Mapp, L. K.; Coles, S.; Aitipamula, S., Novel solid forms of lonidamine : crystal structures and physicochemical properties. CrystEngComm 2017, 19 (21), 2925-2935.
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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Funding Info:
This work was funded by the Science and Engineering Research Council of A*STAR. Lucy Mapp would like to thank A*STAR for funding under the A*STAR Research Attachment Programme (ARAP) jointly with the University of Southampton.