Preparation, characterization, pharmacokinetics, and tissue distribution of curcumin nanosuspension with TPGS as stabilizer

Abstract

Background: CUR is a promising drug candidate based on its good bioactivity, but use of CUR is potentially restricted because of its poor solubility and bioavailability. Aim: The aim of this study was to prepare an aqueous formulation of curcumin nanosuspension (CUR-NS) to improve its solubility and change its in vivo behavior. Methods: CUR-NS was prepared by high-pressure homogenization method. Drug state in CUR-NS was evaluated by powder X-ray diffraction. Pharmacokinetics and biodistribution of CUR-NS after intravenous administration in rabbits and mice were studied. Results: The solubility and dissolution of CUR in the form of CUR-NS were significantly higher than those of crude CUR. X-ray crystallography diffraction indicated that the crystalline state of CUR in nanosuspension was preserved. Pharmacokinetics and biodistribution results of CUR-NS after intravenous administration in rabbits and mice showed that CUR-NS presented a markedly different pharmacokinetic property as compared to the CUR solution. AUC0−∞ of CUR-NS (700.43 ± 281.53 μg/mL, min) in plasma was approximately 3.8-fold greater than CUR solution (145.42 ± 9.29 μg/mL min), and the mean residence time (194.57 ± 32.18 versus 15.88 ± 3.56 minutes) was 11.2-fold longer. Conclusion: Nanosuspension could serve as a promising intravenous drug-delivery system for curcumin.