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Tumor‐targeted photodynamic therapy (PDT) is desirable as it can achieve efficient killing of tumor cells with no or less harm to normal cells. Herein, a facile molecular engineering strategy is developed for photosensitizers (PSs) with aggregation induced emission (AIE) characteristics and responsive properties to the acidic tumor microenvironment (TME). By the marriage of pH‐sensitive sulfonamide moieties with AIE PSs, two near‐infrared AIE luminogens called DBP‐SPy and DBP‐SPh are designed and synthesized. Both luminogens can form negatively charged nanoaggregates in the aqueous medium at physiological pH. The DBP‐SPy nanoaggregates undergo surface charge conversion to become positive at pH close to the signature pH of TME, while DBP‐SPh nanoaggregates show no such property. The endowed response to acidic TME enables the enhanced cellular uptake of DBP‐SPy at pH = 6.8. By contrast, its cellular uptake is much sacrificed at pH 7.4. As a result, under white light irradiation, DBP‐SPy nanoaggregates demonstrate a considerable photodynamic therapeutic effect on cancer cells in vitro and excellent tumor growth inhibition in vivo. Hence, this study not only provides an acidic TME‐responsive AIE PS for precise PDT, but also inspires new design strategies for AIE‐based theragnostic systems with targeting characteristics. [ABSTRACT FROM AUTHOR]

Antimicrobial photodynamic therapy (aPDT) is an effective strategy to eliminate bacteria without inducing bacterial resistance. As typical aPDT photosensitizers, most of boron-dipyrromethene (BODIPY) are hydrophobic, and nanometerization is imperative to render them dispersible in physiological media. Recently, carrier-free nanoparticles (NPs) are formed via the self-assembly of BODIPYs without the help of any surfactants or auxiliaries, arousing people's interest. So as to fabricate carrier-free NPs, BODIPYs usually need to be derived into dimers, trimers, or amphiphiles through complex reactions. Few unadulterated NPs were obtained from BODIPYs with precise structures. Herein, BNP1-BNP3 were synthesized by the self-assembly of BODIPY, which showed excellent anti- Staphylococcus aureus ability. Among them, BNP2 could effectively fight bacterial infections and promote wound healing in vivo. • BNP1-BNP3 were synthesized and their photophysical properties were characterized. • BNP2 had highest the singlet oxygen generation efficacy. • BNP2 could effectively kill S. aureus and possess excellent biofilm inhibition ability. • BNP2 could effectively fight bacterial infections and promote wound healing in vivo. [ABSTRACT FROM AUTHOR]

Microbial infection often accompanies most diseases such as cancer, which has been testified to severely decrease the efficacy of cancer therapy. It is imperative and significant to develop the single therapeutic agents with high antimicrobial and antitumor efficacy. Herein, fluoroalkylated boron dipyrromethene (BDP) (named as B-F) and its counterpart alkylated BDP (named as B-H) were synthesized. Fluoroalkylation could facilitate the spontaneous self-assembly of B-F into nanoparticles (NPs) and dramatically enhance its intracellular delivery efficiency. Furthermore, compared with B-H NPs, B-F NPs possessed enhanced capacity of generating reactive oxygen species (ROS) upon irradiation, which endowed B-F NPs with photodynamic destroying Gram-positive bacteria and cancer cells. This work contributes to strategical design of the nanoscale photosensitizers (PSs) for antimicrobial photoinactivation and photodynamic therapy (PDT). [Display omitted] [ABSTRACT FROM AUTHOR]