Journal
JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS
Volume 32, Issue 2, Pages 116-123Publisher
WILEY
DOI: 10.1111/j.1365-2885.2008.01009.x
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Funding
- National High Technology Research and Development Program ('863'Program) of China [2006AA10A203]
- National Key Technology RD Program [2006BAD04A16]
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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 similar to 230 nm, -6.5 similar to-12.5 mV, 40.3 similar to 59.2% and 5.7 similar to 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 mu g/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 (T1/2 ab) and half-life of elimination (T1/2 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.
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