National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang, 550025, China.
College of Chemistry and Chemical Engineering, Guizhou University of Engineering Science, Bijie, 551700, China.
J Nanobiotechnology. 2024 Mar 19;22(1):121. doi: 10.1186/s12951-024-02386-8.
Traditional pesticides are poorly water-soluble and suffer from low bioavailability. N-succinyl chitosan (NSCS) is a water-soluble chitosan derivative, has been recently used to encapsulate hydrophobic drugs to improve their bioavailability. However, it remains challenging to synthesize pesticides of a wide variety of water-soluble drugs and to scale up the production in a continuous manner.
A synthetic method for preparing water-soluble nanopesticides with a polymer carrier was applied. The bioactive molecule BTL-11 was loaded into hollow NSCS to promote drug delivery, improve solubility and anti-fungal activity. The synthesized nanopesticides had well controlled sizes of 606 nm and the encapsulation rate was 80%. The release kinetics, drug toxicity and drug activity were further evaluated. The inhibitory activity of nanopesticides against Rhizoctonia solani (R. solani) was tested in vivo and in vitro. In vivo against R. solani trials revealed that BTL-11 has excellent control efficiency for cultivated rice leaf and sheath was 79.6 and 76.5%, respectively. By contrast, for BTL-11@NSCS NPs, the anti-fungal ability was strongly released and afforded significant control efficiencies of 85.9 and 81.1%. Those effects were significantly better than that of the agricultural fungicide azoxystrobin (51.5 and 66.5%). The proposed mechanism was validated by successfully predicting the synthesis outcomes.
This study demonstrates that NSCS is a promising biocompatible carrier, which can enhance the efficacy of pesticides, synergistically improve plant disease resistance, protect crop growth, and can be used for the delivery of more insoluble pesticides.
传统农药水溶性差,生物利用度低。N-琥珀酰壳聚糖(NSCS)是一种水溶性壳聚糖衍生物,最近已被用于包封疏水性药物以提高其生物利用度。然而,合成各种水溶性药物的农药并以连续的方式扩大生产仍然具有挑战性。
应用了一种用聚合物载体制备水溶性纳米农药的合成方法。将活性分子 BTL-11 载入中空 NSCS 中,以促进药物传递、提高溶解度和抗真菌活性。合成的纳米农药具有良好的控制粒径为 606nm,包封率为 80%。进一步评估了释放动力学、药物毒性和药物活性。还在体内和体外测试了纳米农药对 Rhizoctonia solani(R. solani)的抑制活性。体内对 R. solani 的试验表明,BTL-11 对水稻叶片和叶鞘的防治效果分别为 79.6%和 76.5%。相比之下,BTL-11@NSCS NPs 的抗真菌能力得到了强烈释放,防治效果分别达到了 85.9%和 81.1%。这些效果明显优于农业杀菌剂肟菌酯(51.5%和 66.5%)。通过成功预测合成结果验证了该机制。
本研究表明 NSCS 是一种有前途的生物相容性载体,可增强农药的功效,协同提高植物的抗病能力,保护作物生长,并可用于输送更多不溶性农药。