Importance of chemical polymorphism in modern crop protection

Abstract

The development of agrochemical products faces many scientific challenges. After selection of an agrochemical candidate its properties will have to be optimized to guarantee best bioavailability and stability under many different conditions in various formulation types. These challenges are influenced by the solid-state properties of the active ingredient and this makes the selection of an optimized solid-state form of modern agrochemicals at early development stages very valuable. The increasing awareness of the solid state of agrochemicals is reflected in the importance of polymorphism patent applications, which may enhance the risk of litigations. This review aims to present strategies for the solid-form selection process of agrochemical development candidates. It introduces the different techniques for crystallization and analytics and demonstrates the influence of the solid state on different formulation types.

Design and Synthesis of a Water-Based Nanodelivery Pesticide System for Improved Efficacy and Safety

“…The solid-state crystal structure of EB is one of the important factors affecting its dissolution and bioavailability . XRD analysis revealed an amorphous peak for the EBWNS sample, and such peaks corresponding to SurEB and EB were not observed .…”

“…The solid-state crystal structure of EB is one of the important factors affecting its dissolution and bioavailability. 41 XRD analysis revealed an amorphous peak for the EBWNS sample, and such peaks corresponding to SurEB and EB were not observed. 42 The results implied that EB had improved water solubility in the EBWNS, which can be attributed to the joint action of SurEB and EB to facilitate the dissolution of lipid-soluble pesticides in water 43 (Figure S2).…”

Pursuing Green and Efficient Agriculture from Molecular Assembly: A Review of Solid-State Forms on Agrochemicals

“…For instance, fluoxastrobin's unexpected butyrolactone solvate can instigate precipitation due to solvate formation, leading active ingredients (AIs) to aggregate or inflate, potentially obstructing delivery systems and drastically undercutting efficacy. 21 Furthermore, in the quest for eco-friendly water suspensions, heightened vigilance may be required. The formation of hydrates and the likely ensuing Ostwald ripening could also severely impair efficiency.…”

“…20 Recently, Olenik further emphasized that "The organic solid state has been receiving increasing scientific attention in modern agrochemical chemistry" and advocated the importance of chemical polymorphism in modern crop protection. 21 a thorough comprehension and subsequent implementation of the solid-state form strategy can imbue existing agrochemicals with renewed appeal.…”

“…This cocrystal manifestation of the fungicides pyrimethanil and dithianon exhibits superior synergistic and sustained-release properties compared to products composed exclusively of pyrimethanil . Recently, Olenik further emphasized that “The organic solid state has been receiving increasing scientific attention in modern agrochemical chemistry” and advocated the importance of chemical polymorphism in modern crop protection . Evidently, a thorough comprehension and subsequent implementation of the solid-state form strategy can imbue existing agrochemicals with renewed appeal.…”