| Summary: | 博士 === 國立中正大學 === 化學工程研究所 === 101 === Innovated cationic solid lipid nanoparticles (CSLNs) containing cacao butter, cholesterol, stearylamine, and esterquat 1 (EQ 1) were fabricated. The effect of noncovalent interactions, lipid matrix and surface molecular composition on the electrophoretic mobility, zeta potential and particle size of CSLNs were investigated. The fixed charge density on CSLNs was evaluated using Ohshima’s soft particle theory. In addition, the entrapment and release of SQV in CSLNs with the mediation of cholesterol were also studied. The cytotoxicity of CSLNs to human brain-microvascular endothelial cells (HBMECs) was assessed. The permeability across the blood–brain barrier (BBB) using SQV-loaded CSLNs (SQV-CSLNs) was estimated by an in vitro model comprising a monolayer of human brain-microvascular endothelial cells (HBMECs) with regulation of human astrocytes (HAs). The results revealed that the average diameter of CSLNs is in the range from 88 ± 9 nm to 275 ± 16 nm, and decreased when the weight percentage of cholesterol and EQ 1 increased. X-ray photoelectron spectroscopy and Fourier-transform infrared spectroscopy evidenced strong noncovalent interactions between cholesterol and EQ 1. In addition, an increase in the weight percentage of cholesterol and EQ 1 led to an increase in electrophoretic mobility, zeta potential, and fixed charge density of CSLNs. The results also indicated that an increase in the weight percentage of EQ 1 reduced the entrapment efficiency of SQV. The entrapment efficiency of SQV enhanced, when the weight percentage of cholesterol increased from 0% to 25% (w/w). The reverse was true when cholesterol increased from 0% to 75% (w/w). When the weight percentage of EQ 1 increased, the viability of HBMECs enhanced. An increase in the weight percentage of cholesterol reduced the viability of HBMECs. An increase in the weight percentage of cholesterol and EQ 1 also enhanced the BBB permeability of SQV and promoted the uptake of SQV-CSLNs by HBMECs. Moreover, the fluorescent staining demonstrated that SQV-CSLNs could be internalized by HBMECs.
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