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

Authors Li C, Zhou KX, Chen D, Xu W, Tao Y, Pan Y, Meng K, Shabbir MAB, Liu Q, Huang L, Xie S

Received 20 August 2018

Accepted for publication 19 October 2018

Published 1 March 2019 Volume 2019:14 Pages 1619—1631

DOI https://doi.org/10.2147/IJN.S183479

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Justinn Cochran

Peer reviewer comments 3

Editor who approved publication: Dr Mian Wang


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 Xie1

1National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan Hubei, China; 2MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, Wuhan Hubei, China

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: enrofloxacin, solid lipid nanoparticles, enteric coating, palatability, bioavailability, light stability


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