Improving intestinal absorption and antibacterial effect of florfenicol via nanocrystallisation technology. (3rd October 2022)

• Record Type: Journal Article
• Authors: Liu, Yanling; Fang, Yuqi; Chen, Yuan; Chen, Weibin; Cheng, Ziyu; Yi, Jun; Li, Xiaofang; Gao, Chongkai; Wu, Fang; Guo, Bohong
• Is Part Of: Journal of microencapsulation. Volume 39:Number 7/8(2022)
• Page Start: 589
• Page End: 600
• Publication Date: 2022-10-03
• Subjects: Florfenicol -- nanocrystals -- long-term stability -- intestinal absorption -- antibacterial; Microencapsulation -- Periodicals; Controlled release technology -- Periodicals; 615.19
• DOI: 10.1080/02652048.2022.2145381
• Languages: English
• ISSNs: 0265-2048

Abstract

Abstract: To study the effects of nanocrystallisation technology on the intestinal absorption properties and antibacterial activity of florfenicol (FF). The florfenicol nanocrystals (FF-NC) were prepared by wet grinding and spray drying. Additionally, changes in particle size, charge, morphology, and dissolution of FF-NC in the long-term stability were monitored by laser particle sizer, TEM, SEM, paddle method, and the structure of FF-NC powder was characterised by nuclear magnetic resonance (NMR) test. The antibacterial activity, intestinal absorption and intestinal histocompatibility of FF-NC were investigated by the stiletto, mini broth dilution susceptibility test, in situ single-pass intestinal perfusion (SPIP) and haematoxylin–eosin (H–E) staining. After 12 months of storage, the particle size and zeta potential of FF-NC were 280.43 ± 8.21 nm and −19.64 ± 3.45 mV, and the electron microscopy results showed that FF-NC were nearly circular with no adhesion between particles. In addition, the drug loading, encapsulation efficiency, and dissolution of FF-NC did not change significantly during storage. The inhibition zone of FF-NC against Escherichia coli and Staphylococcus aureus was 21.37 ± 1.70 mm and 25.17 ± 2.47 mm, respectively. Compared with the FF, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of FF-NC are reduced, and the absorption rate constant ( K a ) and efficient permeability coefficient ( P eff ) of FF-NC in the three intestinal segments were increased by 1.28, 0.25, and 9.10 times and 0.59, 0.17, and 6.0 times, respectively. The results of tissue sections showed that FF-NC had little damage to the small intestinal. Nanocrystallisation technology is an effective method to increase the intestinal absorption and antibacterial activity of FF.