Andrade Jayanaraian F M, Matos Breno N, Rocho Rafael V, Barbalho Geisa N, Cunha-Filho Marcilio, Gelfuso Guilherme M, Gratieri Taís
Laboratory of Food, Drugs, and Cosmetics (LTMAC), University of Brasilia (UnB), Brasília 70910-900, DF, Brazil.
Pharmaceutics. 2024 Nov 27;16(12):1524. doi: 10.3390/pharmaceutics16121524.
Although androgenic alopecia is the most prevalent among non-cicatricial alopecia, it still lacks an effective and safe treatment. Dutasteride (DUT) shows promising results in hair regrowth; however, oral DUT intake causes serious sexual adverse events. Hence, we produced liposomes with different bilayer structures and evaluated the capability of such systems in increasing DUT accumulation in the hair follicles. In vitro skin penetration tests were performed with porcine ear skin, and the follicular targeting factor (Tf) was calculated as the ratio between DUT amount in HFs and DUT recovered from the sum of all skin layers. While the stiffer DUT-loaded liposome was not able to target the hair follicles in 12 h (Tf = 0.15), a DUT-loaded liposome with an edge activator in its composition, i.e., transfersomes, promoted better control over DUT release and a higher Tf (0.32) ( < 0.005). Transfersomes present higher affinity with DUT providing a better controlled release; hence, they are a better option for DUT follicle targeting compared to liposomes. Further formulation optimizations are needed aiming to prolong such targeting effect.
尽管雄激素性脱发在非瘢痕性脱发中最为常见,但仍缺乏有效且安全的治疗方法。度他雄胺(DUT)在促进头发生长方面显示出有前景的效果;然而,口服度他雄胺会引发严重的性不良事件。因此,我们制备了具有不同双层结构的脂质体,并评估了此类体系增加度他雄胺在毛囊中蓄积的能力。使用猪耳皮肤进行体外皮肤渗透试验,并将毛囊靶向因子(Tf)计算为毛囊中度他雄胺含量与从所有皮肤层总和中回收的度他雄胺之比。虽然较硬的载有度他雄胺的脂质体在12小时内无法靶向毛囊(Tf = 0.15),但在其组成中含有边缘激活剂的载有度他雄胺的脂质体,即传递体,能更好地控制度他雄胺的释放并具有更高的Tf(0.32)(<0.005)。传递体与度他雄胺具有更高的亲和力,能实现更好的控释;因此,与脂质体相比,它们是度他雄胺靶向毛囊的更好选择。需要进一步进行制剂优化以延长这种靶向效果。