Polymer templated structural evolution of a poorly water-soluble active pharmaceutical ingredient from nanoparticles to hierarchical crystal

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Polymer templated structural evolution of a poorly water-soluble active pharmaceutical ingredient from nanoparticles to hierarchical crystal
Title:
Polymer templated structural evolution of a poorly water-soluble active pharmaceutical ingredient from nanoparticles to hierarchical crystal
Journal Title:
Crystal Growth & Design
Keywords:
Publication Date:
09 April 2018
Citation:
Sheng, F.; Chow, P. S.; Dong, Y. C.; Tan, R. B. H., Polymer templated structural evolution of a poorly water-soluble active pharmaceutical ingredient from nanoparticles to hierarchical crystals. Crystal Growth & Design 2018, 18 (5), 3089-3098.
Abstract:
The hydrate form of a poorly water-soluble active pharmaceutical ingredient (API), spironolactone (SP), was produced using antisolvent precipitation in the presence/absence of polymer templates and stirring. Different crystal habits were observed depending on the polymer added. Superstructures consisting of primary constituent units were obtained in the presence of hydroxypropyl methylcellulose (HPMC), while tubular crystals with highly fused surfaces were observed in the presence of polyvinylpyrrolidone (PVP). In contrast, tubular and dendritic crystals were obtained in the absence of polymer. The structural evolution of the particle formation process was monitored by scanning electron microscopy (SEM), which reveals the growth mechanisms leading to different crystal habits. Superstructures are attributed to self-assembly growth, while tubular and dendritic crystals are formed under diffusion limited growth. The results suggest a potential way to produce crystals with the desired crystal habit by appropriate selection of polymer additive and precipitation conditions.
License type:
PublisherCopyrights
Funding Info:
This work was supported by project grant ICES/16-22KA01 from A*STAR (Agency for Science, Technology, and Research) of Singapore.
Description:
This document is the Accepted Manuscript version of a Published Work that appeared in final form in Crystal Growth & Design, copyright © 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.8b00233.
ISSN:
1528-7483
1528-7505
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