Fluorescent Self-Reporting Theranostic Platforms for Tumour Therapy: From Cytotoxin Release Monitoring to Therapeutic Feedback Evaluation

Abstract

Controlled drug release enables targeted drug delivery, enhances selectivity and safety, and holds broad application prospects in precision tumour therapy. However, conventional switch-based controlled-release therapeutics (including photosensitizers, sonosensitizers, chemical prodrugs, nanocatalytic particles, and functional nucleic acids) are often constrained by unpredictable cytotoxic release and variable therapeutic outcomes. This makes it challenging to achieve synergy between dose or external field stimulation and tumour suppression, thereby undermining the full potential of precision therapy. To address this challenge, fluorescent self-reporting theranostic platforms (FSRTPs) have emerged as a promising approach, enabling real-time monitoring of drug release dynamics and therapeutic efficacy. Leveraging the unique advantages of fluorescence imaging, FSRTPs provide high spatial and temporal resolution for non-invasive visualization of drug distribution and cellular responses at the molecular level. They autonomously provide real-time feedback of critical events such as drug release, intracellular trafficking, and cytotoxic effects, revealing therapeutic mechanisms and enabling dynamic treatment adjustments to optimize outcomes and precision. This paper reviews fluorescent single-/dual-mode imaging-guided controlled-release therapeutics reported in recent years, highlighting their design rationales, imaging strategies, and biological applications. In addition, the characteristics of FSRTPs are critically compared across different therapeutic modalities from the dual perspectives of cytotoxin-release monitoring and therapeuticfeedback evaluation. Finally, future design principles and biomedical prospects for next-generation FSRTPs are outlined, offering valuable insights for the development of more effective and personalized cancer treatment strategies.