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一种治疗需氧菌性阴道炎的新方法:壳聚糖水凝胶包裹阿奇霉素脂质体

A Novel Approach for the Treatment of Aerobic Vaginitis: Azithromycin Liposomes-in-Chitosan Hydrogel.

作者信息

Čačić Ana, Amidžić Klarić Daniela, Keser Sabina, Radiković Maja, Rukavina Zora, Jøraholmen May Wenche, Uzelac Lidija, Kralj Marijeta, Škalko-Basnet Nataša, Šegvić Klarić Maja, Vanić Željka

机构信息

Microbiology and Biology Laboratory, PLIVA Croatia Ltd., Prilaz Baruna Filipovića 25, 10000 Zagreb, Croatia.

Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovačića 1, 10000 Zagreb, Croatia.

出版信息

Pharmaceutics. 2023 Apr 28;15(5):1356. doi: 10.3390/pharmaceutics15051356.

Abstract

Biocompatible mucoadhesive formulations that enable a sustained drug delivery at the site of action, while exhibiting inherent antimicrobial activity, are of great importance for improved local therapy of vaginal infections. The aim of this research was to prepare and evaluate the potential of the several types of azithromycin (AZM)-liposomes (180-250 nm) incorporated into chitosan hydrogel (AZM-liposomal hydrogels) for the treatment of aerobic vaginitis. AZM-liposomal hydrogels were characterized for in vitro release, and rheological, texture, and mucoadhesive properties under conditions simulating the vaginal site of application. The role of chitosan as a hydrogel-forming polymer with intrinsic antimicrobial properties was explored against several bacterial strains typical for aerobic vaginitis as well as its potential effect on the anti-staphylococcal activity of AZM-liposomes. Chitosan hydrogel prolonged the release of the liposomal drug and exhibited inherent antimicrobial activity. Additionally, it boosted the antibacterial effect of all tested AZM-liposomes. All AZM-liposomal hydrogels were biocompatible with the HeLa cells and demonstrated mechanical properties suitable for vaginal application, thus confirming their potential for enhanced local therapy of aerobic vaginitis.

摘要

生物相容性粘膜粘附制剂能够在作用部位实现持续给药,同时展现出固有的抗菌活性,这对于改善阴道感染的局部治疗至关重要。本研究的目的是制备并评估几种类型的阿奇霉素(AZM)脂质体(180 - 250纳米)包封于壳聚糖水凝胶中形成的制剂(AZM脂质体水凝胶)用于治疗需氧性阴道炎的潜力。对AZM脂质体水凝胶进行了体外释放特性以及在模拟阴道给药部位条件下的流变学、质地和粘膜粘附性能的表征。研究了壳聚糖作为具有固有抗菌特性的水凝胶形成聚合物,对几种需氧性阴道炎典型细菌菌株的作用,以及其对AZM脂质体抗葡萄球菌活性的潜在影响。壳聚糖水凝胶延长了脂质体药物的释放,并展现出固有抗菌活性。此外,它增强了所有测试的AZM脂质体的抗菌效果。所有AZM脂质体水凝胶与HeLa细胞具有生物相容性,并表现出适合阴道给药的机械性能,从而证实了它们在增强需氧性阴道炎局部治疗方面的潜力。

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