Preparation and cytotoxicity of lipid nanocarriers containing a hydrophobic flavanone

Abstract

Hesperetin is a flavanone with recognized biological activities. However, such activities are limited due to its restricted aqueous solubility and stability. In this regard, the main aim of this study was to develop and characterize lipid nanocarriers containing hesperetin. Nanostructured lipid carriers (NLC) were prepared using phase inversion temperature method and characterized by size, polydispersity index (PdI), zeta potential, physical stability, TEM analysis, encapsulation efficiency, in vitro release, and in vitro cytotoxic effect in cell line. Lipid nanocarriers presented diameter below 80 nm, narrow PdI (<0.2), and negative zeta potential (–20 mV). Accelerated stability studies of NLC demonstrated good physical stability for a period of 12 months. According to TEM, NLC were almost spherical with particle size <100 nm and homogeneous size distribution. DSC curves showed that formulations presented lipid core with a higher degree of crystalline disorder. Lipid nanocarriers were able to entrap hesperitin with efficiency 72.7 % (±0.92). In vitro release studies confirmed that NLC could modulate hesperetin release during 72 h. In vitro cytotoxicity assay of hesperitin-loaded NLC on T98G glioblastoma grade IV cells presented significant cytotoxic effect. Therefore, NLC were able to encapsulate successfully hesperetin and demonstrated excellent in vitro cytotoxicity on glioblastoma cells.