Effect of folate-targeted Erlotinib loaded human serum albumin nanoparticles on tumor size and survival rate in a rat model of glioblastoma

The aim of this study was to prepare folate-targeted Erlotinib loaded human serum albumin nanoparticles (FA-ERL-HSA NPs) and investigate in vitro cytotoxic and apoptotic effects using cell lines (U87MG and C6 cells) and an in vivo rat bearing C6 glioma model. The mean size of the FA-ERL-HSA NPs prepared using a desolvation method was 135 nm. In vitro MTT assays demonstrated that FA-ERL-HSA NPs had an IC50 value of 52.18 mu g/mL and 17.53 mu g/mL compared to free ERL which had an IC50 value of 119.8 mu g/mL and 103.2 mu g/mL for U87MG and C6 cells for 72 h, respectively. Flow cytometry results showed the apoptosis rate with FA-ERL-HSA NPs (100 mu g/mL, 72 h) was higher compared to free ERL for both U87MG and C6 cells. Experiments using a rat glio-blastoma model via TUNEL assay indicated that the apoptosis index of FA-ERL-HSA NPs was 48 % compared to 21 % for free ERL and the tumor size effectively decreased after a daily injection of 220 mu g (2.5 mg/kg) from 87.45 mm3 (19th day) to 1.28 mm3 (60th day). The median survival rate of the rats increased after treatment to >100 days which was greater than controls.

Automated summary

The study aimed to prepare folate-targeted Erlotinib loaded human serum albumin nanoparticles (FA-ERL-HSA NPs) and investigate their cytotoxic and apoptotic effects using cell lines and a rat glioma model. The average size of FA-ERL-HSA NPs prepared using a desolvation method was 135 nm. In vitro experiments showed that FA-ERL-HSA NPs had lower IC50 values and induced higher apoptosis rates compared to free ERL in both cell lines. TUNEL assay indicated that FA-ERL-HSA NPs had a higher apoptosis index and effectively reduced tumor size in the rat model, leading to increased median survival rate.