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Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement

Crystalline carriers such as dextrose, sucrose, galactose, mannitol, sorbitol, and isomalt have been reported to increase the solubility, and dissolution rates of poorly soluble drugs when employed as carriers in solid dispersions (SDs). However, synthetic polymers dominate the preparation of drugs:...

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Autores principales: Poka, Madan Sai, Milne, Marnus, Wessels, Anita, Aucamp, Marique
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10675835/
https://www.ncbi.nlm.nih.gov/pubmed/38004536
http://dx.doi.org/10.3390/pharmaceutics15112557
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author Poka, Madan Sai
Milne, Marnus
Wessels, Anita
Aucamp, Marique
author_facet Poka, Madan Sai
Milne, Marnus
Wessels, Anita
Aucamp, Marique
author_sort Poka, Madan Sai
collection PubMed
description Crystalline carriers such as dextrose, sucrose, galactose, mannitol, sorbitol, and isomalt have been reported to increase the solubility, and dissolution rates of poorly soluble drugs when employed as carriers in solid dispersions (SDs). However, synthetic polymers dominate the preparation of drugs: excipient SDs have been created in recent years, but these polymer-based SDs exhibit the major drawback of recrystallisation upon storage. Also, the use of high-molecular-weight polymers with increased chain lengths brings forth problems such as increased viscosity and unnecessary bulkiness in the resulting dosage form. An ideal SD carrier should be hydrophilic, non-hygroscopic, have high hydrogen-bonding propensity, have a high glass transition temperature (T(g)), and be safe to use. This review discusses sugars and polyols as suitable carriers for SDs, as they possess several ideal characteristics. Recently, the use of low-molecular-weight excipients has gained much interest in developing SDs. However, there are limited options available for safe, low molecular excipients, which opens the door again for sugars and polyols. The major points of this review focus on the successes and failures of employing sugars and polyols in the preparation of SDs in the past, recent advances, and potential future applications for the solubility enhancement of poorly water-soluble drugs.
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spelling pubmed-106758352023-10-30 Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement Poka, Madan Sai Milne, Marnus Wessels, Anita Aucamp, Marique Pharmaceutics Review Crystalline carriers such as dextrose, sucrose, galactose, mannitol, sorbitol, and isomalt have been reported to increase the solubility, and dissolution rates of poorly soluble drugs when employed as carriers in solid dispersions (SDs). However, synthetic polymers dominate the preparation of drugs: excipient SDs have been created in recent years, but these polymer-based SDs exhibit the major drawback of recrystallisation upon storage. Also, the use of high-molecular-weight polymers with increased chain lengths brings forth problems such as increased viscosity and unnecessary bulkiness in the resulting dosage form. An ideal SD carrier should be hydrophilic, non-hygroscopic, have high hydrogen-bonding propensity, have a high glass transition temperature (T(g)), and be safe to use. This review discusses sugars and polyols as suitable carriers for SDs, as they possess several ideal characteristics. Recently, the use of low-molecular-weight excipients has gained much interest in developing SDs. However, there are limited options available for safe, low molecular excipients, which opens the door again for sugars and polyols. The major points of this review focus on the successes and failures of employing sugars and polyols in the preparation of SDs in the past, recent advances, and potential future applications for the solubility enhancement of poorly water-soluble drugs. MDPI 2023-10-30 /pmc/articles/PMC10675835/ /pubmed/38004536 http://dx.doi.org/10.3390/pharmaceutics15112557 Text en © 2023 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 Review
Poka, Madan Sai
Milne, Marnus
Wessels, Anita
Aucamp, Marique
Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement
title Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement
title_full Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement
title_fullStr Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement
title_full_unstemmed Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement
title_short Sugars and Polyols of Natural Origin as Carriers for Solubility and Dissolution Enhancement
title_sort sugars and polyols of natural origin as carriers for solubility and dissolution enhancement
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10675835/
https://www.ncbi.nlm.nih.gov/pubmed/38004536
http://dx.doi.org/10.3390/pharmaceutics15112557
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