Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion-Melt Dispersion Technique
Authors
Mudrić, JelenaŠavikin, Katarina

Đekić, Ljiljana
Pavlović, Stefan

Kurćubić, Ivana
Ibrić, Svetlana

Đuriš, Jelena

Article (Published version)
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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 / SLM / gastroretentive system / Gelucire 43/01 / Gelucire 39/01 / Sylysia 350 / gentiopicroside / double (W/O/W) emulsion / mucoadhesion / direct compression / biphasic releaseSource:
Pharmaceutics, 2021, 13, 12, 2095-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)
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IHTMTY - JOUR AU - Mudrić, Jelena AU - Šavikin, Katarina AU - Đekić, Ljiljana AU - Pavlović, Stefan AU - Kurćubić, Ivana AU - Ibrić, Svetlana AU - Đuriš, Jelena PY - 2021 UR - https://cer.ihtm.bg.ac.rs/handle/123456789/4891 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 SP - 2095 DO - 10.3390/pharmaceutics13122095 ER -
@article{ author = "Mudrić, Jelena and Šavikin, Katarina and Đekić, Ljiljana and Pavlović, Stefan and Kurćubić, Ivana and Ibrić, Svetlana and Đuriš, 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", pages = "2095", doi = "10.3390/pharmaceutics13122095" }
Mudrić, J., Šavikin, K., Đekić, L., Pavlović, S., Kurćubić, I., Ibrić, S.,& Đuriš, J.. (2021). Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion-Melt Dispersion Technique. in Pharmaceutics MDPI., 13(12), 2095. https://doi.org/10.3390/pharmaceutics13122095
Mudrić J, Šavikin K, Đekić L, Pavlović S, Kurćubić I, Ibrić S, Đuriš J. Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion-Melt Dispersion Technique. in Pharmaceutics. 2021;13(12):2095. doi:10.3390/pharmaceutics13122095 .
Mudrić, Jelena, Šavikin, Katarina, Đekić, Ljiljana, Pavlović, Stefan, Kurćubić, Ivana, Ibrić, Svetlana, Đuriš, Jelena, "Development of Lipid-Based Gastroretentive Delivery System for Gentian Extract by Double Emulsion-Melt Dispersion Technique" in Pharmaceutics, 13, no. 12 (2021):2095, https://doi.org/10.3390/pharmaceutics13122095 . .