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Volume 13
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10.3390/pharmaceutics13060889
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Review

Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

by
Kaijie Qian
1,
Lorenzo Stella
2,3,
David S. Jones
1,
Gavin P. Andrews
1,4,
Huachuan Du
5,6,* and
Yiwei Tian
1,*
1
Pharmaceutical Engineering Group, School of Pharmacy, Queen’s University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UK
2
Atomistic Simulation Centre, School of Mathematics and Physics, Queen’s University Belfast, 7–9 College Park E, Belfast BT7 1PS, UK
3
David Keir Building, School of Chemistry and Chemical Engineering, Queen’s University Belfast, Stranmillis Road, Belfast BT9 5AG, UK
4
School of Pharmacy, China Medical University, No.77 Puhe Road, Shenyang North New Area, Shenyang 110122, China
5
Laboratory of Applied Mechanobiology, Department of Health Sciences and Technology, ETH Zurich, Vladimir-Prelog-Weg 4, 8093 Zurich, Switzerland
6
Simpson Querrey Institute, Northwestern University, 303 East Superior Street, 11th Floor, Chicago, IL 60611, USA
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2021, 13(6), 889; https://doi.org/10.3390/pharmaceutics13060889
Submission received: 20 May 2021 / Revised: 8 June 2021 / Accepted: 10 June 2021 / Published: 15 June 2021
(This article belongs to the Special Issue Solid Dispersions for Drug Delivery: Applications and Preparation Methods)
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Abstract

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.
Keywords: amorphous solid dispersion; drug-rich phase; liquid-liquid phase separation; permeability enhancement; bioavailability enhancement amorphous solid dispersion; drug-rich phase; liquid-liquid phase separation; permeability enhancement; bioavailability enhancement
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MDPI and ACS Style

Qian, K.; Stella, L.; Jones, D.S.; Andrews, G.P.; Du, H.; Tian, Y. Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? Pharmaceutics 2021, 13, 889. https://doi.org/10.3390/pharmaceutics13060889

AMA Style

Qian K, Stella L, Jones DS, Andrews GP, Du H, Tian Y. Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? Pharmaceutics. 2021; 13(6):889. https://doi.org/10.3390/pharmaceutics13060889

Chicago/Turabian Style

Qian, Kaijie, Lorenzo Stella, David S. Jones, Gavin P. Andrews, Huachuan Du, and Yiwei Tian. 2021. "Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?" Pharmaceutics 13, no. 6: 889. https://doi.org/10.3390/pharmaceutics13060889

APA Style

Qian, K., Stella, L., Jones, D. S., Andrews, G. P., Du, H., & Tian, Y. (2021). Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery? Pharmaceutics, 13(6), 889. https://doi.org/10.3390/pharmaceutics13060889

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