title: Preparation, characterization and biocompatibility studies on risperidone-loaded solid lipid nanoparticles (SLN): high pressure homogenization versus ultrasound.
abstract: The suitability of solid lipid nanoparticles (SLN) for the encapsulation of risperidone (RISP), an antipsychotic lipophilic drug, was assessed for oral administration. The hot high pressure homogenization (HPH) and the ultrasound (US) technique were used as production methods for SLN. All the studies on the SLN formulations were done in parallel, in order to compare the results and conclude about the advantages and limitations of both techniques. The particle sizes were in the nanometer range for all prepared SLN formulations and the zeta potential absolute values were high, predicting good long-term stability. Optical analyses demonstrated the achievement of stable colloidal dispersions. Physicochemical characterization of dispersions and bulk lipids, performed by differential scanning calorimetry (DSC) and X-ray assays, support prediction of occurrence of drug incorporation in the SLN and good long term stability of the systems. The toxicity of SLN with Caco-2 cells and the existence of contaminations derived from the production equipments were assessed by the (4,5-dimethylthiazol-2-yl)2,5-diphenyl-tetrazolium bromide (MTT) assay. The results showed 90% of cell viability after SLN exposure, with no significant differences within all prepared formulations (p > 0.05). From this study, we conclude that SLN can be considered as efficient carriers for RISP encapsulation. Moreover, HPH and US revealed to be both effective methods for SLN production.
authors.affiliation: Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, Porto University, 4200-047 Porto, Portugal. ana.silva@ff.up.pt
authors.forename: A C
authors.initials: AC
authors.lastname: Silva
authors.forename: E
authors.initials: E
authors.lastname: González-Mira
authors.forename: M L
authors.initials: ML
authors.lastname: García
authors.forename: M A
authors.initials: MA
authors.lastname: Egea
authors.forename: J
authors.initials: J
authors.lastname: Fonseca
authors.forename: R
authors.initials: R
authors.lastname: Silva
authors.forename: D
authors.initials: D
authors.lastname: Santos
authors.forename: E B
authors.initials: EB
authors.lastname: Souto
authors.forename: D
authors.initials: D
authors.lastname: Ferreira
mesh_terms: D002151:Calorimetry; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D018967:Risperidone / Q000737:chemistry*
chemical_list: D008055:Lipids; D018967:Risperidone