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将非那雄胺载入醚醇纳米载体用于靶向毛囊皮脂腺单位的制备与评价。

Development and evaluation of finasteride loaded ethosomes for targeting to the pilosebaceous unit.

机构信息

a Department of Pharmaceutics , PSG College of Pharmacy , Coimbatore , India.

b Nanobiotechnology Laboratory , PSG Institute of Advanced Studies , Coimbatore , India.

出版信息

Artif Cells Nanomed Biotechnol. 2018 Dec;46(8):1892-1901. doi: 10.1080/21691401.2017.1396221. Epub 2017 Oct 31.

Abstract

Androgenetic alopecia, a major cause for baldness, is caused by the deposition of dihydrotestosterone (DHT) at the androgen receptors present in the pilosebaceous unit (PSU). Finasteride (FIN) is a potent 5α-reductase inhibitor capable of preventing the conversion of testosterone to DHT. But, its oral administration in males causes infertility. An attempt was made to prepare ethosomes of FIN with a size range 100-300 nm to enhance its delivery to the PSU. Finasteride loaded ethosomes (FES) were prepared using an ultra-probe sonicator and characterized for its size, morphology, surface charge and entrapment efficiency. The ability of FES to permeate across rat skin and frontal scalp skin of human cadaver was also evaluated. The spherical shaped ethosomes of different batches were in the size range of 107.8 ± 2.50 to 220.4 ± 6.92 nm and showed good permeation across rat skin and frontal scalp skin of human cadaver when compared to the unencapsulated FIN. The results portrayed the ability of FES to permeate across the stratum corneum to reach the PSU of the hair follicle. Although additional use of permeation enhancer increases the permeation of FIN across the skin, its addition may not be a favourable option for the deposition of ethosomes in the PSU.

摘要

雄激素性脱发是导致秃顶的主要原因,它是由双氢睾酮 (DHT) 在毛囊皮脂腺单位 (PSU) 中的雄激素受体沉积引起的。非那雄胺 (FIN) 是一种有效的 5α-还原酶抑制剂,能够阻止睾酮转化为 DHT。但是,它在男性中的口服给药会导致不育。人们试图制备 FIN 的醇质体,其粒径范围为 100-300nm,以增强其向 PSU 的传递。使用超声探针制备了载有非那雄胺的醇质体 (FES),并对其粒径、形态、表面电荷和包封效率进行了表征。还评估了 FES 穿过大鼠皮肤和人尸体额头皮的能力。不同批次的球形醇质体的粒径范围为 107.8±2.50 至 220.4±6.92nm,与未包封的 FIN 相比,其穿过大鼠皮肤和人尸体额头皮的能力较好。结果表明 FES 能够穿透角质层到达毛囊的 PSU。尽管额外使用渗透增强剂可以增加 FIN 穿过皮肤的渗透,但将其添加到 PSU 中可能不是醇质体沉积的有利选择。

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