Novel fast dissolving freeze dried sublingual baicalin tablets for enhanced hepatoprotective effect : in-vitro characterization, cell viability, and in-vivo evaluation
Baicalin (BG), a natural product, has been used in the prevention and treatment of drug-induced liver injury (DILI); however, its poor solubility and extensive liver metabolism limit its pharmacological use. The aim of the present study was the formulation of fast-dissolving freeze-dried sublingual tablets (FFSTs) to increase BG dissolution, avoid first-pass metabolism, and overcome swallowing difficulties. FFSTs were prepared following a 23 factorial design. The effect of three independent variables namely matrix former, Maltodextrin, concentration (4%, and 6%), binder concentration (2%, and 3%), and binder type (Methocel E5, and Methocel E15) on the FFSTs' in-vitro disintegration time and percentage dissolution was studied along with other tablet characteristics. Differential scanning calorimetry, scanning electron microscopy, in-vitro HepG2 cell viability assay, and in-vivo characterization were also performed. F8 (6% Maltodextrin, 2% Mannitol, 2% Methocel E5), with desirability of 0.852, has been furtherly enhanced using 1%PEG (F10). F10 has achieved an in-vitro disintegration time of 41 secs, and 60.83% in-vitro dissolution after 2 min. Cell viability assay, in-vivo study in rats, and histopathological studies confirmed that pretreatment with F10 has achieved a significant hepatoprotective effect against acetaminophen-induced hepatotoxicity. The outcome of this study demonstrated that FFSTs may present a patient-friendly dosage form against DILI.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - year:2024 |
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| Enthalten in: |
Pharmaceutical development and technology - (2024) vom: 13. Apr., Seite 1-12 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Abdelrazek, Farida N [VerfasserIn] |
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| Links: |
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| Themen: |
Baicalin |
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| Anmerkungen: |
Date Revised 13.04.2024 published: Print-Electronic Citation Status Publisher |
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| doi: |
10.1080/10837450.2024.2341243 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM371027837 |
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| 520 | |a Baicalin (BG), a natural product, has been used in the prevention and treatment of drug-induced liver injury (DILI); however, its poor solubility and extensive liver metabolism limit its pharmacological use. The aim of the present study was the formulation of fast-dissolving freeze-dried sublingual tablets (FFSTs) to increase BG dissolution, avoid first-pass metabolism, and overcome swallowing difficulties. FFSTs were prepared following a 23 factorial design. The effect of three independent variables namely matrix former, Maltodextrin, concentration (4%, and 6%), binder concentration (2%, and 3%), and binder type (Methocel E5, and Methocel E15) on the FFSTs' in-vitro disintegration time and percentage dissolution was studied along with other tablet characteristics. Differential scanning calorimetry, scanning electron microscopy, in-vitro HepG2 cell viability assay, and in-vivo characterization were also performed. F8 (6% Maltodextrin, 2% Mannitol, 2% Methocel E5), with desirability of 0.852, has been furtherly enhanced using 1%PEG (F10). F10 has achieved an in-vitro disintegration time of 41 secs, and 60.83% in-vitro dissolution after 2 min. Cell viability assay, in-vivo study in rats, and histopathological studies confirmed that pretreatment with F10 has achieved a significant hepatoprotective effect against acetaminophen-induced hepatotoxicity. The outcome of this study demonstrated that FFSTs may present a patient-friendly dosage form against DILI | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Baicalin | |
| 650 | 4 | |a fast dissolving | |
| 650 | 4 | |a freeze drying | |
| 650 | 4 | |a hepatoprotective | |
| 650 | 4 | |a patient-friendly dosage form | |
| 650 | 4 | |a sublingual tablets | |
| 700 | 1 | |a Shalaby, Rodayna A |e verfasserin |4 aut | |
| 700 | 1 | |a Fahim, Sally A |e verfasserin |4 aut | |
| 700 | 1 | |a Essam, Reham M |e verfasserin |4 aut | |
| 700 | 1 | |a Anis, Shady E |e verfasserin |4 aut | |
| 700 | 1 | |a Attia, Yasmin M |e verfasserin |4 aut | |
| 700 | 1 | |a Abd El Malak, Nevine S |e verfasserin |4 aut | |
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