Microwave-induced in situ amorphization: A new strategy for tackling the stability issue of amorphous solid dispersions

Wei Qiang, Korbinian Löbmann, Colin P. McCoy, Gavin P. Andrews, Min Zhao*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

1 Citation (Scopus)
48 Downloads (Pure)

Abstract

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.

Original languageEnglish
Article number655
Pages (from-to)1-19
JournalPharmaceutics
Volume12
Issue number7
DOIs
Publication statusPublished - 11 Jul 2020

Keywords

  • Amorphous solid dispersions
  • In situ amorphization
  • Microwave irradiation
  • Physical stability
  • Poorly soluble drugs

ASJC Scopus subject areas

  • Pharmaceutical Science

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