Abstract
Nine types of solid lipid nanoparticle (SLN) formulations were produced using tripalmitin (TPM), glyceryl monostearate (GM) or stearic acid (SA), stabilized with lecithin S75 and polysorbate 80. Formulations were prepared presenting PI values within 0.25 to 0.30, and the physicochemical properties, stability upon storage and biocompatibility were evaluated. The average particle size ranged from 116 to 306 nm, with a negative surface charge around −11 mV. SLN presented good stability up to 60 days. The SLN manufactured using SA could not be measured by DLS due to the reflective feature of this formulation. However, TEM images revealed that SA nanoparticles presented square/rod shapes with an approximate size of 100 nm. Regarding biocompatibility aspects, SA nanoparticles showed toxicity in fibroblasts, causing cell death, and produced high hemolytic rates, indicating toxicity to red blood cells. This finding might be related to lipid type, as well as, the shape of the nanoparticles. No morphological alterations and hemolytic effects were observed in cells incubated with SLN containing TPM and GM. The SLN containing TPM and GM showed long-term stability, suggesting good shelf-life. The results indicate high toxicity of SLN prepared with SA, and strongly suggest that the components of the formulation should be analyzed in combination rather than separately to avoid misinterpretation of the results.
Highlights
The development of nanoparticles has received considerable attention in the pharmaceutical sciences field due to the potential to modulate the pharmacological effect of nanoencapsulating active substances [1,2,3]
A cubic phase occurs in some systems with chain lengths above C14, which structure consist of two interpenetrating networks of rod-like aggregates and it has been suggested from theoretical point of view that there are two fundamentally different alternatives for cubic lipid-water structures, (i) structures with continuous regions of both water and hydrocarbon chains and (ii) structures composed of closed aggregates of ―oil-in-water‖ or ―water-in-oil’’ type, this added to the effects of surfactant could explain the formation of particles with regions showing domains with different electron-densities seen on Transmission Electron Microscopy (TEM), deeper studies should be performed to understand the formation of the presented Solid Lipid Nanoparticles (SLN) [23,24]
The SLNs prepared with stearic acid as the matrix lipid seem to have a pearlized appearance, which impaired the dynamic light scattering (DLS)
Summary
The development of nanoparticles has received considerable attention in the pharmaceutical sciences field due to the potential to modulate the pharmacological effect of nanoencapsulating active substances [1,2,3]. The elucidation of cell responses to the SLN application may provide valuable information for the development of safe and efficient formulations To this end, we prepared SLNs composed of three types of major matrix lipids (tripalmitin, glyceryl monostearate or stearic acid), stabilized with two surfactants (lecithin S75 and polysorbate 80) in three different concentrations. We prepared SLNs composed of three types of major matrix lipids (tripalmitin, glyceryl monostearate or stearic acid), stabilized with two surfactants (lecithin S75 and polysorbate 80) in three different concentrations This set of SLNs was evaluated in terms of physicochemical properties, stability upon storage and biocompatibility, which included extensive analysis of the mechanisms whereby the SLNs interfere with the cell cycle, mitochondrial functioning, enzymes related to the regulation of cell death as well as erythrocyte hemolysis
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