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Toltrazuril mixed nanomicelle delivery system based on sodium deoxycholate–Brij C20 polyethylene ether–triton x100: Characterization, solubility, and bioavailability study

Zhang, Li, Ren, Dandan, Zhou, Jianyu, Peng, Guangneng, Shu, Gang, Yuan, Zhixiang, Shi, Fei, Zhao, Ling, Yin, Lizi, Fan, Guoqing, Liu, Chang, Fu, Hualin
Colloids and surfaces 2018 v.163 pp. 125-132
X-ray diffraction, bioavailability, coccidiosis, colloids, differential scanning calorimetry, drugs, mammals, micelles, particle size, pharmacokinetics, polyethylene, poultry, poultry diseases, scanning electron microscopy, sodium, solubility, surfactants, toltrazuril, transmission electron microscopy
Toltrazuril (Tol) is a broad-spectrum anticoccidiosis drug that is widely used in the prevention and treatment of coccidiosis infection in poultry and mammals. However, the drug has poor aqueous solubility (25 °C, 0.41 μg/mL), and its dose escalation for systemic administration remains challenging. We engineered a Tol mixed nanomicelle (TMNM) delivery system based on sodium deoxycholate–Brij C20 polyethylene ether–triton x100 (NaDC–Brij58–Tx100) as surfactants by film hydration method. The physical properties of TMNM were characterized, and the pharmacokinetic parameters of Tol and TMNM were compared. The average particle size, drug loading, saturated solubility, and critical micelle concentration (CMC) of the TMNM system were 12.28 ± 0.48 nm, 3.38 ± 0.12%, 3921.70 ± 0.01 μg/mL (8170-fold compared with Tol), and 0.0172 mg/mL, respectively. Transmission electron microscopy (TEM), scanning electron microscopy (SEM) micrographs, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were performed, and the results showed TMNM formation. Furthermore, the TMNM had greater bioavailability (215%) than the Tol solution. The significant increase in the drug solubility and bioavailability of TMNM suggested the TMNM is a potential oral and parenteral delivery system for Tol and has wide application prospects in the clinical context.