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

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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.

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Acknowledgements

The authors would like to express their gratitude to the Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University for extended instrumental facility in successful accomplishment of the present work.

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Authors and Affiliations

  1. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Ain Helwan, Cairo, 11795, Egypt

    Rania S. Abdel-Rashid, Eman S. El-leithy & Raghda Abdel-monem

  2. Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Cairo, Egypt

    Eman S. El-leithy

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  1. Rania S. Abdel-Rashid
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Contributions

All authors conceived and designed the experiments; Rania S. Abdel-Rashid: performed the formulations and experiment, supervision, contribution in data analysis, and writing; Eman S. El-leithy: supervision, funding, data analysis, editing; Raghda Abdel-monem: methodology, supervision, contribution in data analysis, writing and drafting manuscript to appear in its final form.

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Correspondence to Rania S. Abdel-Rashid.

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Animals experimental protocol was ethically approved by the Animal Research Ethical Committee, Faculty of Pharmacy, Helwan University.

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Abdel-Rashid, R.S., El-leithy, E.S. & Abdel-monem, R. Formulation and Evaluation of Topical Biodegradable Films Loaded with Levofloxacin Lipid Nanocarriers. AAPS PharmSciTech 23, 34 (2022). https://doi.org/10.1208/s12249-021-02189-2

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