Repurposing Disulfiram as an Antifungal Agent: Development of a New Disulfiram Vaginal Mucoadhesive Gel

Alternative formulations need to be developed to improve the efficacy of treatments administered via the vaginal route. Mucoadhesive gels with disulfiram, a molecule that was originally approved as an antialcoholism drug, offer an attractive alternative to treat vaginal candidiasis. The aim of the c...

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Published inPharmaceutics Vol. 15; no. 5; p. 1436
Main Authors Lajarin-Reinares, Maria, Naveira-Souto, Iria, Mallandrich, Mireia, Suñer-Carbó, Joaquim, Llagostera Casas, Montserrat, Calvo, Maria Angels, Fernandez-Campos, Francisco
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 08.05.2023
MDPI
Subjects
Asymptomatic
ATP-binding cassette
Candida spp
Carrageenin
Disulfiram
Drug approval
Drug delivery systems
Drugs
Ethanol
Infections
Mechanical properties
Medical research
Medicine, Experimental
mucoadhesion
Polyethylene glycol
Polymers
Polyols
resistant
Vagina
vaginitis
Vehicles
United States > US
Spain
Candida spp
ATP-binding cassette
resistant
disulfiram
mucoadhesion
vaginitis
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Summary:Alternative formulations need to be developed to improve the efficacy of treatments administered via the vaginal route. Mucoadhesive gels with disulfiram, a molecule that was originally approved as an antialcoholism drug, offer an attractive alternative to treat vaginal candidiasis. The aim of the current study was to develop and optimize a mucoadhesive drug delivery system for the local administration of disulfiram. Such formulations were composed of polyethylene glycol and carrageenan to improve the mucoadhesive and mechanical properties and to prolong the residence time in the vaginal cavity. Microdilution susceptibility testing showed that these gels had antifungal activity against , , and . The physicochemical properties of the gels were characterized, and the in vitro release and permeation profiles were investigated with vertical diffusion Franz cells. After quantification, it was determined that the amount of the drug retained in the pig vaginal epithelium was sufficient to treat candidiasis infection. Together, our findings suggest that mucoadhesive disulfiram gels have the potential to be an effective alternative treatment for vaginal candidiasis.
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ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15051436