Fluorescent self-reporting theranostic platforms for tumour therapy: from cytotoxin release monitoring to therapeutic feedback evaluation

Abstract

Controlled drug release, which enables targeted drug delivery, enhances selectivity and safety, and holds broad application prospects in precision tumour therapy, is frequently limited by unpredictable cytotoxic release and variable therapeutic effects. 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. This paper reviews fluorescence single-/dual-mode imaging-guided controlled-release therapeutics developed 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 therapeutic-feedback evaluation. A core focus is achieving high-resolution intracellular drug tracking and real-time biomarker sensing (e.g., Caspase-3) to enable prompt assessment of tumour cell apoptosis. Finally, we identify key bottlenecks in imaging depth, drug quantification, and pharmacokinetics and propose next-generation design principles to facilitate the clinical translation of adaptive, personalized cancer therapies.