Synthetic SIGLEC9-based chimeric switch receptor augments the efficacy of CAR macrophages against glioblastoma

Z Zhipeng Fu (State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University) X Xiaotian Zhao (Shenyang National Laboratory for Materials Science Institute of Metal Research Chinese Academy of Sciences) Q Qikang Zhang (Jinan Microecological Biomedicine Shandong Laboratory, Jinan Medical and Health Science and Technology Innovation Industrial Park) M Maosen Han (State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University) J Jing Zhang Z Zhenmei Yang (State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University) Y Yan Wang Z Zichao Yao (State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University) Y Ying Liu C Chunwei Tang (State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University) K Kaiyan Xi (Jinan Microecological Biomedicine Shandong Laboratory, Jinan Medical and Health Science and Technology Innovation Industrial Park) Z Zhanyan Liu (State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University) Y Yi Zhang K Kun Zhao N Na Li Y Yulin Zhang Y Yudong Song (State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University) X Xinyi Jiang (State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University) C Chen Chen

Abstract

Chimeric antigen receptor macrophage (CAR-M) therapy represents a promising therapeutic approach for treating glioblastoma multiforme (GBM). However, durable antitumorigenic macrophage phenotype of CAR-Ms is limited by the highly immunosuppressive tumor microenvironment (TME), wherein Siglec–sialic acid signaling directly drives macrophage polarization toward a protumorigenic phenotype. We here report an in situ synthetic SIGLEC9-based chimeric switch receptor (CSR) for diverting the inhibitory signal into positive ones, augmenting the sustained proinflammatory phenotype and tumoricidal immunity of CAR-Ms in the GBM niche. Specifically, our results showed that macrophage-targeted ionizable lipid nanoparticles efficiently introduce dual circRNAs into macrophages to generate CSR functionalized CAR-Ms in vitro and in vivo. The modified macrophages maintained a proinflammatory state, exhibited superior phagocytic activity, resulting in rapid and efficient eradication of IL13Rα2-positive tumor cells. Moreover, an injectable nanoparticle–hydrogel system for reprogramming macrophages surrounding the glioma resection cavity initiated a locoregional antitumor immune response and elicited robust long-term immunological memory, inhibiting tumor relapse in the postoperative GBM model. In sum, our findings establish that the engineered SIGLEC9-based CSR significantly promotes the maintenance of an antitumoral phenotype of CAR-Ms in the hypersialylated acidic TME, contributing to the improvement of engineered macrophage-based immunotherapy against GBM.

Article Details

Volume / Issue Vol. 123, Issue 12
Published March 24, 2026
ISSN 0027-8424
Publisher National Academy of Sciences

Authors (19)

Z

Zhipeng Fu

State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University

X

Xiaotian Zhao

Shenyang National Laboratory for Materials Science Institute of Metal Research Chinese Academy of Sciences

Q

Qikang Zhang

Jinan Microecological Biomedicine Shandong Laboratory, Jinan Medical and Health Science and Technology Innovation Industrial Park

M

Maosen Han

State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University

J

Jing Zhang

Z

Zhenmei Yang

State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University

Y

Yan Wang

Z

Zichao Yao

State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University

Y

Ying Liu

C

Chunwei Tang

State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University

K

Kaiyan Xi

Jinan Microecological Biomedicine Shandong Laboratory, Jinan Medical and Health Science and Technology Innovation Industrial Park

Z

Zhanyan Liu

State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University

Y

Yi Zhang

K

Kun Zhao

N

Na Li

Y

Yulin Zhang

Y

Yudong Song

State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University

X

Xinyi Jiang

State Key Laboratory of Discovery and Utilization of Functional Components in Traditional Chinese Medicine, Shandong Key Laboratory of Targeted Drug Delivery and Advanced Pharmaceutics, National Medical Products Administration Key Laboratory for Technology Research and Evaluation of Drug Products and Key Laboratory of Chemical Biology (Ministry of Education), Department of Pharmaceutics, School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University

C

Chen Chen