Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis

The purpose of this study was to design a novel vaginal delivery system composed of metronidazole microspheres dispersed within a bioadhesive gel. Microspheres were prepared by solvent evaporation method using Eudragit RS-100 and RL-100 polymers with different drug/polymer ratios. Microspheres we...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autores principales: Hani, Umme, Bhat, Sudeendra R., Shivakumar, Hosakote G.
Formato: Articulo
Lenguaje:Inglés
Publicado: 2011
Materias:
Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/8116
http://www.latamjpharm.org/resumenes/30/1/LAJOP_30_1_1_24.pdf
Aporte de:
id I19-R120-10915-8116
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Farmacia
Metronidazol
bioadhesive gel; metronidazole microspheres; vaginal candidiasis
Candidiasis Vulvovaginal
spellingShingle Farmacia
Metronidazol
bioadhesive gel; metronidazole microspheres; vaginal candidiasis
Candidiasis Vulvovaginal
Hani, Umme
Bhat, Sudeendra R.
Shivakumar, Hosakote G.
Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis
topic_facet Farmacia
Metronidazol
bioadhesive gel; metronidazole microspheres; vaginal candidiasis
Candidiasis Vulvovaginal
description The purpose of this study was to design a novel vaginal delivery system composed of metronidazole microspheres dispersed within a bioadhesive gel. Microspheres were prepared by solvent evaporation method using Eudragit RS-100 and RL-100 polymers with different drug/polymer ratios. Microspheres were characterized by SEM, DSC, FT-IR and particle size analysis and evaluated for morphology, drug loading and in vitro drug release in simulated vaginal fluid. The % yield, actual drug loading and encapsulation were found to range between 79 ± 0.5 to 94 ± 0.6%, 19.6 ± 0.27 to 35.91 ± 0.66 %, 69.3 ± 0.78 to 81.2 ± 0.36 %, respectively. The FT-IR and DSC spectra revealed that there was no chemical interaction between drug and polymers used. SEM revealed that microspheres were spherical with nearly smooth surface morphology with a mean particle size ranging from 177 ± 0.4 to 456 ± 0.5 µm. The formulation F9 have shown better in vitro release 99 % at 10 h. To achieve bioadhesion to mucosal tissue, formulation F9 was incorporated in the bioadhesive gel made of carbopol 934P. Metronidazole microspheres gel (MTZMG) was characterized by in vitro drug release and antifungal activity. The drug release was controlled up to12 h. Inhibition effect on the C. albicans j1012 growth, suggested their effectiveness in the treatment of vaginal candidiasis. It may be concluded from present study that MTZ-MG can be used as a novel delivery system for local therapy of vaginal candidiasis.
format Articulo
Articulo
author Hani, Umme
Bhat, Sudeendra R.
Shivakumar, Hosakote G.
author_facet Hani, Umme
Bhat, Sudeendra R.
Shivakumar, Hosakote G.
author_sort Hani, Umme
title Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis
title_short Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis
title_full Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis
title_fullStr Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis
title_full_unstemmed Formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis
title_sort formulation design and evaluation of metronidazole microspheres in a bioadhesive gel for local therapy of vaginal candidiasis
publishDate 2011
url http://sedici.unlp.edu.ar/handle/10915/8116
http://www.latamjpharm.org/resumenes/30/1/LAJOP_30_1_1_24.pdf
work_keys_str_mv AT haniumme formulationdesignandevaluationofmetronidazolemicrospheresinabioadhesivegelforlocaltherapyofvaginalcandidiasis
AT bhatsudeendrar formulationdesignandevaluationofmetronidazolemicrospheresinabioadhesivegelforlocaltherapyofvaginalcandidiasis
AT shivakumarhosakoteg formulationdesignandevaluationofmetronidazolemicrospheresinabioadhesivegelforlocaltherapyofvaginalcandidiasis
bdutipo_str Repositorios
_version_ 1764820487706247168