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Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres

The investigation of the usability of solid insoluble β-cyclodextrin polymers (βCDP) in micro-sized, controlled drug delivery systems has only recently attracted interest. Our aim was to form complexes with poorly soluble active pharmaceutical ingredients (APIs) with two types of βCDP for drug deliv...

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Autores principales: Haimhoffer, Ádám, Vas, Alexandra, Árvai, Gabriella, Fenyvesi, Éva, Jicsinszky, László, Budai, István, Bényei, Attila, Regdon, Géza, Rusznyák, Ágnes, Vasvári, Gábor, Váradi, Judit, Bácskay, Ildikó, Vecsernyés, Miklós, Fenyvesi, Ferenc
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9313285/
https://www.ncbi.nlm.nih.gov/pubmed/35883488
http://dx.doi.org/10.3390/biom12070931
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author Haimhoffer, Ádám
Vas, Alexandra
Árvai, Gabriella
Fenyvesi, Éva
Jicsinszky, László
Budai, István
Bényei, Attila
Regdon, Géza
Rusznyák, Ágnes
Vasvári, Gábor
Váradi, Judit
Bácskay, Ildikó
Vecsernyés, Miklós
Fenyvesi, Ferenc
author_facet Haimhoffer, Ádám
Vas, Alexandra
Árvai, Gabriella
Fenyvesi, Éva
Jicsinszky, László
Budai, István
Bényei, Attila
Regdon, Géza
Rusznyák, Ágnes
Vasvári, Gábor
Váradi, Judit
Bácskay, Ildikó
Vecsernyés, Miklós
Fenyvesi, Ferenc
author_sort Haimhoffer, Ádám
collection PubMed
description The investigation of the usability of solid insoluble β-cyclodextrin polymers (βCDP) in micro-sized, controlled drug delivery systems has only recently attracted interest. Our aim was to form complexes with poorly soluble active pharmaceutical ingredients (APIs) with two types of βCDP for drug delivery applications. Solid insoluble cyclodextrin polymer of irregular shape (βCDPIS) and cyclodextrin microbeads (βCDPB) were used in the experiments. Morphology, surface area, size distribution and swelling capacity of carriers were investigated. We created complexes with two APIs, curcumin and estradiol, and applied powder X-ray diffraction, FTIR and thermal analysis (TGA/DSC) to prove the complexation. Finally, the dissolution, biocompatibility and permeation of APIs on Caco-2 cells were investigated. The size of the beads was larger than 100 µm, their shape was spherical and surfaces were smooth; while the βCDPIS particles were around 4 µm with irregular shape and surface. None of the polymers showed any cytotoxic effect on Caco-2 cells. Both carriers were able to extract curcumin and estradiol from aqueous solutions, and the dissolution test showed prolonged estradiol release. Caco-2 permeability tests were in accordance with the complexation abilities and dissolution of the complexes. This study offers useful data for further pharmaceutical applications of insoluble cyclodextrin polymers.
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spelling pubmed-93132852022-07-26 Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres Haimhoffer, Ádám Vas, Alexandra Árvai, Gabriella Fenyvesi, Éva Jicsinszky, László Budai, István Bényei, Attila Regdon, Géza Rusznyák, Ágnes Vasvári, Gábor Váradi, Judit Bácskay, Ildikó Vecsernyés, Miklós Fenyvesi, Ferenc Biomolecules Article The investigation of the usability of solid insoluble β-cyclodextrin polymers (βCDP) in micro-sized, controlled drug delivery systems has only recently attracted interest. Our aim was to form complexes with poorly soluble active pharmaceutical ingredients (APIs) with two types of βCDP for drug delivery applications. Solid insoluble cyclodextrin polymer of irregular shape (βCDPIS) and cyclodextrin microbeads (βCDPB) were used in the experiments. Morphology, surface area, size distribution and swelling capacity of carriers were investigated. We created complexes with two APIs, curcumin and estradiol, and applied powder X-ray diffraction, FTIR and thermal analysis (TGA/DSC) to prove the complexation. Finally, the dissolution, biocompatibility and permeation of APIs on Caco-2 cells were investigated. The size of the beads was larger than 100 µm, their shape was spherical and surfaces were smooth; while the βCDPIS particles were around 4 µm with irregular shape and surface. None of the polymers showed any cytotoxic effect on Caco-2 cells. Both carriers were able to extract curcumin and estradiol from aqueous solutions, and the dissolution test showed prolonged estradiol release. Caco-2 permeability tests were in accordance with the complexation abilities and dissolution of the complexes. This study offers useful data for further pharmaceutical applications of insoluble cyclodextrin polymers. MDPI 2022-07-02 /pmc/articles/PMC9313285/ /pubmed/35883488 http://dx.doi.org/10.3390/biom12070931 Text en © 2022 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
Haimhoffer, Ádám
Vas, Alexandra
Árvai, Gabriella
Fenyvesi, Éva
Jicsinszky, László
Budai, István
Bényei, Attila
Regdon, Géza
Rusznyák, Ágnes
Vasvári, Gábor
Váradi, Judit
Bácskay, Ildikó
Vecsernyés, Miklós
Fenyvesi, Ferenc
Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres
title Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres
title_full Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres
title_fullStr Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres
title_full_unstemmed Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres
title_short Investigation of the Drug Carrier Properties of Insoluble Cyclodextrin Polymer Microspheres
title_sort investigation of the drug carrier properties of insoluble cyclodextrin polymer microspheres
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9313285/
https://www.ncbi.nlm.nih.gov/pubmed/35883488
http://dx.doi.org/10.3390/biom12070931
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