Parenteral nanoemulsions of risperidone for enhanced brain delivery in acute psychosis: Physicochemical and in vivo performances.

摘要: Abstract This work aimed to deepen the lately acquired knowledge about parenteral nanoemulsions as carriers for brain delivery of risperidone, a poorly water-soluble antipsychotic drug, through establishing prospective relationship between their physicochemical, pharmacokinetic, biodistribution, and behavioral performances. For this purpose, two optimized risperidone-loaded nanoemulsions, stabilized by lecithin or lecithin/polysorbate 80 mixture, costabilized sodium oleate, were produced high-pressure homogenization. The characterization revealed favorable droplet size, narrow size distribution, high surface charge, with proven stability autoclaving long-term at least one year 25 ± 2 °C. Pharmacokinetic tissue distribution results demonstrated improved plasma, liver, pharmacokinetic parameters, resulting in 1.2–1.5-fold increased relative bioavailability, 1.1–1.8-fold decreased liver 1.3-fold uptake risperidone active moiety following intraperitoneal administration solution rats. In study, investigated showed pronounced reduction basal and, more pertinently, amphetamine-induced locomotor activity rats, an early onset action, effect lasted 90 min after drug injection. Together, these findings corroborate applicability enhanced further suggesting promise acute psychosis treatment other emergency situations.