Cationic solid lipid nanoparticles with primary and quaternary amines for release of saquinavir and biocompatibility with endothelia

Application of cationic solid lipid nanoparticles (CSLNs), comprising complex internal matrix and lipid-regulated external surface, is an intriguing issue in current bionanotechnology. This study presents dissolution kinetics of saquinavir (SQV) from CSLNs with cholesterol-mediated esterquat 1 (EQ 1) and biocompatibility of SQV-loaded CSLNs with human brain-microvascular endothelial cells (HBMECs). CSLNs with SQV in lipid cores containing cholesterol were dissolved and incubated with HBMECs. The results revealed that an increase in the weight percentage of EQ 1 reduced the entrapment efficiency of SQV. In addition, 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). The dissolution profiles demonstrated that the mediation of cholesterol favored the sustained release of SQV. When the weight percentage of EQ 1 increased, the viability of HBMECs enhanced. An increase in the weight percentage of cholesterol, however, reduced the viability of HBMECs. The innovated CSLNs containing cholesterol can be effective in controlled release of SQV without inducing significant endothelial toxicity.

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► An increase in the weight percentage of EQ 1 reduced the entrapment efficiency of SQV in CSLNs.
► 25% (w/w) cholesterol yields the maximal entrapment efficiency of SQV in CSLNs.
► Cholesterol-mediated hydrogen bonds favor the sustained release of SQV.
► When the weight percentage of EQ 1 increases, the viability of endothelia enhances.
► An increase in the weight percentage of cholesterol reduces the viability of endothelia.