{Reference Type}: Journal Article
{Title}: Riboflavin-targeted polymers improve tolerance of paclitaxel while maintaining therapeutic efficacy.
{Author}: Darguzyte M;Rama E;Rix A;Baier J;Hermann J;Rezvantalab S;Khedri M;Jankowski J;Kiessling F;
{Journal}: Nanomedicine
{Volume}: 58
{Issue}: 0
{Year}: 2024 Jun 3
{Factor}: 6.458
{DOI}: 10.1016/j.nano.2024.102751
{Abstract}: Active targeting can enhance precision and efficacy of drug delivery systems (DDS) against cancers. Riboflavin (RF) is a promising ligand for active targeting due to its biocompatibility and high riboflavin-receptor expression in cancers. In this study, RF-targeted 4-arm polyethylene glycol (PEG) stars conjugated with Paclitaxel (PTX), named PEG PTX RF, were evaluated as a targeted DDS. In vitro, PEG PTX RF exhibited higher toxicity against tumor cells compared to the non-targeted counterpart (PEG PTX), while free PTX displayed the highest acute toxicity. In vivo, all treatments were similarly effective, but PEG PTX RF-treated tumors showed fewer proliferating cells, pointing to sustained therapy effects. Moreover, PTX-treated animals' body and liver weights were significantly reduced, whereas both remained stable in PEG PTX and PEG PTX RF-treated animals. Overall, our targeted and non-targeted DDS reduced PTX's adverse effects, with RF targeting promoted drug uptake in cancer cells for sustained therapeutic effect.