Management of intraocular pressure and inflammation using febuxostat film: in vitro - in vivo correlation
Background and purpose: Urate crystal accumulation may lead to the condition of ocular tophaceous gout, causing ocular inflammation and increased intraocular pressure (IOP) due to the triggering of several inflammatory receptors like NLRP3, A2A, and TLR4. The study has been undertaken to manage int...
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International Association of Physical Chemists (IAPC)
2025-01-01
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| Series: | ADMET and DMPK |
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| Online Access: | https://pub.iapchem.org/ojs/index.php/admet/article/view/2601 |
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| author | Mouli Das Sk Habibullah Tanisha Das Rakesh Swain Subrata Mallick |
| author_facet | Mouli Das Sk Habibullah Tanisha Das Rakesh Swain Subrata Mallick |
| author_sort | Mouli Das |
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Background and purpose: Urate crystal accumulation may lead to the condition of ocular tophaceous gout, causing ocular inflammation and increased intraocular pressure (IOP) due to the triggering of several inflammatory receptors like NLRP3, A2A, and TLR4. The study has been undertaken to manage intraocular pressure and inflammation using febuxostat (FBX) film formulation for sustained and improved activity, particularly for long-term tophaceous gout patients. Experimental approach: Hydroxypropyl methyl-cellulose K100 matrix-based hydrogel film of FBX has been fabricated in the presence of plasticizers like triethanolamine, dimethyl-sulphoxide (DMSO), or polyethylene glycol 600 using casting and evaporation technique. Carrageenan was injected into the upper palpebral region to induce ocular inflammation, and a normotensive rabbit eye model was used for monitoring IOP. Key results: Amorphization of the drug was observed from the differential scanning calorimetry and X-ray diffraction results. In vitro release study revealed an improved and diffusion-controlled sustained drug release for more than 5 h (62.69 to 84.76 %). Compared to its absence, decreased IOP was extended up to 5 h using film (with DMSO). Disappearance of ocular inflammation was also observed in the test animals after 2.5 h of film application, whereas acute inflammation was continued in the group without treatment for more than 4 h. Docking study revealed good binding interaction of drug and NLRP3, A2A, and TLR4 receptor. Conclusion: Febuxostat-loaded hydrogel-forming plasticized film could be utilized to better manage and control ocular inflammation and associated IOP, particularly in ocular tophaceous gout patients.
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| format | Article |
| id | doaj-art-c0f80785aeb449e99d688b53dee4e852 |
| institution | Kabale University |
| issn | 1848-7718 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | International Association of Physical Chemists (IAPC) |
| record_format | Article |
| series | ADMET and DMPK |
| spelling | doaj-art-c0f80785aeb449e99d688b53dee4e8522025-01-24T07:46:41ZengInternational Association of Physical Chemists (IAPC)ADMET and DMPK1848-77182025-01-0110.5599/admet.2601Management of intraocular pressure and inflammation using febuxostat film: in vitro - in vivo correlationMouli Das0Sk Habibullah 1Tanisha Das2Rakesh Swain3Subrata Mallick4School of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar 751003, Odisha, IndiaSchool of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar 751003, Odisha, India.School of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar 751003, Odisha, IndiaSchool of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar 751003, Odisha, IndiaSiksha O Anusandhan (Deemed to be University), School Of Pharmaceutical Sciences Background and purpose: Urate crystal accumulation may lead to the condition of ocular tophaceous gout, causing ocular inflammation and increased intraocular pressure (IOP) due to the triggering of several inflammatory receptors like NLRP3, A2A, and TLR4. The study has been undertaken to manage intraocular pressure and inflammation using febuxostat (FBX) film formulation for sustained and improved activity, particularly for long-term tophaceous gout patients. Experimental approach: Hydroxypropyl methyl-cellulose K100 matrix-based hydrogel film of FBX has been fabricated in the presence of plasticizers like triethanolamine, dimethyl-sulphoxide (DMSO), or polyethylene glycol 600 using casting and evaporation technique. Carrageenan was injected into the upper palpebral region to induce ocular inflammation, and a normotensive rabbit eye model was used for monitoring IOP. Key results: Amorphization of the drug was observed from the differential scanning calorimetry and X-ray diffraction results. In vitro release study revealed an improved and diffusion-controlled sustained drug release for more than 5 h (62.69 to 84.76 %). Compared to its absence, decreased IOP was extended up to 5 h using film (with DMSO). Disappearance of ocular inflammation was also observed in the test animals after 2.5 h of film application, whereas acute inflammation was continued in the group without treatment for more than 4 h. Docking study revealed good binding interaction of drug and NLRP3, A2A, and TLR4 receptor. Conclusion: Febuxostat-loaded hydrogel-forming plasticized film could be utilized to better manage and control ocular inflammation and associated IOP, particularly in ocular tophaceous gout patients. https://pub.iapchem.org/ojs/index.php/admet/article/view/2601Anti-inflammationFebuxostatHydrogel filmIntraocular pressurein-vitro-in-vivo-correlation |
| spellingShingle | Mouli Das Sk Habibullah Tanisha Das Rakesh Swain Subrata Mallick Management of intraocular pressure and inflammation using febuxostat film: in vitro - in vivo correlation ADMET and DMPK Anti-inflammation Febuxostat Hydrogel film Intraocular pressure in-vitro-in-vivo-correlation |
| title | Management of intraocular pressure and inflammation using febuxostat film: in vitro - in vivo correlation |
| title_full | Management of intraocular pressure and inflammation using febuxostat film: in vitro - in vivo correlation |
| title_fullStr | Management of intraocular pressure and inflammation using febuxostat film: in vitro - in vivo correlation |
| title_full_unstemmed | Management of intraocular pressure and inflammation using febuxostat film: in vitro - in vivo correlation |
| title_short | Management of intraocular pressure and inflammation using febuxostat film: in vitro - in vivo correlation |
| title_sort | management of intraocular pressure and inflammation using febuxostat film in vitro in vivo correlation |
| topic | Anti-inflammation Febuxostat Hydrogel film Intraocular pressure in-vitro-in-vivo-correlation |
| url | https://pub.iapchem.org/ojs/index.php/admet/article/view/2601 |
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