Fabrication of an Effective Avermectin Nanoemulsion Using a Cleavable Succinic Ester Emulsifier.

Abstract

In this study, a new emulsifier precursor was prepared via esterification of avermectin with succinic anhydride. The chemical structure of the product was confirmed to be monosubstituted avermectin. After neutralization with triethanolamine, it exhibited adequate emulsification ability for avermectin. Avermectin was then encapsulated in nanoparticles in the nanoemulsion with a high drug loading up to 60 wt % and high stability. The nanoemulsion of nanoparticles that serves as a carrier of avermectin shows highly efficient pesticide characteristics, including low surface tension, high affinity to leaves, and improved photostability. In the presence of esterase or under strongly basic conditions, the ester bonds of the emulsifier can be hydrolyzed, and the encapsulated avermectin molecules can be released in an accelerated manner. The nanoemulsion exhibited improved insecticidal effect compared with commercial emulsifiable concentrate, which was attributed to the cleavage of ester bonds of the emulsifier by esterase in vivo.