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Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies

Poor bioavailability of ophthalmic drops is mainly due to drainage through the nasal-lacrimal duct and a very low permeability through corneal epithelium. The aim of our study was to prepare and characterize an ocular hydrogel of loratadine, as an example of a lipophilic drug, to increase drug conce...

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Autores principales: Sharif Makhmalzadeh, Behzad, Salimi, Anayatollah, Niroomand, Aida
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5985164/
https://www.ncbi.nlm.nih.gov/pubmed/29881404
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author Sharif Makhmalzadeh, Behzad
Salimi, Anayatollah
Niroomand, Aida
author_facet Sharif Makhmalzadeh, Behzad
Salimi, Anayatollah
Niroomand, Aida
author_sort Sharif Makhmalzadeh, Behzad
collection PubMed
description Poor bioavailability of ophthalmic drops is mainly due to drainage through the nasal-lacrimal duct and a very low permeability through corneal epithelium. The aim of our study was to prepare and characterize an ocular hydrogel of loratadine, as an example of a lipophilic drug, to increase drug concentration and residence time at the site of action in the eye. In this study, a 2(3 )full factorial design was employed to design and compare the properties of eight different loratadine containing hydrogel formulations. Results showed a significant correlation between the swelling and porosity ratios of the hydrogels and the Pluronic percentage and Pluronic/carbomer ratio in the formulations. Moreover, the release profiles showed fast and sustained release of all the formulations. Evaluation of hydrogels structure by the FT-IR technique indicated that Pluronic interacts with hydroxyl and carboxylic groups in carbomer, which is the main reason of the hydrogel network formation and interacts with loratadine.The permeation of loratadine through rabbit cornea showed that drug permeation percentages for the F2 and F7 formulations were 15 and 70 folds more than that of the control.
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spelling pubmed-59851642018-06-07 Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies Sharif Makhmalzadeh, Behzad Salimi, Anayatollah Niroomand, Aida Iran J Pharm Res Original Article Poor bioavailability of ophthalmic drops is mainly due to drainage through the nasal-lacrimal duct and a very low permeability through corneal epithelium. The aim of our study was to prepare and characterize an ocular hydrogel of loratadine, as an example of a lipophilic drug, to increase drug concentration and residence time at the site of action in the eye. In this study, a 2(3 )full factorial design was employed to design and compare the properties of eight different loratadine containing hydrogel formulations. Results showed a significant correlation between the swelling and porosity ratios of the hydrogels and the Pluronic percentage and Pluronic/carbomer ratio in the formulations. Moreover, the release profiles showed fast and sustained release of all the formulations. Evaluation of hydrogels structure by the FT-IR technique indicated that Pluronic interacts with hydroxyl and carboxylic groups in carbomer, which is the main reason of the hydrogel network formation and interacts with loratadine.The permeation of loratadine through rabbit cornea showed that drug permeation percentages for the F2 and F7 formulations were 15 and 70 folds more than that of the control. Shaheed Beheshti University of Medical Sciences 2018 /pmc/articles/PMC5985164/ /pubmed/29881404 Text en This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Sharif Makhmalzadeh, Behzad
Salimi, Anayatollah
Niroomand, Aida
Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies
title Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies
title_full Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies
title_fullStr Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies
title_full_unstemmed Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies
title_short Loratadine-Loaded Thermoresponsive Hydrogel: Characterization and Ex-vivo Rabbit Cornea Permeability Studies
title_sort loratadine-loaded thermoresponsive hydrogel: characterization and ex-vivo rabbit cornea permeability studies
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5985164/
https://www.ncbi.nlm.nih.gov/pubmed/29881404
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