Xuhong Yang, H S Yang, Nuo Xu, Yini Zhu, Zhengcheng Yun, Haoge Zhang, Jia Miao, Yinzhuo Xie, Lin Gao, Leqian Ying, Lei Dong, Yuqi Wang, Yicheng Ni, Jinbing Xie
Immune checkpoint inhibitors show promise in the treatment of melanoma brain metastases but are limited by CD73/adenosine axis-mediated immune evasion. Directly targeting CD73 with antibodies faces challenges due to poor blood-brain barrier permeability and metabolic regulators within the tumor microenvironment (IL-17-driven HIF-1α/VEGF-A). To overcome these barriers, we developed a nose-to-brain delivery platform using glycerol as a mucosal penetration enhancer to codeliver anti–IL-17 and anti-CD73 antibodies. Glycerol reversibly opened nasal epithelial tight junction proteins, enhancing the brain delivery of anti–IL-17 and anti-CD73 antibodies by 19.4- and 17.1-fold, respectively, while minimizing systemic exposure. Critically, anti–IL-17 attenuated CD73/adenosine axis-mediated immune evasion, significantly boosting anti-CD73 targeting efficacy. Ultimately, this combination promoted CD8 + T cell activation and residency, pro-inflammatory macrophage polarization, and reduced T reg cell infiltration, thereby eliciting a strong antitumor effect. Our results establish an efficient nose-to-brain delivery platform for macromolecules and propose a therapeutic strategy for tumors using anti–IL-17 to overcome TME-imposed limitations in CD73-targeted immunotherapy.