Development of Doxorubicin-Loaded Nanostructured Lipid Carriers: Preparation, Characterization, and In Vitro Evaluation on MCF-7 Cell Line

Abstract

Nanostructured lipid carriers (NLC) are produced using a blend of solid and liquid lipids; this blend is solid at room temperature. NLC is a second generation of lipid nanoparticles, which offer the advantage of improved drug-loading capability and release properties. The purpose of this study was to find the optimized proportion of liquid and solid lipids for production of doxorubicin (Dox)-loaded NLC (Dox-NLC) to decrease the cytotoxicity of Dox. Dox-NLC was prepared by the solvent emulsification/evaporation method using stearic acid (SA) and oleic acid (OA) as the solid lipid and liquid lipid, respectively. Poloxamer 188 and lecithin were used to stabilize NLC dispersion. The physicochemical characteristic and cytotoxicity of Dox-NLC were evaluated. The NLC prepared by 0.6% of stearic acid and 0.4% of oleic acid, showed optimum results with particle size of 134.0 ± 2.3 nm, zeta potential of −19.0 ± 3.9 mV, drug-loading efficiency of 9.5%, and entrapment efficiency of 75%. The drug loading after freeze drying and also after 60 days storage at 4 °C did not change. In vitro drug release study showed that Dox was released from the NLC in a slow but time-dependent behavior. The cytotoxicity of Dox-NLC on MCF-7 cell line was increased compared with the Dox solution. These results suggested that the Dox-NLC produced by this method could be utilized as a sustained release drug carrier system for improving the effectiveness of chemotherapy.