Construction and formulation optimization of prothioconazole nanoemulsions for the control of Fusarium graminearum: Enhancing activity and reducing toxicity

Pesticides are widely used in crop production as an important tool to improve economic efficiency in the agricultural field [1], [2], [3]. Due to the poor water solubility of most pesticides, which greatly limits their application in production [4], [5], [6], [7], various pesticide formulations, such as emulsifiable concentrates and microemulsions, have been developed to address these disadvantages. However, these traditional pesticide formulations contain a large number of volatile organic compounds, are prone to highly toxic pesticide misuse and other problems [8], [9], [10]. Therefore, new safe, environmentally friendly and efficient pesticide formulations need to be promoted to meet the current challenges while ensuring the safety and efficiency of agricultural production.

Currently, nanoemulsions (NEs) have received special attention and wide application in the development of efficient drug delivery systems and food preservation due to their excellent properties, such as monodispersity, high thermodynamic stability and low viscosity [11], [12]. In addition, many studies have reported the application of NEs to prepare pesticide formulations with low toxicity, environmental friendliness and storage stability to reduce their cost while improving pesticide safety [13], [14], [15]. Most researches have used a single-factor approach to screen formulations of NEs, but this approach cannot integrate multiple factors to study their effects on formulation stability, which may lead to large errors in experimental results. Many studies have been conducted using Boxsingle bondBehnken design (BBD) to investigate the effect of multiple factors on the response values of NEs for screening to obtain their optimal formulations [16]. Therefore, the use of BBD for the preparation low toxicity and high efficiency NEs is necessary to achieve sustainable development and food safety in the field of crop production [17].

As a broad-spectrum triazole fungicide, prothioconazole (Prot) is mainly used to control various diseases of cereals and beans [18], [19], [20]. Notably, as a chiral pesticide, its metabolite prothioconazole-desthio has a higher toxicity to nontarget organisms [21], [22], [23], only internationally registered suspension concentrates, emulsifiable concentrates and oil dispersion, but these formulations have defects such as easy precipitation of particles and poor dispersion [24], [25], [26]. Therefore, it is of great theoretical significance and practical application to develop a new environmentally friendly prothioconazole nanoemulsion ([email protected]) formulation based on the physicochemical properties of Prot, which can improve pesticide activity and penetration while overcoming the shortcomings of existing formulations.

In this study, [email protected] was prepared by a low-energy emulsification process. The appropriate emulsifier was selected by characterization methods such as appearance observation, mean droplet size determination and microscopic observation, and the optimal formulation [email protected] was investigated by Boxsingle bondBehnken design (BBD) with emulsifier concentration, emulsification time and solvent content as factors and mean droplet size as the response value. In addition, the antifungal activity of NEs against Fusarium graminearum and the biosafety of NEs on zebrafish and BEAS-2B cells were evaluated. This study provides a low-toxicity, efficient, safe, eco-friendly and sustainable strategy for the effective control of fungal diseases of wheat.

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