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Lipid nanoparticles for administration of poorly water soluble neuroactive drugs



This study describes the potential of solid lipid
nanoparticles and nanostructured lipid carriers as nano-
formulations to administer to the central nervous system
poorly water soluble drugs. Different neuroactive drugs,
i.e. dimethylfumarate, retinyl palmitate, progesterone and
the endocannabinoid hydrolysis inhibitor URB597 have
been studied. Lipid nanoparticles constituted of tristearin
or tristearin in association with gliceryl monoolein were
produced. The nanoencapsulation strategy allowed to ob-
tain biocompatible and non-toxic vehicles, able to increase
the solubility of the considered neuroactive drugs. To im-
prove URB597 targeting to the brain, stealth nanoparticles
were produced modifying the SLN surface with polysor-
bate 80. A behavioural study was conducted in rats to test
the ability of SLN containing URB597 given by intranasal
administration to alter behaviours relevant to psychiatric
disorders. URB597 maintained its activity after
nanoencapsulation, suggesting the possibility to propose


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