Bodipy-Loaded Micelles Based on Polylactide as Surface Coating for Photodynamic Control of Staphylococcus aureus

Decontaminating coating systems (DCSs) represent a challenge against pathogenic bacteria that may colonize hospital surfaces, causing several important infections. In this respect, surface coatings comprising photosensitizers (PSs) are promising but still controversial for several limitations. PSs act through a mechanism of antimicrobial photodynamic inactivation (aPDI) due to formation of reactive oxygen species (ROS) after light irradiation. However, ROS are partially deactivated during their diffusion through a coating matrix; moreover, coatings should allow oxygen penetration that in contact with the activated PS would generate O-1(2), an active specie against bacteria. In the attempt to circumvent such constraints, we report a spray DCS made of micelles loaded with a PS belonging to the BODIPY family (2,6-diiodo-1,3,5,7-tetramethyl-8-(2,6-dichlorophenyl)-4,4 '-difluoroboradiazaindacene) that is released in a controlled manner and then activated outside the coating. For this aim, we synthesized several amphiphilic copolymers (mPEG-(PLA)(n)), which form micelles, and established the most stable supramolecular system in terms of critical micelle concentration (CMC) and increment G(f) values. We found that micelles obtained from mPEG-(PLLA)(2) were the most thermodynamically stable and able to release BODIPY in a relatively short period of time (about 80% in 6 h). Interestingly, the BODIPY released showed excellent activity against Staphylococcus aureus even at micromolar concentrations.

Automated summary

This study introduces a spray DCS using micelles loaded with a PS from the BODIPY family for controlled release and activation outside the coating. Amphiphilic copolymers were synthesized to form stable micelles, with mPEG-(PLLA)(2) micelles being the most thermodynamically stable and effective in releasing BODIPY against Staphylococcus aureus even at low concentrations.