Multicomponent crystal forms of albendazole for bioavailability improvement
Adegbolagun, M.A.N. Wang, K. Yamaguchi, T. Hamaguchi, T. Yoshida, K. Kawata, S. Harano, A. Han, J. Wang, Z.
Adegbolagun, M.A.N.
Wang, K.
Yamaguchi, T.
Hamaguchi, T.
Yoshida, K.
Kawata, S.
Harano, A.
Han, J.
Wang, Z.
Publication Date
2025-01
End of Embargo
Supervisor
Rights
This document is the Accepted Manuscript version of a Published Work that appeared in final form in Crystal Growth and Design, copyright © 2025 American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://doi.org/10.1021/acs.cgd.4c01208.
Peer-Reviewed
Yes
Open Access status
embargoedAccess
Accepted for publication
2025-01-06
Institution
Department
Awarded
Embargo end date
2026-01-22
Collections
Additional title
Abstract
In this study, a large-scale screening of multicomponent crystal forms of albendazole (ABZ) was carried out, aiming to improve its solubility and dissolution rate for bioavailability improvement. A computational prescreening tool based on the hydrogen bond energy was employed for initial selection of the coformer candidates to shorten the period and number of the experimental investigations, leading to the discovery of eight ABZ multicomponent solids, e.g., 1:1 albendazole-alpha-ketoglutaric acid (ABZ-AKA), 1:1 albendazole - etidronic acid (ABZ-ETA), 1:1 albendazole - (R)-mandelic acid (ABZ-RMA), albendazole - (S)-mandelic acid (1:1 ABZ-SMA), albendazole - citraconic acid (1:1 ABZ-CTA), 1:1 albendazole - mandelic acid (ABZ-MDA), 1:1 albendazole - cyclamic acid (ABZ-CYA), and albendazole - malonic acid (1:1 ABZ-MLA). Although these solids are salt cocrystal adducts based on the ΔpK a rule, they are all salt forms according to the structure analyses and FTIR results. The dissolution study has shown that the cocrystals of both ABZ-ETA and ABZ-CYA significantly improved the ABZ dissolution performance in comparison with the parent drug of ABZ.
Version
Accepted manuscript
Citation
Adegbolagun MAN, Wang K, Yamaguchi T et al (2025) Multicomponent crystal forms of albendazole for bioavailability improvement. Crystal Growth and Design. 25(3): 540-553.
Link to publisher’s version
Link to published version
Link to Version of Record
Type
Article
Qualification name
Notes
The full-text of this article will be released for public view at the end of the publisher embargo on 22 Jan 2026.