Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity

This study prepared nanocapsules (NCs) with excellent self-controlled antimicrobial activity at pH 6–7 and humidity 45–100%, conditions in which most bacterial and fungal strains thrive. The nanocapsule substrate (NC@SiO(2)) was 676 nm in diameter, and the ligand-grafted capsule (NC@SiO(2)-g-MAA) was 888 nm. The large surface area and outer ligand brush of the NCs induced a rapid, self-controlled antibacterial response in the pH and humidity conditions needed for industrial and medical applications. Ligand-brush NCs containing an anionic antimicrobial drug had a rapid release effect because of the repellent electrostatic force and swelling properties of the ligand brushes. Controlled release of the drug was achieved at pH 6 and humidity of 45% and 100%. As many carboxylic acid groups are deprotonated into carboxylic acids at pH 5, the NC@SiO(2)-g-MAA had a high negative charge density. Carboxylic acid groups are anionized (–COO(−)) at pH 6 and above and push each other out of the capsule, expanding the outer shell as in a polymer brush to create the release behavior. The surface potential of the NC intermediate (NC@SiO(2)-MPS) was −23.45 [mV], and the potential of the capsule surface decreased to −36.4 [mV] when the MAA ligand brushes were grafted onto the surface of the capsule intermediate. In an antimicrobial experiment using Escherichia coli, a clear zone of 13–20 mm formed at pH 6, and the E. coli was eradicated completely at pH 6 and pH 7 when the humidity was 100%.