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Formulation, characterization, and in vitro antifungal evaluation of liposomal terbinafine prepared by the ethanol injection method

Summary

Researchers developed a new way to deliver the antifungal drug terbinafine using tiny fat-based particles called liposomes. These particles are designed to carry the drug more effectively to infected tissues while reducing harmful side effects. The optimized formulation showed promise for treating stubborn fungal infections, especially those affecting the brain, with significantly reduced toxicity compared to the drug alone.

Background

Fungal infections affect millions annually with significant mortality. Terbinafine is a potent antifungal agent but suffers from poor solubility, low bioavailability, and toxicity. Liposomal encapsulation represents a promising approach to overcome these limitations by enhancing drug solubility, enabling controlled release, and reducing systemic toxicity.

Objective

This study aimed to develop and optimize terbinafine-loaded liposomes using the ethanol injection method with improved physicochemical properties and reduced cytotoxicity. The research focused on central nervous system-targeted delivery to combat resistant fungal infections while minimizing systemic toxicity.

Results

Optimized formulation F12 exhibited sub-100 nm size (72.21 nm), zeta potential of -14.8 mV, high encapsulation efficiency of 73.48%, and sustained drug release (32% at 24 hours). Cytotoxicity was significantly reduced in liposomal forms (6.77% at 25 mg/mL) compared to free drug (14.73%). Liposomal terbinafine showed good in vitro activity against both triazole-susceptible and -resistant Aspergillus isolates (MIC50=0.5 µg/mL).

Conclusion

Formulation F12 with its sub-100 nm size, sustained release profile, and reduced cytotoxicity emerged as a promising candidate for brain-targeted antifungal therapy. The high encapsulation efficiency and colloidal stability support further evaluation in in vivo models to optimize central nervous system biodistribution and therapeutic efficacy.
  • Published in:Current Medical Mycology,
  • Study Type:Experimental Research,
  • Source: PMC12536810, PMID: 41122127, doi: 10.22034/cmm.2025.345248.1686
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