New Formulations Loading Caspofungin for Topical Therapy of Vulvovaginal Candidiasis.

Noelia Pérez-González,José A Morales-Molina,Beatriz Clares-Naveros,José L Soriano-Ruiz,Francisco Fernández-Campos,Nuria Bozal-De Febrer,María J Rodríguez-Lagunas,Ana C Calpena-Campmany,Anna Nardi-Ricart

doi:10.3390/gels7040259

Abstract

Vulvovaginal candidiasis (VVC) poses a significant problem worldwide affecting women from all strata of society. It is manifested as changes in vaginal discharge, irritation, itching and stinging sensation. Although most patients respond to topical treatment, there is still a need for increase the therapeutic arsenal due to resistances to anti-infective agents. The present study was designed to develop and characterize three hydrogels of chitosan (CTS), Poloxamer 407 (P407) and a combination of both containing 2% caspofungin (CSP) for the vaginal treatment of VVC. CTS was used by its mucoadhesive properties and P407 was used to exploit potential advantages related to increasing drug concentration in order to provide a local effect. The formulations were physically, mechanically and morphologically characterized. Drug release profile and ex vivo vaginal permeation studies were performed. Antifungal efficacy against different strains of Candida spp. was also evaluated. In addition, tolerance of formulations was studied by histological analysis. Results confirmed that CSP hydrogels could be proposed as promising candidates for the treatment of VVC.

Highlights

IntroductionVulvovaginal candidiasis (VVC) is a health problem that affects approximately 70–75%
Vulvovaginal candidiasis (VVC) is a health problem that affects approximately 70–75%of women worldwide at least once during their lifetime [1,2]
When the formulations were mixed with simulated vaginal fluid (SVF), the pH of CSP-CTS and CSP-CTS/Poloxamer 407 (P407) remained unaltered, while the pH of CSP-P407 decreased to 4.58 ± 0.10

Summary

Introduction

Vulvovaginal candidiasis (VVC) is a health problem that affects approximately 70–75%. Of women worldwide at least once during their lifetime [1,2]. It has been estimated that about 50% of women will suffer VVC again and 8% will develop chronic VVC [3]. The symptoms include changes in vaginal discharge, irritation and itching sensation, stinging, burning sensation inside and/or outside the vagina, pain during urination and discomfort during sexual intercourse. Other symptoms include scratching lesions, swelling and vulvar redness [4]. Candidiasis is commonly caused by Candida spp. The predominant species are C. albicans, followed by C. glabrata, C. tropicalis, C. krusei and C. parapsilosis [5]. VVC is estimated to be the second most common cause of vaginitis after bacterial vaginosis.

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