Abstract

Increased human epidermal growth factor receptor 2 (HER2) expression is a hallmark of HER2+ breast cancer. HER2 promotes the growth of cancer cells and makes them particularly aggressive. Currently, trastuzumab is the only HER2-targeted therapeutic agent approved by the FDA for HER2-overexpressing breast cancer treatment. However, clinical efficacy of trastuzumab is limited greatly by the occurrence of drug resistance. In this study, an aptamer (HA1) specific for HER2-overexpressing breast cancer cells was selected using Cell-SELEX. This allowed the development of grapefruit-derived nanovectors (GNVs) conjugated with HA1 that targeted specifically HER2+ breast cancer cells. In vitro experiments demonstrated that HA1 effectively promoted the internalisation of GNVs into cancer cells and tumour spheroids. In vivo data showed that drug delivery to tumour tissues and antitumor activities were dramatically enhanced by conjugating HA1 with drug-loaded GNVs. This study indicates that aptamers mediating targeted drug delivery by GNVs represent a promising strategy for HER2+ breast cancer therapy.