Stability and Biological Activity Evaluation of Chlorantraniliprole Solid Nanodispersions Prepared by High Pressure Homogenization

PLoS One. 2016 Aug 8;11(8):e0160877. doi: 10.1371/journal.pone.0160877. eCollection 2016.

Abstract

Poorly water-soluble compounds are difficult to develop as pesticide products and face great challenges in water-based and environmentally friendly formulation development. In this study, high pressure homogenization combined with lyophilization was adopted to prepare the solid nanodispersions of chlorantraniliprole with poor solubility and high melting point. The mean particle sizes of the solid nanodispersions with different pesticide contents were all less than 75 nm, even when the content was up to 91.5%. For the 2.5% chlorantraniliprole solid nanodispersion with the mean particle size of 29 nm, the suspensibility and wetting time in water were 97.32% and 13 s, respectively. The re-dispersibility and wettability were superior to those of conventional water dispersible granules. The retention on the rice leaf of 18.7 mg/cm2 was 1.5 and 3 times that of commercial aqueous suspension concentrate and pure water. The bioassay result to diamondback moths indicated that the toxicity of the solid nanodispersion was 3.3 and 2.8 times that of technical and aqueous suspension concentrate, respectively. Moreover, the solid nanodispersion has the advantages of total avoidance of organic solvents, significant reduction of surfactants and feasibility of obtaining high concentration nanoformulations. The solid nanodispersion is an attractive candidate for improving pesticide solubility and efficacy, and its application in crop production will reduce both residues in food and environmental pollution of pesticide.

Publication types

  • Evaluation Study

MeSH terms

  • Animals
  • Brassica / drug effects
  • Brassica / growth & development*
  • Drug Compounding
  • Drug Stability
  • Excipients / chemistry*
  • Larva / drug effects
  • Larva / growth & development*
  • Moths
  • Nanotechnology / methods*
  • Particle Size
  • Pressure
  • Solubility
  • Solvents
  • Surface-Active Agents / chemistry*
  • Wettability
  • ortho-Aminobenzoates / chemistry*
  • ortho-Aminobenzoates / pharmacology*

Substances

  • Excipients
  • Solvents
  • Surface-Active Agents
  • ortho-Aminobenzoates
  • chlorantranilipole

Grants and funding

This research was supported by Major National Scientific Research Program of China (No. 2014CB932200) and Basic Scientific Research Foundation of National non-Profit Scientific Institute of China (No. BSRF201406). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.