College of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, China; Precision Medicine Translational Research Center, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.
Precision Medicine Translational Research Center, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.
J Colloid Interface Sci. 2025 Jan 15;678(Pt C):690-703. doi: 10.1016/j.jcis.2024.09.158. Epub 2024 Sep 17.
Photodynamic therapy (PDT) employs reactive oxygen species (ROS) from a photosensitizer (PS) under light, inhibiting multi-drug resistance in bacteria. However, hypoxic conditions in infection sites and biofilms challenge PDT efficiency. We developed fluorinated small molecular micelles (PF-CBMs) as PS carriers to address this, relieving hypoxia and enhancing PS penetration into biofilms. Perfluorocarbons in PF-CBMs transport more oxygen due to their excellent oxygen-dissolving capability. Fluorination enhances loading capacity and serum stability, reduces premature release, and improves cellular uptake, to improve PDT efficacy. PF-CBMs, with acid-induced surface charge transformation, exhibit superior biofilm penetration, resulting in increased antibiofilm activity of PDT. Compared to fluorine-free micelles (PC-CBMs), PF-CBMs demonstrate better serum stability, higher drug loading, and reduced premature release, leading to significantly improved antibacterial efficacy in vitro and in vivo. In conclusion, fluorinated micelles with surface charge reversal enhance PDT for antibacterial and antibiofilm applications.
光动力疗法（PDT）利用光敏剂（PS）在光下产生的活性氧物质（ROS），抑制细菌的多药耐药性。然而，感染部位和生物膜中的缺氧条件挑战了 PDT 的效率。我们开发了氟化小分子胶束（PF-CBMs）作为 PS 载体来解决这个问题，缓解缺氧并增强 PS 穿透生物膜。PF-CBMs 中的全氟碳由于其出色的溶解氧能力而运输更多的氧气。氟化增强了载药量和血清稳定性，减少了过早释放，并提高了细胞摄取，以提高 PDT 的疗效。PF-CBMs 具有酸诱导的表面电荷转变，表现出优异的生物膜穿透能力，从而提高 PDT 的抗生物膜活性。与无氟胶束（PC-CBMs）相比，PF-CBMs 具有更好的血清稳定性、更高的载药量和减少的过早释放，从而显著提高了体外和体内的抗菌疗效。总之，具有表面电荷反转的氟化胶束增强了 PDT 在抗菌和抗生物膜方面的应用。
