Solid-state and particle size control of pharmaceutical cocrystals using atomization-based techniques

Aaron O'Sullivan, Barry Long, Vivek Verma, Kevin M. Ryan, Luis Padrela

Research output: Contribution to journalReview articlepeer-review

Abstract

Poor bioavailability and aqueous solubility represent a major constraint during the development of new API molecules and can influence the impact of new medicines or halt their approval to the market. Cocrystals offer a novel and competitive advantage over other conventional methods with respect towards the substantial improvement in solubility profiles relative to the single-API crystals. Furthermore, the production of such cocrystals through atomization-based methods allow for greater control, with respect to particle size reduction, to further increase the solubility of the API. Such atomization-based methods include supercritical fluid methods, conventional spray drying and electrohydrodynamic atomization/electrospraying. The influence of process parameters such as solution flow rates, pressure and solution concentration, in controlling the solid-state and final particle size are discussed in this review with respect to atomization-based methods. For the last decade, literature has been attempting to catch-up with new regulatory rulings regarding the classification of cocrystals, due in part to data sparsity. In recent years, there has been an increase in cocrystal publications, specifically employing atomization-based methods. This review considers the benefits to employing atomization-based methods for the generation of pharmaceutical cocrystals, examines the most recent regulatory changes regarding cocrystals and provides an outlook towards the future of this field.

Original languageEnglish
Article number121798
Pages (from-to)121798
JournalInternational Journal of Pharmaceutics
Volume621
DOIs
Publication statusPublished - 10 Jun 2022

Keywords

  • Antisolvent
  • Multicomponent systems
  • Nanoparticles
  • Precipitation
  • Regulatory
  • Spray drying
  • Supercritical fluids

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