RESUMEN
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 GE11conjugated liposomes (RSVGL) 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 RSVGL and RSVloaded liposome (RSVL) nanoparticulate systems. The epidermal growth factor receptor (EGFR)overexpressing squamous cell carcinoma HN cells specifically internalized GE11 surfaceconjugated liposome in a manner that was markedly increased compared with that of the nontargeted carrier. Consistently, RSVGL exhibited a significantly increased cytotoxic effect compared with that of the nontargeted nanoparticles. Notably, RSVGL 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 EGFRtargeted peptideconjugated liposome system for RSV delivery has not been studied previously in the treatment of head and neck cancer. In addition, RSVGL exhibited the greatest antitumor efficacy compared with any other group. RSVGL exhibited a 2fold decrease in tumor volume compared with the free RSV and a 3fold decrease in volume compared with the control. Overall, the nanomedicine strategy described in the present study may potentially advance the chemotherapybased treatment of head and neck cancer, with promising applications in other EGFRoverexpressing tumors.