Targeted delivery of neurological therapeutic to the brain has been attracting more and more attention to the treatment of central nervous system (CNS) diseases. Nonetheless, the main obstacle in this road map is the existence of a blood-brain barrier (BBB) which limits the penetration efficiency of most CNS drugs into the brain parenchyma. This present investigation describes a facile synthetic strategy to prepare a highly biocompatible calcium-doped mesoporous silica nanoparticles (MSNs) functionalized by polysorbate-80 (PS) as targeting ligand to deliver rivastigmine (RV) into the brain via crossing the BBB. The developed nanosystem was characterized by scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), transmission electron microscopy (TEM), Zeta potential, and N2-adsorption-desorption analysis. In vitro hemolysis studies were carried out to confirm the biocompatibility of the nanocarriers. Our in vivo studies in an animal model of rats showed that the RV-loaded nanosystem was able to enhance the brain-to-plasma concentration ratio, brain uptake clearance, and plasma elimination half-life of the drug compared to the free one drug following intravenous (IV) administration. The results revealed that functionalization of MSNs by PS is crucial to deliver RV into the brain, suggesting PS-functionalized MSNs could be an effective carrier to deliver RV to the brain while overcoming BBB.
Keywords: Alzheimer’s disease; Blood-brain barrier; Central nervous system; Drug delivery; Mesoporous silica; Pharmacokinetics.
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