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. 2019 Dec;26(1):273-280.
doi: 10.1080/10717544.2019.1580798.

Exploitation of enrofloxacin-loaded docosanoic acid solid lipid nanoparticle suspension as oral and intramuscular sustained release formulations for pig

Yanfei Tao  1 , Fei Yang  2 , Kuiyu Meng  2 , Dongmei Chen  1 , Yujuan Yang  2 , Kaixiang Zhou  2 , Wanhe Luo  2 , Wei Qu  2 , Yuanhu Pan  2 , Zonghui Yuan  1   2 , Shuyu Xie  2
Affiliations

Exploitation of enrofloxacin-loaded docosanoic acid solid lipid nanoparticle suspension as oral and intramuscular sustained release formulations for pig

Yanfei Tao et al. Drug Deliv. 2019 Dec.

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.

Keywords: Enrofloxacin; docosanoic acid-solid lipid nanoparticles; intramuscular formulation; oral formulation; suspension.

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Figures

Figure 1.
Figure 1.
Photographs of enrofloxacin-loaded docosanoic acid SLN. A: Optical microscope (Magnification × 40); B: Scanning electron microscope (Magnification × 10000).
Figure 2.
Figure 2.
The pathological maps of gluteus medius of injection site. Left figure: Saline control group; Right figure: Enrofloxacin-loaded docosanoic acid SLN suspension.
Figure 3.
Figure 3.
The release profiles of native enrofloxacin and enrofloxacin-loaded docosanoic acid SLN suspension in pH 1.2 and 7.4 PBS buffers. ENR: Native Enrofloxacin; DAS: Enrofloxacin-loaded docosanoic acid SLN suspension.
Figure 4.
Figure 4.
Mean plasma concentration-time curves of enrofloxacin after intramuscular injection at a dosage of 2.5 mg/kg. Baytril: Baytril solution; DAS: Enrofloxacin-loaded docosanoic acid SLN suspension.
Figure 5.
Figure 5.
Mean plasma concentration-time curves of enrofloxacin after intragastric administration at a dosage of 5 mg/kg. DAS: enrofloxacin-loaded docosanoic acid SLN suspension.
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Grants and funding

This work was supported by the National Key Research and Development Program of China (2017YFD0501400), National Natural Science Foundation of China (31772797).
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