新型绿色靶向高效氯氟氰菊酯/海藻酸钠/二氧化硅纳米球悬乳剂的构建及药效评价

This project aims to develop and prepare a ‘smart’, eco-friendly, and auto-targeted pesticide delivery system, lambda-cyhalothrin/sodium alginate/silica nanosphere (LC/ALG/SiO2), by using LC as model pesticide and hollow mesoporous silica nanosphere as delivery carriers. We will study the effects of pore size, inner volume, surface area and group modification of silica nanosphere to the pesticide loading and encapsulation efficiency. The controlled release of LC with high accuracy from nanosphere could be obtained by explore the interaction between LC and nanosphere, and the release mechanism of active ingredients from nanosphere. By modifying with pesticide directing group to the pesticide molecule or on the surface of delivery system, and mixing with insect pheromones to the delivery system, a novel pesticide delivery system with target affinity and controlled release will be developed. We will also construct suspension by using LC/ALG/SiO2 with decent stability and low surface tension. The interfacial properties and biological activity of LC/ALG/SiO2 suspension will be explored to develop the relationship model of pesticide-interface-effect, which could be used for the further pesticide formulation sieving. Such eco-friendly, targeted nano-pesticide formulation with high efficiency and low toxicity could solve the problems of LC, such as the solubility, stability and high toxicity.

课题选用高效氯氟氰菊酯作为模型药物，中空介孔二氧化硅纳米球作为载体，设计构建“智慧型”绿色靶向菊酯/海藻酸钠/二氧化硅纳米球（LC/ALG/SiO2）。研究纳米球介孔孔径、内部中空体积、比表面积、表面官能团修饰等对LC载药量和包封率的影响，理解药物与纳米球的相互作用，探讨药物分子在载体中的载药机制和释放机理，实现农药释放的精准调控；通过对载体表面及农药分子导向基修饰，或将昆虫信息素负载于纳米载体或悬乳剂配方等方法，构建靶标亲和型纳米农药，实现农药传导的精确靶向；将LC/ALG/SiO2纳米球作为悬浮相，筛选获得绿色、稳定性好、低表面张力的LC/ALG/SiO2纳米球悬乳液配方，研究其在靶标作物叶面的界面性质并进行药效评价，构建纳米制剂-界面-药效关系模型，阐明智慧型靶向纳米农药对农作物的影响，用于指导配方筛选，从而改善菊酯等原药的溶解度、稳定性及高毒问题，获得低毒高效的绿色靶向纳米农药。

课题选用高效氯氟氰菊酯（脂溶性）及 吡虫啉（水溶性）作为模型药物，设计构建了高效氯氟氰菊酯聚多巴胺微囊悬浮剂、基于MOF材料的高效氯氟氰菊酯纳米农药系统（UiO-66@LC）及磁性可回收的吡虫啉纳米农药系统（IMI@Fe3O4@PDA@UiO-66）， 温度响应型吡虫啉/介孔二氧化硅纳米粒、光热响应型吡虫啉介孔二氧化硅纳米粒的及酶响应型菊酯/二氧化硅纳米粒等。研究纳米载体内部结构修饰对农药活性分子载药量和包封率的影响，理解药物与纳米载体的相互作用，探讨药物分子在载体中的载药机制和释放机理，实现农药释放的精准调控，通过对载体表面导向基修饰构建靶标亲和型纳米农药，实现农药传导的精确靶向；将载药纳米粒作为悬浮相，筛选获得绿色、稳定性好、低表面张力的载药纳米球悬乳液配方，研究其在靶标作物叶面的界面性质并进行药效评价，阐明智慧型靶向纳米农药对农作物的影响，用于指导配方筛选，从而改善农药原药的溶解度、稳定性及高毒问题，获得低毒高效的绿色靶向纳米农药。