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Dutasteride nanoemulsion preparation to inhibit 5-alpha-hair follicle reductase enzymes in the hair follicle; an ex vivo study.
IET Nanobiotechnology ( IF 2.3 ) Pub Date : 2022-10-31 , DOI: 10.1049/nbt2.12101
Mehri Memar Bashi Aval 1 , Elham Hoveizi 2 , Reza Mombeiny 3 , Mostafa Kazemi 3 , Saeedeh Saeedi 4, 5 , Shima Tavakol 6
Affiliation  

Alopecia is a treatable disorder that usually occurs due to high levels of 5-alpha dihydrotestosterone in hair follicles. To enhance the storage capacity of hair follicles and alleviate the inherent characteristics of dutasteride, 5-alpha reductase inhibitor, a prolonged-release nanocarrier was synthesised, and its influence on rat abdomen's skin was investigated. Results showed the lower ratio of S/Co (higher ethanol concentration) increased the hydrodynamic nanocarriers' particle size due to thermodynamic disturbance and Ostwald ripening. In contrast, an increase in surfactant through a decrease in interfacial tension resulted in smaller nanocarriers of 32.4 nm. Moreover, an increase in viscosity had an inverse correlation with the nanoemulsions' particle size. Nanocarriers containing ethanol showed less entrapment efficacy, perhaps due to the rapid dissolution of dutasteride into ethanol during nanoemulsification, while, based on Stokes' equation, the addition of ethanol resulted in smaller particle size and stability of the system. Skin permeation analysis using Franz diffusion cells showed nanocarriers could pass through the skin and release dutasteride for 6 days. In conclusion, the optimum concentration of ingredients is decisive in guaranteeing the ideal particle size, stability, and skin permeation of nanocarriers. The Present dutasteride nanocarrier would promise a prolonged and sustained-release drug delivery system for Alopecia therapy.

中文翻译:

抑制毛囊5-α-毛囊还原酶的度他雄胺纳米乳制剂;体外研究。

脱发是一种可治疗的疾病,通常是由于毛囊中 5-α 二氢睾酮水平过高所致。为了增强毛囊的储存能力并减轻度他雄胺、5-α还原酶抑制剂的固有特性,合成了一种缓释纳米载体,并研究了其对大鼠腹部皮肤的影响。结果表明,由于热力学扰动和奥斯特瓦尔德熟化,较低的 S/Co 比率(较高的乙醇浓度)增加了流体力学纳米载体的粒径。相反,通过降低界面张力来增加表面活性剂会导致 32.4 nm 的纳米载体更小。此外,粘度的增加与纳米乳液的粒径呈负相关。含有乙醇的纳米载体表现出较低的包封效果,可能是由于度他雄胺在纳米乳化过程中迅速溶解到乙醇中,而根据 Stokes 方程,乙醇的加入导致更小的粒径和系统的稳定性。使用 Franz 扩散池的皮肤渗透分析显示纳米载体可以穿过皮肤并释放度他雄胺 6 天。总之,成分的最佳浓度对于保证纳米载体的理想粒径、稳定性和皮肤渗透性具有决定性作用。本发明的度他雄胺纳米载体有望为脱发治疗提供延长和持续释放的药物输送系统。使用 Franz 扩散池的皮肤渗透分析显示纳米载体可以穿过皮肤并释放度他雄胺 6 天。总之,成分的最佳浓度对于保证纳米载体的理想粒径、稳定性和皮肤渗透性具有决定性作用。本发明的度他雄胺纳米载体有望为脱发治疗提供延长和持续释放的药物输送系统。使用 Franz 扩散池的皮肤渗透分析显示纳米载体可以穿过皮肤并释放度他雄胺 6 天。总之,成分的最佳浓度对于保证纳米载体的理想粒径、稳定性和皮肤渗透性具有决定性作用。本发明的度他雄胺纳米载体有望为脱发治疗提供延长和持续释放的药物输送系统。
更新日期:2022-10-31
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