Microwave-Induced In Situ Amorphization: A New Strategy for Tackling the Stability Issue of Amorphous Solid Dispersions

• Published in: Pharmaceutics Vol. 12; no. 7; p. 655
• Main Authors: Qiang, Wei, Löbmann, Korbinian, McCoy, Colin P., Andrews, Gavin P., Zhao, Min
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 11.07.2020; MDPI
• Subjects: amorphous solid dispersions; Crystallization; Drug dosages; Humidity; Hydrogen bonds; in situ amorphization; microwave irradiation; Microwaves; Pharmaceuticals; physical stability; Polymer solubility; poorly soluble drugs; R&D; Research & development; Review
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics12070655

The thermodynamically unstable nature of amorphous drugs has led to a persistent stability issue of amorphous solid dispersions (ASDs). Lately, microwave-induced in situ amorphization has been proposed as a promising solution to this problem, where the originally loaded crystalline drug is in situ amorphized within the final dosage form using a household microwave oven prior to oral administration. In addition to circumventing issues with physical stability, it can also simplify the problematic downstream processing of ASDs. In this review paper, we address the significance of exploring and developing this novel technology with an emphasis on systemically reviewing the currently available literature in this pharmaceutical arena and highlighting the underlying mechanisms involved in inducing in situ amorphization. Specifically, in order to achieve a high drug amorphicity, formulations should be composed of drugs with high solubility in polymers, as well as polymers with high hygroscopicity and good post-plasticized flexibility of chains. Furthermore, high microwave energy input is considered to be a desirable factor. Lastly, this review discusses challenges in the development of this technology including chemical stability, selection criteria for excipients and the dissolution performance of the microwave-induced ASDs.