A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity

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• 作者：Mingshuang Sun^a ; Yunyun Gao^a ; Zhihong Zhu^a ; Huixin Wang^a ; Cuiyan Han^b ; Xinggang Yang^a ; Weisan Pan^a ; ^{pppwwwsss@163.com}
• 关键词：Poly-arginine ; NLC ; Cellular uptake ; Mechanisms ; Cytotoxicity
• 刊名：Asian Journal of Pharmaceutical Sciences
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：12
• 期：1
• 页码：51-58
• 全文大小：1225 K
• 卷排序：12

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.