Yang Qin, Guo Peng, Lei Pengkun, Yang Qiaolin, Liu Yuchun, Tian Ya, Shi Wen, Zhu Chunxiao, Lei Min, Zeng Rui, Zhang Chen, Qu Yan
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.
Lu Huo Snow area E Se Limited Liability Company, Chengdu 626500, China.
Regen Biomater. 2024 Jul 16;11:rbae086. doi: 10.1093/rb/rbae086. eCollection 2024.
The skin stratum corneum (SC) barrier function will interfere with the absorption of topical treatment and reduce the drug's therapeutic effect on alopecia. Microneedles (MNs) can penetrate the skin barrier and deliver drugs to the dermis. Furthermore, MNs can mechanically stimulate the skin, which promotes hair growth. Thus, we designed a green and dissolvable composite microneedle made of hyaluronic acid (HA) and polysaccharide (BSP) to encapsulate cholesterol-free ginsenoside Rg3 liposomes (Rg3-LPs) to avoid cholesterol metabolism-producing testosterone to inhibit hair regeneration and minimize the effect of the SC barrier on liposomes absorption. HA and BSP can enhance the mechanical strength of Rg3-MNs to ensure the transport of liposomes to the hair follicle (HF) region while causing minimal skin irritation and guaranteeing cell compatibility. In addition, HA increased hair density and was more conducive to hair regeneration. In telogen effluvium (TE) and testosterone-induced androgenetic alopecia (AGA) animals, Rg3-MNs achieved comparable efficacy to minoxidil with low-frequency treatment and the quality of regenerated hair was higher. Furthermore, quantitative characterization and transcriptome sequencing results showed that Rg3-MNs promoted hair regeneration by promoting the expression of Wnt3a and Wnt10b genes, activating the Wnt/β-catenin pathway. Therefore, Rg3-MNs present broad prospects in the treatment of alopecia.
皮肤角质层（SC）的屏障功能会干扰局部治疗药物的吸收，并降低药物对脱发的治疗效果。微针（MNs）可以穿透皮肤屏障并将药物递送至真皮层。此外，微针还能对皮肤产生机械刺激，从而促进头发生长。因此，我们设计了一种由透明质酸（HA）和多糖（BSP）制成的绿色可溶解复合微针，用于包裹无胆固醇人参皂苷Rg3脂质体（Rg3-LPs），以避免胆固醇代谢产生睾酮抑制头发生长，并将SC屏障对脂质体吸收的影响降至最低。HA和BSP可以增强Rg3微针的机械强度，确保脂质体向毛囊（HF）区域的转运，同时使皮肤刺激最小化并保证细胞相容性。此外，HA可增加毛发密度，更有利于头发生长。在休止期脱发（TE）和睾酮诱导的雄激素性脱发（AGA）动物模型中，Rg3微针在低频治疗时达到了与米诺地尔相当的疗效，且再生毛发质量更高。此外，定量表征和转录组测序结果表明，Rg3微针通过促进Wnt3a和Wnt10b基因的表达、激活Wnt/β-连环蛋白通路来促进头发生长。因此，Rg3微针在脱发治疗方面具有广阔前景。
