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Experimental and theoretical solubility advantage screening of bi-component solid curcumin formulations

Abstract

A comprehensive experimental and theoretical screening was performed for identification of curcumin solubilizers. Experimental data led to formulation of a non-linear QSPR model correlating molecular descriptors with measured solubilities. The majority of synthesized binary systems exhibited a moderate enhancement of curcumin solubility, which was found to be the highest in the case of curcumin cocrystallized with pyrogallol. New excipients for curcumin were found by utilization of the model within its applicability domain. It appears that a five-fold rise of curcumin solubility is the upper limit for this kind of formulations what was inferred from the screened 230 thousand compounds. Finally, theoretical analysis was extended on naturally occurring curcumin analogues, including demethoxycurcumin, bisdemethoxycurcumin, α-, β- and Ar-turmerones. In all cases, a list of coformers suitable for binary solids preparation with potential enhanced solubility was obtained. They can be treated as first choice lists for further experimental exploration of solubility enhancement of curcumin and its analogues.

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Authors (5)

  • Photo of  Łukasz Recki

    Łukasz Recki

  • Photo of  Karina Mroczyńska

    Karina Mroczyńska

  • Photo of  Tomasz Jeliński

    Tomasz Jeliński

  • Photo of  Piotr Cysewski

    Piotr Cysewski

Details

Category:
Magazine publication
Type:
Magazine publication
Published in:
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY no. 50, pages 125 - 135,
ISSN: 1773-2247
Publication year:
2019
DOI:
Digital Object Identifier (open in new tab) 10.1016/j.jddst.2019.01.023
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