Biotinylated PLGA-PEG nanoparticles for the delivery of antibiotic Polymyxin B sulfate to inhibit Helicobacter pylori

초록

Helicobacter pylori (H. pylori) is a major causative agent of inflammatory infections in the gastrointestinal system. Due to its high recurrence rate, advanced therapeutic strategies have been developed to effectively manage gastrointestinal inflammation. Additionally, pH variability in the digestive system, particularly in the stomach, compromises the stability and therapeutic efficacy of antibacterial and anti-inflammatory drugs. To address these challenges, this study aimed to enhance biotin receptor-targeted drug delivery by loading the anti-H. pylori drug polymyxin B (PMB) into biotinylated PLGA-PEG copolymer nanoparticles (PLGA-PEG-Bio NPs). The successful synthesis of the biotinylated copolymer was confirmed through 1H NMR and FTIR analyses. The resulting PMB-loaded PLGA-PEG-Bio NPs were spherical, with an average particle size of 136.32 ± 52.26 nm, and displayed a dark surface layer under TEM analysis. Additionally, the NPs exhibited a negative zeta potential of −15.63 ± 2.58 mV. The PLGA-PEG-Bio NPs effectively delivered PMB in a simulated gastrointestinal pH environment (1.2, 7.2, and 6.8), achieving burst (0–23.35 %), moderate (23.35–28.87 %), and sustained release (28.87–46.94 %) profiles, respectively. Furthermore, PLGA-PEG-Bio-PMB NPs demonstrated significant antibacterial activity against Gram-negative bacteria, including H. pylori, as confirmed through CLSM analysis using a bacterial live/dead assay. These experimental results suggest that this PLGA-PEG-Bio-based drug delivery strategy holds promise for effectively targeting gastrointestinal infections. © 2025 Elsevier B.V.

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