TY - JOUR
T1 - Sorbitol-coated indomethacin and naproxen particles produced by supercritical CO2-assisted spray drying
AU - Méndez Cañellas, Fidel
AU - Geertman, Robert
AU - Tajber, Lidia
AU - Padrela, Luis
N1 - Publisher Copyright:
© 2023 The Authors
PY - 2023/8
Y1 - 2023/8
N2 - Co-spraying active pharmaceutical ingredients (APIs) with excipients is a strategy to create excipient matrices containing API particles to address formulation challenges such as the reconstitution of powders into homogeneous suspensions. In this work, indomethacin and naproxen were co-sprayed with/without sorbitol using supercritical CO2-assisted spray drying (SASD), followed by particle collection in a filter paper, and resuspension in an aqueous excipient solution. SASD yielded particles in the range of 0.4–7.6 µm, naproxen crystalline Form 1 particles in an amorphous sorbitol matrix, and a partially crystalline indomethacin-sorbitol mixture. Most naproxen-sorbitol mixtures successfully constituted homogenous microparticle suspensions where sorbitol matrix dissolved upon contact with water releasing naproxen particles, while indomethacin-sorbitol mixtures were not reconstitutable and not studied further. The API-sorbitol interactions were studied in detail by thermal analysis and COSMO-RS modelling. Overall, the work presented herein provides a better understanding of co-spraying of APIs with excipients for the formulation of reconstitutable dried microparticles.
AB - Co-spraying active pharmaceutical ingredients (APIs) with excipients is a strategy to create excipient matrices containing API particles to address formulation challenges such as the reconstitution of powders into homogeneous suspensions. In this work, indomethacin and naproxen were co-sprayed with/without sorbitol using supercritical CO2-assisted spray drying (SASD), followed by particle collection in a filter paper, and resuspension in an aqueous excipient solution. SASD yielded particles in the range of 0.4–7.6 µm, naproxen crystalline Form 1 particles in an amorphous sorbitol matrix, and a partially crystalline indomethacin-sorbitol mixture. Most naproxen-sorbitol mixtures successfully constituted homogenous microparticle suspensions where sorbitol matrix dissolved upon contact with water releasing naproxen particles, while indomethacin-sorbitol mixtures were not reconstitutable and not studied further. The API-sorbitol interactions were studied in detail by thermal analysis and COSMO-RS modelling. Overall, the work presented herein provides a better understanding of co-spraying of APIs with excipients for the formulation of reconstitutable dried microparticles.
KW - Active pharmaceutical ingredients
KW - Design of experiments
KW - Microparticles
KW - Polymorphism
KW - Supercritical CO
UR - http://www.scopus.com/inward/record.url?scp=85158851912&partnerID=8YFLogxK
U2 - 10.1016/j.supflu.2023.105969
DO - 10.1016/j.supflu.2023.105969
M3 - Article
AN - SCOPUS:85158851912
SN - 0896-8446
VL - 199
SP - -
JO - Journal of Supercritical Fluids
JF - Journal of Supercritical Fluids
M1 - 105969
ER -