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易于使用的将各种溶解的活性剂通过粒子介导运输到毛囊中的方法——一种新型平台技术。

Easy to use particle-mediated transport of various dissolved active agents into the hair follicles - A novel platform technology.

作者信息

Klein Anna Lena, Busch Loris, Lademann Jürgen, Meinke Martina C, Keck Cornelia M

机构信息

Charité - Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin and Humboldt-Universität zu Berlin, Department of Dermatology, Venereology and Allergology, Center of Experimental and Applied Cutaneous Physiology, Charitéplatz 1, 10117 Berlin, Germany.

Charité - Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin and Humboldt-Universität zu Berlin, Department of Dermatology, Venereology and Allergology, Center of Experimental and Applied Cutaneous Physiology, Charitéplatz 1, 10117 Berlin, Germany; Department of Pharmaceutics and Biopharmaceutics, Philipps University Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany.

出版信息

Int J Pharm. 2025 Feb 10;670:125200. doi: 10.1016/j.ijpharm.2025.125200. Epub 2025 Jan 8.

Abstract

The use of nanoparticulate systems for the transport of active ingredients into hair follicles has been researched for almost two decades, resulting in countless publications with a wide variety of particle types, release mechanisms and active ingredients. The production of a stable dispersion is often time-consuming and costly. In this publication, we demonstrate for the first time that simply adding diverse submicron particles to a drug solution significantly increases follicular penetration depth by over 160% to 190%, allowing the targeting of subinfundibular structures. Our results indicate that the increase in follicular penetration is independent of the type or sphericity of the particles (nanocrystals (NC) or lipid submicron particles (LN)). Furthermore, this principle can be used with both small molecules and large molecule therapeutics, as demonstrated with the model drugs fluorescein sodium, 6-carboxyfluorescein, green fluorescent protein and FITC-BSA. This highlights the high versatility of this new formulation principle. The system may be used for various hair follicle-associated diseases such as alopecia or for the preoperative disinfection of hair follicles and the transfollicular transport of active pharmaceutical and/or cosmetic ingredients.

摘要

将纳米颗粒系统用于将活性成分输送到毛囊的研究已经进行了近二十年,产生了无数关于各种颗粒类型、释放机制和活性成分的出版物。制备稳定的分散体通常既耗时又昂贵。在本出版物中,我们首次证明,只需向药物溶液中添加不同的亚微米颗粒,就能使毛囊渗透深度显著增加160%至190%,从而实现对漏斗下部结构的靶向。我们的结果表明,毛囊渗透的增加与颗粒(纳米晶体(NC)或脂质亚微米颗粒(LN))的类型或球形度无关。此外,这一原理可用于小分子和大分子治疗药物,如荧光素钠、6-羧基荧光素、绿色荧光蛋白和FITC-BSA等模型药物所示。这突出了这种新配方原理的高度通用性。该系统可用于各种与毛囊相关的疾病,如脱发,或用于毛囊的术前消毒以及活性药物和/或化妆品成分的经毛囊转运。

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