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Acta Pharmaceutica

The Journal of Croatian Pharmaceutical Society

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1846-9558
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Volume 62, Issue 1 (Mar 2012)

Issues

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

El-Sayed Ibrahim / Sayed Ismail / Gihan Fetih / Omar Shaaban / Khaled Hassanein
  • Department of Pathology and Clinical Pathology, Faculty of Veterinary Medicine, Assiut University, Egypt
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ Noura Abdellah
Published Online: 2012-04-03 | DOI: https://doi.org/10.2478/v10007-012-0009-y

Development and characterization of thermosensitive pluronic-based metronidazole in situ 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 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.

Razvoj i karakterizacija in situ gelirajućih pripravaka metronidazola na bazi pluronika za vaginalnu primjenu

Cilj rada bio je razviti pripravke metronidazola (MTZ) za liječenje bakterijske vaginoze koji imaju sposobnost geliranja in situ, produljeno vrijeme zadržavanja na mjestu primjene, kontrolirano oslobađanje ljekovite tvari, povećanu učinkovitost te smanjiti ponovnu pojavu vaginoze i povećati suradljivost pacijenta. Pripravci koji geliraju in situ pripravljeni su koristeći različite koncentracije pluronika F-127 (PF-127), samog ili u kombinaciji s pluronikom F-68 (PF-68). Ispitivana je temperatura geliranja (Tgel) formulacija, in vitro oslobađanje ljekovite tvari, reološka svojstva, mukoadhezijska svojstva te kako ih podnaša vaginalna sluznica u slojevima tkiva. Uočeno je da se s povećanjem koncentracije PF-127 snižava Tgel. Dodatkom različitih količina PF-68 dobiveni su pripravci s rasponom Tgel od 25 do 37 ºC. S povećanjem koncentracije pluronika smanjilo se oslobađanje ljekovite tvari in vitro, a povećala se viskoznost i mukoadhezivnost. Histopatološ ka ispitivanja na zečicama ispitivane i kontrolne skupine dala su normalni histološ ki nalaz njihovih vagina i cerviksa. Na temelju in vitro evaluacije, formulacija s PF-127/PF-68 (20/10 %, m/m) izabrana je za daljnja klinička ispitivanja.

Keywords: metronidazole; in situ gelling; mucoadhesion; pluronics

Keywords: metronidazol; in situ geliranje; mukoadhezija; pluronici

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About the article


Published Online: 2012-04-03

Published in Print: 2012-03-01


Citation Information: Acta Pharmaceutica, ISSN (Online) 1846-9558, ISSN (Print) 1330-0075, DOI: https://doi.org/10.2478/v10007-012-0009-y.

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