Formulation and Evaluation of Topical Biodegradable Films Loaded with Levofloxacin Lipid Nanocarriers

Abstract

Skin ulcers have increased sharply due to rise in the incidence of obesity and diabetes. This study investigated lipid nanocarriers as a strategy to improve the efficacy of levofloxacin (LV) in penetrating skin. Two surfactant types and different lipid mixtures were used in preparation of lipid nanocarriers. Mean particle size, percentage entrapment efficiency (%EE), in vitro release, and antimicrobial activity were examined. The selected formula was incorporated into a chitosan (CS) film that was subjected to physic-chemical characterization and ex vivo permeation study. The selected formula showed particle size, PDI, and ZP: 80.3 nm, −0.21, and −26 mV, respectively, synchronized with 82.12 %EE. In vitro release study showed slow biphasic release of LV from lipid nanocarriers. The antimicrobial effect illustrated statistically significant effect of lipid nanocarriers on decreasing the minimum effective concentration (MIC) of LV, particularly against E. coli. The optimized nanocarriers’ formula loaded into CS film was clear, colorless, translucent, and smooth in texture. Based on the release profiles, it could be speculated that the CS film loaded with LV nanocarriers can maintain the antibacterial activity for 4 consecutive days. Thus, the local delivery of the drug in a sustained release manner could be predicted to enhance the therapeutic effect. Further clinical studies are strongly recommended. [Figure not available: see fulltext.] © 2021, The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists