Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals
Highly hygroscopic pharmaceutical and nutraceutical solids are prone to significant changes in their physicochemical properties due to chemical degradation and/or solid-state transition, resulting in adverse effects on their therapeutic performances and shelf life. Moisture absorption also leads to...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-09-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/10/2015 |
| _version_ | 1797470409696739328 |
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| author | Liu Han Ng Jordy Kim Ung Ling Kunn Hadinoto |
| author_facet | Liu Han Ng Jordy Kim Ung Ling Kunn Hadinoto |
| author_sort | Liu Han Ng |
| collection | DOAJ |
| description | Highly hygroscopic pharmaceutical and nutraceutical solids are prone to significant changes in their physicochemical properties due to chemical degradation and/or solid-state transition, resulting in adverse effects on their therapeutic performances and shelf life. Moisture absorption also leads to excessive wetting of the solids, causing their difficult handling during manufacturing. In this review, four formulation strategies that have been employed to tackle hygroscopicity issues in oral solid dosage forms of pharmaceuticals/nutraceuticals were discussed. The four strategies are (1) film coating, (2) encapsulation by spray drying or coacervation, (3) co-processing with excipients, and (4) crystal engineering by co-crystallization. Film coating and encapsulation work by acting as barriers between the hygroscopic active ingredients in the core and the environment, whereas co-processing with excipients works mainly by adding excipients that deflect moisture away from the active ingredients. Co-crystallization works by altering the crystal packing arrangements by introducing stabilizing co-formers. For hygroscopic pharmaceuticals, coating and co-crystallization are the most commonly employed strategies, whereas coating and encapsulation are popular for hygroscopic nutraceuticals (e.g., medicinal herbs, protein hydrolysates). Encapsulation is rarely applied on hygroscopic pharmaceuticals, just as co-crystallization is rarely used for hygroscopic nutraceuticals. Therefore, there is potential for improved hygroscopicity reduction by exploring beyond the traditionally used strategy. |
| first_indexed | 2024-03-09T19:35:59Z |
| format | Article |
| id | doaj.art-d9a88b3d0297452bbd08a571a0de8fb5 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T19:35:59Z |
| publishDate | 2022-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-d9a88b3d0297452bbd08a571a0de8fb52023-11-24T01:53:52ZengMDPI AGPharmaceutics1999-49232022-09-011410201510.3390/pharmaceutics14102015Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and NutraceuticalsLiu Han Ng0Jordy Kim Ung Ling1Kunn Hadinoto2School of Chemistry, Chemical Engineering and Biotechnology, Nanyang Technological University, Singapore 637459, SingaporeSchool of Chemistry, Chemical Engineering and Biotechnology, Nanyang Technological University, Singapore 637459, SingaporeSchool of Chemistry, Chemical Engineering and Biotechnology, Nanyang Technological University, Singapore 637459, SingaporeHighly hygroscopic pharmaceutical and nutraceutical solids are prone to significant changes in their physicochemical properties due to chemical degradation and/or solid-state transition, resulting in adverse effects on their therapeutic performances and shelf life. Moisture absorption also leads to excessive wetting of the solids, causing their difficult handling during manufacturing. In this review, four formulation strategies that have been employed to tackle hygroscopicity issues in oral solid dosage forms of pharmaceuticals/nutraceuticals were discussed. The four strategies are (1) film coating, (2) encapsulation by spray drying or coacervation, (3) co-processing with excipients, and (4) crystal engineering by co-crystallization. Film coating and encapsulation work by acting as barriers between the hygroscopic active ingredients in the core and the environment, whereas co-processing with excipients works mainly by adding excipients that deflect moisture away from the active ingredients. Co-crystallization works by altering the crystal packing arrangements by introducing stabilizing co-formers. For hygroscopic pharmaceuticals, coating and co-crystallization are the most commonly employed strategies, whereas coating and encapsulation are popular for hygroscopic nutraceuticals (e.g., medicinal herbs, protein hydrolysates). Encapsulation is rarely applied on hygroscopic pharmaceuticals, just as co-crystallization is rarely used for hygroscopic nutraceuticals. Therefore, there is potential for improved hygroscopicity reduction by exploring beyond the traditionally used strategy.https://www.mdpi.com/1999-4923/14/10/2015hygroscopic pharmaceuticalspharmaceutical coatingnutraceutical encapsulationcocrystalssolid dosage formulation |
| spellingShingle | Liu Han Ng Jordy Kim Ung Ling Kunn Hadinoto Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals Pharmaceutics hygroscopic pharmaceuticals pharmaceutical coating nutraceutical encapsulation cocrystals solid dosage formulation |
| title | Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals |
| title_full | Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals |
| title_fullStr | Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals |
| title_full_unstemmed | Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals |
| title_short | Formulation Strategies to Improve the Stability and Handling of Oral Solid Dosage Forms of Highly Hygroscopic Pharmaceuticals and Nutraceuticals |
| title_sort | formulation strategies to improve the stability and handling of oral solid dosage forms of highly hygroscopic pharmaceuticals and nutraceuticals |
| topic | hygroscopic pharmaceuticals pharmaceutical coating nutraceutical encapsulation cocrystals solid dosage formulation |
| url | https://www.mdpi.com/1999-4923/14/10/2015 |
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