Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of <i>H. pylori</i>: Preparation and In Vitro Characterization
Metronidazole has the potential to produce local stomach specific action in order to treat <i>Helicobacter pylori</i> induced peptic ulcer disease. The current project executes the development of osmotically controlled bioadhesive metronidazole loaded effervescent floating tablets with o...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-01-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/3/519 |
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| author | Faiza Naseem Shefaat Ullah Shah Sheikh Abdur Rashid Arshad Farid Mazen Almehmadi Saad Alghamdi |
| author_facet | Faiza Naseem Shefaat Ullah Shah Sheikh Abdur Rashid Arshad Farid Mazen Almehmadi Saad Alghamdi |
| author_sort | Faiza Naseem |
| collection | DOAJ |
| description | Metronidazole has the potential to produce local stomach specific action in order to treat <i>Helicobacter pylori</i> induced peptic ulcer disease. The current project executes the development of osmotically controlled bioadhesive metronidazole loaded effervescent floating tablets with optimized floating and swelling behavior. Direct compression technique was used to prepare the tablets. The designed formulations exhibited physico-chemical properties within acceptable optimum limits as per pharmacopeial requirements. The results of tablet floating studies revealed that all formulations, except F1 and F5, had good buoyancy characteristics (TFT > 12 h except F2 and F8 with TFT of 6 h). Formulation F2 containing guar gum in higher concentration with carbopol and formulation F8 containing guar gum in 50% decreased concentration in combination with HPMC and carbopol had enhanced FLT appreciably, with least TFT as compared to formulations F3, F4, and F6 (ANOVA; <i>p</i> ≤ 0.05). Formulation batches of F3, F4, and F6 exhibited appreciable FLT as well as TFT and were optimized formulations. Out of the above mentioned optimized batches, F4 and F6 formulations showed low FLT (4 and 5 s respectively). The results of the swelling study indicated a proportionate increase in the swelling index with increase in time. A significantly higher swelling ratio was found with formulation F6 and F4 compared with that of F7 and F8 (ANOVA; <i>p</i> ≤ 0.05). Additionally, the impact of pH change, agitational intensity, as well as increasing concentration of NaCl was investigated on drug release. It was observed that agitational intensity had no effect on drug release rate while increasing concentration of NaCl produced an increased drug release from the dosage form as compared to the drug release exhibited by the formulations in the absence of NaCl. Overall, this project could have valuable contribution in the fabrication of metronidazole loaded effervescent floating tablets. Gastro-retentive systems are expected to enhance local stomach specific action of anti <i>H. pylori</i> agents based on their buoyancy and swelling behavior. |
| first_indexed | 2024-03-09T23:17:09Z |
| format | Article |
| id | doaj.art-f8016575d5244b72a51e7132b1d7ea72 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-09T23:17:09Z |
| publishDate | 2022-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-f8016575d5244b72a51e7132b1d7ea722023-11-23T17:35:11ZengMDPI AGPolymers2073-43602022-01-0114351910.3390/polym14030519Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of <i>H. pylori</i>: Preparation and In Vitro CharacterizationFaiza Naseem0Shefaat Ullah Shah1Sheikh Abdur Rashid2Arshad Farid3Mazen Almehmadi4Saad Alghamdi5Skin/Regenerative Medicine and Drug Delivery Research, GCPS, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanSkin/Regenerative Medicine and Drug Delivery Research, GCPS, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanSkin/Regenerative Medicine and Drug Delivery Research, GCPS, Faculty of Pharmacy, Gomal University, Dera Ismail Khan 29050, PakistanGomal Center of Biochemistry and Biotechnology, Gomal University, Dera Ismail Khan 29050, PakistanClinical Laboratory Sciences Department, College of Applied Medical Sciences, Taif University, Taif 26571, Saudi ArabiaLaboratory Medicine Department, Faculty of Applied Medical Sciences, Umm Al-Qura University, Makkah al-Mukarramah 24382, Saudi ArabiaMetronidazole has the potential to produce local stomach specific action in order to treat <i>Helicobacter pylori</i> induced peptic ulcer disease. The current project executes the development of osmotically controlled bioadhesive metronidazole loaded effervescent floating tablets with optimized floating and swelling behavior. Direct compression technique was used to prepare the tablets. The designed formulations exhibited physico-chemical properties within acceptable optimum limits as per pharmacopeial requirements. The results of tablet floating studies revealed that all formulations, except F1 and F5, had good buoyancy characteristics (TFT > 12 h except F2 and F8 with TFT of 6 h). Formulation F2 containing guar gum in higher concentration with carbopol and formulation F8 containing guar gum in 50% decreased concentration in combination with HPMC and carbopol had enhanced FLT appreciably, with least TFT as compared to formulations F3, F4, and F6 (ANOVA; <i>p</i> ≤ 0.05). Formulation batches of F3, F4, and F6 exhibited appreciable FLT as well as TFT and were optimized formulations. Out of the above mentioned optimized batches, F4 and F6 formulations showed low FLT (4 and 5 s respectively). The results of the swelling study indicated a proportionate increase in the swelling index with increase in time. A significantly higher swelling ratio was found with formulation F6 and F4 compared with that of F7 and F8 (ANOVA; <i>p</i> ≤ 0.05). Additionally, the impact of pH change, agitational intensity, as well as increasing concentration of NaCl was investigated on drug release. It was observed that agitational intensity had no effect on drug release rate while increasing concentration of NaCl produced an increased drug release from the dosage form as compared to the drug release exhibited by the formulations in the absence of NaCl. Overall, this project could have valuable contribution in the fabrication of metronidazole loaded effervescent floating tablets. Gastro-retentive systems are expected to enhance local stomach specific action of anti <i>H. pylori</i> agents based on their buoyancy and swelling behavior.https://www.mdpi.com/2073-4360/14/3/519metronidazoledirect compressionswelling indextotal floating timeagitational intensity |
| spellingShingle | Faiza Naseem Shefaat Ullah Shah Sheikh Abdur Rashid Arshad Farid Mazen Almehmadi Saad Alghamdi Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of <i>H. pylori</i>: Preparation and In Vitro Characterization Polymers metronidazole direct compression swelling index total floating time agitational intensity |
| title | Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of <i>H. pylori</i>: Preparation and In Vitro Characterization |
| title_full | Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of <i>H. pylori</i>: Preparation and In Vitro Characterization |
| title_fullStr | Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of <i>H. pylori</i>: Preparation and In Vitro Characterization |
| title_full_unstemmed | Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of <i>H. pylori</i>: Preparation and In Vitro Characterization |
| title_short | Metronidazole Based Floating Bioadhesive Drug Delivery System for Potential Eradication of <i>H. pylori</i>: Preparation and In Vitro Characterization |
| title_sort | metronidazole based floating bioadhesive drug delivery system for potential eradication of i h pylori i preparation and in vitro characterization |
| topic | metronidazole direct compression swelling index total floating time agitational intensity |
| url | https://www.mdpi.com/2073-4360/14/3/519 |
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