Cargando…

Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients

Zein is an insoluble, yet swellable, biopolymer that has been extensively studied for its applications in drug delivery. Here, we screened the effect of co-excipients on the swelling and drug release of zein tablets. All throughout the study the behavior of zein was benchmarked against that of hydro...

Descripción completa

Detalles Bibliográficos
Autores principales: Berardi, Alberto, Abdel Rahim, Safwan, Bisharat, Lorina, Cespi, Marco
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836314/
https://www.ncbi.nlm.nih.gov/pubmed/31590273
http://dx.doi.org/10.3390/pharmaceutics11100513
_version_ 1783466878103977984
author Berardi, Alberto
Abdel Rahim, Safwan
Bisharat, Lorina
Cespi, Marco
author_facet Berardi, Alberto
Abdel Rahim, Safwan
Bisharat, Lorina
Cespi, Marco
author_sort Berardi, Alberto
collection PubMed
description Zein is an insoluble, yet swellable, biopolymer that has been extensively studied for its applications in drug delivery. Here, we screened the effect of co-excipients on the swelling and drug release of zein tablets. All throughout the study the behavior of zein was benchmarked against that of hydroxypropyl methylcellulose (HPMC) and ethylcellulose (EC). Tablets containing either zein, HPMC, or EC alone or in combination with co-excipients, namely lactose, dicalcium phosphate (DCP), microcrystalline cellulose (MCC), polyvinylpyrrolidone (PVP), or sodium lauryl sulfate (SLS) were prepared by direct compression. Matrix swelling was studied by taking continuous pictures of the tablets over 20 h, using a USB microscope connected to a PC. The overall size change and the axial and radial expansion of the tablets were automatically extrapolated from the pictures by image analysis. Moreover, drug release from tablets containing ternary mixtures of zein, co-excipients and 10% propranolol HCl was also studied. Results showed that zein matrices swelled rapidly at first, but then a plateau was reached, resulting in an initial rapid drug burst followed by slow drug release. HPMC tablets swelled to a greater extent and more gradually, providing a more constant drug release rate. EC did not practically swell, giving a nearly constant drug release pattern. Among the additives studied, only MCC increased the swelling of zein up to nearly three-fold, and thus suppressed drug burst from zein matrices and provided a nearly constant drug release over the test duration. Overall, the incorporation of co-excipients influenced the swelling behavior of zein to a greater extent compared to that of HPMC and EC, indicating that the molecular interactions of zein and additives are clearly more complex and distinct.
format Online
Article
Text
id pubmed-6836314
institution National Center for Biotechnology Information
language English
publishDate 2019
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-68363142019-11-21 Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients Berardi, Alberto Abdel Rahim, Safwan Bisharat, Lorina Cespi, Marco Pharmaceutics Article Zein is an insoluble, yet swellable, biopolymer that has been extensively studied for its applications in drug delivery. Here, we screened the effect of co-excipients on the swelling and drug release of zein tablets. All throughout the study the behavior of zein was benchmarked against that of hydroxypropyl methylcellulose (HPMC) and ethylcellulose (EC). Tablets containing either zein, HPMC, or EC alone or in combination with co-excipients, namely lactose, dicalcium phosphate (DCP), microcrystalline cellulose (MCC), polyvinylpyrrolidone (PVP), or sodium lauryl sulfate (SLS) were prepared by direct compression. Matrix swelling was studied by taking continuous pictures of the tablets over 20 h, using a USB microscope connected to a PC. The overall size change and the axial and radial expansion of the tablets were automatically extrapolated from the pictures by image analysis. Moreover, drug release from tablets containing ternary mixtures of zein, co-excipients and 10% propranolol HCl was also studied. Results showed that zein matrices swelled rapidly at first, but then a plateau was reached, resulting in an initial rapid drug burst followed by slow drug release. HPMC tablets swelled to a greater extent and more gradually, providing a more constant drug release rate. EC did not practically swell, giving a nearly constant drug release pattern. Among the additives studied, only MCC increased the swelling of zein up to nearly three-fold, and thus suppressed drug burst from zein matrices and provided a nearly constant drug release over the test duration. Overall, the incorporation of co-excipients influenced the swelling behavior of zein to a greater extent compared to that of HPMC and EC, indicating that the molecular interactions of zein and additives are clearly more complex and distinct. MDPI 2019-10-04 /pmc/articles/PMC6836314/ /pubmed/31590273 http://dx.doi.org/10.3390/pharmaceutics11100513 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
Berardi, Alberto
Abdel Rahim, Safwan
Bisharat, Lorina
Cespi, Marco
Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients
title Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients
title_full Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients
title_fullStr Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients
title_full_unstemmed Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients
title_short Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients
title_sort swelling of zein matrix tablets benchmarked against hpmc and ethylcellulose: challenging the matrix performance by the addition of co-excipients
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6836314/
https://www.ncbi.nlm.nih.gov/pubmed/31590273
http://dx.doi.org/10.3390/pharmaceutics11100513
work_keys_str_mv AT berardialberto swellingofzeinmatrixtabletsbenchmarkedagainsthpmcandethylcellulosechallengingthematrixperformancebytheadditionofcoexcipients
AT abdelrahimsafwan swellingofzeinmatrixtabletsbenchmarkedagainsthpmcandethylcellulosechallengingthematrixperformancebytheadditionofcoexcipients
AT bisharatlorina swellingofzeinmatrixtabletsbenchmarkedagainsthpmcandethylcellulosechallengingthematrixperformancebytheadditionofcoexcipients
AT cespimarco swellingofzeinmatrixtabletsbenchmarkedagainsthpmcandethylcellulosechallengingthematrixperformancebytheadditionofcoexcipients