Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s Eye
<b>Background/objectives:</b> The aim of the study was to create a nanofiber insert incorporating Timolol (TIM) and Dorzolamide (DOR), targeting the management of glaucoma. This condition encompasses a variety of chronic, advancing ocular disorders typically associated with elevated intr...
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2025-01-01
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| author | Ahmad Karami Shahla Mirzaeei Leila Rezaei Ali Nokhodchi |
| author_facet | Ahmad Karami Shahla Mirzaeei Leila Rezaei Ali Nokhodchi |
| author_sort | Ahmad Karami |
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| description | <b>Background/objectives:</b> The aim of the study was to create a nanofiber insert incorporating Timolol (TIM) and Dorzolamide (DOR), targeting the management of glaucoma. This condition encompasses a variety of chronic, advancing ocular disorders typically associated with elevated intraocular pressure (IOP). <b>Methods:</b> The insert was made of Eudragite RL100 (EUD) polymer, a biocompatible material with high bioavailability, using the electrospinning method. The inserts were studied for morphology, drug–polymer interaction, physicochemical properties, and in vitro drug-release study. The pharmacokinetic properties of fibers were examined alongside consideration for irritation using a rabbit model and cell compatibility. <b>Results:</b> The results of the in vitro drug-release test showed retention and controlled release of both DOR/TIM over 80 h. Morphological examination demonstrated uniform nanofibers with mean diameters < 465 nm. The cell compatibility test showed a high percentage of cell survival, and none of the formulations irritated the rabbit’s eye. The Area Under the Curve (AUC0-72) for DOR and TIM in EDT formulations was approximately 3216.63 ± 63.25 µg·h/mL and 2598.89 ± 46.65 µg·h/mL, respectively, with Mean Residence Times (MRTs) of approximately 21.6 ± 0.19 h and 16.29 ± 6.44 h. <b>Conclusions:</b> Based on the results, the dual drug-loaded nanofiber preservative-free system can potentially be a suitable alternative to eye drops and can be used to reduce fluctuation and dose frequency. |
| format | Article |
| id | doaj-art-559977d3816647aca6b679afaf7a6d4f |
| institution | Kabale University |
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| language | English |
| publishDate | 2025-01-01 |
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| spelling | doaj-art-559977d3816647aca6b679afaf7a6d4f2025-01-24T13:24:23ZengMDPI AGBiomedicines2227-90592025-01-0113120010.3390/biomedicines13010200Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s EyeAhmad Karami0Shahla Mirzaeei1Leila Rezaei2Ali Nokhodchi3Nano Drug Delivery Research Centre, Health Technology Institute, Kermanshah University of Medical Sciences, Kermanshah 6715847141, IranPharmaceutical Sciences Research Center, Health Institute, Kermanshah University of Medical Sciences, Kermanshah 6715847141, IranDepartment of Ophthalmology, Kermanshah University of Medical Sciences, Kermanshah 6715847141, IranSchool of Life Sciences, University of Sussex, Brighton BN1 9QG, UK<b>Background/objectives:</b> The aim of the study was to create a nanofiber insert incorporating Timolol (TIM) and Dorzolamide (DOR), targeting the management of glaucoma. This condition encompasses a variety of chronic, advancing ocular disorders typically associated with elevated intraocular pressure (IOP). <b>Methods:</b> The insert was made of Eudragite RL100 (EUD) polymer, a biocompatible material with high bioavailability, using the electrospinning method. The inserts were studied for morphology, drug–polymer interaction, physicochemical properties, and in vitro drug-release study. The pharmacokinetic properties of fibers were examined alongside consideration for irritation using a rabbit model and cell compatibility. <b>Results:</b> The results of the in vitro drug-release test showed retention and controlled release of both DOR/TIM over 80 h. Morphological examination demonstrated uniform nanofibers with mean diameters < 465 nm. The cell compatibility test showed a high percentage of cell survival, and none of the formulations irritated the rabbit’s eye. The Area Under the Curve (AUC0-72) for DOR and TIM in EDT formulations was approximately 3216.63 ± 63.25 µg·h/mL and 2598.89 ± 46.65 µg·h/mL, respectively, with Mean Residence Times (MRTs) of approximately 21.6 ± 0.19 h and 16.29 ± 6.44 h. <b>Conclusions:</b> Based on the results, the dual drug-loaded nanofiber preservative-free system can potentially be a suitable alternative to eye drops and can be used to reduce fluctuation and dose frequency.https://www.mdpi.com/2227-9059/13/1/200glaucomaophthalmic nanofiber insertcontrolled releasedrug-loaded Dorzolamide and Timololfixed combination |
| spellingShingle | Ahmad Karami Shahla Mirzaeei Leila Rezaei Ali Nokhodchi Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s Eye Biomedicines glaucoma ophthalmic nanofiber insert controlled release drug-loaded Dorzolamide and Timolol fixed combination |
| title | Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s Eye |
| title_full | Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s Eye |
| title_fullStr | Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s Eye |
| title_full_unstemmed | Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s Eye |
| title_short | Development and Evaluation of Polymethacrylate-Based Ophthalmic Nanofiber Inserts Containing Dual Drug-Loaded Dorzolamide and Timolol: In Vivo Study in Rabbit’s Eye |
| title_sort | development and evaluation of polymethacrylate based ophthalmic nanofiber inserts containing dual drug loaded dorzolamide and timolol in vivo study in rabbit s eye |
| topic | glaucoma ophthalmic nanofiber insert controlled release drug-loaded Dorzolamide and Timolol fixed combination |
| url | https://www.mdpi.com/2227-9059/13/1/200 |
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