School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China.
Department of Traditional Chinese Medicine, Guangzhou Red Cross Hospital of Jinan University, Guangzhou 510000, China.
Int J Pharm. 2022 Sep 25;625:122109. doi: 10.1016/j.ijpharm.2022.122109. Epub 2022 Aug 13.
Alopecia affected approximately 16.6% of all people in China, however, treatment options remain limited due to the side effects. Plant bioactive compound baicalin (BC) possesses hair growth-promotion activity, but poor water solubility and unsuitable log P value restrict its topical application, and natural Glycyrrhizin (GL) can exactly overcome these drawbacks. Here, BC was encapsulated in GL to form GL-BC micelles for alopecia treatment. Simultaneously, tween 80 (TW) as carriers was incorporated in the GL-BC to form GL-TW-BC micelles. The topical penetration, penetration pathways, cellular uptake and the underlying mechanisms behind the hair loss reconstruction of the GL micelles were investigated. We found the optimal GL-BC and GL-TW-BC formulations significantly improved the penetration and accumulation of BC in the porcine skin predominantly through the hair follicles pathways without causing skin irritation, which resulted in a targeted treatment. The proliferation of human dermal papilla cells (hDPCs) and effective cellular uptake was also enhanced. Moreover, the activation of the Wnt/β-catenin pathway, up-expression of vascular endothelial growth factor (VEGF), α-melanocyte-stimulating hormone (α-MSH) and interleukin-10 (IL-10) were the mechanisms of micelles for the hair recovery. Interestingly, GL and BC exhibited a synergistic treatment of alopecia. Collectively, GL-BC and GL-TW-BC can be used as promising approaches for the treatment of alopecia.
在中国,大约有 16.6%的人受到脱发的影响,然而,由于副作用的存在,治疗选择仍然有限。植物生物活性化合物黄芩苷(BC)具有促进头发生长的活性,但由于水溶性差和不合适的 log P 值,限制了其在局部的应用,而天然甘草酸(GL)正好可以克服这些缺点。在这里,BC 被包裹在 GL 中形成 GL-BC 胶束,用于治疗脱发。同时,将吐温 80(TW)作为载体加入到 GL-BC 中,形成 GL-TW-BC 胶束。研究了 GL 胶束治疗脱发的透皮渗透、渗透途径、细胞摄取和头发重建的潜在机制。我们发现,最佳的 GL-BC 和 GL-TW-BC 配方显著提高了 BC 在猪皮中的渗透和积累,主要通过毛囊途径,而不会引起皮肤刺激,从而实现了靶向治疗。人真皮乳头细胞(hDPCs)的增殖和有效的细胞摄取也得到了增强。此外,Wnt/β-catenin 通路的激活、血管内皮生长因子(VEGF)、α-促黑色素细胞激素(α-MSH)和白细胞介素-10(IL-10)的表达上调是胶束促进头发生长的机制。有趣的是,GL 和 BC 对脱发表现出协同治疗作用。总之,GL-BC 和 GL-TW-BC 可以作为治疗脱发的有前途的方法。