Dual-Mechanism Gastroretentive Tablets with Encapsulated Gentian Root Extract
<b>Background/Objectives:</b> This study aimed to develop gastroretentive tablets based on mucoadhesive–floating systems with encapsulated gentian (<i>Gentiana lutea</i>, Gentianaceae) root extract to overcome the low bioavailability and short elimination half-life of gentiop...
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MDPI AG
2025-01-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/17/1/71 |
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| author | Jelena Mudrić Ljiljana Đekić Nemanja Krgović Đorđe Medarević Katarina Šavikin Milica Radan Nada Ćujić Nikolić Tijana Ilić Bojana Vidović Jelena Đuriš |
| author_facet | Jelena Mudrić Ljiljana Đekić Nemanja Krgović Đorđe Medarević Katarina Šavikin Milica Radan Nada Ćujić Nikolić Tijana Ilić Bojana Vidović Jelena Đuriš |
| author_sort | Jelena Mudrić |
| collection | DOAJ |
| description | <b>Background/Objectives:</b> This study aimed to develop gastroretentive tablets based on mucoadhesive–floating systems with encapsulated gentian (<i>Gentiana lutea</i>, Gentianaceae) root extract to overcome the low bioavailability and short elimination half-life of gentiopicroside, a dominant bioactive compound with systemic effect. The formulation also aimed to promote the local action of the extract in the stomach. <b>Methods:</b> Tablets were obtained by direct compression of sodium bicarbonate (7.5%) and solid lipid microparticles (92.5%), which were obtained with lyophilizing double emulsions. A quality by design (QbD) was employed to evaluate the impact of formulation factors and processing parameters on emulsion viscosity, powder characteristics (moisture content, encapsulation efficiency, flowability), and tablet characteristics (floating lag time, gentiopicroside release, and assessment of dispersibility during in vitro dissolution). <b>Results:</b> The trehalose content and high-shear-homogenization (HSH) time of primary emulsion were critical factors. Trehalose content positively influenced emulsion viscosity, moisture content, floating lag time, encapsulation efficiency, and the release rate of gentiopicroside. HSH time positively affected powder stability and negatively gentiopicroside release. The selected powder had a high gentiopicroside encapsulation efficiency (95.13%), optimal stability, and good flowability. The developed tablets exhibited adequate floating lag time (275 s), mucoadhesive properties, and gentiopicroside biphasic release (29.04% in 45 min; 67.95% in 6 h). Furthermore, the optimal tablet formulation remained stable for 18 months and was primarily digested by duodenal enzymes. <b>Conclusions:</b> Dual-mechanism gastroretentive tablets with encapsulated gentian root extract were successfully developed. The in vitro digestion study demonstrated that the optimal formulation effectively resisted gastric enzymes, ensuring the release of its contents in the small intestine, even in the case of premature gastric evacuation. |
| format | Article |
| id | doaj-art-7a1ef89c550f450a8738d787acecee2c |
| institution | Kabale University |
| issn | 1999-4923 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj-art-7a1ef89c550f450a8738d787acecee2c2025-01-24T13:45:49ZengMDPI AGPharmaceutics1999-49232025-01-011717110.3390/pharmaceutics17010071Dual-Mechanism Gastroretentive Tablets with Encapsulated Gentian Root ExtractJelena Mudrić0Ljiljana Đekić1Nemanja Krgović2Đorđe Medarević3Katarina Šavikin4Milica Radan5Nada Ćujić Nikolić6Tijana Ilić7Bojana Vidović8Jelena Đuriš9Institute for Medicinal Plants Research “Dr. Josif Pančić”, 11000 Belgrade, SerbiaFaculty of Pharmacy, University of Belgrade, 11221 Belgrade, SerbiaInstitute for Medicinal Plants Research “Dr. Josif Pančić”, 11000 Belgrade, SerbiaFaculty of Pharmacy, University of Belgrade, 11221 Belgrade, SerbiaInstitute for Medicinal Plants Research “Dr. Josif Pančić”, 11000 Belgrade, SerbiaInstitute for Medicinal Plants Research “Dr. Josif Pančić”, 11000 Belgrade, SerbiaInstitute for Medicinal Plants Research “Dr. Josif Pančić”, 11000 Belgrade, SerbiaFaculty of Pharmacy, University of Belgrade, 11221 Belgrade, SerbiaFaculty of Pharmacy, University of Belgrade, 11221 Belgrade, SerbiaFaculty of Pharmacy, University of Belgrade, 11221 Belgrade, Serbia<b>Background/Objectives:</b> This study aimed to develop gastroretentive tablets based on mucoadhesive–floating systems with encapsulated gentian (<i>Gentiana lutea</i>, Gentianaceae) root extract to overcome the low bioavailability and short elimination half-life of gentiopicroside, a dominant bioactive compound with systemic effect. The formulation also aimed to promote the local action of the extract in the stomach. <b>Methods:</b> Tablets were obtained by direct compression of sodium bicarbonate (7.5%) and solid lipid microparticles (92.5%), which were obtained with lyophilizing double emulsions. A quality by design (QbD) was employed to evaluate the impact of formulation factors and processing parameters on emulsion viscosity, powder characteristics (moisture content, encapsulation efficiency, flowability), and tablet characteristics (floating lag time, gentiopicroside release, and assessment of dispersibility during in vitro dissolution). <b>Results:</b> The trehalose content and high-shear-homogenization (HSH) time of primary emulsion were critical factors. Trehalose content positively influenced emulsion viscosity, moisture content, floating lag time, encapsulation efficiency, and the release rate of gentiopicroside. HSH time positively affected powder stability and negatively gentiopicroside release. The selected powder had a high gentiopicroside encapsulation efficiency (95.13%), optimal stability, and good flowability. The developed tablets exhibited adequate floating lag time (275 s), mucoadhesive properties, and gentiopicroside biphasic release (29.04% in 45 min; 67.95% in 6 h). Furthermore, the optimal tablet formulation remained stable for 18 months and was primarily digested by duodenal enzymes. <b>Conclusions:</b> Dual-mechanism gastroretentive tablets with encapsulated gentian root extract were successfully developed. The in vitro digestion study demonstrated that the optimal formulation effectively resisted gastric enzymes, ensuring the release of its contents in the small intestine, even in the case of premature gastric evacuation.https://www.mdpi.com/1999-4923/17/1/71double emulsionsolid lipid microparticles (SLMs)quality by designtrehalosein vitro digestiongentiopicroside |
| spellingShingle | Jelena Mudrić Ljiljana Đekić Nemanja Krgović Đorđe Medarević Katarina Šavikin Milica Radan Nada Ćujić Nikolić Tijana Ilić Bojana Vidović Jelena Đuriš Dual-Mechanism Gastroretentive Tablets with Encapsulated Gentian Root Extract Pharmaceutics double emulsion solid lipid microparticles (SLMs) quality by design trehalose in vitro digestion gentiopicroside |
| title | Dual-Mechanism Gastroretentive Tablets with Encapsulated Gentian Root Extract |
| title_full | Dual-Mechanism Gastroretentive Tablets with Encapsulated Gentian Root Extract |
| title_fullStr | Dual-Mechanism Gastroretentive Tablets with Encapsulated Gentian Root Extract |
| title_full_unstemmed | Dual-Mechanism Gastroretentive Tablets with Encapsulated Gentian Root Extract |
| title_short | Dual-Mechanism Gastroretentive Tablets with Encapsulated Gentian Root Extract |
| title_sort | dual mechanism gastroretentive tablets with encapsulated gentian root extract |
| topic | double emulsion solid lipid microparticles (SLMs) quality by design trehalose in vitro digestion gentiopicroside |
| url | https://www.mdpi.com/1999-4923/17/1/71 |
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