Quercetin Nanocrystal Gel: A Novel Topical Therapeutic Strategy for Androgenetic Alopecia.

IF 5.5 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Yaya Su, Yuwen Zhu, Lei Ren, Xiang Deng, Rui Song, Lingling Wu, Zhihui Yang, Hailong Yuan
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Abstract

Purpose: Androgenetic alopecia (AGA) is a common, chronic, non-cicatricial dermatological condition characterized by progressive miniaturization of hair follicles. Although AGA is a benign disorder, it has a considerable impact on patients' quality of life and psychological health. The current treatment options often demonstrate limited efficacy and are frequently associated with undesirable side effects. This study aimed to co-mill two natural compounds, quercetin (QT) and glycyrrhizic acid (GL), to develop follicle-targeted nanocrystals (NCs), thereby enhancing local accumulation, improving the pathological follicular microenvironment associated with AGA, and promoting hair regrowth. Methods: QT nanocrystals (QT-NCs) were fabricated using a top-down wet media milling technique with GL as a bioactive stabilizer. The resulting QT-NCs were characterized regarding their particle size, crystallinity, morphology, and stability. The skin permeation properties of the QT-NCs were further evaluated in vitro, and their therapeutic efficacy was assessed in a dihydrotestosterone (DHT)-induced AGA mouse model. Results: The QT-NCs exhibited an irregular structure with a particle size ranging from 200 to 300 nm, demonstrating uniform dimensions and excellent storage stability. In vitro permeation studies revealed a 2.27-fold increase in cumulative penetration and a 2.47-fold enhancement in skin retention compared to raw QT. In the DHT-induced AGA mouse model, QT-NCs significantly reduced local DHT levels while concurrently modulating the follicular microenvironment, resulting in markedly improved therapeutic outcomes. Notably, when co-administered, QT and GL demonstrated synergistic pharmacological effects, suggesting potential combinatory benefits. Conclusions: This study presents the first demonstration of QT-NCs for AGA treatment, establishing a novel therapeutic strategy with substantial potential for clinical translation.

槲皮素纳米晶体凝胶:一种新的局部治疗雄激素性脱发的策略。
目的:雄激素性脱发(AGA)是一种常见的、慢性的、非瘢痕性皮肤病,其特征是毛囊的进行性小型化。虽然AGA是一种良性疾病,但它对患者的生活质量和心理健康有相当大的影响。目前的治疗方案往往表现出有限的疗效,并经常伴有不良的副作用。本研究旨在将槲皮素(QT)和甘草酸(GL)这两种天然化合物混合,形成毛囊靶向纳米晶体(NCs),从而促进局部积累,改善AGA相关的病理毛囊微环境,促进头发再生。方法:以GL为生物活性稳定剂,采用自顶向下湿介质研磨技术制备QT纳米晶体(QT- ncs)。所得到的QT-NCs在粒径、结晶度、形貌和稳定性方面进行了表征。进一步在体外评估QT-NCs的皮肤渗透特性,并在双氢睾酮(DHT)诱导的AGA小鼠模型中评估其治疗效果。结果:纳米碳管呈不规则结构,粒径在200 ~ 300 nm之间,尺寸均匀,贮存稳定性好。体外渗透研究显示,与原始QT相比,QT- ncs的累积渗透增加了2.27倍,皮肤滞留增加了2.47倍。在DHT诱导的AGA小鼠模型中,QT- ncs显著降低了局部DHT水平,同时调节了毛囊微环境,显著改善了治疗效果。值得注意的是,当共同给药时,QT和GL表现出协同药理作用,表明潜在的联合益处。结论:本研究首次展示了QT-NCs用于AGA治疗,建立了一种具有临床转化潜力的新型治疗策略。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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