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.
Department of Chemical Engineering, National Chung Cheng University, Chia-Yi 62102, Taiwan, ROC. chmyck@ccu.edu.tw
Yung-Chih
YC
Kuo
Cheng-Chin
CC
Wang
D000588:Amines / Q000737:chemistry*; D001672:Biocompatible Materials; D001921:Brain / Q000166:cytology; D002412:Cations / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects; D002784:Cholesterol / Q000737:chemistry; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D042783:Endothelial Cells / Q000187:drug effects; D004727:Endothelium / Q000187:drug effects*; D017320:HIV Protease Inhibitors / Q000008:administration & dosage* / Q000737:chemistry; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D019258:Saquinavir / Q000008:administration & dosage* / Q000737:chemistry; D012997:Solvents
D000588:Amines; D001672:Biocompatible Materials; D002412:Cations; D004337:Drug Carriers; D017320:HIV Protease Inhibitors; D007202:Indicators and Reagents; D008055:Lipids; D012997:Solvents; D002784:Cholesterol; D019258:Saquinavir