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

IF 4.2 4区 医学 Q2 CHEMISTRY, MEDICINAL Drug Development Research Pub Date : 2025-03-18 DOI:10.1002/ddr.70076
Rui Wang, Ying Zhou, Peng Yan, Hailong Zhang, Jinsong Ding
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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.

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一种新的局部复合凝胶负载米诺地尔和托法替尼治疗斑秃:配方,表征和体外/体内评价
虽然外用米诺地尔是斑秃(AA)最常用的药物,但在治疗中重度斑秃患者中,其治疗效果有限,因为它只能促进毛囊生长,改善斑秃患者毛囊变性的特点,不能减轻局部炎症反应。因此,我们设计了一种新的外用复合凝胶负载米诺地尔和Janus激酶(JAK)抑制剂托法替尼。该复合凝胶不仅具有良好的半固体性质和渗透效果,而且在加速条件下稳定性可达3个月,保证了制剂的长期质量。该复方凝胶可通过下调炎症因子干扰素-γ与抗炎因子白介素-4的比值,有效促进毛囊生长,显著减轻局部炎症反应,达到协同治疗AA的目的。米诺地尔与托法替尼首次联合外用,为临床治疗AA提供了新的思路。
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来源期刊
CiteScore
6.40
自引率
2.60%
发文量
104
审稿时长
6-12 weeks
期刊介绍: Drug Development Research focuses on research topics related to the discovery and development of new therapeutic entities. The journal publishes original research articles on medicinal chemistry, pharmacology, biotechnology and biopharmaceuticals, toxicology, and drug delivery, formulation, and pharmacokinetics. The journal welcomes manuscripts on new compounds and technologies in all areas focused on human therapeutics, as well as global management, health care policy, and regulatory issues involving the drug discovery and development process. In addition to full-length articles, Drug Development Research publishes Brief Reports on important and timely new research findings, as well as in-depth review articles. The journal also features periodic special thematic issues devoted to specific compound classes, new technologies, and broad aspects of drug discovery and development.
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