Development of a Mucoadhesive In Situ Gelling Formulation for the Delivery of <i>Lactobacillus gasseri</i> into Vaginal Cavity

Local administration of vaginal probiotics, especially lactobacilli, has been recently proposed as an effective prevention strategy against candidosis recurrences, which affect 40&#8722;50% of women. In this context, the aim of the present work was the development of a mucoadhesive in situ gelli...

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Main Authors: Barbara Vigani, Angela Faccendini, Silvia Rossi, Giuseppina Sandri, Maria Cristina Bonferoni, Pietro Grisoli, Franca Ferrari
Format: Article
Language:English
Published: MDPI AG 2019-10-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/11/10/511
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author Barbara Vigani
Angela Faccendini
Silvia Rossi
Giuseppina Sandri
Maria Cristina Bonferoni
Pietro Grisoli
Franca Ferrari
author_facet Barbara Vigani
Angela Faccendini
Silvia Rossi
Giuseppina Sandri
Maria Cristina Bonferoni
Pietro Grisoli
Franca Ferrari
author_sort Barbara Vigani
collection DOAJ
description Local administration of vaginal probiotics, especially lactobacilli, has been recently proposed as an effective prevention strategy against candidosis recurrences, which affect 40&#8722;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 <i>Lactobacillus gasseri</i>. 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% <i>w</i>/<i>w</i>) with MC (1.5% <i>w</i>/<i>w</i>) produced an increase in gelation extent at 37 &#176;C even after dilution in simulated vaginal fluid (SVF). The presence of 0.5% <i>w</i>/<i>w</i> pectin (PEC) produced a reduction of vehicle pH and viscosity at 25 &#176;C that is the vehicle resistance to flow during administration. The presence of a low concentration of xyloglucan (XYL) (0.25% <i>w</i>/<i>w</i>) increases the mucoadhesive properties and the capability to gelify at 37 &#176;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 <i>L. gasseri</i> to the vaginal cavity. They were able to preserve <i>L. gasseri</i> viability and were cytocompatible towards the HeLa cell line.
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spelling doaj.art-410d145b7bb14b629f5ab76155bdce712022-12-22T02:53:08ZengMDPI AGPharmaceutics1999-49232019-10-01111051110.3390/pharmaceutics11100511pharmaceutics11100511Development of a Mucoadhesive In Situ Gelling Formulation for the Delivery of <i>Lactobacillus gasseri</i> into Vaginal CavityBarbara Vigani0Angela Faccendini1Silvia Rossi2Giuseppina Sandri3Maria Cristina Bonferoni4Pietro Grisoli5Franca Ferrari6Department of Drug Sciences, University of Pavia, V.le Taramelli, 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, V.le Taramelli, 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, V.le Taramelli, 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, V.le Taramelli, 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, V.le Taramelli, 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, V.le Taramelli, 12, 27100 Pavia, ItalyDepartment of Drug Sciences, University of Pavia, V.le Taramelli, 12, 27100 Pavia, ItalyLocal administration of vaginal probiotics, especially lactobacilli, has been recently proposed as an effective prevention strategy against candidosis recurrences, which affect 40&#8722;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 <i>Lactobacillus gasseri</i>. 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% <i>w</i>/<i>w</i>) with MC (1.5% <i>w</i>/<i>w</i>) produced an increase in gelation extent at 37 &#176;C even after dilution in simulated vaginal fluid (SVF). The presence of 0.5% <i>w</i>/<i>w</i> pectin (PEC) produced a reduction of vehicle pH and viscosity at 25 &#176;C that is the vehicle resistance to flow during administration. The presence of a low concentration of xyloglucan (XYL) (0.25% <i>w</i>/<i>w</i>) increases the mucoadhesive properties and the capability to gelify at 37 &#176;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 <i>L. gasseri</i> to the vaginal cavity. They were able to preserve <i>L. gasseri</i> viability and were cytocompatible towards the HeLa cell line.https://www.mdpi.com/1999-4923/11/10/511vaginal candidosis<i>l. gasseri</i>in situ thermogelling vehiclemucoadhesionpoloxamermethylcellulosepectinxyloglucan
spellingShingle Barbara Vigani
Angela Faccendini
Silvia Rossi
Giuseppina Sandri
Maria Cristina Bonferoni
Pietro Grisoli
Franca Ferrari
Development of a Mucoadhesive In Situ Gelling Formulation for the Delivery of <i>Lactobacillus gasseri</i> into Vaginal Cavity
Pharmaceutics
vaginal candidosis
<i>l. gasseri</i>
in situ thermogelling vehicle
mucoadhesion
poloxamer
methylcellulose
pectin
xyloglucan
title Development of a Mucoadhesive In Situ Gelling Formulation for the Delivery of <i>Lactobacillus gasseri</i> into Vaginal Cavity
title_full Development of a Mucoadhesive In Situ Gelling Formulation for the Delivery of <i>Lactobacillus gasseri</i> into Vaginal Cavity
title_fullStr Development of a Mucoadhesive In Situ Gelling Formulation for the Delivery of <i>Lactobacillus gasseri</i> into Vaginal Cavity
title_full_unstemmed Development of a Mucoadhesive In Situ Gelling Formulation for the Delivery of <i>Lactobacillus gasseri</i> into Vaginal Cavity
title_short Development of a Mucoadhesive In Situ Gelling Formulation for the Delivery of <i>Lactobacillus gasseri</i> into Vaginal Cavity
title_sort development of a mucoadhesive in situ gelling formulation for the delivery of i lactobacillus gasseri i into vaginal cavity
topic vaginal candidosis
<i>l. gasseri</i>
in situ thermogelling vehicle
mucoadhesion
poloxamer
methylcellulose
pectin
xyloglucan
url https://www.mdpi.com/1999-4923/11/10/511
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