Development of microemulsion of tamsulosin and dutasteride for benign prostatic hyperplasia therapy.

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.

Atividade antiandrogênica no tratamento da hiperplasia prostática benigna com nanocarreadores transdérmicos de dose combinada (tansulosina e dutasterida) / Antiandrogenic activity in Benign Prostatic Hyperplasia treatment with combined nanocarriers transdermal dose (tamsulosin and dutasteride)

Benign prostatic hyperplasia (BPH) is one of the most common diseases of the urogenital tract. Thisstudy aimed to obtain one transdermal microemulsion of dutasteride and tamsulosin, drugs used in the treatmentof BPH, characterize them and study your in vitro release, evaluating through in vivo studies the antiandrogenicactivity of transdermal microemulsion. The preparation of the formulation involved obtaining the microemulsionwith Dutasteride and Tamsulosin in the equivalent percentage of 0.2% for each drug. To carry out theantiandrogenic activity, were used 32 rats (Wistar) in four groups experimental. The characterization performedall formulations showed good results, in which the evaluation of anti-hyperplastic the microemulsiondemonstrated one reducing the organs testosterone-dependent (prostate and seminal vesicles) corroborated forthe study in question enabling then obtaining promising transdermal formulations for BPH treatment, presentingthus a therapeutic alternative to conventional treatments.(AU)

Atividade antiandrogênica no tratamento da hiperplasia prostática benigna com nanocarreadores transdérmicos de dose combinada (tansulosina e dutasterida) / Antiandrogenic activity in Benign Prostatic Hyperplasia treatment with combined nanocarriers transdermal dose (tamsulosin and dutasteride)

Benign prostatic hyperplasia (BPH) is one of the most common diseases of the urogenital tract. Thisstudy aimed to obtain one transdermal microemulsion of dutasteride and tamsulosin, drugs used in the treatmentof BPH, characterize them and study your in vitro release, evaluating through in vivo studies the antiandrogenicactivity of transdermal microemulsion. The preparation of the formulation involved obtaining the microemulsionwith Dutasteride and Tamsulosin in the equivalent percentage of 0.2% for each drug. To carry out theantiandrogenic activity, were used 32 rats (Wistar) in four groups experimental. The characterization performedall formulations showed good results, in which the evaluation of anti-hyperplastic the microemulsiondemonstrated one reducing the organs testosterone-dependent (prostate and seminal vesicles) corroborated forthe study in question enabling then obtaining promising transdermal formulations for BPH treatment, presentingthus a therapeutic alternative to conventional treatments.