Tilmicosin/γ-Cyclodextrin complexation through supercritical carbon dioxide assistance and its pharmacokinetic and antibacterial study

Abstract

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.