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. 2019 Mar 1:14:1619-1631.
doi: 10.2147/IJN.S183479. eCollection 2019.

Solid lipid nanoparticles with enteric coating for improving stability, palatability, and oral bioavailability of enrofloxacin

Chao Li  1 , Kaixiang Zhou  1 , Dongmei Chen  1   2 , Wei Xu  1 , Yanfei Tao  1 , Yuanhu Pan  2 , Kuiyu Meng  2 , Muhammad Abu Bakr Shabbir  2 , Qianying Liu  1 , Lingli Huang  2 , Shuyu Xie  1
Affiliations

Solid lipid nanoparticles with enteric coating for improving stability, palatability, and oral bioavailability of enrofloxacin

Chao Li et al. Int J Nanomedicine. .

Abstract

Background: The poor palatability, variable oral bioavailability, stimulation to gastric mucosa, and light instability limited the application of enrofloxacin (ENR). The enteric granules combining solid lipid nanoparticles (SLNs) with enteric coating were explored to overcome these disadvantages.

Materials and methods: ENR-loaded SLNs were produced by a hot homogenization and ultrasonic emulsification method and the enteric granules with SLNs as inner core were prepared by wet granulation followed by coating using polyacrylic resin II (PRII). The formulation was optimized by using orthogonal or single factor test screening.

Results: The optimal SLNs with loading capacity (LC) and price as inspection indexes were consisted of 10 mL 3% polyvinyl alcohol per 0.8 g ENR and 2.4 g octadecanoic acid. The sizes, LC, polydispersion index, and zeta potential of the SLNs were 308.5±6.3 nm, 15.73%±0.31%, 0.352±0.015, and -22.3 mv, respectively. The best enteric granules were used 15% PRII as coating materials. The release of the enteric granules in simulated intestine fluid (SIF, pH=8) was significantly faster than in simulated gastric fluid (SGF, pH=2) and simultaneously slower than those of SLNs and native ENR. The granules showed good stability in influencing factor experiment. The granules displayed a similar daily feed intake as the control group and higher daily feed intake than ENR powder and single-coating granules. Compared to the ENR soluble powder, the area under the plasma concentration-time curve and mean retention time of the enteric granules after intragastric administration were increased from 4.26±0.85 µg h/mL and 6.80±2.28 hours to 11.24±3.33 µg h/mL and 17.97±4.01 hours, respectively.

Conclusion: The enteric granules combination SLNs with enteric coating significantly improved the stability, palatability, sustained-release performance and oral bioavailability of ENR. The novel technology will be a potential measure to overcome the similar disadvantages of other drugs.

Keywords: bioavailability; enrofloxacin; enteric coating; light stability; palatability; solid lipid nanoparticles.

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Conflict of interest statement

Disclosure The authors report no conflicts of interest in this work.

Figures

Figure 1
Figure 1
The production process of enrofloxacin enteric granules containing SLNs inner core. Abbreviations: ENR-SLNs, enrofloxacin-loaded SLNs; RT, room temperature; SLNs, solid lipid nanoparticles.
Figure 2
Figure 2
Scanning electron microscopy photographs of enrofloxacin-loaded SLNs. Abbreviation: SLNs, solid lipid nanoparticles.
Figure 3
Figure 3
The accumulation release profiles of SLNs and granules in the simulated SGF (pH=2) (n=3). Abbreviations: EC, ethyl cellulose; ENR, enrofloxacin; ENR-SLNs, enrofloxacin-loaded SLNs; PR, polyacrylic resin; SGF, simulated gastric fluid; SLNs, solid lipid nanoparticles.
Figure 4
Figure 4
The accumulation release profiles of SLNs and granules in the simulated SIF (pH=8) (n=3). Abbreviations: ENR, enrofloxacin; ENR-SLNs, enrofloxacin-loaded SLNs; PR, polyacrylic resin; SIF, simulated intestine fluid; SLNs, solid lipid nanoparticles.
Figure 5
Figure 5
The influence of influencing factors experiments to release ability of enteric granules (n=3). Notes: (A) The influence of high temperature to release ability of enteric granules. (B) The influence of high humidity to release ability of enteric granules. (C) The influence of high light to release ability of enteric granules. HT: high temperature (40°C); HI: high humidity (25°C, 90%±5%); HL: high light (4,500±500 lx).
Figure 6
Figure 6
The plasma enrofloxacin concentration profiles – time of the prepared granules and reference formulation (soluble powder) in pigs (n=6). Notes: Granules: 10% enrofloxacin enteric granules; powder: 5% enrofloxacin soluble powder.
Figure 7
Figure 7
The transfer process of enrofloxacin granules in gastrointestinal tract of pigs. Abbreviations: ENR-SLNs, enrofloxacin-loaded SLNs; SLNs, solid lipid nanoparticles.
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