Quatiepine, an effective atypical anti psychotic administered as fumarate or hemifumarate salts by intravenous
injection shows poor brain uptake due to low partitioning and/or Pgp efflux. In order to improve their brain availability,
solid lipid nanoparticles (SLN) loaded with Quetiapine fumarate or hemifumarate were prepared using glyceryl
monostearate (GMS), poloxamer 407 and hydrogenated soya phosphatidylcholine (HSPC) as stabilizers–using a hot melt
emulsification high- pressure homogenization technique. They were characterized for physical characteristics like particle
size, polydispersity (PDI), shape and entrapment efficiency (EE). Fomulation and process parameters were optimized
based on particle size, PDI and EE. SLNs with a mean particle size of 101.1 nm were obtained for quetiapine fumarate
and 93.6 nm for quetiapine hemifumarate. In vitro drug release study showed the release followed Higuchi kinetics model
for both the formulations. In vivo studies showed a significant increase in the percentage of drug reaching the brain when
administered in the form of SLN’s as compared to the respective drug solutions and the increase was greater in case of
quetiapine hemifumarate salt.
Keywords: Brain delivery, parentral, quetiapine fumarate, quetiapine hemifumarate schizophrenia, solid lipid nanoparticles.
Rights & PermissionsPrintExport