Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?
Among many methods to mitigate the solubility limitations of drug compounds, amorphous solid dispersion (ASD) is considered to be one of the most promising strategies to enhance the dissolution and bioavailability of poorly water-soluble drugs. The enhancement of ASD in the oral absorption of drugs...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-06-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/6/889 |
| _version_ | 1797530065746001920 |
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| author | Kaijie Qian Lorenzo Stella David S. Jones Gavin P. Andrews Huachuan Du Yiwei Tian |
| author_facet | Kaijie Qian Lorenzo Stella David S. Jones Gavin P. Andrews Huachuan Du Yiwei Tian |
| author_sort | Kaijie Qian |
| collection | DOAJ |
| description | Among many methods to mitigate the solubility limitations of drug compounds, amorphous solid dispersion (ASD) is considered to be one of the most promising strategies to enhance the dissolution and bioavailability of poorly water-soluble drugs. The enhancement of ASD in the oral absorption of drugs has been mainly attributed to the high apparent drug solubility during the dissolution. In the last decade, with the implementations of new knowledge and advanced analytical techniques, a drug-rich transient metastable phase was frequently highlighted within the supersaturation stage of the ASD dissolution. The extended drug absorption and bioavailability enhancement may be attributed to the metastability of such drug-rich phases. In this paper, we have reviewed (i) the possible theory behind the formation and stabilization of such metastable drug-rich phases, with a focus on non-classical nucleation; (ii) the additional benefits of the ASD-induced drug-rich phases for bioavailability enhancements. It is envisaged that a greater understanding of the non-classical nucleation theory and its application on the ASD design might accelerate the drug product development process in the future. |
| first_indexed | 2024-03-10T10:22:37Z |
| format | Article |
| id | doaj.art-93ca77855d664805acc33a8eec12abec |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T10:22:37Z |
| publishDate | 2021-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-93ca77855d664805acc33a8eec12abec2023-11-22T00:15:53ZengMDPI AGPharmaceutics1999-49232021-06-0113688910.3390/pharmaceutics13060889Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?Kaijie Qian0Lorenzo Stella1David S. Jones2Gavin P. Andrews3Huachuan Du4Yiwei Tian5Pharmaceutical Engineering Group, School of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKAtomistic Simulation Centre, School of Mathematics and Physics, Queen’s University Belfast, 7–9 College Park E, Belfast BT7 1PS, UKPharmaceutical Engineering Group, School of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKPharmaceutical Engineering Group, School of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKLaboratory of Applied Mechanobiology, Department of Health Sciences and Technology, ETH Zurich, Vladimir-Prelog-Weg 4, 8093 Zurich, SwitzerlandPharmaceutical Engineering Group, School of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UKAmong many methods to mitigate the solubility limitations of drug compounds, amorphous solid dispersion (ASD) is considered to be one of the most promising strategies to enhance the dissolution and bioavailability of poorly water-soluble drugs. The enhancement of ASD in the oral absorption of drugs has been mainly attributed to the high apparent drug solubility during the dissolution. In the last decade, with the implementations of new knowledge and advanced analytical techniques, a drug-rich transient metastable phase was frequently highlighted within the supersaturation stage of the ASD dissolution. The extended drug absorption and bioavailability enhancement may be attributed to the metastability of such drug-rich phases. In this paper, we have reviewed (i) the possible theory behind the formation and stabilization of such metastable drug-rich phases, with a focus on non-classical nucleation; (ii) the additional benefits of the ASD-induced drug-rich phases for bioavailability enhancements. It is envisaged that a greater understanding of the non-classical nucleation theory and its application on the ASD design might accelerate the drug product development process in the future.https://www.mdpi.com/1999-4923/13/6/889amorphous solid dispersiondrug-rich phaseliquid-liquid phase separationpermeability enhancementbioavailability enhancement |
| spellingShingle | Kaijie Qian Lorenzo Stella David S. Jones Gavin P. Andrews Huachuan Du Yiwei Tian Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? Pharmaceutics amorphous solid dispersion drug-rich phase liquid-liquid phase separation permeability enhancement bioavailability enhancement |
| title | Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? |
| title_full | Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? |
| title_fullStr | Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? |
| title_full_unstemmed | Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? |
| title_short | Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? |
| title_sort | drug rich phases induced by amorphous solid dispersion arbitrary or intentional goal in oral drug delivery |
| topic | amorphous solid dispersion drug-rich phase liquid-liquid phase separation permeability enhancement bioavailability enhancement |
| url | https://www.mdpi.com/1999-4923/13/6/889 |
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