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2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques

It is extremely important for pharmaceutical formulators to have analytical methodology that provides efficient detection and quantification of HPβCD aggregates. Five different methods were then evaluated for their potential to detect these aggregates and to determine critical aggregation concentrat...

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Detalles Bibliográficos
Autores principales: Sá Couto, André Rodrigues, Ryzhakov, Alexey, Loftsson, Thorsteinn
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6212962/
https://www.ncbi.nlm.nih.gov/pubmed/30322145
http://dx.doi.org/10.3390/ma11101971
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author Sá Couto, André Rodrigues
Ryzhakov, Alexey
Loftsson, Thorsteinn
author_facet Sá Couto, André Rodrigues
Ryzhakov, Alexey
Loftsson, Thorsteinn
author_sort Sá Couto, André Rodrigues
collection PubMed
description It is extremely important for pharmaceutical formulators to have analytical methodology that provides efficient detection and quantification of HPβCD aggregates. Five different methods were then evaluated for their potential to detect these aggregates and to determine critical aggregation concentration (cac): osmometry, viscometry, tensiometry, dynamic light scattering (DLS), and permeability studies. Overall, tensiometry was an inadequate method with which to study HPβCD aggregation, since the addition of HPβCD to water resulted in only minor changes in surface tension. Osmolality and viscosity studies have shown that for HPβCD, solute–solvent interactions are the main contributors for the observed deviation from ideality. These deviations might be related to the presence of aggregates. The DLS method proved to be an effective method with which to detect HPβCD aggregates and estimate their hydrodynamic diameter, although it presented some limitations concerning their quantification. In terms of the assessed methods, permeation studies were shown to be the best to study HPβCD aggregation phenomena, since they were the only method where the detection of aggregates and the determination of apparent cac values was possible. Also, it was the least invasive for the HPβCD samples and the method that provided more conclusive data. Results suggested that HPβCD, as expected, has less tendency to form aggregates than βCD.
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spelling pubmed-62129622018-11-14 2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques Sá Couto, André Rodrigues Ryzhakov, Alexey Loftsson, Thorsteinn Materials (Basel) Article It is extremely important for pharmaceutical formulators to have analytical methodology that provides efficient detection and quantification of HPβCD aggregates. Five different methods were then evaluated for their potential to detect these aggregates and to determine critical aggregation concentration (cac): osmometry, viscometry, tensiometry, dynamic light scattering (DLS), and permeability studies. Overall, tensiometry was an inadequate method with which to study HPβCD aggregation, since the addition of HPβCD to water resulted in only minor changes in surface tension. Osmolality and viscosity studies have shown that for HPβCD, solute–solvent interactions are the main contributors for the observed deviation from ideality. These deviations might be related to the presence of aggregates. The DLS method proved to be an effective method with which to detect HPβCD aggregates and estimate their hydrodynamic diameter, although it presented some limitations concerning their quantification. In terms of the assessed methods, permeation studies were shown to be the best to study HPβCD aggregation phenomena, since they were the only method where the detection of aggregates and the determination of apparent cac values was possible. Also, it was the least invasive for the HPβCD samples and the method that provided more conclusive data. Results suggested that HPβCD, as expected, has less tendency to form aggregates than βCD. MDPI 2018-10-13 /pmc/articles/PMC6212962/ /pubmed/30322145 http://dx.doi.org/10.3390/ma11101971 Text en © 2018 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
Sá Couto, André Rodrigues
Ryzhakov, Alexey
Loftsson, Thorsteinn
2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques
title 2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques
title_full 2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques
title_fullStr 2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques
title_full_unstemmed 2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques
title_short 2-Hydroxypropyl-β-Cyclodextrin Aggregates: Identification and Development of Analytical Techniques
title_sort 2-hydroxypropyl-β-cyclodextrin aggregates: identification and development of analytical techniques
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6212962/
https://www.ncbi.nlm.nih.gov/pubmed/30322145
http://dx.doi.org/10.3390/ma11101971
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