Influence of Surfactant and Lipid Type on the Physicochemical Properties and Biocompatibility of Solid Lipid Nanoparticles

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.

Tripalmitin nanoparticle formulations significantly enhance paclitaxel antitumor activity against breast and lung cancer cells in vitro

“…S2B ).These results demonstrate the hemocompatibility of all tripalmitin. NPs assayed and support the previously demonstrated suitability of the solid lipid NPs for in vivo administration 7 , 34 .…”

In vitro cytotoxicity of co-exposure to superparamagnetic iron oxide and solid lipid nanoparticles

“…SLNs were prepared using the ultrasound method as previously described by Patil and Pandit (2007), with slight modifications (Pizzol et al, 2014). Firstly, glycerol monostearate (2% (w/v)) and lecithin S75 surfactant (0.3%) were heated to about 56–70°C.…”

“…The particle size distribution was given by the polydispersity index (PDI). The size and shape of SLNs and SPIONs have been previously determined in our laboratory using transmission electron microscopy (TEM) (Dalmina et al, 2019; Pizzol et al, 2014).…”

“…SPIONs were tested at concentrations ranging from 100 µg/mL to 189 µg/mL, while SLNs were tested from 55 µg/mL to 2200 µg/mL. The concentrations of SPIONs and SLNs were chosen based on previous studies on biomedical applications (Mojica et al, 2013; Pizzol et al, 2014; Silva et al, 2012). The concentration required to reduce the cell viability by 50% (CC 50 ) of SLNs was combined in 1:1 with 189 µg/mL of SPIONs in the co-exposure (MIX) study performed with HEK-293, MCF-7, and MDA-MB-231 cells.…”

Application of Response Surface Method for Preparation, Optimization, and Characterization of Nicotinamide Loaded Solid Lipid Nanoparticles

“… 3 - 5 Their advantages include biocompatibility, safety, stability, ability to be control-released, and ease of large scale production. 6 - 8 SLNs have the ability of delivering hydrophilic drugs through lipid membranes of the body. However, the loading efficiency of hydrophilic drugs is negatively impacted due to their rapid dissolving within the aqueous phase.…”