Development of a Mucoadhesive in Situ Gelling Formulation for the Delivery of Lactobacillus gasseri into Vaginal Cavity.

Barbara Vigani,Giuseppina Sandri,Silvia Rossi,Franca Ferrari,Angela Faccendini,Pietro Grisoli,Maria Cristina Bonferoni

doi:10.3390/pharmaceutics11100511

Barbara Vigani, Giuseppina Sandri + Show 5 more

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https://doi.org/10.3390/pharmaceutics11100511

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Journal: Pharmaceutics	Publication Date: Oct 3, 2019
Citations: 23	License type: CC BY 4.0

Affiliation: University of Pavia

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Local administration of vaginal probiotics, especially lactobacilli, has been recently proposed as an effective prevention strategy against candidosis recurrences, which affect 40–50% of women. In this context, the aim of the present work was the development of a mucoadhesive in situ gelling formulation for the vaginal administration of Lactobacillus gasseri. Mixtures of poloxamer 407 (P407) and methylcellulose (MC), two thermosensitive polymers, were prepared and subjected to rheological analyses for the assessment of their sol/gel transition temperature. The association of P407 (15% w/w) with MC (1.5% w/w) produced an increase in gelation extent at 37 °C even after dilution in simulated vaginal fluid (SVF). The presence of 0.5% w/w pectin (PEC) produced a reduction of vehicle pH and viscosity at 25 °C that is the vehicle resistance to flow during administration. The presence of a low concentration of xyloglucan (XYL) (0.25% w/w) increases the mucoadhesive properties and the capability to gelify at 37 °C of the formulation after dilution with SVF. A three-component (P407/MC/PEC; 3cM) and a four-component (P407/MC/PEC/XYL; 4cM) mixture were selected as promising candidates for the delivery of L. gasseri to the vaginal cavity. They were able to preserve L. gasseri viability and were cytocompatible towards the HeLa cell line.

Highlights

Vulvovaginal candidosis (VVC) is an opportunistic infection of vaginal mucosa, mainly caused by Candida sp. that represents one of the most frequent causes of gynecologic counseling
The aim of the present work was the development of a mucoadhesive in situ gelling formulation for the vaginal administration of Lactobacillus gasseri
The presence of a low concentration of xyloglucan (XYL) (0.25% w/w) increases the mucoadhesive properties and the capability to gelify at 37 ◦C of the formulation after dilution with simulated vaginal fluid (SVF)

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Introduction

Vulvovaginal candidosis (VVC) is an opportunistic infection of vaginal mucosa, mainly caused by Candida sp. that represents one of the most frequent causes of gynecologic counseling. Vulvovaginal candidosis (VVC) is an opportunistic infection of vaginal mucosa, mainly caused by Candida sp. Candidosis symptoms, even though not related to high mortality, negatively affect the patient quality of life: VVC is frequently associated to vaginal inflammation (vaginitis) with irritation and pruritus, dysuria and dyspareunia, a “cottage cheese-like” vaginal discharge, vulvar burning and fissuring, often accompanied by mucosal lesions and slight bleeding [1,2]. A change in vaginal microbiota composition in terms of a reduction of lactobacilli species favors the overgrowth of pathogens like Candida [3]. Candidosis affects 70–75% of women at least once in their life, during reproductive age; it has been reported that 40–50% of women experience one or more recurrences after the apparent resolution of the first infective episode. Most recurrences may be caused by the persistency of some yeast strains in the vaginal lumen despite antifungal treatment, along with some predisposing factors, rather than exogenous reinfections [4,5]

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