Glutathione-responsive PEGylated florfenicol via disulfide linkage enhances antibacterial activity, pharmacokinetics, and biosafety

文献类型： 外文期刊

第一作者： Niu, Ming

作者： Niu, Ming;Wang, Rourou;Zhou, Jing;Pu, Lumei;Xu, Weibing;Pan, Fei;Zhou, Yaxin;Zhang, Zhenghua

作者机构：

关键词： mPEG; Florfenicol; Conjugate; Disulfide bond; Antibacterial activity

期刊名称：MATERIALS & DESIGN （ 影响因子：7.9； 五年影响因子：8.9 ）

ISSN： 0264-1275

年卷期： 2025 年 255 卷

页码：

收录情况： SCI

摘要： Developing intelligent and responsive antimicrobial materials is critically important for the sustainable advancement of livestock production. This study prepares a glutathione-responsive mPEG-SS-florfenicol conjugate using disulfide bonds as a linker. A non-responsive conjugate is also synthesized using an alkyl carbon chain as a linker. The structures of both conjugates are characterized through various analytical techniques, including MALDI-TOF MS. The self-assembled microstructures of the responsive and non-responsive conjugates are spherical and lamellar, respectively. At a DTT concentration of 10 mM, 90 % of florfenicol is released from the responsive conjugate within 10 h. The antibacterial activity of the responsive conjugate is 1.6 times greater than that of pure florfenicol at a concentration of 64 mu g/mL. At the same concentration, the uptake of the responsive conjugate by E. coli is ten times higher than that of the non-responsive conjugate. Compared with the non-responsive conjugate, the responsive conjugate induces more pronounced damage to the bacterial cell membrane. Molecular dynamics simulations confirm that the responsive conjugate binds to bacterial membranes more rapidly and with lower binding energy. The elimination half-life, maximum concentration (Cmax), and area under the curve of the responsive conjugate are 1.3, 1.7, and 2.4 times higher than those of commercial trimethoprim tablets, respectively.

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