Just Accepted – O’Sullivan et al. – Solid-State and Particle Size Control of Pharmaceutical Cocrystals using Atomization-Based Techniques – International Journal of Pharmaceutics, 2022, 621, 121798

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

SSPC Research Centre, Department of Chemical Sciences, Bernal Institute, University of Limerick, Limerick, Ireland

Received 25 January 2022, Revised 28 April 2022, Accepted 29 April 2022, Available online 4 May 2022, Version of Record 10 May 2022.
Link to Paper:

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.