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Abstract
The blood-brain barrier is a major barrier in the neurological diseases treatment and precludes the entry of drugs from blood to brain. Here, we developed 29-amino-acid peptide derived from rabies virus glycoprotein (RVG29) peptide conjugated itraconazole-loaded albumin nanoparticles (RVG29-ITZ-NPs). The RVG29 peptide was conjugated to the albumin NPs using biotin-binding streptavidin as crosslinker. The NPs were characterized in terms of particle size, zeta potential, drug loading and release behavior in vitro. Cellular uptake of RVG29-ITZ-NPs was investigated by flow cytometry. Pharmacokinetics and brain distribution of RVG29-ITZ-NPs were investigated after intravenous administration of NPs. The particle size of RVG29-ITZ-NPs was 89.3 ± 1.9 nm as determined by dynamic light scattering. The zeta potential of RVG29-ITZ-NPs was −33.1 ± 0.9 mV. RVG29-ITZ-NPs exhibited a sustained release profile within 24 h. In vitro cellular uptake studies demonstrated that RVG29 significantly facilitated the intracellular delivery of NPs. A significant (P < 0.05) accumulation of ITZ in brain was observed for RVG29-ITZ-NPs as compared with ITZ-NPs and cyclodextrin formulation of ITZ (ITZ-CD). These results suggested that RVG29-ITZ-NPs can be exploited as a potential therapeutic formulation for the intracranial fungal infection.
Acknowledgements
We are very grateful to Prof. Yaocheng Rui, Department of Pharmacology, School of Pharmacy, The second Military Medical University, for providing the bEnd.3 cell line.
Declaration of interest
This work was supported by National Basic Research Program of China (973 Program, No. 2007CB935800), National Science and Technology Major Project (No. 2009ZX09310-006) and Shanghai key Technologies R&D Program (No. 074319117).