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AAPS PHARMSCITECH · 2022 ·Vol. 24 ·期 1 ·1-13 · IF 4.026

Nanosizing Coamorphous Drugs Using Top-Down Approach: The Effect of Particle Size Reduction on Dissolution Improvement

Wang Guoliang,Li Yanchao,Qin Zhiguo,Liu Tao

Nanotechnology and coamorphous are both advanced technologies that can effectively improve the solubility of drugs. This study has been the first attempt to combine these two approaches to construct the coamorphous nanoparticles to improve the dissolution and investigated the effect of physical properties of coamorphous solid on the nanosizing process. Two types of coamorphous solid, i.e., curcumin-artemisinin and quercetin-lysine, were selected as models. Coamorphous curcumin-artemisinin could highly contribute to the size reduction during milling compared to the crystalline form, which might attribute to the change of crystallinity. Nanosized coamorphous curcumin-artemisinin showed higher dissolution than nanocrystals and single coamorphous sample. However, quercetin-lysine coamorphous nanoparticles did not reflect significant dissolution improvement compared with the microsized sample. The difference of initial dissolutions for both could be the main reason. The directly mixing and drying method was confirmed to be an effective and simple approach to maintain the dissolution of nanosized coamorphous sample.

研究领域: 药剂学 · 纳米医学
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PEST MANAGEMENT SCIENCE · 2025 · IF 3.8

Improving the herbicidal activity of mesosulfuron-methyl oil dispersion against Aegilops tauschii by decreasing particle size and adding adjuvant polyvinyl alcohol

Haiyan Yu,Tao Zhang,Cunyu Wei,Juan Yang,Xinle Ma,Jingchao Chen,Hailan Cui,Feng Liu,Xiangju Li

BACKGROUND Mesosulfuron-methyl (MSM) is currently the only available selective herbicide for controlling Aegilops tauschii in wheat fields. Improving the control performance of MSM against Ae. tauschii is crucial for ensuring wheat yield. Herein, strategies to improve the bioactivity of MSM against Ae. tauschii and the underlying mechanism were investigated. RESULTS The efficacy of MSM oil dispersion (MSM-OD, GR 50 = 21.62 g a.i. ha −1 ) on Ae. tauschii was higher than emulsion in water (GR 50 = 59.96 g a.i. ha −1 ) and emulsifiable concentrate (GR 50 = 77.34 g a.i. ha −1 ). A greater retention on Ae. tauschii leaves was responsible for the increased MSM-OD bioactivity. As the particle size decreased from 13.58 to 1.20 μm, the herbicidal activity of MSM-OD towards Ae. tauschii increased 3.07-fold, which was attributed to the small particle size-enabled faster plant absorption of MSM. Polyvinyl alcohol (PVA, 3%) addition in MSM-OD with a small particle size (MSM-OD-S + PVA) increased MSM residue on Ae. tauschii leaves after washing, and thus herbicidal activity. The increased wettability on Ae. tauschii leaves was related to the PVA-induced rainfastness increase of MSM-OD-S. Importantly, MSM-OD-S + PVA at the recommended field rate did not show an adverse effect on wheat growth. CONCLUSION A suitable formulation, reduced particle size and PVA addition can increase the herbicidal activity of MSM against Ae. tauschii , particularly under rainy conditions. These results can provide guidance for the development and application of other herbicides. © 2025 Society of Chemical Industry.

研究领域: 农业化学 · 杂草科学 · 农药制剂 · 植物生理学 · 作物保护
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