Fecha de publicación:
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Fuente:
PubMed "industrial biotechnology"
J Pharm Sci. 2026 Sep 24:104515. doi: 10.1016/j.xphs.2026.104515. Online ahead of print.ABSTRACTTherapeutic eutectic solvents (TES) represent liquid forms of active pharmaceutical ingredients (APIs) that can circumvent the issues of low aqueous solubility and polymorphism associated with conventional solid crystalline APIs. Due to their viscous liquid nature, TES applications beyond transdermal drug delivery have been rarely explored. The present work aimed to develop oral tablets of TES to facilitate their delivery via oral ingestion, which represents the most commonly used route of drug administration. A poorly soluble API ibuprofen (IBU) paired with menthol (MEN) at 1:3 molar ratio was used as the model TES. Oral tablets of IBU-MEN TES were prepared by a three-step process comprising (1) emulsification, (2) spray immobilization into excipient microparticles, and (3) direct compression. Two immobilization approaches were investigated pre-compression, i.e., (1) spray ionotropic gelation with alginate and (2) spray drying with maltodextrin. Both approaches produced TES-loaded microparticles having similar physical characteristics (e.g., TES content, size, flowability) and immobilization yield, but distinct IBU release profiles due to different dissolution rates between alginate and maltodextrin matrices. The IBU-MEN TES remained in its liquid non-crystalline form upon immobilization and during three months of accelerated storage. Both TES-containing microparticles were successfully transformed into TES tablets exhibiting satisfactory pharmacopeial qualities (i.e., drug content uniformity, weight/thickness variations, friability), albeit different tablet formulations were needed. Importantly, immobilization and tableting did not adversely affect the supersaturation-generation capability of the IBU-MEN TES.PMID:42785635 | DOI:10.1016/j.xphs.2026.104515