TY - JOUR
T1 - Repurposing Disulfiram as an Antifungal Agent :
T2 - Development of a New Disulfiram Vaginal Mucoadhesive Gel
AU - Lajarin-Reinares, Maria
AU - Naveira-Souto, Iria
AU - Mallandrich, Mireia
AU - Suñer-Carbó, Joaquim
AU - Llagostera Casas, Montserrat
AU - Calvo Torras, Ma. de los Ángeles
AU - Fernandez-Campos, Francisco
N1 - Publisher Copyright:
© 2023 by the authors.
PY - 2023/5/8
Y1 - 2023/5/8
N2 - 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 Candida albicans, Candida parapsilosis, and Nakaseomyces glabratus. 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.
AB - 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 Candida albicans, Candida parapsilosis, and Nakaseomyces glabratus. 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.
KW - Disulfiram
KW - Candida spp
KW - Mucoadhesion
KW - ATP-binding cassette
KW - Resistant
KW - Vaginitis
UR - http://www.scopus.com/inward/record.url?scp=85160414198&partnerID=8YFLogxK
UR - https://www.mendeley.com/catalogue/277252bc-d1e2-365b-ad94-a23f6c035c3b/
U2 - 10.3390/pharmaceutics15051436
DO - 10.3390/pharmaceutics15051436
M3 - Article
C2 - 37242678
SN - 1999-4923
VL - 15
JO - Pharmaceutics
JF - Pharmaceutics
IS - 5
M1 - 1436
ER -