EGF-liposomes promote efficient EGFR targeting in xenograft colocarcinoma model

Abstract

Aim: Development of EGF-liposomes (LP-EGF) for selective molecules delivery in tumors expressing EGFR.

Material & methods: In vitro cellular interaction of EGF-LP and nontargeted liposomes (LP-N) was assayed at 37 and 4 °C in cells expressing different EGFR levels. Receptor-mediated uptake was investigated by competition with a monoclonal antibody anti-EGFR. Selective intracellular drug delivery and efficacy was tested by oxaliplatin encapsulation. In vivo biodistribution of LP-N and LP-EGF was done in xenograft model.

Results: LP-EGF was internalized by an active and selective mechanism through EGFR without receptor activation. Oxaliplatin LP-EGF decreased IC50 between 48 and 13% in cell EGFR+. LP-EGF was accumulated in tumor over 72 h postdosing, while LP-N in spleen.

Conclusion: LP-EGF represents an attractive nanosystem for cancer therapy or diagnosis.

Keywords: EGF; EGFR; cetuximab; colorectal cancer; oxaliplatin; targeted liposomes.