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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| Format: | Article |
| Language: | English |
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MDPI AG
2018-08-01
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| Series: | Pharmaceutics |
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| Online Access: | http://www.mdpi.com/1999-4923/10/3/135 |
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| author | Ludmila A. G. Pinho Saulo G. Souza Ricardo N. Marreto Livia L. Sa-Barreto Tais Gratieri Guilherme M. Gelfuso Marcilio Cunha-Filho |
| author_facet | Ludmila A. G. Pinho Saulo G. Souza Ricardo N. Marreto Livia L. Sa-Barreto Tais Gratieri Guilherme M. Gelfuso Marcilio Cunha-Filho |
| author_sort | Ludmila A. G. Pinho |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-04-11T21:52:42Z |
| format | Article |
| id | doaj.art-f39a0148bcf446a8ab41a56d000c9b1b |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-11T21:52:42Z |
| publishDate | 2018-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-f39a0148bcf446a8ab41a56d000c9b1b2022-12-22T04:01:12ZengMDPI AGPharmaceutics1999-49232018-08-0110313510.3390/pharmaceutics10030135pharmaceutics10030135Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt ExtrusionLudmila A. G. Pinho0Saulo G. Souza1Ricardo N. Marreto2Livia L. Sa-Barreto3Tais Gratieri4Guilherme M. Gelfuso5Marcilio Cunha-Filho6Laboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília (UnB), 70910-900 Brasília, DF, BrazilLaboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília (UnB), 70910-900 Brasília, DF, BrazilSchool of Pharmacy, Federal University of Goiás, 74 605-170 Goiânia, GO, BrazilLaboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília (UnB), 70910-900 Brasília, DF, BrazilLaboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília (UnB), 70910-900 Brasília, DF, BrazilLaboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília (UnB), 70910-900 Brasília, DF, BrazilLaboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasília (UnB), 70910-900 Brasília, DF, BrazilThe 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.http://www.mdpi.com/1999-4923/10/3/135hot-melt extrusioncocoa extractmixture designflowabilitydissolution rate |
| spellingShingle | Ludmila A. G. Pinho Saulo G. Souza Ricardo N. Marreto Livia L. Sa-Barreto Tais Gratieri Guilherme M. Gelfuso Marcilio Cunha-Filho Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion Pharmaceutics hot-melt extrusion cocoa extract mixture design flowability dissolution rate |
| 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 | hot-melt extrusion cocoa extract mixture design flowability dissolution rate |
| url | http://www.mdpi.com/1999-4923/10/3/135 |
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