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Merck

Lipid nanoparticles for administration of poorly water soluble neuroactive drugs.

Biomedical microdevices (2017-05-21)
Elisabetta Esposito, Markus Drechsler, Paolo Mariani, Federica Carducci, Michela Servadio, Francesca Melancia, Patrizia Ratano, Patrizia Campolongo, Viviana Trezza, Rita Cortesi, Claudio Nastruzzi
ZUSAMMENFASSUNG

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 obtain biocompatible and non-toxic vehicles, able to increase the solubility of the considered neuroactive drugs. To improve URB597 targeting to the brain, stealth nanoparticles were produced modifying the SLN surface with polysorbate 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 this kind of vehicle as alternative to unphysiological mixtures usually employed for animal and clinical studies.

MATERIALIEN
Produktnummer
Marke
Produktbeschreibung

Tristearin, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
URB597, ≥98% (HPLC), powder