Yao Junwei, Cui Bo, Zhao Xiang, Zhi Heng, Zeng Zhanghua, Wang Yan, Sun Changjiao, Liu Guoqiang, Gao Jinming, Cui Haixin
Institute of Environment and Sustainable Development in Agriculture, Chinese Academy of Agricultural Sciences, Beijing, 100081, China.
Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, China.
Nanomaterials (Basel). 2018 Oct 19;8(10):857. doi: 10.3390/nano8100857.
Size-controlled azoxystrobin-poly (lactic acid) microspheres (MS) were prepared by an oil/water emulsion solvent evaporation approach. The hydrated mean particle sizes of the MS1, MS2, and MS3 aqueous dispersions were 130.9 nm, 353.4 nm, and 3078.0 nm, respectively. The drug loading and encapsulation efficiency of the azoxystrobin microspheres had a positive relationship with particle size. However, the release rate and percentage of cumulative release were inversely related to particle size. The smaller-sized microspheres had a greater potential to access the target mitochondria. As a result, the more severe oxidative damage of Sacc and higher antagonistic activity were induced by the smaller particle size of azoxystrobin microspheres. The 50% lethal concentrations against Sacc of MS1, MS2, and MS3 were 2.0386 μg/mL, 12.7246 μg/mL, and 21.2905 μg/mL, respectively. These findings reveal that particle size is a critical factor in increasing the bioavailability of insoluble fungicide.
采用油/水乳液溶剂蒸发法制备了粒径可控的嘧菌酯-聚乳酸微球(MS)。MS1、MS2和MS3水分散体的水合平均粒径分别为130.9 nm、353.4 nm和3078.0 nm。嘧菌酯微球的载药量和包封率与粒径呈正相关。然而,释放速率和累积释放百分比与粒径呈负相关。较小尺寸的微球更有可能进入目标线粒体。因此,较小粒径的嘧菌酯微球诱导了更严重的酿酒酵母氧化损伤和更高的拮抗活性。MS1、MS2和MS3对酿酒酵母的50%致死浓度分别为2.0386 μg/mL、12.7246 μg/mL和21.2905 μg/mL。这些发现表明粒径是提高不溶性杀菌剂生物利用度的关键因素。