PMID- 30880969 OWN - NLM STAT- MEDLINE DCOM- 20190429 LR - 20220408 IS - 1178-2013 (Electronic) IS - 1176-9114 (Print) IS - 1176-9114 (Linking) VI - 14 DP - 2019 TI - Solid lipid nanoparticles with enteric coating for improving stability, palatability, and oral bioavailability of enrofloxacin. PG - 1619-1631 LID - 10.2147/IJN.S183479 [doi] AB - 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 microg h/mL and 6.80+/-2.28 hours to 11.24+/-3.33 microg 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. FAU - Li, Chao AU - Li C AD - National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan Hubei, China, snxsy1@126.com. FAU - Zhou, Kaixiang AU - Zhou K AD - National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan Hubei, China, snxsy1@126.com. FAU - Chen, Dongmei AU - Chen D AD - National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan Hubei, China, snxsy1@126.com. AD - MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, Wuhan Hubei, China. FAU - Xu, Wei AU - Xu W AD - National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan Hubei, China, snxsy1@126.com. FAU - Tao, Yanfei AU - Tao Y AD - National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan Hubei, China, snxsy1@126.com. FAU - Pan, Yuanhu AU - Pan Y AD - MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, Wuhan Hubei, China. FAU - Meng, Kuiyu AU - Meng K AD - MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, Wuhan Hubei, China. FAU - Shabbir, Muhammad Abu Bakr AU - Shabbir MAB AD - MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, Wuhan Hubei, China. FAU - Liu, Qianying AU - Liu Q AD - National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan Hubei, China, snxsy1@126.com. FAU - Huang, Lingli AU - Huang L AD - MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, Wuhan Hubei, China. FAU - Xie, Shuyu AU - Xie S AD - National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan Hubei, China, snxsy1@126.com. LA - eng PT - Journal Article DEP - 20190301 PL - New Zealand TA - Int J Nanomedicine JT - International journal of nanomedicine JID - 101263847 RN - 0 (Drug Carriers) RN - 0 (Lipids) RN - 0 (Tablets, Enteric-Coated) RN - 3DX3XEK1BN (Enrofloxacin) SB - IM MH - Administration, Oral MH - Animals MH - Biological Availability MH - Body Fluids/chemistry MH - Drug Carriers MH - Enrofloxacin/*administration & dosage/blood/*pharmacokinetics MH - Intestine, Small MH - Lipids/*chemistry MH - Nanoparticles/*chemistry/ultrastructure MH - Particle Size MH - Solubility MH - Swine MH - Tablets, Enteric-Coated PMC - PMC6402439 OTO - NOTNLM OT - bioavailability OT - enrofloxacin OT - enteric coating OT - light stability OT - palatability OT - solid lipid nanoparticles COIS- Disclosure The authors report no conflicts of interest in this work. EDAT- 2019/03/19 06:00 MHDA- 2019/04/30 06:00 PMCR- 2019/03/01 CRDT- 2019/03/19 06:00 PHST- 2019/03/19 06:00 [entrez] PHST- 2019/03/19 06:00 [pubmed] PHST- 2019/04/30 06:00 [medline] PHST- 2019/03/01 00:00 [pmc-release] AID - ijn-14-1619 [pii] AID - 10.2147/IJN.S183479 [doi] PST - epublish SO - Int J Nanomedicine. 2019 Mar 1;14:1619-1631. doi: 10.2147/IJN.S183479. eCollection 2019.