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J Pharm Sci ; 105(7): 2188-93, 2016 07.
Artículo en Inglés | MEDLINE | ID: mdl-27220471

RESUMEN

This study proposed to investigate and to compare colloidal carrier systems containing Zidovudine (3'-azido-3'-deoxythymidine) (AZT) for transdermal administration and optimization of antiretroviral therapy. Microemulsion (ME) and lamellar phase (LP) liquid crystal were obtained and selected from pseudoternary diagrams previously developed. Small-angle X-ray scattering and rheology analysis confirmed the presence of typical ME and liquid crystalline structures with lamellar arrangement, respectively. Both colloidal carrier systems, ME, and LP remained stable, homogeneous, and isotropic after AZT addition. In vitro permeation study (using pig ear skin) showed that the amount of permeated drug was higher for ME compared to the control and LP, obtaining a permeation enhancing effect on the order of approximately 2-fold (p < 0.05). Microscopic examination after in vivo skin irritation studies using mice suggested few histological changes in the skin of animals treated with the ME compared to the control group (hydrogel). Thus, ME proved to be adequate and have promising effects, being able to promote the drug permeation without causing apparent skin irritation. On the order hand, LP functioned as a drug reservoir reducing AZT partitioning into the skin.


Asunto(s)
Fármacos Anti-VIH/administración & dosificación , Sistemas de Liberación de Medicamentos , Zidovudina/administración & dosificación , Administración Cutánea , Animales , Fármacos Anti-VIH/efectos adversos , Fármacos Anti-VIH/farmacocinética , Emulsiones , Femenino , Hidrogeles , Irritantes , Cristales Líquidos , Ratones , Nanotecnología , Dispersión de Radiación , Absorción Cutánea , Porcinos , Rayos X , Zidovudina/efectos adversos , Zidovudina/farmacocinética
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