Preparation and Pharmacokinetic Study of Mebendazole Complex with HPbeta-Cyclodextrin

Charles Ding¹Yili Ding^1*zhe xu¹Peini Wang¹Shufeng Xu²

• ¹College of Science, Mathematics and Technology, Kean University-Wenzhou, Wenzhou, Zhejiang Province, China
• ²Life Science Department, Foshan University, Foshan, Guangdong Province, China

to expel intestinal parasite infections, was found to exhibit multiple anti-cancer activities. However, due to the poor water-solubility (0.33 ± 0.02 µg/mL), its clinical applications were greatly limited. Scientists in Wenzhou-Kean university have developed a formulation that could increase its water solubility as much as 18333 times to reach 6.05 mg/mL as the best result so far. Through the complexation with HPbeta-cyclodextrin, 80% of mebendazole in the complex was released in vitro in five min., and only 20% of Mebendazole was released under the same conditions for the pure drug, in dog's in vivo pharmacokinetic study with a dose of 5 mg/kg, the Cmax of Mebendazole was increased from 8.96 ± 0.15 μg/mL to 17.34 ± 2.02 μg/mL, Tmax of Mebendazole was shorted from 12.00 ± 0.50 hours to 10 ± 0.50 hours, the half lift time was prolonged from 5.81 ± 0.36 hours to 10.01 ± 2.07 hours, the AUC0-24 was increased from 151.32 ± 5.92 μg•h/mL to 289.02 ± 15.83 μg•h/mL, and the bioavailability was increased 91%, indicated this complex can be pushed to the next step as an anti-tumor agent for its clinic practice.