Department of Applied Chemistry, Northeast Agricultural University, Harbin, China.
Pest Manag Sci. 2020 Sep;76(9):3264-3272. doi: 10.1002/ps.5885. Epub 2020 May 16.
Thiabendazole (TBZ) is a poorly water-soluble benzimidazole fungicide. However, the water solubility of TBZ can be significantly enhanced by inclusion complexation with cyclodextrins. In this study, a thiabendazole/hydroxypropyl-β-cyclodextrin (TBZ/HPβCD) complex was synthesized and electrospinning was performed to produce a TBZ/HPβCD nanofibrous (TBZ/HPβCD-NF) complex that improved water solubility and antifungal activity.
The formation of TBZ/HPβCD-NF was characterized by Fourier transform infrared spectroscopy, X-ray diffraction and nuclear magnetic resonance. The morphology of TBZ/HPβCD-NF was studied by scanning electron microscopy. A phase solubility experiment showed that HPβCD exerted a great solubilization effect on TBZ, and TBZ/HPβCD-NF had better antifungal activity compared to that of TBZ alone.
In summary, the solid fungicidal nanodispersion prepared in the present study is a new type of formulation that can enhance the water solubility of TBZ. This formulation, which demonstrated potential as a new fast dissolving formulation type with increased efficacy, is expected to be conducive to the sustainable development of agriculture. © 2020 Society of Chemical Industry.
噻菌灵（TBZ）是一种水溶性较差的苯并咪唑类杀菌剂。然而，通过与环糊精形成包合物可以显著提高 TBZ 的水溶性。在本研究中，合成了噻菌灵/羟丙基-β-环糊精（TBZ/HPβCD）复合物，并通过静电纺丝制备了噻菌灵/羟丙基-β-环糊精纳米纤维（TBZ/HPβCD-NF）复合物，提高了水溶性和抗真菌活性。
通过傅里叶变换红外光谱、X 射线衍射和核磁共振对 TBZ/HPβCD-NF 的形成进行了表征。通过扫描电子显微镜研究了 TBZ/HPβCD-NF 的形态。相溶解度实验表明，HPβCD 对 TBZ 有很好的增溶作用，并且 TBZ/HPβCD-NF 的抗真菌活性优于单独的 TBZ。
综上所述，本研究制备的固体杀菌纳米分散体是一种新型制剂，可提高 TBZ 的水溶性。这种制剂有望成为一种新型的快速溶解制剂类型，具有增效作用，有利于农业的可持续发展。© 2020 英国化学学会。
