10.3390/pharmaceutics13122095
ER  - 
@article{
author = "Mudrić, Jelena and Šavikin, Katarina and Ðekić, Ljiljana and Pavlović, Stefan and Kurćubić, Ivana and Ibrić, Svetlana and Ðuriš, Jelena",
year = "2021",
abstract = "Gentian (Gentiana lutea L., Gentianaceae) root extract (GRE) is used for the treatment of gastrointestinal disorders. However, its bioactive potential is limited in conventional forms due to the low bioavailability and short elimination half-life of the dominant bioactive compound, gentiopicroside. The aim of study was to encapsulate GRE in the lipid-based gastroretentive delivery system that could provide high yield and encapsulation efficiency, as well as the biphasic release of gentiopicroside from the tablets obtained by direct compression. Solid lipid microparticles (SLM) loaded with GRE were prepared by freeze-drying double (W/O/W) emulsions, which were obtained by a multiple emulsion–melt dispersion technique, with GRE as the inner water phase, Gelucire® 39/01 or 43/01, as lipid components, with or without the addition of porous silica (Sylysia® 350) in the outer water phase. Formulated SLM powders were examined by SEM and mercury intrusion porosimetry, as well as by determination of yield, encapsulation efficiency, and flow properties. Furthermore, in vitro dissolution of gentiopicroside, the size of the dispersed systems, mechanical properties, and mucoadhesion of tablets obtained by direct compression were investigated. The results have revealed that SLM with the macroporous structure were formulated, and, consequently, the powders floated immediately in the acidic medium. Formulation with porous silica (Sylysia® 350) and Gelucire® 43/01 as a solid lipid was characterized with the high yield end encapsulation efficiency. Furthermore, the mucoadhesive properties of tablets obtained by direct compression of that formulation, as well as the biphasic release of gentiopicroside, presence of nanoassociates in dissolution medium, and optimal mechanical properties indicated that a promising lipid-based gastroretentive system for GRE was developed.",
publisher = "MDPI",
journal = "Pharmaceutics",
title = "Development of lipid-based gastroretentive delivery system for gentian extract by double emulsion–melt dispersion technique",
volume = "13",
number = "12",
doi = "10.3390/pharmaceutics13122095"
}
Mudrić, J., Šavikin, K., Ðekić, L., Pavlović, S., Kurćubić, I., Ibrić, S.,& Ðuriš, J.. (2021). Development of lipid-based gastroretentive delivery system for gentian extract by double emulsion–melt dispersion technique. in Pharmaceutics
MDPI., 13(12).
https://doi.org/10.3390/pharmaceutics13122095
Mudrić J, Šavikin K, Ðekić L, Pavlović S, Kurćubić I, Ibrić S, Ðuriš J. Development of lipid-based gastroretentive delivery system for gentian extract by double emulsion–melt dispersion technique. in Pharmaceutics. 2021;13(12).
doi:10.3390/pharmaceutics13122095 .
Mudrić, Jelena, Šavikin, Katarina, Ðekić, Ljiljana, Pavlović, Stefan, Kurćubić, Ivana, Ibrić, Svetlana, Ðuriš, Jelena, "Development of lipid-based gastroretentive delivery system for gentian extract by double emulsion–melt dispersion technique" in Pharmaceutics, 13, no. 12 (2021),
https://doi.org/10.3390/pharmaceutics13122095 . .

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