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

[Display omitted] •Dutasteride (DU) and Tamsulosin (TA) was loaded in transdermal microemulsions.•A simultaneous quantification of DU and TA was developed by the UV–vis spectroscopy.•DU–TA loaded Microemulsions showed nanometric size, stability and low viscosity.•DU–TA loaded Microemulsions has grea...

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Bibliographic Details
Published in:	Colloids and surfaces, B, Biointerfaces Vol. 185; p. 110573
Main Authors:	Ciríaco, Shayara Lopes, Carvalho, Ivana Pereira Santos, Alves Terceiro Neto, José, de Sousa Lima Neto, José, de Oliveira, Daniel Henrique Bento, Cunha, Ana Paula Gomes Pereira, Cavalcante, Ykro Talvanis Duarte, da Silva, Dayane Tomaz Casimiro, da Silva, José Alexsandro, Mineiro, Ana Lys Bezerra Barradas, de Lima Chagas Moreno Fernandes, Maria Zenaide, Carvalho, André Luis Menezes
Format:	Journal Article
Language:	English
Published:	Elsevier B.V 01-01-2020
Subjects:	Dutasteride Hyperplasia Microemulsion Prostate Tamsulosin Transdermal Dutasteride Tamsulosin Transdermal Microemulsion Prostate Hyperplasia
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Summary:	[Display omitted] •Dutasteride (DU) and Tamsulosin (TA) was loaded in transdermal microemulsions.•A simultaneous quantification of DU and TA was developed by the UV–vis spectroscopy.•DU–TA loaded Microemulsions showed nanometric size, stability and low viscosity.•DU–TA loaded Microemulsions has great potential for benign prostatic hyperplasia. 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.
ISSN:	0927-7765 1873-4367
DOI:	10.1016/j.colsurfb.2019.110573