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Open AccessArticle

Synthesis of Tilmicosin Nanostructured Lipid Carriers for Improved Oral Delivery in Broilers: Physiochemical Characterization and Cellular Permeation

1
Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Nanjing Agricultural University, 1 Weigang, Nanjing 210095, China
2
Department of Animal Pharmacy, Jiangsu Agri-Animal Husbandry Vocational College, Taizhou 225300, China
*
Author to whom correspondence should be addressed.
Molecules 2020, 25(2), 315; https://doi.org/10.3390/molecules25020315
Received: 29 November 2019 / Revised: 5 January 2020 / Accepted: 10 January 2020 / Published: 13 January 2020
This study aimed to develop nanostructured lipid carriers (NLCs) for improved oral absorption of tilmicosin (TMS) in broilers. Thus, palmitic acid, lauric acid, and stearic acid were selected as solid lipids to formulate TMS-pNLCs, TMS-lNLCs, and TMS-sNLCs, respectively. They showed similar physicochemical properties and meanwhile possessed excellent storage and gastrointestinal stability. The TMS interacted with the lipid matrix and was encapsulated efficiently in NLCs in an amorphous structure. NLCs could enhance oral absorption of TMS compared to 10% tilmicosin phosphate solution in broilers, among which the TMS-sNLCs were the most efficient drug delivery carriers, with a relative oral bioavailability of 203.55%. NLCs could inhibit the efflux of P-glycoprotein (P-pg) toward TMS, which may be involved with improved oral absorption. Taken together, these types of solid lipids influenced the enhanced level of NLCs toward oral bioavailability of TMS, and the sNLCs proved to be the most promising oral delivery carriers of TMS. View Full-Text
Keywords: tilmicosin; nanostructured lipid carriers; oral bioavailability; broiler; cellular permeability; P-gp efflux tilmicosin; nanostructured lipid carriers; oral bioavailability; broiler; cellular permeability; P-gp efflux
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MDPI and ACS Style

Sahito, B.; Zhang, Q.; Yang, H.; Peng, L.; Gao, X.; Kashif, J.; ul Aabdin, Z.; Jiang, S.; Wang, L.; Guo, D. Synthesis of Tilmicosin Nanostructured Lipid Carriers for Improved Oral Delivery in Broilers: Physiochemical Characterization and Cellular Permeation. Molecules 2020, 25, 315.

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