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Preparation, characterization, and pharmacokinetics of tilmicosin‐ and florfenicol‐loaded hydrogenated castor oil‐solid lipid nanoparticles
Author(s) -
Ling Z.,
Yonghong L.,
Changqing S.,
Junfeng L.,
Li Z.,
Chunyu J.,
Xianqiang L.
Publication year - 2017
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/jvp.12356
Subject(s) - solid lipid nanoparticle , chemistry , streptococcus uberis , tilmicosin , mastitis , pharmacokinetics , danofloxacin , minimum inhibitory concentration , sonication , chromatography , particle size , pharmacology , streptococcus , in vitro , microbiology and biotechnology , antibiotics , biochemistry , medicine , biology , enrofloxacin , bacteria , ciprofloxacin , genetics
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  μ g/mL for 122 and 6 h. Compared to the control solution, the SLN increased the area under the concentration–time curve ( AUC 0‐t ), elimination half‐life ( T ½ke ), 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.

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