Fabrication of Anti-glaucoma Nanofibers as Controlled-Release Inserts for Ophthalmic Delivery of Brimonidine Tartrate: In Vivo Evaluation in Caprine Eye

Purpose: Chronic ailments usually decrease the quality of life due to the requirement for repetitive administration of drugs. Glaucoma is a chronic eye disease occurred because of increased intraocular pressure (IOP). Controlled-release inserts can overcome this challenge by a gradual release of the...

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Main Authors: Fariba Shaikhi Shoushtari, Mohammadshakib Naghshbandy, Leila Rezaei, Saba Mehrandish, Shahla Mirzaeei
Format: Article
Language:English
Published: Tabriz University of Medical Sciences 2024-07-01
Series:Advanced Pharmaceutical Bulletin
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Online Access:https://apb.tbzmed.ac.ir/PDF/apb-14-378.pdf
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author Fariba Shaikhi Shoushtari
Mohammadshakib Naghshbandy
Leila Rezaei
Saba Mehrandish
Shahla Mirzaeei
author_facet Fariba Shaikhi Shoushtari
Mohammadshakib Naghshbandy
Leila Rezaei
Saba Mehrandish
Shahla Mirzaeei
author_sort Fariba Shaikhi Shoushtari
collection DOAJ
description Purpose: Chronic ailments usually decrease the quality of life due to the requirement for repetitive administration of drugs. Glaucoma is a chronic eye disease occurred because of increased intraocular pressure (IOP). Controlled-release inserts can overcome this challenge by a gradual release of the antiglaucoma drugs. This study aimed to fabricate ocular inserts of brimonidine tartrate (BMD) for the management of glaucoma. Methods: Different polymers including poly (D, L-lactide), polycaprolactone, cellulose acetate, and Eudragit RL100® were used to develop the BMD-loaded nanofibrous inserts by electrospinning technique. The inserts were characterized. The morphology and drug-polymer compatibility were examined by scanning electron microscopy (SEM), and Fourier-transform infrared (FTIR) spectroscopy and in vitro drug release in PBS. The IOP-lowering efficacy and irritancy of optimized formulation were assessed in the caprines. Results: SEM images demonstrated nanofibers with uniform morphology and a mean diameter<300 nm were fabricated. The nanofibers were high-strength and flexible enough to be placed in the conjunctival sac. FTIR showed drug-polymer compatibility. In vitro release study indicated a sustained-release profile of the drug during 6 days for inserts. In vivo evaluation indicated that the optimized formulation is capable of maintaining the IOP in a non-glaucomatous range for an extended duration of 6 days. In addition, the formulation was non-irritant to the caprine eye. Conclusion: Due to the prolonged IOP-lowering efficiency, BMD-loaded nanofibrous inserts can be considered suitable for the controlled release of drugs and thus enhance patient compliance by reducing the frequency of administration.
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spelling doaj-art-299fa41cec104e2e9e06c59d31e9d20c2025-08-20T03:11:26ZengTabriz University of Medical SciencesAdvanced Pharmaceutical Bulletin2228-58812251-73082024-07-0114237838710.34172/apb.2024.025apb-39175Fabrication of Anti-glaucoma Nanofibers as Controlled-Release Inserts for Ophthalmic Delivery of Brimonidine Tartrate: In Vivo Evaluation in Caprine EyeFariba Shaikhi Shoushtari0Mohammadshakib Naghshbandy1Leila Rezaei2Saba Mehrandish3Shahla Mirzaeei4Department of Ophthalmology, Faculty of Medicine, Kermanshah University of Medical Sciences, Kermanshah, Iran.Department of Ophthalmology, Faculty of Medicine, Kermanshah University of Medical Sciences, Kermanshah, Iran.Department of Ophthalmology, Kermanshah University of Medical Sciences, Kermanshah, Iran.Pharmaceutical Sciences Research Center, Rahesh Daru Novine, Kermanshah 6715847141, Iran.Pharmaceutical Sciences Research Center, Health Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran.Purpose: Chronic ailments usually decrease the quality of life due to the requirement for repetitive administration of drugs. Glaucoma is a chronic eye disease occurred because of increased intraocular pressure (IOP). Controlled-release inserts can overcome this challenge by a gradual release of the antiglaucoma drugs. This study aimed to fabricate ocular inserts of brimonidine tartrate (BMD) for the management of glaucoma. Methods: Different polymers including poly (D, L-lactide), polycaprolactone, cellulose acetate, and Eudragit RL100® were used to develop the BMD-loaded nanofibrous inserts by electrospinning technique. The inserts were characterized. The morphology and drug-polymer compatibility were examined by scanning electron microscopy (SEM), and Fourier-transform infrared (FTIR) spectroscopy and in vitro drug release in PBS. The IOP-lowering efficacy and irritancy of optimized formulation were assessed in the caprines. Results: SEM images demonstrated nanofibers with uniform morphology and a mean diameter<300 nm were fabricated. The nanofibers were high-strength and flexible enough to be placed in the conjunctival sac. FTIR showed drug-polymer compatibility. In vitro release study indicated a sustained-release profile of the drug during 6 days for inserts. In vivo evaluation indicated that the optimized formulation is capable of maintaining the IOP in a non-glaucomatous range for an extended duration of 6 days. In addition, the formulation was non-irritant to the caprine eye. Conclusion: Due to the prolonged IOP-lowering efficiency, BMD-loaded nanofibrous inserts can be considered suitable for the controlled release of drugs and thus enhance patient compliance by reducing the frequency of administration.https://apb.tbzmed.ac.ir/PDF/apb-14-378.pdfbrimonidine tartratecaprineelectrospinningglaucomananofibersophthalmic drug delivery
spellingShingle Fariba Shaikhi Shoushtari
Mohammadshakib Naghshbandy
Leila Rezaei
Saba Mehrandish
Shahla Mirzaeei
Fabrication of Anti-glaucoma Nanofibers as Controlled-Release Inserts for Ophthalmic Delivery of Brimonidine Tartrate: In Vivo Evaluation in Caprine Eye
Advanced Pharmaceutical Bulletin
brimonidine tartrate
caprine
electrospinning
glaucoma
nanofibers
ophthalmic drug delivery
title Fabrication of Anti-glaucoma Nanofibers as Controlled-Release Inserts for Ophthalmic Delivery of Brimonidine Tartrate: In Vivo Evaluation in Caprine Eye
title_full Fabrication of Anti-glaucoma Nanofibers as Controlled-Release Inserts for Ophthalmic Delivery of Brimonidine Tartrate: In Vivo Evaluation in Caprine Eye
title_fullStr Fabrication of Anti-glaucoma Nanofibers as Controlled-Release Inserts for Ophthalmic Delivery of Brimonidine Tartrate: In Vivo Evaluation in Caprine Eye
title_full_unstemmed Fabrication of Anti-glaucoma Nanofibers as Controlled-Release Inserts for Ophthalmic Delivery of Brimonidine Tartrate: In Vivo Evaluation in Caprine Eye
title_short Fabrication of Anti-glaucoma Nanofibers as Controlled-Release Inserts for Ophthalmic Delivery of Brimonidine Tartrate: In Vivo Evaluation in Caprine Eye
title_sort fabrication of anti glaucoma nanofibers as controlled release inserts for ophthalmic delivery of brimonidine tartrate in vivo evaluation in caprine eye
topic brimonidine tartrate
caprine
electrospinning
glaucoma
nanofibers
ophthalmic drug delivery
url https://apb.tbzmed.ac.ir/PDF/apb-14-378.pdf
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