Tilmicosin, as an effective broad-spectrum antibacterial drug, has incomplete absorption and low bioavailability due to its low water solubility, which limits its veterinary clinical applications. As a non-polymeric drug carrier, γ-cyclodextrin was complexed with tilmicosin through supercritical carbon dioxide assistance for the first time, and confirmed by FTIR, X-ray diffraction, proton NMR and scanning electron microscopy. The water solubility of tilmicosin was increased 57-fold through complexation with γ-cyclodextrin, and the release and bioavailability of tilmicosin in the complex were significantly improved. The tilmicosin in complex showed better anti-Streptococcus agalactiae activity than that of tilmicosin alone in MIC, MBC and drug susceptibility studies.
Keywords: In vitro and in vivo pharmaceutical properties, anti-bacterial study; Inclusion complex; Supercritical carbon dioxide assistance; Tilmicosin; γ-cyclodextrin.
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