Song Yang,Mengya Hu,Wenqing Liu,Nuohan Hou,Kaidi Yin,Chen Shen,Qing Shang
In this study, a novel PLGA in situ forming implants (ISFIs) were fabricated and methods for testing the in vitro release profiles were also developed. The correlations between in vitro release profiles and in vivo performances (in vitro–in vivo correlation, IVIVC) were also studied. PLGA with different molecular weights were selected as the polymeric matrix. Biocompatible N-methy1-2-pyrrolidone (NMP) or glyceryl triacetate (GTA) were used as the solvents with the ratios of NMP/GTA from 60/40 (vol/vol) to 20/80 (vol/vol). Eprinomectin (EPR) was chosen as the model therapeutic. In vitro release profiles of the EPR-loaded PLGA ISFIs were investigated using various methods (i.e. ‘tubule’ sample-and-separate and dialysis method). Sprague–Dawley rats were used to study the in vivo pharmacokinetics of EPR-loaded PLGA ISFIs. The release data obtained via ‘tubule’ sample-separate method had a good IVIVC (Level A, R2 > 0.99). These results showed that the ‘tubule’ sample-separate method was capable of discriminating the EPR-loaded ISFIs which were equivalent in formulation composition with manufacturing differences. Meanwhile, this method could be used to predict the in vivo performances of ISFIs in the investigated animal model.
Jiawen Ji,Siyue Zhu,Xinping Hu,Jianhui Zhu,Sen Pang,Yongqiang Ma,Xuefeng Li
Abamectin is one of the most widely used pesticides globally, known for its effectiveness in protecting crops and animal health. However, the residual risk of abamectin in agricultural products and the environment may be exacerbated by other pollutants, indicating greater potential hazards. One such emerging environmental pollutant is N-(1,3-dimethylbutyl)-N′-phenyl-p-phenylenediamine (6PPD), a common tire antioxidant found in various environments, including agricultural products and human urine. Our study first revealed the co-existence of 6PPD and abamectin in water and soil, and demonstrated that 6PPD significantly enhances the residual persistence of abamectin in environmental media and vegetables. Specifically, 6PPD extended the half-life of abamectin by 79% in pak choi and by 70% in cabbage. Additionally, 6PPD increased the photolysis half-life of abamectin in water by 191% and by 50% on soil surfaces. Furthermore, 6PPD also prolonged the photolysis half-life of four other macrolides in water. This study reveals the mechanism through which 6PPD extends the half-life of abamectin: by scavenging free radicals and inhibiting hydroxylation and oxidation, thus slowing its degradation. And this paper highlights that 6PPD significantly exacerbates the environmental risks and food safety issue associated with abamectin. Moreover, it provides valuable insights for studying the safe use of pesticides in complex environments with multiple contaminants.
危险品化学品经营许可证（带存储）