Please use this identifier to cite or link to this item:
Title: Optimization of Innovative Three-Dimensionally-Structured Hybrid Vesicles to Improve the Cutaneous Delivery of Clotrimazole for the Treatment of Topical Candidiasis
Author: Manca, Maria Letizia
Usach, Iris
Peris, José Esteban
Ibba, Antonella
Orrù, Germano
Valenti, Donatella
Escribano Ferrer, Elvira
Gomez-Fernandez, Juan Carmelo
Aranda, Francisco José
Fadda, Anna Maria
Manconi, Maria
Keywords: Fosfolípids
Microscòpia electrònica
Raigs X
Electron microscopy
Issue Date: 6-Jun-2019
Publisher: MDPI
Abstract: New three-dimensionally-structured hybrid phospholipid vesicles, able to load clotrimazole in a high amount (10 mg/mL), were obtained for the first time in this work by significantly reducing the amount of water (≤10%), which was replaced with a mixture of glycerol and ethanol (≈90%). A pre-formulation study was carried out to evaluate the effect of both the composition of the hydrating medium and the concentration of the phospholipid on the physico-chemical properties of hybrid vesicles. Four different three-dimensionally-structured hybrid vesicles were selected as ideal systems for the topical application of clotrimazole. An extensive physico-chemical characterization performed using transmission electron microscopy (TEM), cryogenic transmission electron microscopy (cryo-TEM), 31P-NMR, and small-angle X-ray scattering (SAXS) displayed the formation of small, multi-, and unilamellar vesicles very close to each other, and was capable of forming a three-dimensional network, which stabilized the dispersion. Additionally, the dilution of the dispersion with water reduced the interactions between vesicles, leading to the formation of single unilamellar vesicles. The evaluation of the in vitro percutaneous delivery of clotrimazole showed an improved drug deposition in the skin strata provided by the three-dimensionally-structured vesicles with respect to the commercial cream (Canesten®) used as a reference. Hybrid vesicles were highly biocompatible and showed a significant antifungal activity in vitro, greater than the commercial cream Canesten®. The antimycotic efficacy of formulations was confirmed by the reduced proliferation of the yeast cells at the site of infection in vivo. In light of these results, clotrimazole-loaded, three-dimensionally-structured hybrid vesicles appear to be one of the most innovative and promising formulations for the treatment of candidiasis infections.
Note: Reproducció del document publicat a:
It is part of: Pharmaceutics, 2019, vol. 11, num. 6, p. 263
Related resource:
ISSN: 1999-4923
Appears in Collections:Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)

Files in This Item:
File Description SizeFormat 
690923.pdf2.86 MBAdobe PDFView/Open

This item is licensed under a Creative Commons License Creative Commons