| Autor: |
Tan, Jiangbing, Jing, Pei, Xiao, Xiao, Liao, Yulong, Liao, Chunyan, Zhang, Shiyong |
| Zdroj: |
SCIENCE CHINA Chemistry; Sep2023, Vol. 66 Issue 9, p2654-2663, 10p |
| Abstrakt: |
The H2O2-triggered prodrug activation represents a hot topic while the low H2O2 level of cancer cells hindered the complete activation of parent drugs and resulted in the poor therapeutic effect. Here, we developed an H2O2 amplifier fabricated by cross-linked lipoic acid nanocapsules (cLANCs), which would selectively elevate the intracellular H2O2 level of cancer cells 3.4-fold higher than that of untreated cancer cells so as to speed up the activation of parent drug from the loaded prodrugs (Pro-5-FU). The cytotoxicity showed that the killing effect of Pro-5-FU loaded in cLANCs (Pro-5-FU@cLANCs) arrived up to 1.6-time higher than that of Pro-5-FU alone against A549 cells, and was even close to free 5-FU. The in vivo anticancer evaluation gave the tumor inhibition rate (TIR) and survival rate (SR) of Pro-5-FU@cLANCs against A549 tumor-bearing nude mice up to 73.1% and 80%, respectively, much higher than those of Pro-5-FU (TIR: 41.2%, SR: 20%) or free 5-FU (TIR: 50.6%, SR: 0%). This nanodrug constructed the first example that utilizes the drug carriers as H2O2 amplifier to strengthen the prodrug activation. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
|
Full text from SpringerLink