组氨酸
中国仓鼠卵巢细胞
肽
细胞穿透肽
内吞作用
化学
药物输送
生物物理学
精氨酸
氨基酸
脂质体
细胞
膜
生物化学
生物
受体
有机化学
作者
Lei Zhang,Xu Jiang,Feng Wang,Yong Ding,Toby Wang,Grace Jin,Matthew Martz,Zhongzheng Gui,Pingkai Ouyang,Pu Chen
出处
期刊:Langmuir
[American Chemical Society]
日期:2019-01-23
卷期号:35 (9): 3513-3523
被引量:44
标识
DOI:10.1021/acs.langmuir.8b03175
摘要
In this work, we report a drug delivery system based on the pH-responsive self-assembly and -disassembly behaviors of peptides. Here, a systematically designed histidine-rich lipidated peptide (NP1) is presented to encapsulate and deliver an anticancer drug ellipticine (EPT) into two model cells: non-small-cell lung carcinoma and Chinese hamster ovary cells. The mechanism of pH-responsive peptide self-assembly and -disassembly involved in the drug encapsulation and release process are extensively investigated. We found that NP1 could self-assemble as a spherical nanocomplex (diameter = 34.43 nm) in a neutral pH environment with EPT encapsulated and positively charged arginine amino acids aligned outward and EPT is released in an acidic environment due to the pH-triggered disassembly. Furthermore, the EPT-encapsulating peptide could achieve a mass loading ability of 18% (mass of loaded-EPT/mass of NP1) with optimization. More importantly, it is revealed that the positively charged arginine on the periphery of the NP1 peptides could greatly facilitate their direct translocation through the negatively charged plasma membrane via electrostatic interaction, instead of via endocytosis, which provides a more efficient uptake pathway.
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