Increased bioaffinity and anti-inflammatory activity of florfenicol nanocrystals by wet grinding method

Abstract

Context: The main objective of the current study is to improve the water solubility of florfenicol (FF) and evaluate changes in its pharmacokinetics and anti-inflammatory activity.

Materials and methods: Florfenicol nanocrystals (FF-NC) were prepared by wet grinding combined with spray drying. The characterisations, pharmacokinetics, and anti-inflammatory activity of FF-NC were evaluated.

Results: The particle size, polydispersity index (PDI), and zeta potential of FF-NC were 276.4 ± 19.4 nm, 0.166 ± 0.011, and –18.66 ± 5.25 mV, respectively. Compared with FF, FF-NC showed a better dissolution rate in media at different pH. Pharmacokinetic experiments showed the area under the curve (AUC_0–t), maximum concentration (C_max), and mean residence time (MRT) of FF-NC were about 4.62-fold, 2.86-fold, and 1.68-fold higher compared with FF, respectively. In vitro anti-inflammatory experiments showed that FF inhibited the secretion of tumour necrosis factor-α (TNF-α), interleukin-6 (IL-6), and synthesis of NO in a dose-dependent manner, while FF-NC showed a stronger anti-inflammatory effect than FF under the same dose.

Conclusion: FF-NC are an effective way to improve the bioaffinity and anti-inflammatory effects of FF.

Keywords:

• Wet grinding
• florfenicol nanocrystals
• solubility
• pharmacokinetics
• anti-inflammatory

Disclosure statement

The authors confirm that there are no conflicts of interest in this article.

Additional information

Funding

This work was financially supported by the “Yang Fan Plan” Team Project of Guangdong Province [No. 2017YT05S137].