Targeted pH-responsive chitosan nanogels with Tanshinone IIA for enhancing the antibacterial/anti-biofilm efficacy

Abstract

Persistent bacterial infection caused by biofilms is one of the most serious problems that threatened human health. The development of antibacterial agents remains a challenge to penetrate biofilm and effectively treat the underlying bacterial infection. In the current study, chitosan-based nanogels were developed for encapsulating the Tanshinone IIA (TA) to enhance the antibacterial and anti-biofilm efficacy against Streptococcus mutans (S. mutans). The as-prepared nanogels (TA@CS) displayed excellent encapsulation efficiency (91.41 ± 0.11 %), uniform particle sizes (393.97 ± 13.92 nm), and enhanced positive potential (42.27 ± 1.25 mV). After being coated with CS, the stability of TA under light and other harsh environments was greatly improved. In addition, TA@CS displayed pH responsiveness, allowing it to selectively release more TA in acidic conditions. Furthermore, the positively charged TA@CS were equipped to target negatively charged biofilm surfaces and efficiently penetrate through biofilm barriers, making it promising for remarkable anti-biofilm activity. More importantly, when TA was encapsulated into CS nanogels, the antibacterial activity of TA was enhanced at least 4-fold. Meanwhile, TA@CS inhibited 72 % of biofilm formation at 500 μg/mL. The results demonstrated that the nanogels constituted CS and TA had antibacterial/anti-biofilm properties with synergistic enhanced effects, which will benefit pharmaceutical, food, and other fields.