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Studies in Development and Statistical Optimization of Levofloxacin Solid Lipid Nanoparticles for the Treatment of Tuberculosis

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Abstract

Background

WHO acclaims superiority of levofloxacin for the treatment of drug-resistant tuberculosis.

Purpose

The purpose of this research was to develop levofloxacin-loaded solid lipid nanoparticles (LEV-SLN) for use in tuberculosis treatment. The goal was to make LEV-SLN with a mean particle size of less than 300 nm, a drug release duration of more than 12 h, and an LEV-SLN MMAD of less than 5 µm.

Methods

LEV-SLN was made using a single emulsification process, followed by solvent evaporation and lyophilization. A Plackett–Burman screening design and a 32 full factorial design were employed sequentially to explore the impact of various formulation and process parameters on mean particle size, % entrapment efficiency, and in vitro drug release.

Results

According to the Pareto chart from the Plackett–Burman screening design, the amount of poloxamer and homogenization speed had a significant influence on the mean particle size (p < 0.05). LEV-SLN had a minimum inhibitory concentration of 0.7 µg/ml, whereas pure drug had a minimum inhibitory value of 1.0 µg/ml. The F-ratio for each model developed was higher than the theoretical value (p < 0.05) in a follow-up analysis employing 32 full factorial design, showing that each model was significant.

Conclusion

The best formulation had a mean particle size of 79.70 nm, lasted 12 h in simulated lung fluid, and had an MMAD of 3.71 µm, confirming that the drug may reach up to deep lungs. In the future, preclinical study is needed to develop a realistic dosing regimen and determine the pharmacokinetics and pharmacodynamics of LEV-SLN.

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Acknowledgements

The authors are thankful to Baroque Pharmaceuticals for gift sample of levofloxacin and GUJCOST for providing research grant

Funding

Gujarat Council of Science and Technology (GUJCOST), Gandhinagar, provided a Minor Research Grant titled “Application of nanotechnology for treatment of Tuberculosis” via letter no. GUJCOST/MRP/2016–17/429.

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Authors and Affiliations

  1. B. K. Mody Government Pharmacy College, Rajkot, Gujarat, India

    Sunny Shah, Nirav Shah, Dhaval Mori, Moinuddin Soniwala & Jayant Chavda

  2. Xylopia Labs Private Limited, Ahmedabad, Gujarat, India

    Saurin Amin

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  1. Sunny Shah
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  2. Nirav Shah
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  3. Saurin Amin
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Correspondence to Sunny Shah.

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Shah, S., Shah, N., Amin, S. et al. Studies in Development and Statistical Optimization of Levofloxacin Solid Lipid Nanoparticles for the Treatment of Tuberculosis. J Pharm Innov 17, 1322–1332 (2022). https://doi.org/10.1007/s12247-022-09617-1

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  • DOI: https://doi.org/10.1007/s12247-022-09617-1

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