BIOLOGICAL SAFETY EVALUATION OF
STEALTH SOLID LIPID NANOPARTICLES OF
RISPERIDONE: EFFECT OF SURFACE
CHARACTERISTICS ON THEIR
HYDROPHOBICITY, HAEMOLYSIS AND
MACROPHAGE PHAGOCYTOSIS
JALEH VARSHOSAZ1*, HOJJAT SADEGHI2, FAEZEH SHAFIPOUR1
1 Department of Pharmaceutics, Faculty of Pharmacy and Isfahan
Pharmaceutical Sciences Research Centre, Isfahan University of Medical
Sciences, Isfahan, Iran.
2 Department of Biotechnology, Faculty of Pharmacy and Isfahan
Pharmaceutical Sciences Research Centre, Isfahan University of Medical
Sciences, Isfahan, Iran.
*Corresponding author: varshosaz@pharm.mui.ac.ir
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Abstract:

The aim of this study was to prepare stealth solid lipid nanoparticles (SLNS) 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% PEG40 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 SLNS of risperidone are suitable for i.v. administration..

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