Abstract
In our previous study, enrofloxacin-loaded docosanoic acid solid lipid nanoparticles (SLNs) could be effectively delivered to cells in vitro. In this study, its properties and exploitation as possible oral and intramuscular sustained release formulations for pigs were studied after being made into suspension. The re-dispersed time and sedimentation rate of the nanosuspension were 55 s and 1, respectively. It showed good stability when stored away from light and sustained release in pH = 7.4 PBS buffer. The suspension exhibited no irritation at the injection site and good palatability. Compared with commercial injection and soluble powder, the nanosuspension increased the bioavailability of enrofloxacin by 1.63 and 2.38 folds, and extended the mean residence time (MRT) of the drug from 11.27 and 12.33 to 37.76 and 35.15 h after intragastric and intramuscular administration, respectively. These results suggest that docosanoic acid SLN suspension (DAS) might be a promising oral and intramuscular sustained release formulation to enhance the pharmacological activity of enrofloxacin.
Highlights
Enrofloxacin is widely used to treat bacterial infections in livestock and poultry due to its strong and broad-spectrum antibacterial activity (Elsheikh et al, 2002; Elmas et al, 2007; Harada et al, 2014; Ruennarong et al, 2016)
The optical microscope and scanning electron microscopy studies demonstrated that the solid lipid nanoparticles (SLNs) were well dispersed with good particle size distributions and spherical (Figure 1)
After 6 months of storage at 40 ± 2 C and 75 ± 5% relative humidity away from light, the loading capacity (LC), polydispersity index (PDI) and zeta potential of the nanoparticles were no evident change except a little increase in the size
Summary
Enrofloxacin is widely used to treat bacterial infections in livestock and poultry due to its strong and broad-spectrum antibacterial activity (Elsheikh et al, 2002; Elmas et al, 2007; Harada et al, 2014; Ruennarong et al, 2016). Its poor aqueous solubility causes variable bioavailability and results in difficulties, in the design of pharmaceutical formulations (Martinez et al, 2006). Its bitter taste is unacceptable for animals, especially for pigs. The commercially available oral formulations cannot effectively mask the bitter taste and limit their clinical applications for pigs. The drug has short elimination half-life (T1/2ke) and mean residence time (MRT) in most mammals (Haritova et al, 2003). The repeated and high doses should be needed in the clinic and might result in animal inconvenience, drug resistance, and environmental contamination. Alternative formulations should be developed to mask the bitter taste, enhance the absorption and reduce the frequency of drug administration (Yang et al, 2015)
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