Itraconazole-loaded micelles based on linear-dendritic poly (ethylene glycol)-b-poly (ε-caprolactone)

Abstract

A copolymeric micelle formulation of itraconazole (ITR-M) was prepared using linear-dendritic monoallyloxy poly (ethylene glycol)-b-poly (ε-caprolactone) (APEG-PCL) as drug carrier materials. DL and EE values of ITR-M were 5.70 ± 0.12% and 91.30 ± 1.90%, respectively. The micelle formulation enhanced the ITR solubility up to 30.42 μg/mL. In vitro release of ITR from the ITR-M was mainly drug diffusion process followed by the copolymer’s degradation. ITR-M showed similar anti-Candida albicans activity to that of crude ITR although its release of ITR was slow and continuous. The in vivo pharmacokinetic study demonstrated that the ITR-M could improve tissue distribution of ITR. In conclusion, APEG-PCL could be a potential carrier in the development of antifungal drug delivery system.

Keywords:

• Antifungal
• Itraconazole
• Linear-dendritic copolymer
• Micelles

Additional information

Funding

This work is supported by [Natural Science Foundation of Shandong Province] under Grant [number ZR2016BL15]; and [Science and Technology Project of University of Jinan] under Grant [number XKY1732].