Antibacterial and Biofilm-Targeting Performance of Cefuroxime Axetil-Loaded Eudragit® Nanoparticles

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Soyer P., Çevikelli T., Güven Bölgen U. M., Öztürk A. A.

ANTIBIOTICS, cilt.15, sa.11, ss.1-28, 2026 (SCI-Expanded)

Özet

Background/Objectives: Cefuroxime axetil (CA) is a poorly water-soluble second-

generation cephalosporin. This study aimed to develop CA-loaded Eudragit® RS100/RL100

nanoparticles (NPs) and investigate the influence of polymer composition and drug-to-

polymer ratio on their physicochemical, antibacterial, and antibiofilm properties. Methods:

Six CA-loaded NPs (NP-1–NP-6) were prepared using nano spray drying with Eudragit®

RS100, RL100, or their 1:1 mixture at drug-to-polymer ratios of 1:1 and 1:2. Particle char-

acteristics, drug content, and structural properties were evaluated. Antibacterial activity

was assessed using agar well diffusion, broth microdilution, and time-kill assays, while

antibiofilm activity against pre-established Staphylococcus aureus and Escherichia coli biofilms

was determined using crystal violet staining. Additional analyses included drug-content-

normalized MIC, MIC-normalized time-kill exposure, and concentration–response area

under the curve (AUC). Results: All drug-loaded NPs retained antibacterial activity and

reduced established biofilm biomass, whereas blank NPs showed no detectable activity.

FT-IR and 1 H-NMR analyses indicated no evidence of new covalent interactions. Free CA

exhibited greater planktonic antibacterial potency, including after drug-content normaliza-

tion. Among the NPs, NP-1 showed the most favorable MIC profile, while MIC-normalized

time-kill analysis revealed NP-dependent exposure differences without consistent bacterici-

dal activity. At 500 μg/mL, all CA-loaded NPs reduced biofilm biomass by more than 95%

against both bacterial species. NP-6 exhibited the highest numerical antibiofilm AUC values

against S. aureus (133.37) and E. coli (128.85), although these differences were descrip-

tive and did not establish statistical superiority. Conclusions: CA-loaded Eudragit® NPs

demonstrated formulation-dependent antibacterial and antibiofilm responses, with NP-1

performing favorably in planktonic inhibition and NP-6 in integrated biofilm biomass re-

duction. These findings support further investigation of Eudragit® -based antibiotic delivery

systems, although superiority over free CA and therapeutic advantages remain unverified.