Novel solid forms of lonidamine: crystal structures and physicochemical properties

Mapp, Lucy K., Coles, Simon J. and Aitipamula, Srinivasulu (2017) Novel solid forms of lonidamine: crystal structures and physicochemical properties. CrystEngComm, 2017 (19), 2925-2935. (doi:10.1039/C7CE00651A).

Record type: Article

Abstract

Lonidamine finds potential applications in cancer treatments, and its current marketed solid form, the sodium salt, displays poor solubility. The presence of a single carboxylic acid group makes it an ideal target for co-crystal design as design strategies involving carboxylic acid groups are well-established. CSD statistics combined with known hydrogen bonding preferences allowed suitable co-former selection which resulted in nine new multicomponent crystals with pharmaceutically acceptable co-formers. These included co-crystals, salts and some hybrid (co-crystal salt) structures. All the solid forms were characterized by X-ray diffraction techniques with subsequent measurement of physicochemical properties, such as stability, solubility, and dissolution rate. It was found that the co-formers were able to modulate the properties of lonidamine.

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Submitted Manuscript_LON_CrystEngComm_postreviewers - Accepted Manuscript

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