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Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone

In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the preparation of SMTs, the cogrinding technique and freez...

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Autores principales: Kim, Hyeongmin, Lee, Chung-Lyol, Lee, Seohyun, Lee, Tae Jin, Haleem, Iqra, Lee, Younghong, Hwang, Na Jung, Shim, Kyusun, Kim, Dohyun, Lee, Jaehwi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6630442/
https://www.ncbi.nlm.nih.gov/pubmed/31185692
http://dx.doi.org/10.3390/pharmaceutics11060271
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author Kim, Hyeongmin
Lee, Chung-Lyol
Lee, Seohyun
Lee, Tae Jin
Haleem, Iqra
Lee, Younghong
Hwang, Na Jung
Shim, Kyusun
Kim, Dohyun
Lee, Jaehwi
author_facet Kim, Hyeongmin
Lee, Chung-Lyol
Lee, Seohyun
Lee, Tae Jin
Haleem, Iqra
Lee, Younghong
Hwang, Na Jung
Shim, Kyusun
Kim, Dohyun
Lee, Jaehwi
author_sort Kim, Hyeongmin
collection PubMed
description In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the preparation of SMTs, the cogrinding technique and freeze–thaw method were used to disperse β-lapachone in SMTs in an amorphous state and to enhance the swelling and mechanical properties of SMTs, respectively. As a result, the crystallinity of coground β-lapachone incorporated in the SMTs was found to be considerably decreased; thereby, the dissolution rates of the drug in a simulated gastric fluid could be substantially increased. The SMTs of β-lapachone also demonstrated significantly enhanced swelling and mechanical properties compared to those of a marketed product. The reason for this might be because the physically crosslinked polymeric networks with a porous structure that were formed in SMTs through the freeze–thaw method. In addition, β-lapachone was gradually released from the SMTs in 6 h. Therefore, SMTs of β-lapachone developed in this study could be used as GRDDS with appropriate swelling and mechanical properties for improving the dissolution behavior of hydrophobic drugs such as β-lapachone.
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spelling pubmed-66304422019-08-19 Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone Kim, Hyeongmin Lee, Chung-Lyol Lee, Seohyun Lee, Tae Jin Haleem, Iqra Lee, Younghong Hwang, Na Jung Shim, Kyusun Kim, Dohyun Lee, Jaehwi Pharmaceutics Article In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the preparation of SMTs, the cogrinding technique and freeze–thaw method were used to disperse β-lapachone in SMTs in an amorphous state and to enhance the swelling and mechanical properties of SMTs, respectively. As a result, the crystallinity of coground β-lapachone incorporated in the SMTs was found to be considerably decreased; thereby, the dissolution rates of the drug in a simulated gastric fluid could be substantially increased. The SMTs of β-lapachone also demonstrated significantly enhanced swelling and mechanical properties compared to those of a marketed product. The reason for this might be because the physically crosslinked polymeric networks with a porous structure that were formed in SMTs through the freeze–thaw method. In addition, β-lapachone was gradually released from the SMTs in 6 h. Therefore, SMTs of β-lapachone developed in this study could be used as GRDDS with appropriate swelling and mechanical properties for improving the dissolution behavior of hydrophobic drugs such as β-lapachone. MDPI 2019-06-10 /pmc/articles/PMC6630442/ /pubmed/31185692 http://dx.doi.org/10.3390/pharmaceutics11060271 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
Kim, Hyeongmin
Lee, Chung-Lyol
Lee, Seohyun
Lee, Tae Jin
Haleem, Iqra
Lee, Younghong
Hwang, Na Jung
Shim, Kyusun
Kim, Dohyun
Lee, Jaehwi
Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone
title Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone
title_full Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone
title_fullStr Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone
title_full_unstemmed Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone
title_short Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone
title_sort mechanically robust gastroretentive drug-delivery systems capable of controlling dissolution behaviors of coground β-lapachone
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6630442/
https://www.ncbi.nlm.nih.gov/pubmed/31185692
http://dx.doi.org/10.3390/pharmaceutics11060271
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