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Colloids Surf B Biointerfaces ; 185: 110573, 2020 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-31675643

RESUMO

Benign prostatic hyperplasia (BPH) is a condition characterized by a benign enlargement of the prostate that interferes with the normal flow of urine. This disease is treated with the oral administration of combination therapy comprising α-blockers (tamsulosin) and 5α-reductase inhibitors (dutasteride). However, these compounds have low bioavailability. Thus, transdermal microemulsions aimed at promoting permeation and efficient targeted drug delivery through the skin are used. The objectives of this study were to obtain microemulsions of the combined doses of dutasteride and tamsulosin and evaluate their anti-hyperplastic activity in vivo. A phase diagram (4:1) was obtained for the choice of microemulsions. The microemulsions were characterized in terms of the droplet size, rheology, pH, conductivity, refractive index, in vitro release profile, and antihyperplastic effect in vivo. A method for the simultaneous quantification of drugs was developed using UV-vis spectroscopy. The microemulsions had an average size less than 116 nm, an acidic pH and low viscosity. The conductivity ranged from 6.18 to 185.2 µS/cm. The in vitro release profile was sustained for 6 h. Microemulsions promoted the reduction in the size of testosterone-dependent organs (prostate and seminal vesicles). Transdermal formulations for the treatment of BPH were obtained as a therapeutic alternative to conventional treatments.


Assuntos
Dutasterida/uso terapêutico , Emulsões/química , Hiperplasia Prostática/tratamento farmacológico , Tansulosina/uso terapêutico , Animais , Liberação Controlada de Fármacos , Masculino , Transição de Fase , Próstata/efeitos dos fármacos , Próstata/patologia , Ratos Wistar , Reprodutibilidade dos Testes
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