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Hydrogel Microparticle‐Templated Anti‐Solvent Crystallization of Small‐Molecule Drugs
Author(s) -
Bora Meghali,
Hsu Myat Noe,
Khan Saif A,
Doyle Patrick S
Publication year - 2022
Publication title -
advanced healthcare materials
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.288
H-Index - 90
eISSN - 2192-2659
pISSN - 2192-2640
DOI - 10.1002/adhm.202102252
Subject(s) - crystallization , materials science , microparticle , nanocrystal , dissolution , nanotechnology , chemical engineering , particle size , excipient , drug delivery , particle (ecology) , nanoparticle , active ingredient , fabrication , solvent , chromatography , chemistry , organic chemistry , bioinformatics , oceanography , geology , engineering , biology , medicine , alternative medicine , pathology
Conventional formulation strategies for hydrophobic small‐molecule drug products frequently include mechanical milling to decrease active pharmaceutical ingredient (API) crystal size and subsequent granulation processes to produce an easily handled powder. A hydrogel‐templated anti‐solvent crystallization method is presented for the facile fabrication of microparticles containing dispersed nanocrystals of poorly soluble API. Direct crystallization within a porous hydrogel particle template yields core–shell structures in which the hydrogel core containing API nanocrystals is encased by a crystalline API shell. The process of controllable loading (up to 64% w/w) is demonstrated, and tailored dissolution profiles are achieved by simply altering the template particle size. API release is well described by a shrinking core model. Overall, the approach is a simple, scalable and potentially generalizable method that enables novel means of independently controlling both API crystallization and excipient characteristics, offering a “designer” drug particle system.