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Preparation and Evaluation of Nanofibrous and Film-Structured Ciprofloxacin Hydrochloride Inserts for Sustained Ocular Delivery: Pharmacokinetic Study in Rabbit’s Eye

Conventional anti-infective eye drops are the most common forms of drugs prescribed for the management of topical ocular infections. Despite their convenience, topical eye drops face multiple challenges, including limited bioavailability and repetitive administration. The present study aimed to prep...

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Autores principales: Taghe, Shiva, Mirzaeei, Shahla, Ahmadi, Arian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10141354/
https://www.ncbi.nlm.nih.gov/pubmed/37109442
http://dx.doi.org/10.3390/life13040913
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author Taghe, Shiva
Mirzaeei, Shahla
Ahmadi, Arian
author_facet Taghe, Shiva
Mirzaeei, Shahla
Ahmadi, Arian
author_sort Taghe, Shiva
collection PubMed
description Conventional anti-infective eye drops are the most common forms of drugs prescribed for the management of topical ocular infections. Despite their convenience, topical eye drops face multiple challenges, including limited bioavailability and repetitive administration. The present study aimed to prepare, evaluate, and compare film-structured and nanofibrous ocular inserts using biocompatible polymers of polyvinyl alcohol (PVA) and polycaprolactone (PCL) to achieve sustained ciprofloxacin Hydrochloride (CIP) delivery. The nanofibrous formulations were prepared by electrospinning and glutaraldehyde crosslinking while the film formulation was prepared by solvent casting. Nanofibrous inserts had mean diameters in the range 330–450 nm. Both film and nanofibrous inserts were strong, although the nanofibers had higher flexibility. In vitro antibacterial efficacy against Staphylococcus aureus and Escherichia coli was observed for all formulations and cell viability of more than 70% confirmed their non-toxicity. In vitro release studies showed prolonged release of 2 days for the film and 5 days for the nanofibers compared with a 10-h release of CIP from the eye drop. Pharmacokinetic studies of rabbits’ eyes showed 4.5–5-folds higher AUC for the nanofiber formulations compared with the eye drop. Thus, prolonged-release film-structured and nanofibrous inserts are suitable carriers for ocular delivery of CIP.
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spelling pubmed-101413542023-04-29 Preparation and Evaluation of Nanofibrous and Film-Structured Ciprofloxacin Hydrochloride Inserts for Sustained Ocular Delivery: Pharmacokinetic Study in Rabbit’s Eye Taghe, Shiva Mirzaeei, Shahla Ahmadi, Arian Life (Basel) Article Conventional anti-infective eye drops are the most common forms of drugs prescribed for the management of topical ocular infections. Despite their convenience, topical eye drops face multiple challenges, including limited bioavailability and repetitive administration. The present study aimed to prepare, evaluate, and compare film-structured and nanofibrous ocular inserts using biocompatible polymers of polyvinyl alcohol (PVA) and polycaprolactone (PCL) to achieve sustained ciprofloxacin Hydrochloride (CIP) delivery. The nanofibrous formulations were prepared by electrospinning and glutaraldehyde crosslinking while the film formulation was prepared by solvent casting. Nanofibrous inserts had mean diameters in the range 330–450 nm. Both film and nanofibrous inserts were strong, although the nanofibers had higher flexibility. In vitro antibacterial efficacy against Staphylococcus aureus and Escherichia coli was observed for all formulations and cell viability of more than 70% confirmed their non-toxicity. In vitro release studies showed prolonged release of 2 days for the film and 5 days for the nanofibers compared with a 10-h release of CIP from the eye drop. Pharmacokinetic studies of rabbits’ eyes showed 4.5–5-folds higher AUC for the nanofiber formulations compared with the eye drop. Thus, prolonged-release film-structured and nanofibrous inserts are suitable carriers for ocular delivery of CIP. MDPI 2023-03-30 /pmc/articles/PMC10141354/ /pubmed/37109442 http://dx.doi.org/10.3390/life13040913 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Taghe, Shiva
Mirzaeei, Shahla
Ahmadi, Arian
Preparation and Evaluation of Nanofibrous and Film-Structured Ciprofloxacin Hydrochloride Inserts for Sustained Ocular Delivery: Pharmacokinetic Study in Rabbit’s Eye
title Preparation and Evaluation of Nanofibrous and Film-Structured Ciprofloxacin Hydrochloride Inserts for Sustained Ocular Delivery: Pharmacokinetic Study in Rabbit’s Eye
title_full Preparation and Evaluation of Nanofibrous and Film-Structured Ciprofloxacin Hydrochloride Inserts for Sustained Ocular Delivery: Pharmacokinetic Study in Rabbit’s Eye
title_fullStr Preparation and Evaluation of Nanofibrous and Film-Structured Ciprofloxacin Hydrochloride Inserts for Sustained Ocular Delivery: Pharmacokinetic Study in Rabbit’s Eye
title_full_unstemmed Preparation and Evaluation of Nanofibrous and Film-Structured Ciprofloxacin Hydrochloride Inserts for Sustained Ocular Delivery: Pharmacokinetic Study in Rabbit’s Eye
title_short Preparation and Evaluation of Nanofibrous and Film-Structured Ciprofloxacin Hydrochloride Inserts for Sustained Ocular Delivery: Pharmacokinetic Study in Rabbit’s Eye
title_sort preparation and evaluation of nanofibrous and film-structured ciprofloxacin hydrochloride inserts for sustained ocular delivery: pharmacokinetic study in rabbit’s eye
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10141354/
https://www.ncbi.nlm.nih.gov/pubmed/37109442
http://dx.doi.org/10.3390/life13040913
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