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载丹参酮 IIA 的靶向 pH 响应性壳聚糖纳米凝胶增强抗菌/抗生物膜效果。

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

机构信息

State Key Laboratory of Chemical Resource Engineering, Beijing University of Chemical Technology, Beijing 100029, PR China.

Department of Prosthodontics, Peking University School and Hospital of Stomatology & National Center of Stomatology & National Clinical Research Center for Oral Diseases & National Engineering Research Center of Oral Biomaterials and Digital Medical Devices, Beijing 100081, China.

出版信息

Int J Biol Macromol. 2023 May 15;237:124177. doi: 10.1016/j.ijbiomac.2023.124177. Epub 2023 Mar 25.

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.

摘要

生物膜引起的持续性细菌感染是威胁人类健康的最严重问题之一。抗菌剂的开发仍然是一个挑战,需要穿透生物膜并有效治疗潜在的细菌感染。在目前的研究中,开发了基于壳聚糖的纳米凝胶来包封丹参酮 IIA(TA),以增强对变形链球菌(S. mutans)的抗菌和抗生物膜功效。所制备的纳米凝胶(TA@CS)显示出优异的包封效率(91.41±0.11%)、均匀的粒径(393.97±13.92nm)和增强的正电势(42.27±1.25mV)。在被 CS 包覆后,TA 在光照和其他恶劣环境下的稳定性得到了极大的提高。此外,TA@CS 表现出 pH 响应性,允许其在酸性条件下选择性释放更多的 TA。此外,带正电荷的 TA@CS 被装备来靶向带负电荷的生物膜表面,并有效地穿透生物膜屏障,因此具有显著的抗生物膜活性。更重要的是,当 TA 被包封到 CS 纳米凝胶中时,TA 的抗菌活性至少增强了 4 倍。同时,TA@CS 在 500μg/mL 时抑制了 72%的生物膜形成。结果表明,由 CS 和 TA 构成的纳米凝胶具有协同增强的抗菌/抗生物膜特性,这将有益于制药、食品和其他领域。

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