The aim of the present study was to develop a poly-arginine modified nanostructured lipid carrier(R-NLC) by fusion-emulsification method and to test its pharmaceutical characteristics. The influence of R-NLC on A549 c...The aim of the present study was to develop a poly-arginine modified nanostructured lipid carrier(R-NLC) by fusion-emulsification method and to test its pharmaceutical characteristics. The influence of R-NLC on A549 cells like cellular uptake and cytotoxicity was also appraised using unmodified NLC as the controlled group. As the results revealed, R-NLC had an average diameter of about 40 nm and a positive zeta potential of about +17 mv, the entrapment efficiency decreased apparently, and no significant difference on the in vitro drug release was found after R8-modification. The cellular uptake and cytotoxicity increased obviously compared with unmodified NLC. The cellular uptake mechanisms of R-NLC involved energy, macropinocytosis, clathrin-mediated endocytosis, and caveolin-mediated endocytosis. The outcomes of the present study strongly support the theory that cell penetrating peptides have the ability of enhancing the cellular uptake of nanocarriers.展开更多
基金the support of the National Natural Science Foundation of China (No. 81273447)the General projects of the Department of Education, Heilongjiang Province (No. 12531787)
文摘The aim of the present study was to develop a poly-arginine modified nanostructured lipid carrier(R-NLC) by fusion-emulsification method and to test its pharmaceutical characteristics. The influence of R-NLC on A549 cells like cellular uptake and cytotoxicity was also appraised using unmodified NLC as the controlled group. As the results revealed, R-NLC had an average diameter of about 40 nm and a positive zeta potential of about +17 mv, the entrapment efficiency decreased apparently, and no significant difference on the in vitro drug release was found after R8-modification. The cellular uptake and cytotoxicity increased obviously compared with unmodified NLC. The cellular uptake mechanisms of R-NLC involved energy, macropinocytosis, clathrin-mediated endocytosis, and caveolin-mediated endocytosis. The outcomes of the present study strongly support the theory that cell penetrating peptides have the ability of enhancing the cellular uptake of nanocarriers.
