{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,5]],"date-time":"2026-05-05T17:53:25Z","timestamp":1778003605547,"version":"3.51.4"},"reference-count":47,"publisher":"MDPI AG","issue":"8","license":[{"start":{"date-parts":[[2020,8,4]],"date-time":"2020-08-04T00:00:00Z","timestamp":1596499200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100012166","name":"National key research and development program of China","doi-asserted-by":"publisher","award":["2017YFD0501402"],"award-info":[{"award-number":["2017YFD0501402"]}],"id":[{"id":"10.13039\/501100012166","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["31772797"],"award-info":[{"award-number":["31772797"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>Developing a targeted oral delivery system to improve the efficacy of veterinary antibiotics and reduce their consumption and environmental risks is urgent. To achieve the duodenum-targeted release of tilmicosin, the enteric granule containing tilmicosin-loaded solid lipid nanoparticles (TIL-SLNs) was prepared based on its absorption site and transport characteristics. The in vitro release, release mechanisms, stability, palatability, and pharmacokinetics of the optimum enteric granules were studied. The intestine perfusion indicated that the main absorption site of tilmicosin was shifted to duodenum from ileum by TIL-SLNs, while, the absorption of TIL-SLNs in the duodenum was hindered by P-glycoprotein (P-gp). In contrast with TIL-SLNs, the TIL-SLNs could be more effectively delivered to the duodenum in intact form after enteric coating. Its effective permeability coefficient was enhanced when P-gp inhibitors were added. Compared to commercial premix, although the TIL-SLNs did not improve the oral absorption of tilmicosin, the time to reach peak concentration (Tmax) was obviously shortened. After the enteric coating of the granules containing SLNs and P-gp inhibitor of polysorbate-80, the oral absorption of tilmicosin was improved 2.72 fold, and the Tmax was shortened by 2 h. The combination of duodenum-targeted release and P-gp inhibitors was an effective method to improve the oral absorption of tilmicosin.<\/jats:p>","DOI":"10.3390\/pharmaceutics12080731","type":"journal-article","created":{"date-parts":[[2020,8,4]],"date-time":"2020-08-04T10:45:17Z","timestamp":1596537917000},"page":"731","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":24,"title":["Solid Lipid Nanoparticles for Duodenum Targeted Oral Delivery of Tilmicosin"],"prefix":"10.3390","volume":"12","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-1411-9531","authenticated-orcid":false,"given":"Kaixiang","family":"Zhou","sequence":"first","affiliation":[{"name":"National Reference Laboratory of Veterinary Drug Residues (H.Z.A.U.) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yuanyuan","family":"Yan","sequence":"additional","affiliation":[{"name":"National Reference Laboratory of Veterinary Drug Residues (H.Z.A.U.) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dongmei","family":"Chen","sequence":"additional","affiliation":[{"name":"MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lingli","family":"Huang","sequence":"additional","affiliation":[{"name":"MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Chao","family":"Li","sequence":"additional","affiliation":[{"name":"National Reference Laboratory of Veterinary Drug Residues (H.Z.A.U.) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kuiyu","family":"Meng","sequence":"additional","affiliation":[{"name":"National Reference Laboratory of Veterinary Drug Residues (H.Z.A.U.) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shuge","family":"Wang","sequence":"additional","affiliation":[{"name":"National Reference Laboratory of Veterinary Drug Residues (H.Z.A.U.) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Samah Attia","family":"Algharib","sequence":"additional","affiliation":[{"name":"National Reference Laboratory of Veterinary Drug Residues (H.Z.A.U.) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Wuhan 430070, China"},{"name":"Department of Clinical Pathology, Faculty of Veterinary Medicine, Benha University, Moshtohor, Toukh 13736, Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zonghui","family":"Yuan","sequence":"additional","affiliation":[{"name":"MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shuyu","family":"Xie","sequence":"additional","affiliation":[{"name":"MOA Laboratory for Risk Assessment of Quality and Safety of Livestock and Poultry Products, Huazhong Agricultural University, Wuhan 430070, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2020,8,4]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"398","DOI":"10.1038\/499398a","article-title":"MRSA: Farming up trouble","volume":"499","author":"Mole","year":"2013","journal-title":"Nature"},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"2857","DOI":"10.1080\/10408398.2015.1077192","article-title":"Antimicrobial resistance: A global emerging threat to public health systems","volume":"57","author":"Ferri","year":"2017","journal-title":"Crit. 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