Abstract
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.
Highlights
Vulvovaginal candidiasis (VVC) is an ever-living problem affecting 70–75% of women of reproductive age at least once during their life
The vaginal site is regarded as one of the most highly challenging sites for drug action and different approaches have been proposed as superior treatments in topical vaginal therapy
Liposomes are suitable for vaginal delivery because they are not interfering with vaginal microbiota and are able to protect active substances against external enzymatic degradation and rapid perturbations that can occur in the vaginal cavity [22]
Summary
Vulvovaginal candidiasis (VVC) is an ever-living problem affecting 70–75% of women of reproductive age at least once during their life. Around 40–50% of them will experience a recurrence, and especially serious is VVC among pregnant women. Other non-albicans related species, are the major causative agents of VVC [1,2]. C. albicans is a commensal microorganism, the perturbation of vaginal homeostasis could facilitate the overgrowth of this opportunistic fungus and the onset of symptomatic candidiasis. Even if VVC is not a life-threatening problem, it can impair the quality of life of patients leading to several physical and sexual impediments, with economic costs estimated at one billion dollars per year [1,2,3].
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