Ziyan Guo, Lele Wu, Yu Niu, Yan Dong, Guangsheng Wu, Pengyu Zhao, Yichen Li, Jiayi Li, Yimin Zhao, Liang Kong, Zhongshan Wang
Diabetic wound healing is critically impaired by dysregulated macrophage polarization, compromised endothelial angiogenic function, and diminished fibroblast proliferation/migration under persistent hyperglycemia. Current therapies, predominantly focused on single-cell targeting, lack coordinated modulation across these key cellular components. We developed a novel triple-targeting core-shell nanoparticle (miR-RPC) leveraging the shared integrin αvβ3 receptor on macrophages, endothelial cells, and fibroblasts to address this limitation. miR-RPC features an RGD/phosphatidylserine (PS)-modified lipid shell encapsulating a chitosan/miR-146a-5p core. This miRNA was selected as a model RNA because of its widely recognized beneficial role in three key cell types in wound healing. The RGD peptide enables specific αvβ3-mediated triple-targeting. The anionic lipid PS facilitates core-shell assembly via electrostatic interaction with the cationic chitosan/RNA core and mimics apoptotic signals to enhance macrophage phagocytosis and phenotypic transition. miR-RPC effectively reprogrammed macrophages towards the M2 phenotype, restored endothelial angiogenic capacity under high glucose, and stimulated fibroblast proliferation, migration, and collagen secretion. Incorporated into a gelatin methacrylate (GelMA)/oxidized hyaluronic acid (OHA) double cross-linked hydrogel (GelO), miR-RPC@GelO significantly accelerated diabetic wound healing in rat models, demonstrating reduced inflammation, increased vascular density, and enhanced collagen deposition. This innovative triple-targeting system achieves coordinated diabetic wound repair through synergistic "immunomodulation-angiogenesis-collagen deposition" mechanisms, offering a promising therapeutic approach. Furthermore, the successful preparation of miR-RPC expands the application of anionic lipids in RNA delivery systems and highlights its potential as a versatile gene delivery vector.