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四环素与壬二酸二甘氨酸钾(氮杂甘氨酸)在水凝胶中的协同作用:稳定性、抗菌活性及物理化学性质评估

Synergy of Tetracyclines and Potassium Azeloyl Diglycinate (Azeloglycine) in Hydrogels: Evaluation of Stability, Antimicrobial Activity, and Physicochemical Properties.

作者信息

Kostrzębska Agnieszka, Junka Adam, Musiał Witold

机构信息

Department of Physical Chemistry and Biophysics, Pharmaceutical Faculty, Wroclaw Medical University, Borowska 211, 50-556 Wroclaw, Poland.

Platform for Unique Models Application P.U.M.A., Department of Pharmaceutical Microbiology and Parasitology, Wroclaw Medical University, Borowska 211, 50-556 Wroclaw, Poland.

出版信息

Int J Mol Sci. 2025 May 29;26(11):5239. doi: 10.3390/ijms26115239.

Abstract

Acne vulgaris is one of the most common dermatological diseases and has a complex etiology. Despite the wide range of available therapeutic options, modern and effective solutions are still being sought, particularly in the area of topical therapy. The aim of this study was to develop hydrogel formulations that provide stability for the antibiotics they contain-tetracycline or chlortetracycline enriched with azeloglycine-the latter an ingredient supporting acne-prone skin care. The physicochemical parameters, stability, and antimicrobial activity of the obtained formulations were analyzed. HPLC analysis showed that tetracycline exhibited greater stability than chlortetracycline, especially in mildly acidic and neutral environments. The addition of azeloglycine improved the rheological properties of the hydrogels, reduced tetracycline degradation under alkaline conditions, and enhanced the penetration of active ingredients into the model sebum. All tested formulations demonstrated antimicrobial activity against . In the artificial sebum biofilm model, hydrogels containing azeloglycine more effectively reduced staphylococcal biofilm mass. No formulations showed toxicity towards larvae. The results indicate the potential usefulness of the developed hydrogels as modern multifunctional formulations for topical acne treatment. Hydrogel formulations containing tetracycline and azeloglycine may represent a promising future anti-acne preparation exhibiting synergistic antibacterial, anti-inflammatory, and sebum-cleansing effects.

摘要

寻常痤疮是最常见的皮肤病之一,其病因复杂。尽管有多种可用的治疗选择,但仍在寻求现代且有效的解决方案,特别是在局部治疗领域。本研究的目的是开发水凝胶制剂,为其所含的抗生素——四环素或富含壬二酸甘氨酸的金霉素提供稳定性,后者是一种支持易长痤疮皮肤护理的成分。对所得制剂的理化参数、稳定性和抗菌活性进行了分析。高效液相色谱分析表明,四环素比金霉素表现出更高的稳定性,尤其是在微酸性和中性环境中。壬二酸甘氨酸的添加改善了水凝胶的流变学性质,减少了碱性条件下四环素的降解,并增强了活性成分向模型皮脂中的渗透。所有测试制剂均表现出对……的抗菌活性。在人工皮脂生物膜模型中,含壬二酸甘氨酸的水凝胶更有效地减少了葡萄球菌生物膜的量。没有制剂对……幼虫显示出毒性。结果表明,所开发的水凝胶作为用于局部痤疮治疗的现代多功能制剂具有潜在的实用性。含有四环素和壬二酸甘氨酸的水凝胶制剂可能代表一种有前景的未来抗痤疮制剂,具有协同抗菌、抗炎和清洁皮脂的作用。

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