Ali Mohammad Sajid, Alam Mohammad Sarfaraz, Alam Nawazish, Siddiqui Masoom Raza
Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan, K.S.A.
Department of Pharmaceutics, S.B.S College of Pharmacy, Patti, Amritsar, Punjab, India.
Iran J Pharm Res. 2014 Fall;13(4):1125-40.
Benign prostatic hyperplasia (BPH)is the most common condition in aging men, associated with lower urinary tract symptoms. It is caused due to the augmented levels of the androgen dihydrotestosterone. Dutasteride, a 5α-Reductase inhibitor has been recommended for the treatment of BPH upon oral administration. However, long term oral administration of dutasteride may cause sexual problem in man. Therefore the main objective of this study was to develop transdermal patch having nanoemulsion gel of dutasteride in order to enhance physical and chemical stability and eliminate adverse effect of dutasteride. Optimized nanoemulsion was prepared by aqueous phase-titration method and characterized by droplet size, viscosity and refractive index. In-vitro skin permeation of dutasteride through rat abdominal skin was determined by the Franz diffusion cell.Significant increase in the steady state flux (J ss), permeability coefficient (K p) and enhancement ratio (E r) was observed in optimized nanoemulsion formulation A1 (p < 0.05). The Er of optimized nanoemulsion A1 was found to be 1.52 times with respect to control which indicates transdermal delivery may be better approach for BPH. Stability studies were performed for the period of 3 months. It was found that droplet size, viscosity and refractive index were slightly increased at refrigerator and room temperature in 3 months period. However, the changes in these parameters were not statistically significant (p ≥ 0.05). The shelf-life of optimized nanoemulsion A1 was found to be 2.18 years at room temperature. These results indicated that both physical as well as chemical stability of dutasteride in nanoemulsion formulation.
良性前列腺增生（BPH）是老年男性中最常见的病症，与下尿路症状相关。它是由雄激素双氢睾酮水平升高引起的。度他雄胺，一种5α-还原酶抑制剂，已被推荐用于口服治疗BPH。然而，长期口服度他雄胺可能会导致男性出现性功能问题。因此，本研究的主要目的是开发一种含有度他雄胺纳米乳凝胶的透皮贴剂，以提高其物理和化学稳定性，并消除度他雄胺的不良反应。通过水相滴定法制备了优化的纳米乳，并通过粒径、粘度和折射率进行了表征。采用Franz扩散池测定了度他雄胺经大鼠腹部皮肤的体外透皮性能。在优化的纳米乳制剂A1中观察到稳态通量（Jss）、渗透系数（Kp）和增强比（Er）显著增加（p < 0.05）。发现优化的纳米乳A1相对于对照的Er为1.52倍，这表明透皮给药可能是治疗BPH的更好方法。进行了为期3个月的稳定性研究。发现在3个月的时间里，在冰箱和室温下，粒径、粘度和折射率略有增加。然而，这些参数的变化没有统计学意义（p≥0.05）。发现优化的纳米乳A1在室温下的保质期为2.18年。这些结果表明度他雄胺在纳米乳制剂中的物理和化学稳定性均良好。
