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Published on: April 19, 2017
Antifungal activity of a liposomal itraconazole formulation in experimental Aspergillus flavus keratitis with
André Ferraz Goiana Leal1, Melyna Chaves Leite, Caroline Sanuzi Quirino Medeiros
1Department of Mycology, Federal University of Pernambuco, Av. da Engenharia, s/n - Cidade Universitária, Recife, PE, CEP: 50740-550, Brazil, andreferrazleal@yahoo.com.br.
Abstract:
The aim of this study was to assess the efficacy of topical application of a liposomal formulation of itraconazole for the treatment of experimental keratitis with endophthalmitis caused by Aspergillus flavus. The liposomes were obtained by the lipid film hydration method followed by sonication. Adult female Wistar rats (weighing 200-220 g) were immunosuppressed by intraperitoneal injection of 150 mg/kg of cyclophosphamide 3 days before infection by exposure to the fungus A. flavus (10(7) spores/ml). Forty-eight hours later, the animals were treated with the liposomal formulation. For comparison, one group of animals (n = 6) was treated with the same drug not encapsulated. At the end of the experiment, the animals were evaluated for clinical signs and number of colony forming units (CFU/g), along with direct microscopic examination. The results indicated that the liposomal formulation of itraconazole has better antifungal activity than the unencapsulated drug in the treatment of fungal keratitis with endophthalmitis caused experimentally by A. flavus in Wistar rats.
Insights
This study found that liposomal itraconazole is more effective than unencapsulated itraconazole for treating experimental fungal keratitis and endophthalmitis caused by Aspergillus flavus in rats.
Area of Science:
- Ophthalmology
- Mycology
- Pharmaceutics
Background:
- Fungal keratitis and endophthalmitis, particularly those caused by Aspergillus flavus, pose significant challenges in ocular infections.
- Current treatment options may have limitations in efficacy and delivery for severe fungal eye infections.
Purpose of the Study:
- To evaluate the therapeutic efficacy of a novel liposomal formulation of itraconazole.
- To compare the effectiveness of liposomal itraconazole against unencapsulated itraconazole in treating experimental Aspergillus flavus-induced keratitis with endophthalmitis.
Main Methods:
- Liposomes encapsulating itraconazole were prepared using the lipid film hydration method followed by sonication.
- Experimental keratitis and endophthalmitis were induced in immunosuppressed Wistar rats using Aspergillus flavus.
- Animals were treated with either liposomal itraconazole or unencapsulated itraconazole.
- Efficacy was assessed through clinical signs, direct microscopic examination, and colony-forming unit (CFU) counts.
Main Results:
- The liposomal formulation of itraconazole demonstrated superior antifungal activity compared to the unencapsulated drug.
- Quantitative analysis showed a significant reduction in fungal burden (CFU/g) with the liposomal treatment.
- Clinical evaluation indicated improved outcomes in animals treated with liposomal itraconazole.
Conclusions:
- Topical liposomal itraconazole is a promising and more effective therapeutic strategy for managing experimental fungal keratitis and endophthalmitis caused by Aspergillus flavus.
- Liposomal drug delivery enhances the antifungal potency of itraconazole in ocular infections.
