高水溶性纳米尺度植物源农药的通用制备策略及性能研究

Botanical pesticides possess many excellent performances compare with chemical pesticides, such as low toxicity, high selectivity, degradable and renewable characteristics, etc. which up to standard of green pesticides. But, most of the botanical pesticides have two problems which are poor water solubility and low pesticide efficacy, limiting their popularization application. The reports show that nanopesticide technology can significantly increase water solubility and pesticide efficacy of pesticides. For this reason, the project will combine solvent exchange method and borate esterification reaction to develop a simple, green and universal strategy for preparing water-soluble nano-botanical pesticides for numerous hydrophobic botanical pesticides containing hydroxy functional groups. The internal relation between botanical pesticides molecule structure, preparation conditions and sizes, solubility of obtained nanopesticides will be researched in detail. Further, modify the surface of the nanopesticides with polyhydric, water-soluble polymers via the borate esterification reaction to enhance the coagulation stability of the nanopesticides in hard water and adsorption stability of the nanopesticides on crop leaf surface. Study the performances of nanopesticides obtained botanical pesticides possess low toxicity, high selectivity, degradable and renewable characteristics compare with chemical pesticides, conform with the standard of green pesticides. But, most of the botanical pesticides have two problems which are poor water solubility and low pesticide efficacy, limiting their popularization application. The reports show that nanopesticide technology can significantly increase water solubility and pesticide efficacy of pesticides. For this reason, the project will combine solvent exchange method and borate esterification reaction to develop a simple, green and universal method for preparing water-soluble nano-botanical pesticides for numerous hydrophobic botanical pesticides containing hydroxy functional groups. The internal relation between botanical pesticides molecule structure, preparation conditions and sizes, solubility of obtained nanopesticides will be researched in detail. Further, modify the surface of the nanopesticides with polyhydric, water-soluble polymers via the borate esterification reaction to enhance the coagulation stability of the nanopesticides in hard water and adsorption stability of the nanopesticides on crop leaf surface. The performances of the nanopesticides obtained including efficacy, wetting performance, adsorption behavior on the leaf, release kinetics, as well as solubility of solid nanopesticides in water will be detailedly studied in detail and explain structure-function relationship also will be explained. The applicants have accumulated rich experience in related fields; the project is successfully finished that is significant for the popularization of botanical pesticides.

相比化学农药，植物源农药具有低毒、易降解、可再生的特性，符合绿色农药标准；然而，多数植物源农药水溶解性小且药效偏低，极大地限制了其普及应用。研究证明纳米农药技术可以大幅提高农药的水溶解性及药效。鉴于此，针对众多含有羟基特征基团的疏水性植物源农药，申请人拟发展一个简单、绿色、普适性的“交换溶剂/硼酸酯化复合增溶法”策略，用以制备疏水性植物源农药纳米增溶体系。探索农药分子的结构、聚集状态、羟基位置及数量以及制备过程的关键参数对纳米农药水溶解度及尺寸的影响规律，揭示内在关联；进一步用水溶性的多羟基聚合物修饰纳米农药，用以提高硼酸酯增溶的纳米农药体系在高离子强度农业用水环节中的聚结稳定性，以及在农作物叶面上的吸附稳定性；详细研究复合纳米农药的形貌及尺寸对其药效、润湿性能、叶面吸附行为、释放行为以及纳米农药粉末水溶解性的影响，解释结构与性能的关系。本项目的开展对促进绿色农药的普及具有重要意义。

本研究针对众多含有羟基特征基团的疏水性植物源抗菌剂，设计了两个简单的策略，用以制备水溶性纳米植物源农药。主要成果如下：1）创建了交换溶剂/硼酸酯化复合增溶法，对于绝大多数含有2个以上羟基特征基团的固态疏水植物源抗菌剂，利用该方法可以将它们制备成稳定的水溶性纳米制剂，且增溶增效显著；2）设计了一个以液态活性分子自身为油相的自发乳化法，对于疏水的液态香芹酚植物源抗菌剂，可以利用该方法制备其稳定且抗菌性能优异的纳米乳剂；3）将两种方法制得的水溶性纳米植物源抗菌剂与水溶性聚合物复合，制备了多功能的抗菌材料，包括微凝胶、薄膜等，深入研究了这些复合材料在医药、食品、抗菌涂层等领域内的应用。本研究所设计的方法对制备高水溶性纳米尺度的植物源抗菌剂具有重要的参考价值。