TY - JOUR
T1 - Solid-state and particle size control of pharmaceutical cocrystals using atomization-based techniques
AU - O'Sullivan, Aaron
AU - Long, Barry
AU - Verma, Vivek
AU - Ryan, Kevin M.
AU - Padrela, Luis
N1 - Publisher Copyright:
© 2022 The Authors
PY - 2022/6/10
Y1 - 2022/6/10
N2 - 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.
AB - 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.
KW - Antisolvent
KW - Multicomponent systems
KW - Nanoparticles
KW - Precipitation
KW - Regulatory
KW - Spray drying
KW - Supercritical fluids
UR - http://www.scopus.com/inward/record.url?scp=85129835375&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2022.121798
DO - 10.1016/j.ijpharm.2022.121798
M3 - Review article
C2 - 35525471
AN - SCOPUS:85129835375
SN - 0378-5173
VL - 621
SP - 121798
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
M1 - 121798
ER -