Cocrystallisation of Daidzein with pyridine-derived molecules: Screening, structure determination and characterisation

Date

2020-07-13

Advisors

Journal Title

Journal ISSN

ISSN

Volume Title

Publisher

Elsevier

Type

Article

Peer reviewed

Yes

Abstract

Daidzein (7,4' -dihydroxyisoflavone, DAI) is an isoflavone found in soybeans and Pueraria. DAI has potential therapeutic benefits on cancer and osteoporosis yet has quite low solubility, limiting its use. Herein a cocrystal screening of DAI with pyridine-derived molecules, i.e., nicotinamide, isonicotinamide, caffeine, d -Proline, l -Proline and 4,4' -Bipyridine was conducted. A new cocrystal of Daidzein and 4,4' -Bipyridine (DAI-BIP) was successfully generated via grinding and solvent methods. DAI-BIP showed an increased solubility and dissolution rate. In comparison to DAI, there was a 2.03-fold increase of the dissolution performance parameter for DAI-BIP where the concentration observed for DAI quickly reached the equi- librium solubility and continued to reach 1.49 times DAI solubility. A parachute effect was also observed during the dissolution of DAI-BIP, indicating that BIP might be able to maintain the supersaturated state of DAI in solution proving DAI’s ability to form cocrystals of higher solubility and enhanced dissolution properties through co-crystallisation

Description

Daidzein has extremely poor water solubility affecting its bioavailability even with high doses. To achieve the therapeutic effects of Daidzein, the aim of this research project is to design multi-component crystal forms of Daidzein cocrystals with improved solubility and dissolution rate to maximize its therapeutic effect. The file attached to this record is the author's final peer reviewed version. The Publisher's final version can be found by following the DOI link.

Keywords

Cocrystal, Daidzein, bipyridine

Citation

Bolus, L., et al. (2020), Cocrystallisation of Daidzein with pyridine-derived molecules: Screening, structure determination and characterisation. Journal of Molecular Structure, 1222, 128893.

Rights

Research Institute

Leicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)