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Volume 15, Issue 1
  • ISSN: 2210-3031
  • E-ISSN: 2210-304X

Abstract

Background

Uncomplicated skin and soft tissue infections account for approximately 200 million visits to ambulatory care settings annually. Linezolid (LNZ) is an oxazolidinone that has proven its effectiveness in combating skin and soft tissue infections caused by gram-positive pathogens. LNZ is administered oral suspension, tablets, or an intravenous route in most instances. However, its extended therapy leads to undesirable side effects like diarrhoea, thrombocytopenia, myelosuppression, lactic acidosis, . and even life-threatening complications. The dermal administration of LNZ offers an alternative route, ensuring localized and sustained release at the site of infection. This approach may reduce systemic exposure and allow for lower doses compared to oral ingestion, which can decrease the risk of adverse effects.

Objectives

This research aimed to develop a nanostructured lipid carrier (NLC)-based gel for delivering LNZ the dermal route to treat uncomplicated skin and soft tissue infections.

Methods

NLC were developed by high-shear homogenisation and sonication method using glyceryl trimyristate as a solid lipid and neem oil as a liquid lipid. The Taguchi design was employed to optimize NLCs using surfactant concentration (mg), drug-to-lipid ratio, and sonication time (sec) as independent variables. Their effect on particle size, zeta potential, and entrapment efficiency was studied. The optimized nanocarriers were developed into a gel product and evaluated for drug release, permeation, and antibacterial activity.

Results

The optimised process parameters to attain outcomes were 2% surfactant, 1:1 drug-to-lipid ratio and 300 seconds of sonication. The resulting NLC had an average size of 191.2 ± 2.76 nm, a zeta potential of -30.7 ± 4.50 mV, and 84.89 ± 2.76% drug entrapment. NLC-based gel displayed anomalous transport with a 90.16% drug release. The gel showed a strong antibacterial effect against with a 7.57 ± 0.12 cm mean zone of inhibition. skin permeation studies revealed 24.19 ± 0.19% drug permeation and 64.46 ± 0.58% cutaneous deposition. NLC-based gel demonstrated a significant decrease in colony-forming units in infected animal models.

Conclusion

The investigations demonstrated the presence of LNZ at the infection site, enhancing therapeutic effectiveness. and findings illustrated the substantial antibacterial efficacy of LNZ NLC-based gel. The adoption of NLC-based gel exhibits promising potential as a carrier for dermal delivery of LNZ.

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Optimizing Dermal Delivery of Linezolid for Treating Skin and Soft Tissue Infections: NLC-based Gel Formulation using Taguchi Design
Drug Deliv Lett 15, 58 (2025); https://doi.org/10.2174/0122103031307625240904050257
/content/journals/ddl/10.2174/0122103031307625240904050257
/content/journals/ddl/10.2174/0122103031307625240904050257
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  • Article Type:     Research Article
Keyword(s): dermal delivery; linezolid; Nanostructured lipid carrier; skin and soft tissue infection; Taguchi design; tape-stripped skin infection model
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