Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone

The aim of this study was to improve the solubility of amiodarone hydrochloride (AMD) and the drug release using its inclusion complexes with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were prepared by coprecipitation and freeze-drying. The solubility enhancement of AMD/HP-β-C...

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Main Authors: Andreea Creteanu, Daniela Pamfil, Cornelia Vasile, Gladiola Tantaru, Cristina Mihaela Ghiciuc, Lacramioara Ochiuz, Alina Ghilan, Ana Maria Macsim
Format: Article
Language:English
Published: Wiley 2019-01-01
Series:International Journal of Polymer Science
Online Access:http://dx.doi.org/10.1155/2019/1695189
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author Andreea Creteanu
Daniela Pamfil
Cornelia Vasile
Gladiola Tantaru
Cristina Mihaela Ghiciuc
Lacramioara Ochiuz
Alina Ghilan
Ana Maria Macsim
author_facet Andreea Creteanu
Daniela Pamfil
Cornelia Vasile
Gladiola Tantaru
Cristina Mihaela Ghiciuc
Lacramioara Ochiuz
Alina Ghilan
Ana Maria Macsim
author_sort Andreea Creteanu
collection DOAJ
description The aim of this study was to improve the solubility of amiodarone hydrochloride (AMD) and the drug release using its inclusion complexes with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were prepared by coprecipitation and freeze-drying. The solubility enhancement of AMD/HP-β-CD inclusion complexes by 4–22 times was evaluated by the phase solubility method. The inclusion complexes were studied both in solution and in solid state by spectroscopic methods, dynamic light scattering (DLS) and zeta potential analysis, SEM, and DSC. The formulations of AMD/HP-β-CD inclusion complexes both as powdered form and as matrix tablets showed superior pharmacokinetic performance in improving loading and release properties in respect of those of the insoluble AMD drug. In vitro kinetic study reveals a complex mechanism of release occurring in three steps: the first one being attributed to a burst effect and the other two to different bonding existing in inclusion complexes. An in vivo test on matrix tablets containing Kollidon® and chitosan also reveals a multiple (at least two) peaks release diagram because of both structures of the inclusion complexes and also of different sites of absorption in biological media (digestive tract).
format Article
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institution Kabale University
issn 1687-9422
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language English
publishDate 2019-01-01
publisher Wiley
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series International Journal of Polymer Science
spelling doaj-art-023918af4b63465dbb13ab91a84a8c042025-02-03T01:28:37ZengWileyInternational Journal of Polymer Science1687-94221687-94302019-01-01201910.1155/2019/16951891695189Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of AmiodaroneAndreea Creteanu0Daniela Pamfil1Cornelia Vasile2Gladiola Tantaru3Cristina Mihaela Ghiciuc4Lacramioara Ochiuz5Alina Ghilan6Ana Maria Macsim7Department of Pharmaceutical Technology, Faculty of Pharmacy, “Grigore T. Popa” University of Medicine and Pharmacy of Iasi, 16, Universitatii Str., 700115 Iasi, RomaniaPhysical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, RomaniaPhysical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, RomaniaDepartment of Analytical Chemistry, Faculty of Pharmacy, “Grigore T. Popa” University of Medicine and Pharmacy, 16, University Str., 700115 Iasi, RomaniaDepartment of Pharmacology, Faculty of Medicine, “Grigore T. Popa” University of Medicine and Pharmacy, 16, University Str., 700115 Iasi, RomaniaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, “Grigore T. Popa” University of Medicine and Pharmacy of Iasi, 16, Universitatii Str., 700115 Iasi, RomaniaPhysical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, RomaniaPhysical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, RomaniaThe aim of this study was to improve the solubility of amiodarone hydrochloride (AMD) and the drug release using its inclusion complexes with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were prepared by coprecipitation and freeze-drying. The solubility enhancement of AMD/HP-β-CD inclusion complexes by 4–22 times was evaluated by the phase solubility method. The inclusion complexes were studied both in solution and in solid state by spectroscopic methods, dynamic light scattering (DLS) and zeta potential analysis, SEM, and DSC. The formulations of AMD/HP-β-CD inclusion complexes both as powdered form and as matrix tablets showed superior pharmacokinetic performance in improving loading and release properties in respect of those of the insoluble AMD drug. In vitro kinetic study reveals a complex mechanism of release occurring in three steps: the first one being attributed to a burst effect and the other two to different bonding existing in inclusion complexes. An in vivo test on matrix tablets containing Kollidon® and chitosan also reveals a multiple (at least two) peaks release diagram because of both structures of the inclusion complexes and also of different sites of absorption in biological media (digestive tract).http://dx.doi.org/10.1155/2019/1695189
spellingShingle Andreea Creteanu
Daniela Pamfil
Cornelia Vasile
Gladiola Tantaru
Cristina Mihaela Ghiciuc
Lacramioara Ochiuz
Alina Ghilan
Ana Maria Macsim
Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone
International Journal of Polymer Science
title Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone
title_full Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone
title_fullStr Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone
title_full_unstemmed Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone
title_short Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone
title_sort study on the role of the inclusion complexes with 2 hydroxypropyl β cyclodextrin for oral administration of amiodarone
url http://dx.doi.org/10.1155/2019/1695189
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