We have synthesized the LiYF4:Ce3+ nanoparticles – Methotrexate (MTX), targeting pancreatic cancer cells via folate receptors. Under ultralow 0.1 Gy X-ray irradiation (the lowest dose in the world, for 2-3 times), the nanoparticles can exhibit radiosensitization effect,radiosensitizing chemotherapy, because of MTX released by X-ray inducing photocleavage of NPA linker. The dual sensitization effect will enhance ROS production, DNA damage, cell cycle S phase arrest in pancreatic cancer cells. We have also demonstrated the excellent efficacy in AsPC-1PANC-1 xenografted pancreatic mice.

The nanoparticle-MTX drug we developed has several characteristics (1) Folate receptor-guided MTX targeting to treat pancreatic cancer (2) X-ray control of MTX releasethen MTX-inducing chemosensitizing radiotherapy (3) Non-high Z metal material as LiYF4: Ce3+ nanomaterials (4) Only need to use the lowest X-ray dose in the world: 0.1Gy, total for 2-3 times, equivalent to 4 times of radiation doses in receiving abdominalpelvic computerized tomography scan, by which can lead to increase ROS production, DNA damage, cell cycle arrest at S phase, eventually pancreatic cancer cell death.

The nanoparticle-MTX can target deep pancreatic tumor site through folate receptors. Clinically, it would combine ultralow-dose radiotherapy to inhibit tumor growthreduce the side effect of high-dose mono chemotherapyradiotherapy. Synchronization of nanoparticle sensitizationradiosensitizing chemotherapy may significantly prolong the survival of cancer patients. In the future, we will also commercialize this technology through industry-academia cooperation to provide the new nanoplatform for clinical pancreatic tumor treatment.

天使投資人、策略合作夥伴