Synergistic effect of iontophoresis and chemical enhancers on transdermal permeation of tolterodine tartrate for the treatment of overactive bladder
Int. braz. j. urol
;
39(1): 63-76, January-February/2013. tab, graf
Artículo
en Inglés
| LILACS
| ID: lil-670379
ABSTRACT
Purpose The objective of the study was to evaluate the synergistic transdermal permeation effect of chemical enhancers and iontophoresis technique on tolterodine tartrate (TT) transdermal gel and to evaluate its pharmacokinetic properties. Materials and Methods Taguchi robust design was used for optimization of formulations. Skin permeation rates were evaluated using the Keshary-chein type diffusion cells in order to optimize the gel formulation. In-vivo studies of the optimized formulation were performed in a rabbit model and histopathology studies of optimized formulation were performed on rats. Results Transdermal gels were formulated successfully using Taguchi robust design method. The type of penetration enhancer, concentration of penetration enhancer, current density and pulse on/off ratio were chosen as independent variables. Type of penetration enhancer was found to be the significant factor for all the responses. Permeation parameters were evaluated when maximum cumulative amount permeated in 24 hours (Q24) was 145.71 ± 2.00µg/cm2 by CIT4 formulation over control (91.89 ± 2.30µg/cm2). Permeation was enhanced by 1.75 fold by CIT4 formulation. Formulation CIT4 containing nerolidol (5%) and iontophoretic variables applied (0.5mA/cm2 and pulse on/off ratio 31) was optimized. In vivo studies with optimized formulation CIT4 showed increase in AUC and T1/2 when compared to oral suspension in rabbits. The histological studies showed changes in dermis indicating the effect of penetration enhancers and as iontophoresis was continued only for two cycles in periodic fashion so it did not cause any skin damage observed in the slides. Conclusion Results indicated that iontophoresis in combination with chemical enhancers is an effective method for transdermal administration of TT in the treatment of overactive bladder. .
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Índice:
LILACS (Américas)
Asunto principal:
Fenilpropanolamina
/
Compuestos de Bencidrilo
/
Iontoforesis
/
Cresoles
/
Vejiga Urinaria Hiperactiva
/
Agentes Urológicos
Tipo de estudio:
Estudios de evaluación
/
Estudio pronóstico
Límite:
Animales
Idioma:
Inglés
Revista:
Int. braz. j. urol
Asunto de la revista:
Urología
Año:
2013
Tipo del documento:
Artículo
País de afiliación:
India
Institución/País de afiliación:
Osmania University/IN
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