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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

In vivo study of hypericin-loaded poloxamer-based mucoadhesive in situ gelling liquid crystalline precursor system in a mice model of vulvovaginal candidiasis

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Author(s):
de Araujo, Patricia Rocha [1] ; Fioramonti Calixto, Giovana Maria [1, 2] ; Sousa Araujo, Victor Hugo [1] ; Sato, Mariana Rillo [1] ; Rodero, Camila Fernanda [1] ; Oshiro-Junior, Joao Augusto [3] ; Bauab, Tais Maria [1] ; Chorilli, Marlus [1]
Total Authors: 8
Affiliation:
[1] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, BR-14800903 Araraquara, SP - Brazil
[2] Univ Estadual Campinas, UNICAMP, Piracicaba Dent Sch, Dept Biosci, BR-13414903 Piracicaba, SP - Brazil
[3] Paraiba State Univ, BR-58429500 Campina Grande, Paraiba - Brazil
Total Affiliations: 3
Document type: Journal article
Source: Medical Mycology; v. 59, n. 8, p. 821-827, AUG 2021.
Web of Science Citations: 2
Abstract

The present study reports the performance of the pigment hypericin (HYP)-loaded poloxamer-based mucoadhesive in situ gelling liquid crystalline precursor system (LCPS) for the treatment of vulvovaginal candidiasis (VVC) in mice. LCPS composed of 40% of ethoxylated and propoxylated cetyl alcohol, 30% of oleic acid and cholesterol (7:1), 30% of a dispersion of 16% poloxamer 407 and 0.05% of HYP (HYP-LCPS) was prepared and characterized by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS) and ex vivo permeation and retention studies across vaginal porcine mucosa were performed. In addition, the antifungal properties of the HYP-LCPS were evaluated in a murine in vivo model; for this, infected C57BL female mice groups were treated with both HYP in solution and HYP-LCPS, and after 6 days colony forming unit (CFU)/ml count was performed. PLM and SAXS confirmed that HYP-LCPS is a microemulsion situated in boundary transition region confirming its action as an LCPS. When in contact with simulated vaginal fluid, HYP-LCPS became rigid and exhibited maltase crosses and bragg peaks characteristics of lamellar phase. Ex vivo permeation and retention studies showed that HYP-LCPS provides a localized treatment on the superficial layers of porcine vaginal mucosa. HYP-LCPS induced a significant reduction in the number of CFU/ml in the mice; thus this formulation indicated it is as effective as a commercial dosage form. It was concluded that LCPS maintains the biological activity of HYP and provides an adequate drug delivery system for this lipophilic molecule at the vaginal mucosa, being a promising option in cases of VVC. (AU)

FAPESP's process: 19/10261-2 - Evaluation of the potential of nanostructured lipid carriers for co-encapsulation of curcumin and fluconazole dispersed in thermally-responsive hydrogels in the treatment of vulvovaginal candidiasis
Grantee:Victor Hugo Sousa Araujo
Support type: Scholarships in Brazil - Doctorate
FAPESP's process: 16/11198-4 - Nanostructured lipid carriers dispersed in situ gelling hydrogel for vaginal administration of hypericin associated with photodynamic therapy in the treatment of vulvovaginal candidiasis
Grantee:Mariana Rillo Sato
Support type: Scholarships in Brazil - Doctorate