Advances in BODIPY Derivatives for Antibacterial Phototherapy

Abstract

ABSTRACT The escalating threat posed by antibiotic‐resistant bacteria and biofilm‐associated infections has driven increasing interest in non‐antibiotic antibacterial strategies. Antibacterial phototherapy (PT), including photodynamic therapy (PDT) and photothermal therapy (PTT), has attracted considerable attention owing to its spatiotemporal controllability, broad‐spectrum antibacterial activity, and low propensity for inducing drug resistance. Boron‐dipyrromethene (BODIPY) dyes, featuring exceptional structural tunability and favorable photophysical properties, have emerged as versatile scaffolds for the construction of antibacterial phototherapeutic systems. Through molecular engineering strategies including cationization, heavy‐atom incorporation, and π‐conjugation extension, combined with nanoassembly approaches, both the excited‐state processes of BODIPY and its interactions with bacterial interfaces can be precisely regulated. Integration into diverse nanoplatforms further improves aqueous dispersibility, biological stability, and accumulation at bacterial or biofilm interfaces, thereby enhancing reactive oxygen species (ROS) generation or enabling photothermal effects to achieve PDT, PTT, or synergistic antibacterial therapy. This review systematically summarizes the design strategies and structure‐activity relationships of BODIPY‐based antibacterial phototherapy reported over the past five years, covering molecular engineering of small‐molecule photosensitizers and nanoplatforms, bacterial targeting and carrier design, and discussing the challenges and future perspectives associated with clinical translation, particularly in terms of biosafety and targeted delivery.