Bacterial and fungal infections remain major global health threats due to antimicrobial resistance of pathogenic microorganisms. In recent years, phototherapy has shown great promise for treating microbial infectious diseases, owing to its precise controllability, noninvasiveness, high efficiency, and spatiotemporal selectivity, as well as its potential to address antimicrobial resistance. However, its clinical translation is still limited due to the challenges including shallow tissue penetration, poor tissue selectivity, and insufficient phototherapeutic efficiency. This review systematically summarizes recent advances in antimicrobial phototherapeutic agents, with a focus on their core design principles, targeting mechanisms, and applications in treating microbial infectious diseases. Furthermore, the review outlines the current challenges associated with antimicrobial phototherapeutic agents and proposes future research directions, promoting interdisciplinary collaboration among researchers to improve the efficacy and expand the clinical applicability of phototherapy for combating microbial infections. Phototherapy offers a promising strategy against drug-resistant microbial infections, yet its clinical use is limited due to shallow light penetration, low selectivity, and poor therapeutic efficiency. This review summarizes recent advances in antimicrobial phototherapeutic agents, focusing on their design principles, targeting mechanisms, and practical applications. It also highlights key challenges and proposes future research directions to facilitate clinical translation of this treatment approach. • Mechanisms and design principles of photosensitizers in antimicrobial strategies were highlighted. • Electrostatic interaction-based phototherapy agents were introduced. • Receptor–ligand interaction-based phototherapy agents were reviewed. • Infection microenvironment-responsive phototherapy agents were summarized. • Challenges and future research directions of antimicrobial phototherapeutic agents were discussed.
Jiang et al. (2026) studied this question.