Zhao Ziyi, Wang Yue, Xing Hui, Wang Yucheng, Lv Kai, Pan Xiangjun, Chen Tuo, Hu Yunfeng, Li Guowei, Ma Dong
Key Laboratory of Biomaterials of Guangdong Higher Education Institutes, Department of Biomedical Engineering, Jinan University, Guangzhou 510632, China.
The First Affiliated Hospital of Jinan University, Jinan University, Guangzhou 510630, China.
Colloids Surf B Biointerfaces. 2025 Jul 16;255:114956. doi: 10.1016/j.colsurfb.2025.114956.
Minoxidil (Mi) is currently one of the most commonly used drugs for the treatment of hair loss in clinical settings. It works by accelerating blood flow around the hair follicles, enhancing local oxygen and nutrient supply, thereby promoting hair growth. However, traditional formulations of Mi have a short residence time on the skin, are prone to causing allergic reactions, scaling, and may even induce systemic hypertrichosis as side effects. This highlights the urgent need for the development of more efficient and safer delivery systems to improve its therapeutic efficacy. In previous studies, our team developed a high molecular weight hyaluronic acid-based delivery platform (HL) with excellent skin penetration, anti-inflammatory properties, and tissue repair capabilities. In this study, we used the HL delivery material as a carrier for Mi and developed a Mi delivery system with high drug encapsulation efficiency and good biological safety-HL@Mi. This delivery system encapsulates Mi within HL using techniques such as reverse evaporation, high-speed homogenization, and microjet high-pressure methods. Fluorescent labeling and high-performance liquid chromatography (HPLC) were employed to confirm that HL@Mi significantly enhanced the skin penetration and retention of Mi, effectively improving the local bioavailability of Mi. In vitro experiments, HL@Mi significantly reduced the cytotoxicity of Mi, while optimizing the hair follicle microenvironment by promoting angiogenesis and regulating the expression of IL-6, MMP3, and β-catenin genes associated with hair follicle function. In an established androgenetic alopecia animal model, HL@Mi significantly downregulated the expression of inflammatory factors such as IL-6, TNF-α, and TGF-β1 in the skin, while upregulating Ki67 expression in the hair follicle tissue, thereby accelerating hair growth and effectively improving hair loss symptoms. Moreover, HL@Mi exhibited good biocompatibility and safety. In summary, HL@Mi, as a novel transdermal delivery system, not only provides a more efficient and safer clinical alternative for Mi in the treatment of androgenetic alopecia, but also offers valuable technical insights for other local drug delivery strategies.
米诺地尔（Mi）是目前临床上治疗脱发最常用的药物之一。它通过加速毛囊周围的血液流动，增强局部氧气和营养供应，从而促进头发生长。然而，传统的米诺地尔制剂在皮肤上的停留时间短，容易引起过敏反应、脱屑，甚至可能导致全身性多毛症等副作用。这凸显了迫切需要开发更高效、更安全的给药系统以提高其治疗效果。在先前的研究中，我们团队开发了一种具有优异皮肤渗透性、抗炎特性和组织修复能力的高分子量透明质酸基给药平台（HL）。在本研究中，我们使用HL给药材料作为米诺地尔的载体，开发了一种具有高药物包封效率和良好生物安全性的米诺地尔给药系统——HL@Mi。该给药系统采用逆蒸发、高速均质和微射流高压等技术将米诺地尔包裹在HL中。采用荧光标记和高效液相色谱（HPLC）来确认HL@Mi显著增强了米诺地尔的皮肤渗透性和滞留性，有效提高了米诺地尔的局部生物利用度。体外实验中，HL@Mi显著降低了米诺地尔的细胞毒性，同时通过促进血管生成和调节与毛囊功能相关的IL-6、MMP3和β-连环蛋白基因的表达来优化毛囊微环境。在已建立的雄激素性脱发动物模型中，HL@Mi显著下调皮肤中IL-6、TNF-α和TGF-β1等炎症因子的表达，同时上调毛囊组织中Ki67的表达，从而加速头发生长并有效改善脱发症状。此外，HL@Mi表现出良好的生物相容性和安全性。综上所述，HL@Mi作为一种新型透皮给药系统，不仅为米诺地尔治疗雄激素性脱发提供了一种更高效、更安全的临床替代方案，也为其他局部药物递送策略提供了有价值的技术见解。
