Brain-targeted
Tempol-loaded
poly-(lactide-co-glycolide) (PLGA) nanoparticles (NPs) conjugated with a
transferrin antibody (OX 26) were developed using the nanoprecipitation method. These NPs may have utility in treating
neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease. Central to these diseases is an increased production of reactive
oxygen and
nitrogen species which may take part in the development of these conditions. As proof of principle, the NPs were loaded with
Tempol, a
free radical scavenger that has been shown to be protective against oxidative insults. To enhance the delivery of NPs to the central nervous system (CNS), we conjugated the
transferrin receptor antibody covalently to PLGA NPs using the NHS-PEG3500-Maleimide crosslinker. The NPs showed a particle size suitable for blood brain barrier (BBB) permeation (particle size 80-110 nm) and demonstrated a sustained drug release behavior. A high cellular uptake of antibody-conjugated NPs was demonstrated in RG2 rat
glioma cells. The ability of the
Tempol-loaded NPs to prevent cell death by
resveratrol in RG2 cells was determined using the MTT assay. The conjugated NPs containing
Tempol were more effective in preventing cell viability by
resveratrol when compared with unconjugated NPs or free
Tempol in
solution. Our findings suggest that
transferrin-conjugated NPs containing
antioxidants may be useful in the treatment of
neurodegenerative diseases.