<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml">The purpose of this study was to develop pluronic-based <italic>in situ</italic> gelling formulations of metronidazole (MTZ) for treatment of bacterial vaginosis, aimed at prolonging the residence time, controlling drug release, enhancing efficacy, decreasing recurrence, and increasing patient compliance. The <italic>in situ</italic> gel formulations were prepared using different concentrations of pluronic F-127 (PF-127) alone and in combination with pluronic F-68 (PF-68). The prepared formulations were evaluated for their gelation temperature (<italic>T</italic>gel), <italic>in vitro</italic> drug release, rheological properties, mucoadhesion properties and tolerability by vaginal mucosa in tissue levels. The <italic>T</italic>gel decreased with increasing PF-127 concentration. The <italic>T</italic>gel was modulated by addition of PF-68 to be within the acceptable range of 25-37 °C. With increasing pluronic concentration, the <italic>in vitro</italic> drug release decreased, viscosity and mucoadhesive force increased. Histopathological examination of rabbit vaginas from the control and treated groups revealed normal histology of the vagina and cervix. Based on the <italic>in vitro</italic> evaluation of prepared formulations, the <italic>in situ</italic> gelling liquid formulated with PF-127/PF-68 (20/10 %, <italic>m/m</italic>) was selected for further clinical evaluation.</abstract>

The purpose of this study was to develop pluronic-based in situ gelling formulations of metronidazole (MTZ) for treatment of bacterial vaginosis, aimed at prolonging the residence time, controlling drug release, enhancing efficacy, decreasing recurrence, and increasing patient compliance. The in situ gel formulations were prepared using different concentrations of pluronic F-127 (PF-127) alone and in combination with pluronic F-68 (PF-68). The prepared formulations were evaluated for their gelation temperature (Tgel), in vitro drug release, rheological properties, mucoadhesion properties and tolerability by vaginal mucosa in tissue levels. The Tgel decreased with increasing PF-127 concentration. The Tgel was modulated by addition of PF-68 to be within the acceptable range of 25-37 °C. With increasing pluronic concentration, the in vitro drug release decreased, viscosity and mucoadhesive force increased. Histopathological examination of rabbit vaginas from the control and treated groups revealed normal histology of the vagina and cervix. Based on the in vitro evaluation of prepared formulations, the in situ gelling liquid formulated with PF-127/PF-68 (20/10 %, m/m) was selected for further clinical evaluation.

Development and characterization of thermosensitive pluronic-based metronidazole <italic>in situ</italic> gelling formulations for vaginal application

Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Egypt

Department of Obstetrics and Gynecology, Faculty of Medicine, Assiut University, Egypt

Department of Pathology and Clinical Pathology, Faculty of Veterinary Medicine, Assiut University, Egypt

Acta Pharmaceutica

Development and characterization of thermosensitive pluronic-based metronidazole  gelling formulations for vaginal application

The purpose of this study was to develop pluronic-based in situ gelling formulations of metronidazole (MTZ) for treatment of bacterial vaginosis, aimed at...

Development and characterization of thermosensitive pluronic-based metronidazole in situ gelling formulations for vaginal application

Publié en ligne: 03 avr. 2012

Pages: 59 - 70

DOI: https://doi.org/10.2478/v10007-012-0009-y

Mots clés
metronidazol, geliranje, mukoadhezija, pluronici

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