This invention relates to
Furin /
hydroxyl radical dual-responsive size-changing nanoparticles, their preparation, and applications. The
Furin /
hydroxyl radical dual-responsive size-changing nanoparticles use an AIE
photosensitizer as the core and DSPE-PEG as the substrate. 2K MAL nanoparticles serve as carriers, with functional peptides coupled to their surfaces via Michael addition reactions. The core functional building block is a self-designed and custom-synthesized R1
peptide, which possesses a triple function: high specificity recognition by
Furin protease, OH-responsive
tyrosine oxidation cross-linking, and
coupling with DSPE-PEG nanoparticles. Its simple sequence significantly enhances
tumor selectivity. The
peptide is covalently modified with natural peptides using a nanoprecipitation method, avoiding complex chemical modifications and exogenous orthogonal biological groups, thus mitigating the
toxicity and synthesis costs of traditional systems. Under the dual conditions of Furin
protease overexpression and the presence of OH, size transformation is triggered, enabling deep
tumor penetration with small sizes and long-term intratumoral retention through in-situ large-size
assembly, demonstrating clinical translational potential.