AIEgen-biomacromolecule conjugates: Visualized delivery and light-controlled theranostic platforms

Biomacromolecules play a critical role in advancing disease diagnosis and treatment. Traditional carriers often lack real-time tracking capabilities, controlled drug release, and may induce adverse effects for delivering biomacromolecules. Aggregation-induced emission luminogens (AIEgens) provide significant advantages in biomacromolecule delivery, enabling real-time fluorescence imaging and reactive oxygen species generation for photodynamic therapy (PDT). This dual functionality allows for the visualization of the biomacromolecule delivery process, providing valuable insights into biodistribution, cellular uptake, and drug-cell interactions. Additionally, the light-responsive nature of AIEgens enables precise spatial-temporal control over cargo release and imaging-guided PDT with minimal side effects. In this perspective, we summarize recent advancements in the use of AIEgens for visualized delivery and light-controlled theranostic applications of biomacromolecules, highlighting their potential to overcome challenges in targeted imaging and precision treatments. Key topics covered include covalent linkage strategies and the biomedical applications of AIEgen-functionalized biomacromolecules, including nucleic acids, proteins, polysaccharides, and lipids. We further highlight AIEgen-functionalized gene therapy and PDT for cancer, peptide transport for disease diagnosis, as well as polysaccharides and lipids delivery in antimicrobial treatments. This perspective concludes by addressing future challenges and opportunities, emphasizing the potential of AIEgen-functionalized biomacromolecules to advance precision theranostics.