Suchaoin Wongsakorn, Mahmood Arshad, Netsomboon Kesinee, Bernkop-Schnürch Andreas
Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, A-6020 Innsbruck, Austria.
Faculty of Pharmacy, Thammasat University, Rungsit Campus, Phahonyothin Road, Khlong Luang, Pathumthani 12120, Thailand.
Nanomedicine (Lond). 2017 May;12(9):963-975. doi: 10.2217/nnm-2016-0345. Epub 2017 Apr 25.
The aim of this study was to develop zeta-potential-changing nanoparticles (NPs) combining cell-penetrating peptides for gene delivery.
METHODS & MATERIALS: NPs were formed using phosphorylated carboxymethyl cellulose-glucosamine 6-phosphate (CMC-G6P) and polyethylene imine-polyarginine conjugates. Phosphate release was evaluated using intestinal alkaline phosphatase and cell lines. Transfection studies with plasmid DNA were then performed.
The zeta potential of CMC-G6P/branched PEI NPs was -3 mV and switched to +4 mV after intestinal alkaline phosphatase cleavage. The released phosphate in human colon adenocarcinoma cell line was more pronounced than human embryonic kidney cell line 293. Transfection studies demonstrated the greatest expression of plasmid DNA when being incorporated into CMC-G6P/polyethylene imine-polyarginine NPs.
Novel zeta potential changing NPs combining cell-penetrating peptides are a promising tool to deliver DNA drugs to target cells.
本研究旨在开发结合细胞穿透肽用于基因递送的ζ电位变化纳米颗粒（NPs）。
使用磷酸化羧甲基纤维素-6-磷酸葡萄糖胺（CMC-G6P）和聚乙烯亚胺-聚精氨酸共轭物形成纳米颗粒。使用肠道碱性磷酸酶和细胞系评估磷酸盐释放。然后进行质粒DNA的转染研究。
CMC-G6P/支链聚乙烯亚胺纳米颗粒的ζ电位为-3 mV，经肠道碱性磷酸酶切割后转变为+4 mV。在人结肠腺癌细胞系中释放的磷酸盐比人胚肾细胞系293更明显。转染研究表明，当质粒DNA掺入CMC-G6P/聚乙烯亚胺-聚精氨酸纳米颗粒时，其表达量最高。
结合细胞穿透肽的新型ζ电位变化纳米颗粒是将DNA药物递送至靶细胞的一种有前途的工具。
