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Open AccessFeature PaperArticle

Utilizing Liposomal Quercetin and Gallic Acid in Localized Treatment of Vaginal Candida Infections

1
Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy
2
Drug Transport and Delivery Research Group, Department of Pharmacy, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Universitetsveien 57, 9037 Tromsø, Norway
3
IVF Clinic, Department of Obstetrics and Gynecology, University Hospital of North Norway, Sykehusvegen 38, 9019 Tromsø, Norway
4
Women’s Health and Perinatology Research Group, Department of Clinical Medicine, University of Tromsø The Arctic University of Norway, Universitetsveien 57, 9037 Tromsø, Norway
5
Department of Medical Biology, Faculty of Health Sciences, University of Tromsø The Arctic University of Norway, Sykehusveien 44, 9037 Tromsø, Norway
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(1), 9; https://doi.org/10.3390/pharmaceutics12010009
Received: 19 November 2019 / Revised: 13 December 2019 / Accepted: 17 December 2019 / Published: 20 December 2019
Vulvovaginal candidiasis (VVC) is a widely spread fungal infection that causes itching, pain and inflammation at the vaginal site. Although common, currently available treatment suffers from limited efficacy and high recurrence. In addition, the growing problem of resistance to azole drugs used in current treatments emphasizes the need for superior treatment options. Antimicrobial polyphenols are an attractive approach offering multitargeting therapy. We aimed to develop novel liposomes for simultaneous delivery of two polyphenols (quercetin, Q, and gallic acid, GA) that, when released within the vaginal cavity, act in synergy to eradicate infection while alleviating the symptoms of VVC. Q was selected for its anti-itching and anti-inflammatory properties, while GA for its reported activity against Candida. Novel liposomes containing only Q (LP-Q), only GA (LP-GA) or both polyphenols (LP-Q+GA) were in the size range around 200 nm. Q was efficiently entrapped in both LP-Q and in LP-Q+GA (85%) while the entrapment of GA was higher in LP-Q+GA (30%) than in LP-GA (25%). Liposomes, especially LP-Q+GA, promoted sustained release of both polyphenols. Q and GA acted in synergy, increasing the antioxidant activities of a single polyphenol. Polyphenol-liposomes were not cytotoxic and displayed stronger anti-inflammatory effects than free polyphenols. Finally, LP-GA and LP-Q+GA considerably reduced C. albicans growth. View Full-Text
Keywords: vaginal infection; liposomes; Candida; polyphenols; quercetin; gallic acid vaginal infection; liposomes; Candida; polyphenols; quercetin; gallic acid
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MDPI and ACS Style

Giordani, B.; Basnet, P.; Mishchenko, E.; Luppi, B.; Škalko-Basnet, N. Utilizing Liposomal Quercetin and Gallic Acid in Localized Treatment of Vaginal Candida Infections. Pharmaceutics 2020, 12, 9.

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