Abstract

In the following research, we specifically assessed the feasibility of a novel AS-1411-chitosan (CS)-gold nanoparticle (AuNPs) delivery system to carry methotrexate (MTX) into the cancer cells. The designed system had a spherical shape with average size of 62 ± 2.4 nm, the zeta potential of -32.1 ± 1.4 mV, and released MTX in a controlled pH- and time-dependent manner. CS-AuNPs could successfully penetrate the breast cancer cells and release the therapeutic drug, and ultimately, be accumulated by the nucleolin-AS1411 targeting mechanism within the in vivo environment. The anticancer activity of MTX was attributed to the induction of mitochondria membrane potential loss and nuclear fragmentation, which leads to apoptotic death. Moreover, the cellular internalization confirmed the high potential in the elimination of cancer cells without notable cytotoxicity on non-target cells. Therefore, it was concluded that the AS1411-CS-AuNPs with considerable in vitro and in vivo results could be utilized as a favorable system for breast cancer treatment. © 2022 Maryamsadat Shahidi et al., published by De Gruyter.