School of Pharmacy, Shanxi Medical University, Taiyuan 030001, China; School of Pharmacy & Institute of Materia Medica, Shandong First Medical University & Shandong Academy of Medical Sciences, Jinan 250117, Shandong, China; Medicinal Basic Research Innovation Center of Chronic Kidney Disease, Ministry of Education, Shanxi Medical University, Taiyuan 030001, China; Shanxi Provincial Key Laboratory of Drug Synthesis and Novel Pharmaceutical Preparation Technology, Shanxi Medical University, Taiyuan 030001, China.
School of Pharmacy, Shanxi Medical University, Taiyuan 030001, China; Medicinal Basic Research Innovation Center of Chronic Kidney Disease, Ministry of Education, Shanxi Medical University, Taiyuan 030001, China; Shanxi Provincial Key Laboratory of Drug Synthesis and Novel Pharmaceutical Preparation Technology, Shanxi Medical University, Taiyuan 030001, China.
Int J Pharm. 2024 Apr 10;654:123963. doi: 10.1016/j.ijpharm.2024.123963. Epub 2024 Mar 1.
Inflammation in hair follicles will reduce the effectiveness of minoxidil (MXD) in the treatment of androgen alopecia (AGA) caused by elevated androgen levels. To target multiple physiological and pathological processes in AGA, a novel natural bioactive compound modified transfersomes (MXD-Rg3@TFs) was prepared to replace cholesterol that may disrupt hair growth, with ginsenosides Rg3 (Rg3) that have anti-inflammatory effects on AGA. The effects of MXD, Rg3 and their combination on AGA were evaluated using dihydrotestosterone (DHT) induced human dermal papilla cells (DPCs), and the results showed that the combination of MXD and Rg3 can significantly promote the proliferation, reduce the level of intracellular ROS and inflammatory factors, and inhibit the aging of DHT induced DPCs. Compared with cholesterol membrane transfersomes (MXD-Ch@TFs), MXD-Rg3@TFs has similar deformability, smaller particle size and better stability. MXD-Rg3@TFs has also significant advantages in shortening telogen phase and prolonging the growth period of hair follicles in C57BL/6 mice than MXD-Ch@TFs and commercial MXD tincture. The prominent ability of MXD-Rg3@TFs to inhibit the conversion of testosterone to DHT and reduce the level of inflammatory factors suggested that Rg3 and MXD in MXD-Rg3@TFs have synergistic effect on AGA therapy. MXD-Ch@TFs with no irritation to C57BL/6 mice skin is expected to reduce the dose of MXD and shorten the treatment time, which would undoubtedly provide a promising therapeutic option for treatment of AGA.
毛囊内的炎症会降低米诺地尔（MXD）在治疗因雄激素水平升高引起的雄激素性脱发（AGA）的疗效。为了针对 AGA 的多种生理和病理过程，制备了一种新型天然生物活性化合物修饰传递体（MXD-Rg3@TFs），用具有 AGA 抗炎作用的人参皂苷 Rg3（Rg3）代替可能破坏头发生长的胆固醇。使用二氢睾酮（DHT）诱导的人真皮乳头细胞（DPC）评估 MXD、Rg3 及其组合对 AGA 的影响，结果表明 MXD 和 Rg3 的组合可显著促进增殖，降低细胞内 ROS 和炎症因子水平，并抑制 DHT 诱导的 DPC 衰老。与胆固醇膜传递体（MXD-Ch@TFs）相比，MXD-Rg3@TFs 具有相似的变形性、更小的粒径和更好的稳定性。与 MXD-Ch@TFs 和商业 MXD 酊剂相比，MXD-Rg3@TFs 在缩短休止期和延长毛囊生长期方面也具有显著优势。MXD-Rg3@TFs 抑制睾酮转化为 DHT 和降低炎症因子水平的突出能力表明，MXD-Rg3@TFs 中的 Rg3 和 MXD 对 AGA 治疗具有协同作用。对 C57BL/6 小鼠皮肤无刺激的 MXD-Ch@TFs 有望降低 MXD 剂量并缩短治疗时间，这无疑为治疗 AGA 提供了一种有前途的治疗选择。
