Intranasal administration of brain-targeted HP-β-CD/chitosan nanoparticles for delivery of scutellarin, a compound with protective effect in cerebral ischaemia.

OBJECTIVES: Scutellarin (SCU) is a traditional Chinese medicine used for the treatment of ischaemic cerebrovascular disease, but its clinic applications have been limited due to its poor water solubility, poor bioavailability and short half-life. In comparison with the conventional oral and intravenous administration, nasal administration may help targeting the drug more directly to brain. Thus, we proposed to employ a novel SCU-loaded HP-β-CD/chitosan nanoparticles (CD/CS-SCU-NPs) to deliver SCU to brain through the nasal route.

METHODS: CD/CS-SCU-NPs were prepared by an ionic cross-linking method. The NPs formulation was tested in vivo in C57BL mice. The concentrations of SCU in brain and plasma after intranasal and oral administration of the CD/CS-SCU-NPs and after intranasal administration of SCU solution (SCU-SL) were determined and brain targeting parameters were calculated.

KEY FINDINGS: Compared to the intranasal administration of SCU-SL, intranasal and oral administration of the CD/CS-SCU-NPs increased accumulation of SCU in brain, indicating that CD/CS-SCU-NPs have obvious brain targeting advantage, although the advantage is more evident after intranasal administration.

CONCLUSIONS: Findings from in-vivo study indicated that much higher SCU brain exposure was observed after intranasal administration of the CD/CS-SCU-NPs. Administration of CD/CS-SCU-NPs through the nasal route would have potential to treat ischemic cerebrovascular disease.