Antibacterial efficacy and pharmacokinetics of a poly(mPEG-b-PCEA)-trimethoprim conjugate

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;Zhang, Zhenghua;Zhou, Yaxin

作者机构：

期刊名称：NEW JOURNAL OF CHEMISTRY （ 影响因子：2.5； 五年影响因子：2.7 ）

ISSN： 1144-0546

年卷期： 2025 年 49 卷 28 期

页码：

收录情况： SCI

摘要： Research into antimicrobials is crucial for the sustainable development of the livestock industry. Trimethoprim (TMP) is one of the most widely used antimicrobial agents in the world. However, its efficacy is often limited by poor water solubility and dose-limiting properties. In this work, amphiphilic block polymer carriers are prepared using the oxygen-induced reversible addition-fragmentation chain transfer polymerization reaction. TMP is linked to carriers in different ratios to form poly(mPEG-b-PCEA)-TPM conjugates. The conjugates are characterized using various methods including H-1 NMR, FT-IR, XRD and SEM. The results of in vitro antimicrobial experiments show that poly(mPEG-b-PCEA)-TMP with different ratios has more prominent antimicrobial effects than the same dosage of pure TMP. poly(mPEG-b-PCEA)-TMP80 shows the most significant results, inhibiting E. coli by 87.19% and S. aureus by 97.02%, with a hemolysis rate of <5% and good biocompatibility. In vivo pharmacokinetics show an increase in C-max from 4.81 mu g mL(-1) to 6.57 mu g mL(-1) and AUC(0-48) from 78.55 h mu g mL(-1) to 89.11 h mu g mL(-1) for poly(mPEG-b-PCEA)-TMP80 compared to commercially available TMP tablets. This strategy can effectively improve the antibacterial activity and pharmacokinetics and increase the bioavailability of TMP.

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