摘要

Poor tumor selectivity and high side toxicity have been frequently reported to hinder the application of chemotherapeutic agents. Thus, combining chemotherapeutic agents with other conventional cancer treatment modalities has attracted great attentions of pharmaceutical industries. Phototherapy has been intensively combined with chemotherapy to improve the biosafety and cytotoxicity. Herein, an ATP aptamer/i-motif-grafted multi-functional SPION nanocarrier (AGS) was constructed to co-deliver a chemotherapeutic agent DNM, and a photosensitizer TMPyP to the tumor tissues. The AGS sized around 60 nm was found well dispersed in water and the drug-loading efficiencies have been calculated to be 68.2% and 39.4% for DNM and TMPyP, respectively. The drug-loaded DDS displayed an ATP/pH dual-responsive drug release in vitro, which further exhibited significant cancer/normal cell selectivity, cellular internalization, high ROS production, cell-cycle arresting, and cell apoptosis against tumor cells. In vivo studies showed that the designed dual-drug DDS has satisfactory body safety and outstanding tumor suppression compared with individual and DNM-TMPyP-combined agents.

  • 单位
    广东药学院