Journal
DRUG DELIVERY
Volume 28, Issue 1, Pages 995-1006Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/10717544.2021.1928794
Keywords
Targeting peptide; nanoparticles; polyethyleneimine; siRNA; antitumor
Categories
Funding
- National Natural Science Foundation of China [82003698]
- Scientific and Technological Innovation Programs of Higher Education Institutions in Shanxi (STIP) [2019L0447]
- Applied Basic Research Programs of Shanxi Province [201901D211336]
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The study designed and prepared a novel siRNA delivery system, cRGD-PSH-NP, which showed excellent gene silencing and antitumor activity in HepG2 cells. In vivo, cRGD-PSH-NP/S demonstrated potent tumor inhibition in HepG2-bearing nude mice without inducing toxicity, suggesting further research potential in hepatocarcinoma therapy.
The effective delivery system plays an important role in the application of siRNA in the antitumor study. However, until now, researches on the delivery systems targeting hepatocarcinoma cells are still being explored. Here we designed and prepared a novel siRNA delivery system, cRGD-PSH-NP, which was based on a modified polyethyleneimine (PSH) and DSPE-PEG(2000)-cRGD. cRGD-PSH-NP loaded with survivin siRNA (cRGD-PSH-NP/S) was composed of egg phosphatidylcholine, cationic PSH, PEGylated lipids, survivin siRNA, and cRGD peptide as a targeting ligand. The formulations of cRGD-PSH-NP/S were optimized and characterized. In vitro investigations showed excellent gene silencing and antitumor activity compared with the unmodified nanoparticles in HepG2 cells. In vivo antitumor efficacy of cRGD-PSH-NP/S exhibited potent tumor inhibition (74.71%) in HepG2-bearing nude mice without inducing toxicity. These data suggested further research of cRGD-PSH-NP/S in hepatocarcinoma therapy.
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