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Development and Characterization of Eudragit(®)-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide

Furosemide, a chloride channel blocker ordinarily used as a high-ceiling or loop diuretic, is practically insoluble in water and dilute acids. Due to its acidic nature, furosemide is mostly absorbed in the stomach and in the upper small intestine. Efforts have focused on the development of sustained...

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Autores principales: Vlachou, Marilena, Kikionis, Stefanos, Siamidi, Angeliki, Kyriakou, Sotiria, Tsotinis, Andrew, Ioannou, Efstathia, Roussis, Vassilios
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6781502/
https://www.ncbi.nlm.nih.gov/pubmed/31533252
http://dx.doi.org/10.3390/pharmaceutics11090480
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author Vlachou, Marilena
Kikionis, Stefanos
Siamidi, Angeliki
Kyriakou, Sotiria
Tsotinis, Andrew
Ioannou, Efstathia
Roussis, Vassilios
author_facet Vlachou, Marilena
Kikionis, Stefanos
Siamidi, Angeliki
Kyriakou, Sotiria
Tsotinis, Andrew
Ioannou, Efstathia
Roussis, Vassilios
author_sort Vlachou, Marilena
collection PubMed
description Furosemide, a chloride channel blocker ordinarily used as a high-ceiling or loop diuretic, is practically insoluble in water and dilute acids. Due to its acidic nature, furosemide is mostly absorbed in the stomach and in the upper small intestine. Efforts have focused on the development of sustained release systems of furosemide in order to improve the effectiveness of the drug, which exhibits poor aqueous solubility and poor permeability. Recently, electrospun nanofibrous drug delivery systems have emerged as promising alternative solid-dosage forms due to their advantages of high porosity, high surface to volume ratio, and high drug-loading efficacy. Herein, a number of nanofibrous mats composed of different types of Eudragit(®) polymers in various concentrations and combinations loaded with furosemide were designed, successfully electrospun, and characterized using SEM, FTIR, DSC, and TGA analyses. The nanofibrous nonwovens were formulated in nanofiber tablets and the release profile of furosemide from them was evaluated at pH 1.2 and 6.8 and compared to that of physical mixture matrix tablets of analogous composition as well as to that of a commercial formulation. It was found that the release of furosemide was compatible with the gastroretentive and slower intestinal release requirements with a well-defined absorption window, while some nanofiber formulations could act as furosemide carriers in emergency situations where a relatively fast onset of its action is required, as in the case of critically ill post-traumatic patients.
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spelling pubmed-67815022019-10-30 Development and Characterization of Eudragit(®)-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide Vlachou, Marilena Kikionis, Stefanos Siamidi, Angeliki Kyriakou, Sotiria Tsotinis, Andrew Ioannou, Efstathia Roussis, Vassilios Pharmaceutics Article Furosemide, a chloride channel blocker ordinarily used as a high-ceiling or loop diuretic, is practically insoluble in water and dilute acids. Due to its acidic nature, furosemide is mostly absorbed in the stomach and in the upper small intestine. Efforts have focused on the development of sustained release systems of furosemide in order to improve the effectiveness of the drug, which exhibits poor aqueous solubility and poor permeability. Recently, electrospun nanofibrous drug delivery systems have emerged as promising alternative solid-dosage forms due to their advantages of high porosity, high surface to volume ratio, and high drug-loading efficacy. Herein, a number of nanofibrous mats composed of different types of Eudragit(®) polymers in various concentrations and combinations loaded with furosemide were designed, successfully electrospun, and characterized using SEM, FTIR, DSC, and TGA analyses. The nanofibrous nonwovens were formulated in nanofiber tablets and the release profile of furosemide from them was evaluated at pH 1.2 and 6.8 and compared to that of physical mixture matrix tablets of analogous composition as well as to that of a commercial formulation. It was found that the release of furosemide was compatible with the gastroretentive and slower intestinal release requirements with a well-defined absorption window, while some nanofiber formulations could act as furosemide carriers in emergency situations where a relatively fast onset of its action is required, as in the case of critically ill post-traumatic patients. MDPI 2019-09-17 /pmc/articles/PMC6781502/ /pubmed/31533252 http://dx.doi.org/10.3390/pharmaceutics11090480 Text en © 2019 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Vlachou, Marilena
Kikionis, Stefanos
Siamidi, Angeliki
Kyriakou, Sotiria
Tsotinis, Andrew
Ioannou, Efstathia
Roussis, Vassilios
Development and Characterization of Eudragit(®)-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide
title Development and Characterization of Eudragit(®)-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide
title_full Development and Characterization of Eudragit(®)-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide
title_fullStr Development and Characterization of Eudragit(®)-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide
title_full_unstemmed Development and Characterization of Eudragit(®)-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide
title_short Development and Characterization of Eudragit(®)-Based Electrospun Nanofibrous Mats and Their Formulation into Nanofiber Tablets for the Modified Release of Furosemide
title_sort development and characterization of eudragit(®)-based electrospun nanofibrous mats and their formulation into nanofiber tablets for the modified release of furosemide
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6781502/
https://www.ncbi.nlm.nih.gov/pubmed/31533252
http://dx.doi.org/10.3390/pharmaceutics11090480
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