Hu Dekun, Bian Qiang, Mu Xianfu, Du Fengpei, Tian Hao, Jin Zhichao, Wang Peiyi
State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals of Guizhou University, Guiyang 550025, China.
National Pesticide Engineering Research Center (Tianjin), College of Chemistry, Nankai University, Tianjin 300071, China.
ACS Nano. 2025 Jul 8;19(26):24093-24108. doi: 10.1021/acsnano.5c07377. Epub 2025 Jun 27.
The development of nanopesticides with minimized carriers (NMCs) through prodrug design and molecular self-assembly represents a transformative strategy for enhancing pesticide utilization efficiency and addressing global food security challenges. As a proof of concept, we developed A12@DES, a water-based nanodelivery system that combines a target-specific pesticide with a deep eutectic solvent (DES). The system utilizes a laccase inhibitor (A12, structurally optimized from lead compound PMDD-5Y) to self-assemble into monodisperse nanospheres (∼160 nm diameter) with an alkaline phosphatase (ALP)-responsive DES matrix. The formulation demonstrates multiple functional advantages: (1) a simple preparation process, (2) substantially reduced droplet bouncing and splashing, (3) enhanced foliar wetting performance, and (4) ultimately improved pesticide deposition efficiency. Intriguingly, A12@DES supports rice growth and demonstrates minimal toxicity to nontarget organisms. At a low dose of 200 μg/mL, A12@DES exhibits superior in vivo curative and protective efficacies (74.43%/85.53%) against compared to both the commercial fungicide isoprothiolane (57.48%/63.29%) and A12 alone (66.69%/69.95%). This study provides a reference for the development of multipurpose water-based nanopesticide delivery systems based on prodrug technology and DES conception, improving the comprehensive utilization efficiency of fungicides for high-risk rice blast control.
通过前药设计和分子自组装开发具有最小化载体的纳米农药（NMCs），是提高农药利用效率和应对全球粮食安全挑战的一种变革性策略。作为概念验证，我们开发了A12@DES，这是一种水基纳米递送系统，它将靶向特异性农药与深共晶溶剂（DES）相结合。该系统利用一种漆酶抑制剂（A12，由先导化合物PMDD-5Y结构优化而来）自组装成单分散纳米球（直径约160 nm），其具有碱性磷酸酶（ALP）响应性的DES基质。该制剂具有多种功能优势：（1）制备过程简单；（2）显著减少液滴弹跳和飞溅；（3）增强叶面湿润性能；（4）最终提高农药沉积效率。有趣的是，A12@DES支持水稻生长，并且对非靶标生物表现出最小的毒性。在200 μg/mL的低剂量下，与商业杀菌剂异稻瘟净（57.48%/63.29%）和单独的A12（66.69%/69.95%）相比，A12@DES对[此处原文缺失目标生物信息]表现出优异的体内治疗和保护效果（74.43%/85.53%）。本研究为基于前药技术和DES概念的多功能水基纳米农药递送系统的开发提供了参考，提高了用于高风险稻瘟病防治的杀菌剂的综合利用效率。
