Wheat Germ Agglutinin Modified Liposomes for the Photodynamic Inactivation of Bacteria

Photodynamic inactivation (PDI) of bacteria is a promising approach for combating the increasing emergence of antibiotic resistance in pathogenic bacteria. To further improve the PDI efficiency on bacteria, a bacteria‐targeting liposomal formulation was investigated. A generation II photosensitizer (temoporfin) was incorporated into liposomes, followed by conjugation with a specific lectin (wheat germ agglutinin, WGA) on the liposomal surface. WGA was successfully coupled to temoporfin‐loaded liposomes using an activated phospholipid containing N‐hydroxylsuccinimide residue. Methicillin‐resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa were selected to evaluate the WGA modified liposomes in terms of bacteria targeted delivery and in vitro PDI test. Fluorescence microscopy revealed that temoporfin was delivered to both kinds of bacteria, while flow cytometry demonstrated that WGA‐ modified liposomes delivered more temoporfin to bacteria compared to nonmodified liposomes. Consequently, the WGA‐ modified liposomes eradicated all MRSA and significantly enhanced the PDI of P. aeruginosa. In conclusion, the WGA‐ modified liposomes are a promising formulation for bacteria targeted delivery of temoporfin and for improving the PDI efficiency of temoporfin on both Gram‐positive and Gram‐negative bacterial cells. The surface of temoporfin‐loaded liposomes was modified with a bacteria‐targeting ligand, wheat germ agglutinin, to prepare bacteria‐targeting liposomes, which bind to bacteria and consequently increase the delivery of temoporfin to bacteria. After light illumination, the photosensitizers (temoporfin) generate reactive oxygen species, resulting in photodynamic inactivation of bacteria.