Targeted Delivery of Raloxifene via RGD-functionalized Chitosan Nanoparticle Selectively Attenuates Breast Tumor Growth

Breast cancer is one of the most frequently diagnosed cancers among women around the globe. It is usually addressed through chemotherapy, radiation, and surgical interventions—methods that are often hindered by toxicity, non-specificity, and resistance to drugs. This study, presented at ICRAN 2025, introduces a nanotechnology-based strategy that uses RGD peptide-conjugated chitosan nanoparticles (RGD-CHNPs) for the targeted treatment of breast cancer. Raloxifene (Rlx), a selective estrogen receptor modulator, was incorporated into these nanoparticles to boost therapeutic effectiveness. The RGD-CHNPs demonstrated improved stability and cellular absorption in the acidic tumor environment typical of breast cancer. By targeting the αvβ3 integrin by the conjugation of RGD enhanced the efficient delivery of Rlx to cancer cells, inducing apoptosis and inhibiting both migration and angiogenesis. In vivo imaging validated the selective accumulation of Cy5.5-labeled RGD-CHNPs within tumors, and the Rlx-RGD-CHNPs substantially decreased tumor growth without harming normal tissues. These results highlight the complementary advantages of pH responsiveness and RGD-mediated targeting, positioning RGD-CHNPs as an encouraging platform for safe and effective treatment of breast cancer.