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Issue 46, 2014
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Improving solubility of fisetin by cocrystallization

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Abstract

Fisetin, a naturally occurring polyphenolic compound, has a proven record of in vitro demonstrated anti-carcinogenic, anti-inflammatory and antiviral properties, yet similarly to many promising APIs, its in vivo administration is complicated by low aqueous solubility and unfavourable pharmacokinetics. The presented study was focused on obtaining and characterizing cocrystals of fisetin, with the aim of improving its solubility. Solvent-drop grinding experiments, combined with FT-Raman and XRPD, were conducted to identify new cocrystalline phases, which were afterwards isolated as single-crystals and characterized structurally and in terms of thermal stability and solubility. Dissolution studies of pure fisetin and four cocrystals, namely fisetin–isonicotinamide 1 : 1 (FisInam), fisetin–nicotinamide 1 : 2 hemiethanolate (FisNam), fisetin–nicotinamide 1 : 1 (FisNam2) and fisetin–caffeine 1 : 2 (FisCaf), showed that a 2.5-fold increase of fisetin solubility was achieved for FisNam and to a smaller extent for FisCaf and FisInam (ca. 1.8- and 1.5-fold, respectively).

Graphical abstract: Improving solubility of fisetin by cocrystallization

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Publication details

The article was received on 19 Aug 2014, accepted on 26 Sep 2014 and first published on 26 Sep 2014


Article type: Paper
DOI: 10.1039/C4CE01713G
CrystEngComm, 2014,16, 10592-10601

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    Improving solubility of fisetin by cocrystallization

    M. Sowa, K. Ślepokura and E. Matczak-Jon, CrystEngComm, 2014, 16, 10592
    DOI: 10.1039/C4CE01713G

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