Preparation, characterization, and pharmacokinetics of tilmicosin- and florfenicol-loaded hydrogenated castor oil-solid lipid nanoparticles.
To effectively control bovine mastitis, tilmicosin (TIL)- and florfenicol (FF)-loaded solid lipid nanoparticles (SLN) with hydrogenated castor oil (HCO) were prepared by a hot homogenization and ultrasonication method. In vitro antibacterial activity, properties, and pharmacokinetics of the TIL-FF-SLN were studied. The results demonstrated that TIL and FF had a synergistic or additive antibacterial activity against Streptococcus dysgalactiae, Streptococcus uberis, and Streptococcus agalactiae. The size, polydispersity index, and zeta potential of nanoparticles were 289.1 ± 13.7 nm, 0.31 ± 0.05, and -26.7 ± 1.3 mV, respectively. The encapsulation efficiencies for TIL and FF were 62.3 ± 5.9% and 85.1 ± 5.2%, and the loading capacities for TIL and FF were 8.2 ± 0.6% and 3.3 ± 0.2%, respectively. The TIL-FF-SLN showed no irritation in the injection site and sustained release in vitro. After medication, TIL and FF could maintain about 0.1 μg/mL for 122 and 6 h. Compared to the control solution, the SLN increased the area under the concentration-time curve (AUC0-t), elimination half-life (T½ke), and mean residence time (MRT) of TIL by 33.09-, 23.29-, and 37.53-fold, and 1.69-, 5.00-, and 3.83-fold for FF, respectively. These results of this exploratory study suggest that the HCO-SLN could be a useful system for the delivery of TIL and FF for bovine mastitis therapy.
College of Animal Science and Technology, School of Tarim University, Alar, China.|Key Laboratory of Tarim Animal Husbandry Science and Technology of Xinjiang Production & Construction Corps, Alar, China.|College of Animal Science & Technology, Shihezi University, Shihezi, China.
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Ling
College of Animal Science and Technology, School of Tarim University, Alar, China.|Key Laboratory of Tarim Animal Husbandry Science and Technology of Xinjiang Production & Construction Corps, Alar, China.
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Yonghong
College of Animal Science and Technology, School of Tarim University, Alar, China.|Key Laboratory of Tarim Animal Husbandry Science and Technology of Xinjiang Production & Construction Corps, Alar, China.
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Changqing
Key Laboratory of Tarim Animal Husbandry Science and Technology of Xinjiang Production & Construction Corps, Alar, China.
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Junfeng
College of Animal Science and Technology, School of Tarim University, Alar, China.|Key Laboratory of Tarim Animal Husbandry Science and Technology of Xinjiang Production & Construction Corps, Alar, China.
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Li
College of Animal Science and Technology, School of Tarim University, Alar, China.
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Chunyu
College of Animal Science and Technology, School of Tarim University, Alar, China.|Key Laboratory of Tarim Animal Husbandry Science and Technology of Xinjiang Production & Construction Corps, Alar, China.
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Xianqiang
D000818:Animals; D000900:Anti-Bacterial Agents; D002368:Castor Oil / Q000008:administration & dosage; D002417:Cattle; D002626:Chemistry, Pharmaceutical; D004357:Drug Synergism; D005260:Female; D008055:Lipids / Q000008:administration & dosage; D008414:Mastitis, Bovine / Q000188:drug therapy*; D053758:Nanoparticles; D010316:Particle Size; D013839:Thiamphenicol / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D015645:Tylosin / Q000031:analogs & derivatives* / Q000493:pharmacokinetics
D000900:Anti-Bacterial Agents; D008055:Lipids; D002368:Castor Oil; C035534:florfenicol; D013839:Thiamphenicol; C052319:tilmicosin; D015645:Tylosin