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Hydrogenated castor oil nanoparticles as carriers for the subcutaneous administration of tilmicosin: in vitro and in vivo studies
Author(s) -
HAN C.,
QI C. M.,
ZHAO B. K.,
CAO J.,
XIE S. Y.,
WANG S. L.,
ZHOU W. Z.
Publication year - 2009
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/j.1365-2885.2008.01009.x
Subject(s) - tilmicosin , chemistry , pharmacology , in vivo , nanoparticle , pharmacokinetics , chromatography , oral administration , nuclear chemistry , biochemistry , materials science , medicine , nanotechnology , microbiology and biotechnology , antibiotics , biology
Tilmicosin‐loaded solid lipid nanoparticles (SLN) were prepared with hydrogenated castor oil (HCO) by o/w emulsion–solvent evaporation technique. The nanoparticle diameters, surface charges, drug loadings and encapsulation efficiencies of different formulations were 90∼230 nm, −6.5∼−12.5 mV, 40.3∼59.2% and 5.7∼11.7% (w/w), respectively. In vitro release studies of the tilmicosin‐loaded nanoparticles showed a sustained release and the released tilmicosin had the same antibacterial activity as that of the free drug. Pharmacokinetics study after subcutaneous administration to Balb/c mice demonstrated that a single dose of tilmicosin‐loaded nanoparticles resulted in sustained serum drug levels (>0.1 μg/mL) for 8 days, as compared with only 5 h for the same amount of tilmicosin phosphate solution. The time to maximum concentration (Tmax), half‐life of absorption (T½ ab) and half‐life of elimination (T½ el) of tilmicosin‐loaded nanoparticles were much longer than those of tilmicosin phosphate solution. Tissue section showed that drug‐loaded nanoparticles caused no inflammation at the injection site. Cytotoxicity study in cell culture and acute toxicity test in mice demonstrated that the nanoparticles had little or no toxicity. The results of this exploratory study suggest that the HCO–SLN could be a useful system for the delivery of tilmicosin by subcutaneous administration.