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.
Colloids and surfaces. B, Biointerfaces. 2019 Oct 13 [Epub ahead of print]
Shayara Lopes Ciríaco, Ivana Pereira Santos Carvalho, José Alves Terceiro Neto, José de Sousa Lima Neto, Daniel Henrique Bento de Oliveira, Ana Paula Gomes Pereira Cunha, Ykro Talvanis Duarte Cavalcante, Dayane Tomaz Casimiro da Silva, José Alexsandro da Silva, Ana Lys Bezerra Barradas Mineiro, Maria Zenaide de Lima Chagas Moreno Fernandes, André Luis Menezes Carvalho
Graduate Program in Pharmaceutical Sciences, Department of Biochemistry and Pharmacology, Federal University of Piauí, Teresina, PI, Brazil., School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, São Paulo, Brazil. Electronic address: ., Department of Pharmacy, Federal University of Piauí, Teresina, PI, Brazil., Veterinary Medicine Department, Campus Minister Petronio Portela, Federal University of Piauí, Teresina, PI, Brazil., Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife, PE, Brazil., Department of Agrarian and Extract Sciences, Postgraduate Program in Agroindustry Systems, Federal University of Campina Grande, Pombal, PB, Brazil., Department of Veterinary Clinic and Surgery, Federal University of Piauí, Teresina, PI, Brazil.