Purpose

This investigation was aimed to develop and evaluate lipid nanoemulsion-based gel of finasteride for topical administration, to increase drug availability into the skin for a long duration and to improve the in vivo potential of finasteride against alopecia.

Methods

Nanoemulsion was prepared by a high-speed homogenization method using Vit E oil, cholesterol, and soya lecithin, characterized, and thickened using guar gum (nanoemulgel). Nanoemulgel was evaluated for pH, viscosity, drug release, skin permeability, and in vivo efficacy against alopecia.

Results and Discussion

Size of the drug-loaded nanoemulsion droplets was observed to be 195.20 ± 9.43 nm with uniform size distribution (PDI; 0.25 ± 0.08) and negative zeta potential (− 7.61 ± 1.35 mV). The pH 5.37 ± 0.74 of the developed gel was found to be near to the skin pH. Gel showed slow release (94.77% in 24 h) and restricted permeation through the skin, i.e., 30.7% in 24 h. Macroscopic examination showed improved hair growth in the case of nanoemulgel. Hair diameter and length were observed to be increased significantly in the case of gel as compared with the testosterone treated group. The histological investigation supports the result of macroscopic examination where nanoemulgel restored the conditions (short length hair, necrotic cell appearance with miniaturized follicles) created by testosterone on the skin. Moreover, the developed formulation was observed to be safe and stable for at least 90 days.

Conclusion

The results prove the clinical pertinence of this stable gel as it ensured longer stay over the skin, slower permeation and higher efficacy against alopecia.

中文翻译：

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纳米乳有效地递送非那雄胺抗雄性脱发

目的

这项研究旨在开发和评估用于局部给药的非那雄胺脂质纳米乳基凝胶，以长期增加皮肤中的药物利用率，并提高非那雄胺抗脱发的体内潜力。

方法

通过使用Vit E油，胆固醇和大豆卵磷脂的高速均质化方法制备纳米乳剂，并使用瓜尔豆胶（nanoemulgel）对其进行表征和增稠。评估了纳米乳胶的pH，粘度，药物释放，皮肤通透性和体内对脱发的功效。

结果和讨论

观察到载药纳米乳剂液滴的尺寸为195.20±9.43 nm，具有均匀的尺寸分布（PDI； 0.25±0.08）和zeta负电势（-7.61±1.35 mV）。发现已显影的凝胶的pH 5.37±0.74接近皮肤pH。凝胶显示缓慢释放（24小时内为94.77％），并限制了其透过皮肤的渗透，即24小时内为30.7％。宏观检查显示，在纳米乳剂的情况下，毛发生长得到改善。在凝胶的情况下，与睾丸激素治疗组相比，头发直径和长度明显增加。组织学研究支持了宏观检查的结果，其中纳米乳胶恢复了睾丸激素在皮肤上造成的状况（短发，坏死的细胞外观和微小的卵泡）。此外，

结论

结果证明了这种稳定凝胶的临床相关性，因为它确保了在皮肤上的停留时间更长，渗透速度更慢，并且对脱发的功效更高。