The present study describes the preparation of a dodecapeptide YHWYGYTPQNVI (GE11)-conjugated liposome bound with polyethylene glycol to enhance the therapeutic effect of resveratrol (RSV) in head and neck cancer cells. The results indicated that (RSV)-loaded GE11-conjugated liposomes (RSV-GL) exhibited a high entrapment efficiency of >95%, with an active drug loading level of 19.5% w/w. Release kinetics revealed that RSV was released in a slow and sustained manner from the RSV-GL and RSV-loaded liposome (RSV-L) nanoparticulate systems. The epidermal growth factor receptor (EGFR)-overexpressing squamous cell carcinoma HN cells specifically internalized GE11 surface-conjugated liposome in a manner that was markedly increased compared with that of the non-targeted carrier. Consistently, RSV-GL exhibited a significantly increased cytotoxic effect compared with that of the non-targeted nanoparticles. Notably, RSV-GL induced significantly increased proportions of early (~60%) and late (~10%) apoptotic cells in head and neck cancer cell populations. To the best of our knowledge, the application and development of EGFR-targeted peptide-conjugated liposome system for RSV delivery has not been studied previously in the treatment of head and neck cancer. In addition, RSV-GL exhibited the greatest antitumor efficacy compared with any other group. RSV-GL exhibited a 2-fold decrease in tumor volume compared with the free RSV and a 3-fold decrease in volume compared with the control. Overall, the nanomedicine strategy described in the present study may potentially advance the chemotherapy-based treatment of head and neck cancer, with promising applications in other EGFR-overexpressing tumors.

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