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一种用于治疗斑秃的新型局部复方凝胶,负载米诺地尔和托法替布:制剂、表征及体外/体内评价

A Novel Topical Compound Gel Loading Minoxidil and Tofacitinib for Treatment of Alopecia Areata: Formulation, Characterization, and In Vitro/In Vivo Evaluation.

作者信息

Wang Rui, Zhou Ying, Yang Peng, Zhang Hailong, Ding Jinsong

机构信息

Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, Hunan, China.

School of Life Science and Technology, Harbin Institute of Technology, Harbin, Heilongjiang, China.

出版信息

Drug Dev Res. 2025 Apr;86(2):e70076. doi: 10.1002/ddr.70076.

Abstract

Although topical minoxidil is the most common drug for alopecia areata (AA), it has limited therapeutic effect in the treatment of patients with moderate and severe AA because it can only promote hair follicle growth and improve the characteristics of hair follicle degeneration in AA and cannot alleviate local inflammatory response. Therefore, we designed a novel topical compound gel loading minoxidil and Janus kinases (JAK) inhibitors tofacitinib. The compound gel not only had good semi-solid properties and the effect of permeation but also maintained stability for up to 3 months under accelerated conditions, ensuring the long-term quality of the formulation. This compound gel can effectively improve hair follicle growth and significantly alleviate local inflammatory response by downregulation of the ratio of inflammatory factor interferon-γ to anti-inflammatory factor interleukin-4 in C3H/HeN mice bearing AA, achieving the purpose of synergistic treatment of AA. The first combination of minoxidil and tofacitinib in a topical formulation gives a new idea for the clinical treatment of AA.

摘要

尽管外用米诺地尔是斑秃(AA)最常用的药物,但它对中重度AA患者的治疗效果有限,因为它只能促进毛囊生长,改善AA患者毛囊退化的特征,而不能减轻局部炎症反应。因此,我们设计了一种新型外用复方凝胶,其负载了米诺地尔和Janus激酶(JAK)抑制剂托法替布。该复方凝胶不仅具有良好的半固体性质和渗透效果,而且在加速条件下可保持长达3个月的稳定性,确保了制剂的长期质量。这种复方凝胶可以通过下调C3H/HeN斑秃小鼠中炎性因子干扰素-γ与抗炎因子白细胞介素-4的比例,有效促进毛囊生长并显著减轻局部炎症反应,达到协同治疗AA的目的。米诺地尔和托法替布在局部制剂中的首次联合应用为AA的临床治疗提供了新思路。

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