A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
A systematic in vitro investigation on poly-arginine modified nanostructured lipid carrier: Pharmaceutical characteristics, cellular uptake, mechanisms and cytotoxicity
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DOI：
10.1016/j.ajps.2016.07.007
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发表时间：
2016-08
影响因子：
10.2
通讯作者：
Mingshuang Sun;Yunyun Gao;Zhihong Zhu;Huixin Wang;Cuiyan Han;Xing-gang Yang;W. Pan
中科院分区：
文献类型：
--
作者：
Mingshuang Sun;Yunyun Gao;Zhihong Zhu;Huixin Wang;Cuiyan Han;Xing-gang Yang;W. Pan
本研究的目的是通过融合乳化法制备聚精氨酸修饰的纳米结构脂质载体（R-NLC），并测试其药物特性。以未修饰的NLC为对照组，评价R-NLC对A549细胞的细胞摄取和细胞毒性的影响。结果表明，r8修饰后的R-NLC平均直径约为40 nm， zeta电位约为+17 mv，包封效率明显降低，体外释药效果无显著差异。与未修饰的NLC相比，细胞摄取和细胞毒性明显增加。R-NLC的细胞摄取机制包括能量、巨胞吞、网格蛋白介导的内吞作用和小窝蛋白介导的内吞作用。本研究的结果有力地支持了细胞穿透肽具有增强纳米载体的细胞摄取能力的理论。
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 thein vitrodrug 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.