Design Optimization and Physicochemical/Structural Characterization of Levofloxacin-Loaded Nanoscale Bilosomes for Topical Delivery

نویسندگان

1 College of Pharmacy, University of Basra, Basra, Iraq

2 College of Pharmacy, University of Basra, Basra, Iraq

3 College of Pharmacy, University of Basra, Basra, Iraq

doi
10.22052/JNS.2026.01.026
چکیده

Conventional topical levofloxacin is limited by poor skin penetration and local instability. Bile-salt–stabilized nanovesicles (bilosomes) were engineered to enhance dermal delivery by improving colloidal stability, drug loading, and cutaneous interaction. Levofloxacin-loaded nanoscale bilosomes were prepared by thin-film hydration followed by probe sonication while varying Span 60 and cholesterol to generate twelve formulations (F1–F12). Vesicle size, polydispersity index (PDI), zeta potential, and entrapment efficiency (EE%) were measured in triplicate. Partitioning behavior (log P) was profiled. Morphology and solid-state attributes were assessed by SEM, FTIR, XRD, and DSC. Short-term stability of the optimized batch was monitored at 4 °C and 25 °C for up to three months. One-way ANOVA with Tukey’s HSD was applied according to table footnotes; significance was set at p < 0.05. Composition strongly governed performance. Increasing Span 60 progressively reduced vesicle size to a minimum at 400 mg, after which a slight increase suggested surfactant saturation. Cholesterol showed a biphasic effect: moderate levels compacted bilayers and enhanced EE%, whereas higher levels enlarged vesicles, broadened PDI, and depressed EE%. The optimized formulation (F5; Span 60 = 400 mg, cholesterol = 100 mg) achieved nanoscale size (93 ± 1.2 nm), acceptable PDI (0.398 ± 0.01), highly negative zeta potential (−51.7 ± 0.8 mV), and maximal EE% (91 ± 0.5%). Across screening tables, ANOVA/Tukey identified significant differences relative to the optimized reference, as indicated by bold p-values. FTIR showed band shifts/broadening without new peaks, supporting non-covalent interactions and intact drug structure. XRD demonstrated loss of sharp crystalline peaks and an amorphous halo in the optimized nanobilosomes. Stability testing confirmed minimal drift at 4 °C, whereas 25 °C storage increased size (to ~128 nm) and reduced EE% (to ~79%) by three months, with concurrent zeta-potential attenuation. Rational bilosome engineering produced a robust levofloxacin nanocarrier with favorable size, charge, and payload retention. A composition of ~100 mg cholesterol with 400 mg Span 60 maximized EE% while maintaining colloidal stability. Refrigerated storage is recommended. These data provide a framework for the development of topical nanobilosomes and motivate ex vivo permeation, antimicrobial efficacy, and in vivo confirmation.