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...
Guardado en:
| Autores principales: | , , |
|---|---|
| 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: |
| Sumario: | 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. |
|---|