Revival of an old drug by crystal engineering: development of improved ketoconazole based antifungal products

KET-CRYS

PN-III-P2-2.1-PED- 2016-1521

The goal of the proposed project is to assess the market potential of two co-crystal solid forms of ketoconazole (KET) with fumaric acid (FUM) and p-aminobenzoic acid (PABA) coformers, as APIs with improved properties in terms of solubility / antifungal activity.  The 100-fold increased solubility of KET-FUM compared with commercial KET indicates his pharmaceutical potential for oral drug therapy by reducing the administered dose. On the other hand, KET-PABA with only 10-fold increase solubility, increase antifungal activity and due to its sunscreen coformer has pharmaceutical potential for topical use, especially during summer time. The project results will complete the preliminary preformulation information of KET-FUM and KET-PABA already reported by our research group (protocol for co-crystallization process at small scale – milligrams, solubility and dissolution rate, thermal analysis, FT-IR and antifungal activity for both solid forms and structural characterization of KET-FUM) with common and specific studies/assessment (compatibility with pharmaceutical excipients for KET-FUM – oral therapy; crystal structure characterization for KET-PABA, in vitro and in vivo biocompatibility assessment for both crystalline forms). We will also develop protocol for co-crystallization process at large scale (grams) necessary in pharmaceutical industry for developing a successful industrial co-crystallization process.

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