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Biological Safety Evaluation of Stealth Solid Lipid Nanoparticles of Risperidone: Effect of Surface Characteristics on Their Hydrophobicity, Haemolysis and Macrophage Phagocytosis



Varshosaz J1 ; Sadeghi H2 ; Shafipour F1
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Authors Affiliations
  1. 1. Department of Pharmaceutics, Faculty of Pharmacy and Isfahan Pharmaceutical Sciences Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran
  2. 2. Department of Biotechnology, Faculty of Pharmacy and Isfahan Pharmaceutical Sciences Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran

Source: Farmacia Published:2012

Abstract

The aim of this study was to prepare stealth solid lipid nanoparticles (SLN S) of risperidone, for controlled delivery through the intravenous (i.v.) route to reduce the frequency of administration, dose and adverse effects during the short-term management of manifestation of psychotic disorders. Stealth SLNs were prepared by emulsification-solvent diffusion and sonication method by adding acetone/ethanol containing drug, lipid and stabilizer to aqueous phase, containing surfactant, under homogenization. The effect of lipid type, lipid percentage, stabilizer type and stabilizer percentage were evaluated on the particle size, zeta potential, drug loading efficiency and drug release for optimization of SLNs. Dialysis bag membrane was used to determine drug release, the Rose Bengal binding constant for surface hydrophobicity and serum protein adsorption. The cytotoxicity of SLNs on macrophages and red blood cells were also assessed in order to evaluate the impact of surface modifications on toxicity of the different formulations. The optimized formulation was composed of 0.05% stearyl alcohol (relative to the total volume of dispersion) and 25% PEG 40 stearate (relative to the weight of lipid) using a homogenization speed of 1000 rpm and 4 minutes sonication. The results showed that the in vitro specifications of stealth SLN S of risperidone are suitable for i.v. administration.
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