Manipulated Slow Release of Florfenicol Hydrogels for Effective Treatment of Anti-Intestinal Bacterial Infections.

Objective: The difficulty of establishing slow release at intestinal infection sites, weak antibacterial effects, as well as the limited broad use of florfenicol oral formulations are the main targets of the current study. Novel hydrogels derived from sodium alginate were developed using a complexation form for florfenicol delivery to achieve slow release at the site of intestinal infection and enhance its antibacterial activity against Escherichia coli.

Methods: The optimal formulation, physicochemical properties, stability, pH-responsive performance, antibacterial activity, and in vitro biosafety of the florfenicol hydrogels have been studied systematically.

Results: The created hydrogels had a consistent spherical morphology, with an average diameter of 531.9±12.6 nm. Energy dispersive spectroscopy and Fourier transform infrared indicated that florfenicol hydrogels have been successfully prepared through complexation force. Furthermore, it is shown that florfenicol hydrogels hold outstanding stability, excellent sustained release, and faster swelling and release at intestinal pH due to pH-responsiveness. The florfenicol hydrogels had no obvious structural destruction in simulated gastric juice (pH=1.2) for 12 hrs and were highly stable. However, the hydrogels began to be destroyed after 5 minutes in simulated intestinal fluid (SIF), and this decomposition was continuous. With the decomposition of the structure of florfenicol hydrogels, the encapsulated florfenicol was also slowly released, and thus, it achieves the slow-release effect. Additionally, the florfenicol hydrogels showed a low hemolytic ratio and greater antibacterial activity compared with florfenicol.

Conclusion: The blended formulation creates a promising oral matrix intended for the slow-release of florfenicol along the gastrointestinal tract.