Nanodelivery System Alters an Insect Growth Regulator's Action Mode: From Oral Feeding to Topical Application.

Insect growth regulators (IGRs) guide animal development through injection, oral feeding, or topical application. Among them, lufenuron is a widely used insect cuticle inhibitor but only shows a gastric toxic effect. Lacking contact toxicity limits the effective utilization when spraying the lufenuron pesticide. To overcome this shortcoming, a nanocarrier (star polycation, SPc)-based transdermal delivery system was applied to improve the penetrability and contact toxicity of lufenuron. The fluoride groups in lufenuron could interact with the tertiary amines in the branch-chain of the SPc through electrostatic interaction to form a lufenuron/SPc complex. The above interaction reduced the particle size of lufenuron from 933 to 70 nm. Interestingly, the contact toxicity of SPc-loaded lufenuron was remarkably improved with effects of higher larval mortality and lower egg hatching rate of the devastating pest fall armyworm. The physiological and molecular toxic mechanism was revealed by RNA-Seq analysis. The SPc-loaded lufenuron apparently down-regulated cuticle-related genes and thus inhibited insect cuticle formation. Such contact toxicity was achieved by the transdermal nanodelivery of lufenuron, which up-regulated endocytosis-related genes for drug uptake. This study is the first successful application of a nanoparticle-mediated transdermal delivery system to explore the contact toxicity of an IGR, which alters the IRG's action mode from oral feeding to topical application.