An environmentally safe formulation with enhanced solubility and fungicidal activity: Self-assembly and characterization of Difenoconazole-β-CD inclusion complex

Abstract

Since pesticides have the disadvantages of low utilization rate and pollution to the surrounding environment, it is necessary to consider the development of new pesticide formulations. Difenoconazole (DZ), a common fungicide with poor water solubility, needs to be mixed with a large number of additives during use, which results in excessive use of organic solvents and pesticide residues. In this study, inclusion complex of beta-cyclodextrin (β-CD) and DZ was synthesized by ultrasonic method and was then aim to enhance the water solubility and its antifungal activity against Gibberella sp. of DZ. X-ray diffraction (XRD), nuclear magnetic resonance (1H NMR) analysis and molecular modeling techniques were applied to characterized the formation of DZ/β-CD inclusion complex, the DZ:β-CD stoichiometric ratio of the prepared inclusion complex was calculated in accordance with the result of 1H NMR. Increased water solubility of inclusion complex was illustrated by phase solubility studies. The inclusion complex showed a more significant fungicidal effect against Gibberella sp. than original DZ in the fungicidal effect assay. The inclusion complexation of β-CD on DZ was a new pesticide formulation and provided new development ideas for the application of DZ in agriculture.