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Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion

The aim of this study was to improve the physicochemical properties of cocoa extract (CE) using hot-melt extrusion (HME) for pharmaceutical proposes. A mixture design was applied using three distinct hydrophilic polymeric matrices (Soluplus, Plasdone S630, and Eudragit E). Systems obtained by HME we...

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Autores principales: Pinho, Ludmila A. G., Souza, Saulo G., Marreto, Ricardo N., Sa-Barreto, Livia L., Gratieri, Tais, Gelfuso, Guilherme M., Cunha-Filho, Marcilio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6160995/
https://www.ncbi.nlm.nih.gov/pubmed/30134594
http://dx.doi.org/10.3390/pharmaceutics10030135
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author Pinho, Ludmila A. G.
Souza, Saulo G.
Marreto, Ricardo N.
Sa-Barreto, Livia L.
Gratieri, Tais
Gelfuso, Guilherme M.
Cunha-Filho, Marcilio
author_facet Pinho, Ludmila A. G.
Souza, Saulo G.
Marreto, Ricardo N.
Sa-Barreto, Livia L.
Gratieri, Tais
Gelfuso, Guilherme M.
Cunha-Filho, Marcilio
author_sort Pinho, Ludmila A. G.
collection PubMed
description The aim of this study was to improve the physicochemical properties of cocoa extract (CE) using hot-melt extrusion (HME) for pharmaceutical proposes. A mixture design was applied using three distinct hydrophilic polymeric matrices (Soluplus, Plasdone S630, and Eudragit E). Systems obtained by HME were evaluated using morphologic, chromatographic, thermic, spectroscopic, and diffractometric assays. The flow, wettability, and dissolution rate of HME powders were also assessed. Both CE and its marker theobromine proved to be stable under heating according to thermal analysis and Arrhenius plot under isothermal conditions. Physicochemical analysis confirmed the stability of CE HME preparations and provided evidence of drug–polymer interactions. Improvements in the functional characteristics of CE were observed after the extrusion process, particularly in dissolution and flow properties. In addition, the use of a mixture design allowed the identification of synergic effects by excipient combination. The optimized combination of polymers obtained considering four different aspects showed that a mixture of the Soluplus, Plasdone S630, and Eudragit E in equal proportions produced the best results (flowability index 88%; contact angle 47°; dispersibility 7.5%; and dissolution efficiency 87%), therefore making the pharmaceutical use of CE more feasible.
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spelling pubmed-61609952018-10-01 Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion Pinho, Ludmila A. G. Souza, Saulo G. Marreto, Ricardo N. Sa-Barreto, Livia L. Gratieri, Tais Gelfuso, Guilherme M. Cunha-Filho, Marcilio Pharmaceutics Article The aim of this study was to improve the physicochemical properties of cocoa extract (CE) using hot-melt extrusion (HME) for pharmaceutical proposes. A mixture design was applied using three distinct hydrophilic polymeric matrices (Soluplus, Plasdone S630, and Eudragit E). Systems obtained by HME were evaluated using morphologic, chromatographic, thermic, spectroscopic, and diffractometric assays. The flow, wettability, and dissolution rate of HME powders were also assessed. Both CE and its marker theobromine proved to be stable under heating according to thermal analysis and Arrhenius plot under isothermal conditions. Physicochemical analysis confirmed the stability of CE HME preparations and provided evidence of drug–polymer interactions. Improvements in the functional characteristics of CE were observed after the extrusion process, particularly in dissolution and flow properties. In addition, the use of a mixture design allowed the identification of synergic effects by excipient combination. The optimized combination of polymers obtained considering four different aspects showed that a mixture of the Soluplus, Plasdone S630, and Eudragit E in equal proportions produced the best results (flowability index 88%; contact angle 47°; dispersibility 7.5%; and dissolution efficiency 87%), therefore making the pharmaceutical use of CE more feasible. MDPI 2018-08-21 /pmc/articles/PMC6160995/ /pubmed/30134594 http://dx.doi.org/10.3390/pharmaceutics10030135 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
Pinho, Ludmila A. G.
Souza, Saulo G.
Marreto, Ricardo N.
Sa-Barreto, Livia L.
Gratieri, Tais
Gelfuso, Guilherme M.
Cunha-Filho, Marcilio
Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion
title Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion
title_full Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion
title_fullStr Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion
title_full_unstemmed Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion
title_short Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion
title_sort dissolution enhancement in cocoa extract, combining hydrophilic polymers through hot-melt extrusion
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6160995/
https://www.ncbi.nlm.nih.gov/pubmed/30134594
http://dx.doi.org/10.3390/pharmaceutics10030135
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